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Reference Guide for the Pharmacy Licensing Exam Theory-Third Edition

Krisman

REFERENCE GUIDE FOR THE PHARMACY LICENSING EXAM Theory-Third Edition


THIRD EDITION 2008-2009 MANAN H SHROFF

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Reference Guide for the Pharmacy Licensing Exam Theory-Third Edition

Krisman

This book is not intended as a substitute for the advise of physicians. Students or readers must consult their physician about any existing problem. Do not use information in this book for any kind of self treatment. Do not administer any dose of mentioned drugs in this book without consulting your physician. This is only a review guide for the preparation of the Pharmacy Licensing Exam (NAPLEX) The author is not responsible for any kind of misinterpreted, incorrect, or misleading information or any typographical errors in this book. Any doubtful or questionable answers should be checked in other available reference sources. All rights reserved. No part of this book may be reproduced or transmitted in any form or by any means, electronically photocopying, recording, or otherwise, without prior written permission of the publisher. RXEXAM is a registered trademark of Pharmacy Exam of Krishna Publications Inc. Any unauthorized use of this trademark will be considered a violation of law. NAPLEX and FPGEE are registered trademarks of the National Association of Boards of Pharmacy (NABP). This reference guide is in no way authorized by or sponsored by NABP.

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Reference Guide for the Pharmacy Licensing Exam Theory-Third Edition

Krisman

REFERENCE GUIDE FOR THE PHARMACY LICENSING EXAM Theory-Third Edition


Dedicated To My Parents

Third Edition-2008 to 2009

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Reference Guide for the Pharmacy Licensing Exam Theory-Third Edition

Krisman

PREFACE:
I am very happy to introduce the third edition of the Reference Guide for the Pharmacy Licensing Exam - Theory. It is specifically written for students preparing for the NAPLEX exam. It contains over sixty chapters and includes well organized therapeutic classifications at the beginning of each chapter, with brand and generic names of medications. In this third edition, I added a new chapter that covers all of the antineoplastic agents. This review guide also covers over 2000 drugs; a sound knowledge of these drugs is an important factor in passing the NAPLEX exam. I would also recommend the Reference Guide For the Pharmacy Licensing Exam - Questions and Answers (over 1000 NAPLEX-type questions) and the Reference Guide for Pharmaceutical Calculations (over 500 calculations). I hope my efforts will help you pass your key exam. I wish you the very best of luck, and any questions or comments are always welcome. Good luck, Manan H. Shroff

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Reference Guide for the Pharmacy Licensing Exam Theory-Third Edition

Krisman

TABLE OF CONTENTS
1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 INOTROPIC AGENTS ANTIARRHYTHMIC AGENTS BETA BLOCKERS CENTRALLY ACTING ANTIHYPERTENSIVE CA-CHANNEL BLOCKERS ACE INHIBITORS VASODILATORS ANGINA DIURETICS SPECIFIC ALPHA-1 BLOCKERS ANTIHYPERLIPIDEMIC AGENTS TRANQUILIZERS ANTIEPILEPTICS ANTIDEPRESSANTS ANTIPARKINSONS ATTENTION DEFICIT DISORDER ANTINEUROLEPTICS ANTIBIOTICS ANTI AIDS ACNE PRODUCTS ANORECTAL PRODUCTS PEPTIC ULCERS ANTIHISTAMINES APPETITE SUPPRESSANTS ARTHRITIS ASTHMA BPH COLONY & ERYTHROCYTE STIMULATORS HYPERURICEMIA & GOUT HEMATINIC AGENTS IMMUNOSUPPRESSANTS MIGRAINES NAUSEA MEDICATIONS NONSTEROIDAL ANTI-INFLAMMATORY AGENTS OPIOID ANALGESIC AGENTS OSTEOPOROSIS & HYPOCALCEMIA ANTIPLATELET AGENTS SMOKING CESSATION AGENTS THYROID DISEASE ULCERATIVE COLITIS DIABETES EXPECTORANT & ANTITUSSIVE ACID BASE DISORDERS ORAL CONTRACEPTIVES 07 10 15 18 22 25 31 36 42 48 50 55 59 67 77 83 86 91 117 125 127 128 135 138 141 147 155 157 159 162 164 167 172 176 183 190 197 202 204 207 210 223 226 228

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Reference Guide for the Pharmacy Licensing Exam Theory-Third Edition

Krisman

TABLE OF CONTENTS (Contd)


45 46 47 48 49 50 51 52 53 54 55 56 57 58 59 60 61 62. 63. 64. 65. ANTIGLAUCOMA CYSTIC FIBROSIS PSORIASIS PHARMACY LAW NEW DRUG APPROVAL CLINICAL DRUG LITERATURE PHARMACOKINETIC VITAMINS AND THEIR SOURCES TERATOGENIC DRUGS TPN (TOTAL PARENTERAL NUTRITION) RENAL FAILURE INTERPRETATION OF CLINICAL LABORATORY TESTS DEMENTIA TUBERCULOSIS MULTIPLE SCLEROSIS MUSCLE RELAXANTS HERBAL DRUGS ENURESIS/INCONTINENCE MANAGEMENT IRRITABLE BOWEL SYNDROME AGENTS OPHTHALMIC AGENTS ANTINEOPLASTIC AGENTS 232 234 236 237 244 246 248 252 253 256 258 265 268 270 274 277 280 283 286 289 292

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Reference Guide for the Pharmacy Licensing Exam Theory-Third Edition 1-INOTROPIC AGENTS

Krisman

Lanoxin, Lanoxicap = Digoxin Crystodigin = Digitoxin A. Lanoxin (Digoxin and Digitoxin)

Primacor = Milrinone Dobutrex = Dobutamine

M/A: Digitalis glycoside inhibits Na+ K+ ATP ase pump activity. This causes an increase in the intracellular Ca+2 level, which increases the force of contraction of the heart (+ve inotropic action). * A normal serum therapeutic concentration for Lanoxin (Digoxin) is 0.7 to 1.4 ng/ml, and for Lanoxin (Digitoxin) is 9 to 25 mcg/ml. The first sign of Lanoxin (Digoxin) toxicity in infants is cardiac arrhythmia. In adults it is anorexia, abdominal pain and stomach upset. It is indicated for the treatment of heart failure, cardiogenic shock, atrial flutter and fibrillation. It is available in injection, elixir, capsule and tablet forms. The recommended dose of Lanoxin (Digoxin) for CHF patients is 0.125 mg to 0.25 mg, once a day. Lanoxicap provides more bioavailability compared to a Lanoxin tablet. A tablet form of Lanoxin (Digoxin) provides 60 to 80% bioavailability, elixir form provides 70 to 85% bioavailability, and softgel capsule form provides 90 to 100% bioavailability. The principal route of Lanoxin (Digoxin) excretion is via kidney, while the principal metabolic pathway of Digitoxin is via liver, therefore the administration of Lanoxin (Digoxin) is not recommended in patients with impaired renal or liver function. Hypokalemia, hypomagnesemia and hypercalcemia increase the toxicities of Digitalis. Lanoxin (Digoxin) elixir contains 10% alcohol and should be carefully used for patients on disulfiram therapy, or on drugs that may produce disulfiram-like reactions, such as Diabinese (Chlorpropamide), Flagyl (Metronidazole), Cefazone (Cefoperazone), etc. Lanoxin (Digoxin) injection should never be given intramuscularly as it lacks effectiveness as well as causes extreme pain at the injection site. Lanoxin (Digoxin) I.V. solutions should be diluted at least 4 times or greater to prevent the precipitation of the drug. A rapid digitalization or loading dose is defined as the dose that produced a therapeutically effective plasma concentration of the drug at once.

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Reference Guide for the Pharmacy Licensing Exam Theory-Third Edition


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Krisman

A maintenance dose is defined as the amount of small doses that can be given on regular intervals to replace metabolic losses of the drug. Treatment of overdose of digoxin Condition Recommendation Potassium supplements Lidocaine, phenytoin Digoxin Immune Fab, cholestyramine, activated charcoal

* * * *

Hypokalemia Arrhythmia Toxication

38 mg of Digoxin Immune Fab neutralizes the 0.5mg of Digoxin.

Name of Drug Diuretics Antacids Kaolin pectin Cholestyramine, Colestipol

Drug Interactions Hypokalemia induced by diuretic increases the Digoxins toxicity. Inhibit the absorption of Lanoxin (Digoxin). Inhibits the absorption of Lanoxin (Digoxin). Inhibits the absorption of Lanoxin (Digoxin) by binding to the acidic moiety of the drug.

Quinidine, Quinine

May elevate the serum concentration and toxicities of Lanoxin (Digoxin) . May decrease therapeutic effects of Lanoxin (Digoxin) by enhancing its metabolism. Concurrent use with Lanoxin (Digoxin) may result in excessive bradycardia because of an additive AV node suppression caused by Ca-channel blockers. May elevate the serum concentration and toxicities of Lanoxin (Digoxin). Decreases the renal clearance and increases Digoxins toxicities.

Thyroid supplements

Diltiazem, Verapamil

Amiodarone

Indomethacin

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Reference Guide for the Pharmacy Licensing Exam Theory-Third Edition


B Primacor = Milrinone

Krisman

M/A: It is an inhibitor of cAMP phosphodiesterase enzyme in cardiac and smooth muscles. This inhibitory action increases the intracellular ionized calcium and contractile forces in the heart. It has a positive inotropic action with a vasodilation property, therefore it is also known as an Inodilator. * * It is indicated for the short-term treatment of patients suffering from congestive heart failure. Ventricular arrhythmia, ventricular tachycardia and sudden death are reported side effects of the drug. Primacor (Milrinone) has not been shown to be safe or effective in the longer treatment of patients with CHF. Hypotension, angina, chest pain, thrombocytopenia and tremor are reported side effects of the drug. Primacor (Milrinone) is available in an injection form. Dobutrex = Dobutamine M/A: It is a direct acting inotropic agent with a beta-1 receptor stimulation property. * It is indicated for the short-term treatment of patients with cardiac decompensation due to depressed contractility, resulting either from organic heart disease or from cardiac surgical procedures. Hypotension, tachycardia, ventricular ectopic activity, and increased blood pressure are reported side effects of the drug. Because of the risk of severe physical incompatibilities, Dobutrex (Dobutamine) solutions should not be mixed with alkaline solutions such as Sodium bicarbonate. Dobutrex (Dobutamine) therapy should be monitored by regularly checking ECG and blood pressure.

* C

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Reference Guide for the Pharmacy Licensing Exam Theory-Third Edition 2-ANTIARRHYTHMIC AGENTS
Class IA =

Krisman

Quinidine, Procainamide (Procanbid, Pronestyl, Procan SR), Disopyramide (Norpace, Rythmodan) Lidocaine (Xylocaine), Tocainide (Tonocard), Phenytoin (Dilantin), Mexiletine (Mexitil) Flecainide (Tambocor) Propafenone (Rythmol) Moricizine (Ethmozine)

Class IB

Class IC

Class II Atenolol Acebutolol Metoprolol Labetalol Propranolol Pindolol Carvedilol Class III Bretylium Amiodarone Ibutilide Class IV Nifedipine Verapamil Diltiazem Nicardipine Isradipine * * = = = = = = = = = =

Beta-blockers Tenormin Sectral Lopressor Normodyne, Trandate Inderal Visken Coreg Timolol Nadolol Betaxolol Penbutolol Esmolol Bisoprolol = = = = = = Blocadren Corgard Kerlone Levatol Brevibloc Zebeta

Bretylol Cordarone Corvert

Sotalol Dofetilide

= =

Betapace Tikosyn

Ca channel blockers = = = = = Adalat, Procardia Calan, Isoptin, Verelan Cardizem, Cardene DynaCirc Bepridil Nimodipine Felodipine Amlodipine = = = = Vascor, Bepadin Nimotop Plendil Norvasc

Quinidine induces arrhythmia, and can be treated with glucagon, catecholamine and Na lactate. Quinidine may produce cinchonism at high doses. Tinnitus, blurred vision, hearing loss and excessive salivation are signs of cinchonism. The major adverse effect associated with quinidine therapy is diarrhea. Embolism generally occurs upon restoration of the normal rhythm of the heart after administration of antiarrhythmic agents. It is preferable to use anticoagulant therapy to prevent this consequence.

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Krisman

At higher doses, quinidine produces ventricular fibrillation by stimulation of vagus nerves. Digitalization prior to quinidine therapy prevents this ventricular fibrillation by suppressing the A.V. node. Prolonged administration of Procanbid (Procainamide) results in a positive antinuclear antibody test with or without symptoms of lupus erythematosus-like syndrome. Agranulocytosis, bone marrow depression, neutropenia and thrombocytopenia have been reported with Procainamide therapy, therefore a complete blood count should be performed periodically. Procanbid (Procainamide) induces blood dyscrasia, and usually returns to normal within one month of discontinuation of the drug. Procanbid (Procainamide) therapy should be withdrawn if signs or symptoms of S.L.E-like syndrome, hemolytic anemia or leukopenia are observed. Hypotension generally develops during rapid I.V. administration of Procanbid (Procainamide). Blood pressure should be monitored continuously during therapy. Type IC antiarrhythmic agents like Encainide, Tambocor (Flecainide) and Rythmol (Propafenone) should be reserved for patients with life-threatening arrhythmia. Norpace (Disopyramide) has negative inotropic properties and requires careful monitoring in congestive heart failure patients. Because of the anticholinergic properties of Norpace (Disopyramide), it is contraindicated in patients with glaucoma, M. Gravies, or urinary retention. Lidocaine has central nervous stimulation properties. It is contraindicated in patients with seizures. Blood dyscrasias, agranulocytosis, bone marrow depression and leukopenia are reported side effects of Tonocard (Tocainide). Pulmonary fibrosis and pulmonary edema have been observed with the use of Tonocard (Tocainide). Gingival hyperplasia is a common complication associated with Dilantin (Phenytoin). Gum inflammation is commonly reported during the first six months of treatment with Dilantin (Phenytoin). Ataxia, nystagmus, nausea and vertigo are reported side effects of Dilantin (Phenytoin). A normal therapeutic serum concentration of Dilantin (Phenytoin) is 10 to 20 mcg/ml. Tambocor (Flecainide) should be carefully used in patients with CHF, since it has powerful negative inotropic properties. Pulmonary toxicity has been reported with Cordarone (Amiodarone) when given in doses that exceed 400 mg/day for a prolonged period of time. Cordarone (Amiodarone) causes hypothyroidism as well hyperthyroidism.

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Krisman

Cordarone (Amiodarone) has the longest half-life among all the antiarrhythmic agents of about 45 to 50 days . Tikosyn (Dofetilide) and Corvert (Ibutilide) are classified as type III antiarrhythmic agents. Tikosyn (Dofetilide) and Corvert (Ibutilide) are indicated for the maintenance of normal sinus rhythm in patients with atrial fibrillation and atrial flutter. Ventricular arrhythmia with torsa de pointes and QT interval prolongation are reported side effects of the drugs. The QT interval prolongation is directly reported to the serum concentration of Tikosyn (Dofetilide) and Corvert (Ibutilide), and therefore they should be carefully prescribed in patients with impaired renal or liver functions.

* *

Drug Interactions with Quinidine: Antacids, NaHCO3 and Carbonic Anhydrase Inhibitor Anticholinergic Concurrent use may increase the serum concentration of Quinidine by increasing the renal tubular reabsorption of Quinidine by making the alkaline pH. It may intensify the atropine-like side effects since Quinidine also possesses anticholinergic side effects. Increases the serum concentration of Quinidine by inhibiting its metabolism. Concurrent use of Quinidine with Lanoxin (Digoxin) may increase the serum concentration of Lanoxin (Digoxin). Concurrent use with Quinidine may antagonize the cholinergic effects of Urecholine (Bethanechol). When used with Quinidine it may cause severe cardiac arrhythmias.

Cimetidine

Digoxin

Bethanechol

Pimozide

Drug Interactions with Procainamide: Atropine, Antihistamine Concurrent use with Procanbid (Procainamide) may intensify the anticholinergic effects. Concurrent use with Procainamide may antagonize the cholinergic effects of Urecholine (Bethanechol).

Bethanechol

Drug Interactions with Disopyramide: Diltiazem, Verapamil, beta-blockers Anticholinergic medication An Additive AV node suppression.

May intensify the anticholinergic side effects of such medications.

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Reference Guide for the Pharmacy Licensing Exam Theory-Third Edition


Drug Interactions with Tocainide: Beta-blockers

Krisman

Concurrent use with Tonocard (Tocainide) may result in an additive AV node suppression.

Drug Interactions with Mexiletine: Antacids, Carbonic Anhydrase Inhibitor NH4Cl, Vitamin C Reglan Theophylline An Alkalinization of urine may reduce the renal excretion of Mexitil (Mexiletine). Acidification of urine may increase the renal excretion of Mexitil (Mexiletine). May increase the absorption of Mexitil (Mexiletine). Renal clearance of Theophylline may decrease; toxicities of drug may increase.

Drug Interactions with Phenytoin: Carbamazepine May increase the metabolism of Dilantin (Phenytoin) by its enzyme induction properties. May cause failure of contraception because of induction of metabolism of oral contraceptive by Dilantin (Phenytoin). May raise the serum concentration and toxic effects of Dilantin (Phenytoin). Concurrent use of azoles with Dilantin (Phenytoin) may inhibit the metabolism and increase the toxicities of Dilantin (Phenytoin). Dilantin (Phenytoin) may accelerate the metabolism of Methadone and precipitate withdrawal symptoms in opioid dependent patients. May inhibit the metabolism of Dilantin (Phenytoin) by CP450 inhibition and result in a higher plasma concentration of Dilantin (Phenytoin).

Estrogen and other oral contraceptives Amiodarone

Fluconazole Miconazole Ketoconazole Methadone

Prilosec

Antacids + Sucralfate

May reduce the absorption of Dilantin (Phenytoin) and decrease its bioavailability. May displace Dilantin (Phenytoin) from protein-binding, inhibit the metabolism of the drug, and increase its toxic effects. Increases the clearance of Theophylline and decreases the pharmacological effects of the drug.

Valproic acid

Theophylline

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Reference Guide for the Pharmacy Licensing Exam Theory-Third Edition


(D) Miscellaneous: Nicotinic acid = = = = = = Nicobid Nicolar Slo-Niacin Niacin Time Release Zetia Lovaza

Krisman

Ezetimibe Omega -3 acid ethyl esters (E) Combination Agents: Lovastatin + Niacin Atorvastatin + Amlodipine Pravastatin + Aspirin Simvastatin + Ezetimibe HMG COA Inhibitors :

= = = =

Advicor Caduet Pravigard Pac Vytorin

M/A: The inhibition of HMG COA reductase prevents the conversion of HMG-COA to mevalonate, which is an early step in the synthesis of cholesterol. * Mevacor (Lovastatin) and Zocor (Simvastatin) are prodrugs and need to be converted in betahydroxy acid forms before exerting any pharmacological effects. Mevacor (Lovastatin) has a prolonged duration of action compared to other HMG COA inhibitors. Mevacor (Lovastatin) should be taken with evening meals to increase its absorption. Pravachol (Pravastatin) and Zocor (Simvastatin) can be taken with or without meals at bed time. Lipitor (Atorvastatin) has an advantage over other HMG CoA inhibitors in that it can be taken any time of the day. The recommended starting dose of Lescol (Fluvastatin) is 20 mg daily at bed time. Myopathy is the most significant adverse effect of HMG COA inhibitors. The risk of myopathy is greater in patients with renal impairment, and in patients who are older or taking more than 40 mg of the drug. Rhabdomyolysis with renal dysfunction secondary to myoglobinuria has been reported with nearly all HMG-COA inhibitors. All HMG-COA inhibitors require liver function monitoring.

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Krisman

Crestor (Rosuvastatin) is a new HMG-CoA inhibitor. The recommended dose of the drug is 5 to 10 mg per day. It is classified as pregnancy category X. The risk of myopathy is increased when the drug is taken with fibric acid derivatives, niacin, erythromycin, cyclosporine, or an antifungal azole.

Adverse effects: * * * Myalgia Constipation Diarrhea * * * Insomnia Headache Blurred vision * Impotence

Fibric Acid Derivatives: M/A: Fibric acid derivatives may reduce the plasma concentration of triglycerides (VLDL) and increase the plasma concentration of high density lipoproteins (HDL). They also increase the activity of lipoprotein lipase which enhances the metabolism of VLDL. The anticoagulant therapy should be carefully exercised when fibric acid derivatives are given in combination with them. The frequent monitoring of prothrombin time is required since fibric acid derivatives may inhibit the metabolism of anticoagulants and increase the risk of bleeding. The dosage of anticoagulants should be reduced to half when used in conjugation with Atromid-S (Clofibrate). Lopid (Gemfibrozil) may cause malignancy, gall bladder disease, and abdominal pain when used for prolonged time. Atromid-S (Clofibrate) increases the incidence of cholelithiasis. The recommended dose of Lopid (Gemfibrozil) is 1200 mg in two divided doses, 30 minutes before morning and evening meals. The recommended therapeutic dose of Tricor, Antara, Lofibra, Triglide (Fenofibrate) is 67 to 200 mg once a day with meals. Nausea and abdominal discomfort are the most common adverse effects associated with fibric acid therapy.

Bile acid binding resins: M/A: Questran (Cholestyramine), Welchol (Colesevelam) and Colestid (Colestipol) bind to bile acid in the intestine and increase the excretion of bile acid. This leads to an increase in the conversion of cholesterol in bile acid. Also, bile acid is an important substance for the absorption of cholesterol. Thus, by reducing the bile acid from the body the antihyperlipidemic action is produced. Questran (Cholestyramine), Welchol (Colesevelam) and Colestid (Colestipol) bind to a number of drugs and decrease their absorptions. Patients should take another drug at least 1 hour before, or 4 to 6 hours after the administration of Cholestyramine, Colesevelam, or Colestipol. Take bile acid resin with plenty of water to prevent constipation. This can also be prevented by adding stool softener in therapeutic regimen.

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Krisman

The Questran light (Cholestyramine) contains 17 mg of phenylalanine and should be avoided in patients with phenylketonuria. Questran (Cholestyramine) powder does not contain phenylalanine and can be given to patients suffering from PKU disorder. Questran (Cholestyramine) may increase the bleeding tendency of patients by inducing hypoprothrombinemia. A decrease in vitamin K absorption by resin may be responsible for this. Questran (Cholestyramine) is available in a chewable bar and a powder for oral suspension. Welchol (Colesevelam) is available in tablet dosage form. The recommended dose of the drug is 3 tablets taken twice daily with meals, or 6 tablets once daily with a meal.

* *

Miscellaneous: Niacin (Nicotinic acid): M/A: Niacin (Nicotinic acid) inhibits the VLDL secretion, which decreases the production of low density lipoprotein. Nicotinic acid also reduces the cholesterol synthesis. Liver toxicity is a major adverse effect of Niacin (Nicotinic acid). The usual adult dose of Niacin (Nicotinic acid) is 1 to 2 gm, 2 to 3 times a day. Flushing of the skin occurs frequently and can be minimized by pretreatment with aspirin or NSAIDs. Flushing, pruritus and G.I.distress can be reduced by gradually increasing the dose of Niacin (Nicotinic acid) and by not taking the drug on an empty stomach.

* * * *

Zetia (Ezetimibe): M/A: Zetia (Ezetimibe) reduces the total cholesterol, LDL-cholesterol, and triglycerides, and increases HDL cholesterol in patients with hypercholesterolemia. It reduces the blood cholesterol by inhibiting the absorption of cholesterol by the small intestine. It neither inhibits cholesterol synthesis nor increases the bile acid excretion. The recommended dose of the drug is 10 mg once daily, with or without food. Diarrhea, abdominal pain, back pain, arthralgia and sinusitis are reported side effects of the drug.

* *

Lovaza (Omega-3-acid ethyl ester): M/A: Lovaza may reduce the synthesis of triglycerides (TGs) in the liver because eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) are poor substrates for the enzymes responsible for triglyceride synthesis, and EPA and DHA inhibit esterification of other fatty acids. Lovaza, a lipid-regulating agent, is supplied as a liquid-filled gel capsule for oral administration. Each one gram capsule of Lovaza (omega-3-acid ethyl esters) contains at least 900 mg of the ethyl esters of omega-3 fatty acids. These are predominantly a combination of ethyl esters of eicosapentaenoic acid (EPA - approximately 465 mg) and docosahexaenoic acid (DHA approximately 375 mg).

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Krisman

Lovaza is indicated as an adjunct to diet to reduce triglyceride (TG) levels in adult patients with very high (>500 mg/dL) triglyceride levels. The recommended daily dose of Lovaza is 4 g per day. The daily dose may be taken as a single 4-g dose(4 capsules) or as two 2-g doses (2 capsules given twice daily). The most common side effects reported were burping, infection, flu symptoms, upset stomach, a change in sense of taste, back pain and skin rash.

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Reference Guide for the Pharmacy Licensing Exam Theory-Third Edition 12. TRANQUILIZERS & NARCOLEPSY AGENTS

Krisman

A.

Benzodiazepines: = = = = = = = Restoril Ativan Xanax, Xanax XR, Niravam Valium, Valrelease Librium ProSom Serax Flurazepam Prazepam Quazepam Triazolam Clonazepam Clorazepate = = = = = = Dalmane Centrax Doral Halcion Klonopin Tranxene

Temazepam Lorazepam Alprazolam Diazepam Chlordiazepoxide Estazolam Oxazepam B.

Non-Benzodiazepine Sedative Agents: = = = Ambien, Tovalt ODT Sonata Lunesta

Zolpidem Zaleplon Eszopiclone C.

Melatonin Receptor Agonist: = Rozerem

Ramelteon D.

Narcolepsy Agents: = = = Nuvigil Xyrem Provigil

Armodafinil Sodium oxybate Modafinil

Benzodiazepines and Non-Benzodiazepines: M/A: Benzodiazepine increases the level of an inhibitory neuro transmitter GABA. GABA receptors activate the chloride ion channels, which in turn activate the conductance of Cl- ions and decrease the firing of Cl- ions in the cerebral cortex. Librium (Chlordiazepoxide), Klonopin (Clonazepam) and Valium (Diazepam) are indicated for the relief of acute alcohol withdrawal symptoms. Parenteral, Valium (Diazepam) and Ativan (Lorazepam) are indicated for the treatment of status epileptics. Ativan (Lorazepam) injection is also indicated for the treatment of nausea and vomiting associated with emetogenic cancer therapy. Withdrawal symptoms of benzodiazepines are reported more frequently with short-acting benzodiazepines compared to long-acting benzodiazepines. Xanax (Alprazolam), Ativan (Lorazepam), Serax (Oxazepam), Restoril (Temazepam), and Halcion (Triazolam) are short-acting benzodiazepines, and are more preferable for older or geriatric patients because of their short half-lives.

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Krisman

Short to intermediate duration of benzodiazepines have half-lives of 2 to 3 days, while longacting benzodiazepines have half-lives of 10 to 20 days. Valium (Diazepam), Ativan (Lorazepam) and Librium (Chlordiazepoxide) are indicated in the treatment of tension headaches and in the treatment of senile or action tremor. The I.V. route of Librium (Chlordiazepoxide) is more preferable than the I.M. route since the absorption of drug via I.V. is more rapid than I.M. Librium (Chlordiazepoxide) should not be given intramuscularly since it may cause extreme pain at the injection site. The continuous I.V. infusion of Valium (Diazepam) may not be recommended since the drug may precipitate out in I.V. fluid. Niravam is an orally disintegrating tablet form of Alprazolam. Ambien (Zolpidem), Sonata (Zaleplon) and Lunesta (Eszopiclone) are classified as nonbenzodiazepine class of hypnotic and sedative agents. Tovalt ODT is a disintegrating tablet form of Ambien (Zolpidem tartrate). Sonata (Zaleplon) should be taken immediately before bed time. It has a fast onset of action with a shorter duration of action compared to other tranquilizers. Lunesta (Eszopiclone) should be avoided with or immediately after a heavy, high-fat meal; this results in slower absorption and would be expected to reduce the effect of the drug on sleep latency. Adverse effects: Drowsiness Confusion Severe shakiness Slow heartbeat Slurred speech Ataxia Constipation

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* *

Drug Interactions: Alcohol Concurrent use may potentiate the CNS depression effects of benzodiazepines. They may reduce the pharmacological effects of benzodiazepine by inducing their metabolism. They may inhibit the CP450 enzyme and metabolism of benzodiazepines, which results in elevated serum concentrations of benzodiazepines and their toxicities. Benzodiazepine may competitively inhibit the glucuronidation of Retrovir and may increase its toxicity. Probenecid may impair the glucuronide conjugation of benzodiazepines and increase their adverse effects profile.

Tegretol, Rifampin

Erythromycin, Cimetidine

Retrovir, Probenecid

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(C) M/A: Thiazolidinedion derivatives:

Krisman

Avandia (Rosiglitazone) and Actos (Pioglitazone) increase the response of insulin to target sites without stimulating secretion of insulin from pancreatic cells, therefore chances of hypoglycemia are rare with Avandia (Rosiglitazone) and Actos (Pioglitazone) therapy. The recommended daily dose of Avandia (Rosiglitazone) is 4 to 8 mg per day as a single dose once daily or in divided doses twice daily. For Actos (Pioglitazone), it is 15 mg to 30 mg once a day. Hepatotoxicity with jaundice and liver enzyme elevation has been reported with Avandia (Rosiglitazone) and Actos (Pioglitazone) therapy. Therefore, liver enzyme monitoring is recommended in all patients during the therapy and periodically after stopping the therapy. Weight gain and edema are reported with thiazolidinedion derivatives. Therefore, both Avandia (Rosiglitazone) and Actos (Pioglitazone) should be carefully prescribed to patients suffering from CHF or at risk for heart failure. Headache, sinusitis and upper respiratory tract infections are reported side effects of thiazolidinedion derivatives. Avandia (Rosiglitazone) may increase the total cholesterol and LDL, whereas Actos (Pioglitazone) may decrease mean triglycerides and increase HDL levels.

Drug Interactions: Cholestyramine Reduces the absorption of Troglitazone by 70%. Concurrent use may not be recommended. Troglitazone may enhance the metabolism of oral contraceptives resulting in loss of contraception. The enzyme induction properties of Troglitazone may enhance the metabolism of Terfenadine, which results in the loss of effectiveness of Terfenadine.

Oral contraceptives

Terfenadine

(D)

Oral alpha glucosidase inhibitors:

Precose = Acarbose: M/A: Precose (Acarbose) and Glyset (Miglitol) are classified as oral alpha-glucosidase inhibitors used to manage NIDDM. They inhibit the pancreatic alpha-amylase and alpha-glucosidase. Pancreatic amylase hydrolyzes the complex starch in oligosaccharide in the small intestine, while a glucosidase hydrolyzes the oligosaccharide, trisaccharide and disaccharide in glucose in the small intestine. Precose (Acarbose) and Glyset (Miglitol) are contraindicated in patients suffering from diabetic ketoacidosis, inflammatory bowel disease, colonic ulceration and intestinal obstruction.

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*

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Precose (Acarbose) and Glyset (Miglitol) do not cause hypoglycemia when administered to patients in a fasting state. When Precose (Acarbose) and Glyset (Miglitol) are taken with sulfonylurea or insulin, it is recommended to give dextrose instead of table sugar in case of hypoglycemia, since alpha-gluosidase inhibitors may block the breakdown of table sugar. Precose (Acarbose) and Glyset (Miglitol) are associated with the least risk of hypoglycemia and weight gain among all available diabetic agents. When a dose of Precose (Acarbose) exceeds 50 mg t.i.d, it may elevate the serum transaminase enzyme level. Monitor liver enzyme periodically when patient is on Precose (Acarbose).

Precose (Acarbose) is available in 50 mg and 100 mg of oral strength. The recommended daily dose of Precose (Acarbose) is 50 mg t.i.d with the first bite of meals. Glyset (Miglitol) is available in 25 mg, 50 mg and 100 mg of oral strengths. The recommended dose of Glyset (Miglitol) is 25 mg to 50 mg three times/day. Flatulence, diarrhea, skin rash, and abdominal cramping are common adverse effects associated with alpha-gluosidase inhibitor.

Drug Interactions: Thiazide diuretic, corticosteroid, phenothiazine, estrogen, oral contraceptive, Ca channel blocker Charcoal They may elevate the blood glucose level. Concurrent use may reduce the pharmacological effects of Precose.

Charcoal may reduce the effectiveness of Precose by reducing its intestinal absorption. Amylase and pancreatin are carbohydrate splitting enzyme supplements and may reduce the pharmacological effects of Precose. Concurrent use may not be recommended.

Amylase, Pancreatin

(E)

Prandial Insulin Release Drug:

Repaglinide = Prandin M/A: It stimulates prandial insulin released from functioning beta cells to reduce elevated blood glucose levels. It has a fast onset of action with a shorter duration of action. Risk of hypoglycemia is lower than an oral sulfonylurea agents because it does not cause prolonged insulin stimulation.

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* * Prandin (Repaglinide) has a low risk of weight gain compared to sulfonylurea.

Krisman

Patients should be instructed to take the drug before meals. Patients who skip meals or add an extra meal should be instructed to skip or add a dose for that meal. It is available in 0.5 mg, 1 mg and 2 mg of oral strength.

* Insulin M/A: *

Insulin is a hormone that controls the storage and metabolism of carbohydrates, proteins and fats. Insulin resistance is defined as the use of more than 100 to 200 units of insulin per day. It may result from certain kinds of infections, from over body weight or because of a high concentration of IgG or glucocorticoids. Regular insulin is the only insulin suitable for I.V. administration. For mixing insulins, it is recommended to draw regular insulin first to avoid contamination and claudification of regular insulin by other insulin. It is generally recommended to use the resulting mixture (regular insulin + NPH or lente insulin) immediately after mixing or within 5 minutes of mixing. A mixture of regular insulin and NPH insulin is generally more recommended compared to a mixture of regular insulin and an insulin Zn preparation, since the latter can give an unpredictable result because of the complex formation between Zn and Insulin. When regular insulin is mixed with PZI, it is recommended to keep the ratio of regular insulin to PZI at least 2:1, or more than 2:1, to get the positive effects of mixing. A large single I.V. dose of insulin is not recommended because of the short half-life of insulin. It is recommended to give an insulin preparation by subcutaneous route since it provides slow absorption of insulin and therefore less chance of hypoglycemia. It is recommended to rotate the sight of the insulin injections to avoid lipoatrophy. Regular and Semilente insulin are fast-acting insulin products, Lente and NPH are intermediate acting insulin products, and PZI and Ultralente are long-acting insulin products. Glucagon and Glucose are antidotes for insulin-induced hypoglycemia. Vigorous exercise, overdose of insulin, and skipping of meals may lead to hypoglycemia. Protamine Zn insulin has the longest duration of action among all the insulin products. Patients receiving insulin for a long time may develop antibodies against insulin. It is generally treated by use of Prednisone (60 mg/day) or by multiple injections of regular insulin.

* *

* *

* *

* * * *

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Humalog is an insulin Lispro injection of rDNA origin. This insulin analog has a more rapid onset of action and shorter duration of action than regular insulin. The dose of Humalog should be given 15 minutes before or immediately after the meal. Lantus is a sterile solution of insulin glargine (rDNA) origin. It is a long acting insulin analog with a duration of action is up to 24 hours. Lantus (insulin glargine) must not be diluted or mixed with any other insulins or solutions. The mixing of Lantus (insulin glargine) with any other insulins or solutions may alter the pharmacokinetic and pharmacodynamic properties of the insulin glargine and mixed insulins in an unpredictable manner. The recommended dose of Lantus (insulin glargine) is 10 IU via subcutaneous route once daily at bed time. It should not be administered via I.V. route. Intravenous administration of the usual subcutaneous dose may produce severe hypoglycemia. Novolog (insulin aspart) is a human insulin analog of rapid acting blood glucose-lowering agent. Novolog (insulin aspart) has a more rapid onset of action and shorter duration of action compared to human insulin. It should be given immediately before a meal. The recommended dose of Novolog (insulin aspart) is 0.5-1.0 U/kg/day via subcutaneously. Apidra (insulin glulisine [rDNA origin]) is a human insulin analog that is a rapid-acting, parenteral blood glucose lowering agent. The glucose lowering activities of Apidra (insulin glulisine) and of regular human insulin are equi potent when administered by the intravenous route. After subcutaneous administration, the effect of Apidra (insulin glulisine) is more rapid in onset and of shorter duration compared to regular human insulin. Apidra (insulin glulisine) has a more rapid onset of action and a shorter duration of action than regular human insulin. Apidra (insulin glulisine) should normally be used in regimens that include a longer-acting insulin or basal insulin analog. Apidra (insulin glulisine) differs from regular human insulin by its rapid onset of action and shorter duration of action. When used as a meal time insulin, the dose of Apidra (insulin glulisine) should be given within 15 minutes before or immediately after a meal. To minimize insulin degradation, infusion set occlusion, and loss of the preservative (m-cresol), the infusion sets (reservoir, tubing, and catheter) and the Apidra (insulin glulisine) in the reservoir should be replaced every 48 hours or less and a new infusion site should be selected. If Apidra (insulin glulisine) is mixed with NPH human insulin, Apidra (insulin glulisine) should be drawn into the syringe first. Injection should be made immediately after mixing. Mixtures should not be administered intravenously. Apidra (insulin glulisine) should not be mixed with insulin preparations other than NPH.

* *

* *

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Levemir (insulin detemir) is a long-acting basal insulin analog, with up to 24 hours duration of action, produced by a process that includes expression of recombinant DNA in Saccharomyces cerevisiae followed by chemical modification. The prolonged action of Levemir is mediated by the slow systemic absorption of insulin detemir molecules from the injection site due to strong self-association of the drug molecules, and by slow distribution to peripheral target tissues since insulin detemir in the bloodstream is highly bound to albumin. Levemir (insulin detemir) is indicated for once or twice daily subcutaneous administration for the treatment of adult and pediatric patients with type 1 diabetes mellitus or adult patients with type 2 diabetes mellitus who require basal (long-acting) insulin for the control of hyperglycemia. For patients treated with Levemir once daily, the dose should be administered with the evening meal or at bedtime. For patients who require twice daily dosing for effective blood glucose control, the evening dose can be administered either with the evening meal, at bedtime, or 12 hours after the morning dose. Levemir should not be diluted or mixed with any other insulin preparations. It is not to be used in insulin infusion pumps. Hypoglycemia is the most commonly reported side effect of the drug. Lipodystrophy, redness, pain, itching, hives, swelling, and inflammation are also reported. Unused Levemir should be stored between 2 and 8C (36 to 46F). Do not freeze. Do not use Levemir if it has been frozen. After initial use, vials should be stored in a refrigerator, never in a freezer. If refrigeration is not possible, the in-use vial can be kept unrefrigerated at room temperature, below 30C (86F), for up to 42 days, as long as it is kept as cool as possible and away from direct heat and light. Insulin Onset of action Duration of action

Rapid Acting: Insulin Glulisine Insulin R Prompt Insulin Zn Insulin Lispro Insulin Aspart < 0.5 to 1 hours 0.5 to 1 hours 1 to 1.5 hours 0.25 hours 0.25 hours < 8 to 12 hours 8 to 12 hours 12 to 16 hours 6 to 8 hours 3 to 5 hours

Intermediate Acting: Isophane Insulin Insulin Zn 1 to 1.5 hours 1 to 2.5 hours 24 hours 24 hours

Long Acting: Insulin Glargine Insulin Detemir Protamine Zn Insulin Extended Insulin Zn 1.1 hours 4 to 8 hours 4 to 8 hours 24 hours 24 hours 36 hours 36 hours

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G Miscellaneous:

Krisman

Nateglinide = Starlix M/A: Starlix (Nateglinide) stimulates insulin secretion from functioning beta-cells in the pancreatic islets. However, it is not a sulfonylurea agent. The recommended therapeutic dose of Nateglinide, alone or in combination with Metformin, is 120 mg three times a day before meals. It should be taken 1 to 30 minutes prior to meals. Hypoglycemia, upper respiratory tract infections, flu symptoms, dizziness and diarrhea are reported side effects of the drug. It is available as 60 mg and 120 mg of oral strengths.

Exenatide = Byetta M/A: Byetta (Exenatide) enhances glucose-dependent insulin secretion by the pancreatic beta-cell, suppresses inappropriately elevated glucagon secretion, and slows gastric emptying. Incretins, such as glucagon-like peptide-1 (GLP-1), enhance glucose-dependent insulin secretion and exhibit other antihyperglycemic actions following their release into the circulation from the gut. Exenatide is an incretin mimetic agent that mimics the enhancement of glucose-dependent insulin secretion and several other antihyperglycemic actions of incretins. Byetta (Exenatide) is indicated as adjunctive therapy to improve glycemic control in patients with type 2 diabetes mellitus, who are taking metformin, a sulfonylurea, or a combination of metformin and a sulfonylurea but have not achieved adequate glycemic control. Byetta (Exenatide) therapy should be initiated at 5 mcg per dose, administered twice daily, at any time within the 60-minute period before the morning and evening meals. Byetta (Exenatide) should not be administered after a meal. Based on clinical response, the dose of Byetta (Exenatide) can be increased to 10 mcg twice daily after 1 month of therapy. Each dose should be administered as a SC injection in the thigh, abdomen, or upper arm. Nausea, vomiting, diarrhea, dizziness, headache, and dyspepsia are reported side effects of the drug.

Symlin = Pramlintide M/A: Symlin (Pramlintide acetate) is an antihyperglycemic drug for use in patients with diabetes treated with insulin. Pramlintide is a synthetic analog of human amylin, a naturally occurring neuroendocrine hormone synthesized by pancreatic beta cells that contributes to glucose control during the postprandial period. Symlin (Pramlintide acetate) is given at mealtimes and is indicated for Type I and Type II diabetes as an adjunct treatment in patients who use mealtime insulin therapy and who have failed to achieve desired glucose control despite optimal insulin therapy.

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Symlin (Pramlintide acetate) alone does not cause hypoglycemia. However, Symlin (Pramlintide acetate) is indicated to be co-administered with insulin therapy, and in this setting Symlin (Pramlintide acetate) increases the risk of insulin-induced severe hypoglycemia, particularly in patients with Type I diabetes. Severe hypoglycemia associated with Symlin (Pramlintide acetate) occurs within the first 3 hours following a Symlin (Pramlintide acetate) injection. Symlin (Pramlintide acetate) and insulin should always be administered as separate injections and never be mixed since the pharmacokinetic parameters of Symlin (Pramlintide acetate) were greatly altered when mixed with regular, NPH, and 70/30 premixed formulations of recombinant human insulin. When initiating therapy with Symlin (Pramlintide acetate), initial insulin dose reduction is required in all patients (both type II and type I) to reduce the risk of insulin-induced hypoglycemia. As this reduction in insulin can lead to glucose elevations, patients should be monitored at regular intervals to assess Symlin (Pramlintide acetate) tolerability and the effect on blood glucose, so that individualized insulin adjustments can be initiated. In patients with insulin-using type II diabetes, Symlin (Pramlintide acetate) should be initiated at a dose of 60 mcg and increased to a dose of 120 mcg as tolerated. In patients with type I diabetes, Symlin (Pramlintide acetate) should be initiated at a dose of 15 mcg and titrated at 15 mcg increments to a maintenance dose of 30 mcg or 60 mcg as tolerated. Nausea, vomiting, diarrhea, dizziness, headache, and dyspepsia are reported side effects of the drug. Inhalation Powder: Exubera = Insulin Human, rDNA

(H)

M/A:

Insulin lowers blood glucose concentrations by stimulating peripheral glucose uptake by skeletal muscle and fat, and by inhibiting hepatic glucose production. Insulin inhibits lipolysis in the adipocyte, inhibits proteolysis, and enhances protein synthesis. Exubera consists of blisters containing human insulin inhalation powder, which are administered using the Exubera Inhaler. Exubera blisters contain human insulin produced by recombinant DNA technology utilizing a non-pathogenic laboratory strain of Escherichia coli (K12). Each unit dose blister of Exubera contains a 1 mg or 3 mg dose of insulin in a homogeneous powder formulation. Exubera is indicated for the treatment of adult patients with diabetes mellitus for the control of hyperglycemia. Exubera has an onset of action similar to rapid-acting insulin analogs and has a duration of glucose-lowering activity comparable to subcutaneously administered regular human insulin. In patients with type 1 diabetes, Exubera should be used in regimens that include a longer-acting insulin. In patients with type 2 diabetes, Exubera can be used as monotherapy or in combination with oral agents or longer-acting insulins.

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It differs from regular human insulin by its rapid onset of action. When used as a mealtime insulin, the dose of Exubera should be given within 10 minutes before a meal. Hypoglycemia is the most commonly reported adverse event of insulin therapy, including Exubera. It has a more rapid onset of glucose-lowering activity compared to subcutaneously injected regular human insulin. Exubera has a duration of glucose-lowering activity comparable to subcutaneously injected regular human insulin and longer than rapid-acting insulin. A 1 mg blister of Exubera inhaled insulin is approximately equivalent to 3 IU of subcutaneously injected regular human insulin. A 3 mg blister of Exubera inhaled insulin is approximately equivalent to 8 IU of subcutaneously injected regular human insulin. Chest pain, dry mouth and otitis media are reported side effects of the drug.

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Reference Guide for the Pharmacy Licensing Exam Theory-Third Edition 42. Expectorant, Laxative & Antitussive
Guaifenesin Hydromorphone hydrochloride Diphenhydramine Dextromethorphan hydrobromide Codeine Benzonatate * = = = = = =

Krisman

Hytuss, Glycotuss, Guiatuss, Robitussin, Humibid Dilaudid Benadryl Robitussin DM, Tuss DM, Naldecon senior DX Codeine Tessalon

Guaifenesin increases the production of respiratory tract fluid that helps to reduce the viscosity of a cough. Dextromethorphan, Codeine, Diphenhydramine and Hydromorphone may reduce the cough reflex by their direct effect on the cough center in the medulla. Drug Guaifenesin Dextromethorphan Codeine Benzonatate Diphenhydramine Recommended dose 200 to 400 mg every 4 to 6 hours 10 to 20 mg every 4 to 6 hours 10 to 20 mg every 4 to 6 hours 100 mg t.i.d. 25 mg every 4 to 6 hours

LAXATIVE Bulk forming laxatives Calcium polycarbophil = Psyllium = Methylcellulose = Lubricant laxatives Mineral oil Stimulant Laxatives Bisacodyl Casanthranol Cascara sagrada Phenolphthalein Senna Stool softeners Docusate = Colace, Surfak, Dialose = = = = = Carters pill, Dacodyl, Dulcolax, Fleet Bisacodyl Black drought Generic Ex-lax, Feen a Mint Senokot = Nujol, Agoral, Kondremul, Liqui dose, Neo cultol, Petrogalar, Fleet enema Fibercon, Mitrolan, Equalactin Hydrocil instant, Metamucil, Fiberall, Modane bulk, Reguloid, Perdiem Methylcellulose

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Hyperosmotic Glycerine Lactulose Hyperosmotic saline Magnesium citrate = Magnesium hydroxide = Bulk forming Laxatives * Citroma Milk of Magnesia = =

Krisman

Fleet babylax Cholac, Chronulac, Duphalac, Enulose, Constulose, Kristalose

They absorb a large amount of water and expand. As a result, the bulk and moisture content of the stool increases. Therefore, they should be taken with a large amount of water to reduce the problem of constipation. The onset of action occurs within 12 to 36 hours. The concurrent use of Tetracycline with Calcium polycarbophil may not be recommended since it may reduce the absorption and therapeutic effects of Tetracycline.

* *

Lubricant Laxatives * They increase water retention in stool by forming a water immiscible film on the surface of stool and intestine. The onset of action occurs within 6 to 8 hours. Concurrent use of mineral oil with Coumadin, oral contraceptives, and fat soluble vitamins may not be recommended since they may reduce the absorption of the above drugs.

* *

Stimulant Laxatives * * They increase the peristalsis movement of the intestine. Bisacodyl should not be taken with milk or any antacids products, since it may lose its enteric coating form at an elevated G.I. pH. Weakness, incoordination and hypotension have been reported in elderly patients using stimulant laxatives. Stimulant laxative is contraindicated to use in pregnant women.

Stool softeners * They reduce the interfacial tension between the content of the bowel and water, and promote the permeation of additional liquid in the stool to form a softer mass. The onset of action occurs within 1 to 2 days. Docusate Na is contraindicated in patients with sodium restricted diets.

* *

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Antibiotics and their effects on pregnancy Anti-infective agents * * Amphotericin B Chloramphenicol Category B C Comments Relatively safe

Krisman

Use with caution. It may cause gray baby syndrome in newborns. Relatively safe Use with caution Relatively safe Relatively safe Use with caution Relatively safe May cause fatal abnormalities Use with care May cause damage to the VIII cranial nerve in newborns. Use with caution Mutagen and carcinogen in bacteria and rodents Relatively safe Relatively safe Use with caution. May cause nephro, oto toxicities in infants Extremely teratogenic Permanent yellow and brown staining of teeth. Use with caution during pregnancy Relatively safe

* * * * * * * * *

Cephalosporin Chloroquine Clavulanic acid Clindamycin Clofazimine Clotrimazole Doxorubicin Fluconazole Gentamicin

B C B B C B D C C

* *

Ketoconazole Metronidazole

C C

* * *

Nitrofurantoin Sulfonamide Streptomycin

B B D

* *

Ribavirin Tetracycline

X D

Trimethoprim

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Reference Guide for the Pharmacy Licensing Exam Theory-Third Edition 54-TPN (Total Parenteral Nutrition)

Krisman

Intravenous nutritional therapy is required when normal enteral feeding is not possible or is inadequate for nutritional requirements. TPN (Total Parenteral Nutrition) is a combination of dextrose, amino acids and lipids in one infusion bag. It is also known as 3-in-1 or triple mixture. One or more of the following nutrients are required for TPN: Dextrose Fat Amino acids Vitamins Electrolytes Trace elements Alcohol Dextrose: It is a source of nonprotein calories. It reduces protein and nitrogen losses, promotes glycogen deposition, and prevents ketosis. It is available in various strengths. 2.5%, 5% and 10% strengths are used for peripheral infusion, whereas higher strengths such as 25%, 50% and 70% are normally given by central venous catheter to minimize irritation of skin. 1gm of hydrated dextrose (I.V.) provides 3.4 calories, whereas 1 gm of anhydrous dextrose provides 4.3 calories. Fat emulsion: They provide essential fatty acids and calories. They are available in two strengths: 10% and 20%.

* 1. 2. 3. 4. 5. 6. 7. *

I.V. fat emulsions are prepared from either soybean or sunflower oil. It provides a mixture of neutral triglycerides generally rich in unsaturated fatty acid. The principal component of fatty acids are linoleic acid, palmitic acid, and stearic acid. 1 ml of 10% fat emulsion normally provides 1.1 calories, whereas 1 ml of 20% fat emulsion provides 2 calories. Amino acids/proteins: Protein for parenteral administration is available as synthetic amino acids. Normally, amino acid products which are used for TPN purposes are a mixture of essential, nonessential and semi essential amino acids.

The amino acid requirement may differ for a patient suffering from a particular disease. For example, a patient suffering from a hepatic disease may require more branch chain amino acids and a reduced amount of aromatic amino acids.

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Protein formulations designed for physiological stress are a mixture of branch chain amino acids and standard amino acids. A patient suffering from renal failure may require an increased amount of essential amino acids or only essential amino acids. Each gram of protein or amino acid provides 4 calories. Alcohol: It normally provides calories and helps in replenishing fluid. Each ml of alcohol provides 5.6 calories. Nutrients Kcal/calories 3.4 kcal/gm 4 kcal/gm 9 kcal/gm 1.1 kcal/ml 2 kcal/ml 4.3 kcal/gm 5.6 kcal/ml 8.3 kcal/gm

* * * * * * * *

Dextrose Amino acid Fat Fat emulsion 10% Fat emulsion 20% Glycerol Alcohol Medium chain triglyceride

Solubility of calcium phosphate: Many times, the snowflake precipitates of calcium phosphate may occur in parenteral feeding formulations. Administering a parenteral feeding formulation containing calcium phosphate crystals may occlude blood vessels, which may result in death and respiratory distress. * This can be prevented by using calcium gluconate instead of calcium chloride. When used in a solution, calcium chloride dissociates more than calcium gluconate; thus it may provide more free calcium to associating with phosphate. By using calcium gluconate, the precipitates of calcium phosphate can be controlled to a certain extent.

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Reference Guide for the Pharmacy Licensing Exam Theory-Third Edition 55-Renal Failure

Krisman

* 1. 2. 3.

Renal failure is normally classified as : Acute Renal Failure (ARF) Subacute Renal Failure Chronic Renal Failure (CRF) Acute Renal Failure

Actual Renal Failure: It is defined as when a rapid loss of renal function results in azotemia. Azotemia is defined as an accumulation of nitrogenous products in the blood. Acute rental failure may progress to chronic renal failure (a decline in renal function over months to years). Acute rental failure normally evolves through three phases : Oliguric Phase Diuretic Phase Recovery Phase Oliguric Phase: This phase normally begins with a decrease in urine output to 50 to 400 ml/day. If urine volume is less than 50 ml/day, it will be defined as anuria. This phase may last for several days to a week. Diuretic Phase: The second phase of acute renal failure begins with recovery from the oliguric phase. In this phase, the volume of urine is increased, however patients may still remain azotemic. This phase normally last for several days. Recovery phase: The final phase is defined as the recovery phase. In this phase, the renal function may show a gradual improvement and a decline in azotemia. During this phase, the ability of the kidneys to concentrate or dilute urine returns to normal. The phase continues for the period of weeks to months.

* 1. 2. 3. 1. * *

2. * *

3. *

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Laboratory Tests for assessment of renal function: Creatinine clearance: * *

Krisman

Inulin and creatinine may be used to measure the Glomerular Filtration Rate (GFR). The normal creatinine clearance in a healthy adult is 80 to 120 ml/minute. A creatinine clearance of less than 60 ml/minute indicates renal function impairment. The normal serum creatinine concentration in a healthy individual is 0.6 to 1.2 mg/dl. Increases in the serum creatinine concentration also suggests renal function deterioration. (140 - age in years x weight in kgs) Male (Creatinine Clearance) = 72 x serum creatinine concentration (mg/dL)

where 1dL = 100 ml Female (Creatinine Clearance) = Male Creatinine clearance x 0.85 BUN : Serum creatinine ration * * In normal conditions, BUN:SrCr remains constant at 10:1 or 15:1. When values elevate to 20:1 or more, it indicates significant renal function impairment. Proteinuria: * * * It is defined as when more than 150 mg of protein are lost through urine in 24 hours. Proteinuria in excess of 3.5 gm/1.75 m2 /day is defined as nephrotic syndrome proteinuria. The presence of protein (especially albumin) in urine may primarily indicate a loss of integrity of filtration ability of the glomerular filter. Causes of Acute Renal Failure: A. Prerenal acute failure: Any reduction in blood delivery to the kidneys may cause prerenal acute failure. Volume depletion due to diarrhea, vomiting or diuresis Acute hemorrhage Hypotension Renal artery constriction (ACE inhibitor, NSAID) Heart failure (Beta blocker)

1. 2. 3. 4. 5.

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B.

Krisman

Intrinsic acute renal failure: It is normally caused by any factor that damages renal parenchymal tissues. Intrinsic acute renal failure is also known as parenchymal acute renal failure, intrarenal acute failure and acute tubular necrosis. Glomerulonephritis Post infectious glomerulonephritis Vasculitis Renal ischemia Pyelonephritis Drug induced ischemia Acute tubular necrosis ischemia: Aminoglycosides Amphotericin Interstitial ischemia or nephritis Cimetidine Ciprofloxacin Penicillin Post renal acute failure: This normally results from an obstruction in the urine flow at any point between the renal calces and the urinary bladder. Calculi Uric acid crystals Prostatic hypertrophy Malignancy Chronic Renal Failure

1. 2. 3. 4. 5. 5. A. 1. 2. B. 1. 2. 3. C.

1. 2. 3. 4.

It is a progressive disease. In this type of disease, renal function is impaired for a prolonged period and the prospect of recovery seems unlikely. As CRF progresses, patients usually develop uremia; it is defined as symptomatic renal failure. Terminologies:

1.

Renal reserve: It is the difference between the normal and the maximally achievable glomerular filtration rate. Renal insufficiency: It is defined as when there is a mild reduction in the glomerular filtration rate in the absence of overt signs and symptoms. Azotemia: It is a laboratory diagnosis in which extensive levels of BUN and creatinine have been found due to declined GFR. ESRD: When dialysis becomes necessary to sustain a patients life, it is defined as ESRD (End Stage Renal Disease).

2.

3.

4.

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* The major causes of ESRD: Disease Diabetes Hypertension Glomerulonephritis Cystic kidney disease Interstitial nephritis * * 1. 2. 3. 1. * Percentage 33 28 12 3 3

Krisman

Factors affecting progression of CRF: The progression of chronic renal disease occurs over months to years. Factors that affect CRF are: Hypertension High-protein diet Dyslipoproteinemias Hypertension: Renal injury normally increases single-nephron GFR as one of the adaptive procedures since this mechanism helps the body to maintain hemostasis. However, the increased perfusion of residual nephrone to maintain hemostasis may produce the deleterious effect on the remaining nephrons. Hypertension is directly associated with an increased single-nephron glomerular filtration rate, and therefore untreated systematic hypertension may lead to CRF. High-protein diet: Dietary protein ingestion also increases single-nephron CRF. Restriction of dietary protein and phosphorus may delay the progression of CRF. Dyslipoproteinemia: Renal disease or failure normally alters the metabolism of lipoproteins, and this may increase the serum triglyceride concentration in patients. Although reduction of this elevated serum triglyceride by antihyperlipidemic drugs may not help in delaying the progression of CRF, it may prevent cardiovascular diseases such as atherosclerosis and systematic hypertension. The relationship between other diseases/conditions and CRF:

2. *

3. *

1. 2. 3. 4.

Analgesic nephropathy Lithium nephropathy Sodium/fluid retention Hyperkalemia

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5. 6. 7. 8 Metabolic acidosis Calcium and phosphate abnormalities Diabetes Diabetic nephropathy Analgesic nephropathy: *

Krisman

It is characterized by renal papillary necrosis as a primary lesion, and by chronic interstitial nephritis as a secondary lesion. Analgesic nephropathy is a part of the analgesic syndrome. The prolonged use of acetaminophen or NSAIDs may result in analgesic nephropathy. Management:

* *

Avoid use of NSAIDs and acetaminophen. High fluid intake Lithium nephropathy:

The prolonged use of lithium may cause a decline in renal ability to concentrate urine and GFR. Nephrotoxic risk is higher with elevated lithium serum concentrations. Management:

* *

Avoid lithium containing medication if possible. Monitor serum lithium concentration closely. Sodium/water retention (edema):

Patients with CRF may retain large amounts of sodium and water. This may lead to high blood pressure, weight gain, 2+ pedal edema, and pulmonary congestion. Management:

* 4. *

Restrict sodium and water consumption Hyperkalemia: The normal potassium concentration in serum is 3.5 to 5 mEq/L, which is well maintained during chronic renal failure by the adaptive mechanism of the body. However, an exogenous potassium load in the form of potassium-containing medications or supplements, an endogenous potassium load in case of hemolysis of RBC or rhabdomyolysis, and metabolic or respiratory acidosis may elevate serum potassium concentrations.

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Management: *

Krisman

Hyperkalemia may lead to cardiac arrhythmia. This can be prevented by the administration of calcium in the form of I.V. calcium gluconate. Calcium does not have any effect on the serum potassium concentration, however it will protect the myocardium from the dangerous effects of potassium. An I.V. administration of sodium bicarbonate may also help in reducing an elevated potassium concentration. It encourages the movement of extracellular potassium ions back into cells. The I.V. administration of glucose and insulin is another method to shift extracellular potassium into cells. Insulin stimulates potassium uptake by skeletal muscles and hepatic cells. Glucose is given simultaneously to avoid hypoglycemia. The use of calcium gluconate, sodium bicarbonate, glucose and insulin have no effect on reducing the total body load of potassium. They just shift potassium concentrations from the extracellular region to the intracellular region. Sodium polystyrene sulfonate is a cation exchange resin which exchanges sodium ions for potassium ions in the intestinal tract, and reduces the total body load of potassium. Metabolic acidosis:

A high blood carbon dioxide content, and chloride and potassium concentration is normally observed in patients with CRF. This may lead to metabolic acidosis in individuals suffering from renal diseases. Management:

Patients should receive I.V. sodium bicarbonate to correct metabolic acidosis. Electrolytes and metabolic disturbances:

* *

Hypermagnesemia, hyperphosphatemia and hyperuricemia are reported with CRF patients. Severe hypermagnesemia may cause nausea, vomiting, cardiac function impairment, lethargy and confusion. Hyperphosphatemia and secondary hyperparathyroidism play an important role in the development of osteopathy associated with CRF patients. An elevated serum concentration of phosphate may reduce the serum concentration of ionized calcium, and this may stimulate the release of PTH. Persistent hyperphosphatemia also reduces calcium absorption from the gut. This will lead to severe hypocalcemia in patients suffering from chronic renal failure. To counteract a low serum concentration of calcium, the body stimulates the mobilization of bone calcium to blood, which leads to a softening of bones and osteoporosis. Hyperuricemia is also reported due to diminished urinary excretion of uric acid.

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Management: *

Krisman

Avoid magnesium, phosphate-containing antacids and laxatives. Administer aluminum-containing antacids, calcium carbonate, calcium citrate, and calcium acetate to reduce the elevated level of phosphate. Anemia:

Patients with CRF inevitably develop anemia. The principal cause of this anemia is a decreased production of erythropoietin in the kidneys. This may lead to a reduced formation of erythrocytes. The RBC life span is reduced to 30 to 60% under normal levels in CRF patients. Iron, folic acid and vitamin B12 deficiency may also lead to anemia in CRF patients. Blood loss due to impaired hemostasis of uremia also contributes to iron deficiency anemia. Aluminum intoxication due to overingestion of aluminum containing medication may also lead to anemia in CRF patients. Management:

* * * *

Correct the anemia by administration of vitamin B12, iron and folic acid supplements. By administering recombinant human erythropoietin (Epogen) in CRF patients. By avoiding aluminum containing antacids and related products. By administering hemostatic agents such as cryoprecipitate or DDAVP to prevent uremia induced bleeding. Diabetes:

* *

As CRF progresses, the serum glucose concentration is reduced as well as the insulin requirement. In healthy individuals, six to eight units of insulin are degraded by the kidneys every day. In the case of CRF, less insulin is cleared, and its metabolic half-life is increased. This may provide more insulin to work on available glucose and may lead to severe hypoglycemia. Management:

* *

Monitor the blood glucose concentration. Adjust dose of antidiabetic drugs. Diabetic nephropathy:

It is defined as a urinary albumin excretion rate of 300 mg/24 hours or more in a person with diabetes in the absence of other renal diseases. It accounts for nearly 50% of end stage renal disease. Management:

* * *

Monitor and maintain the blood glucose concentration. Avoid high dietary protein intake. Control systematic hypertension.

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Reference Guide for the Pharmacy Licensing Exam Theory-Third Edition 56-Interpretation Of Clinical Laboratory Tests
Laboratory Tests 1. ALT (SGPT) Normal Units 0 to 3.5 U/L Comments

Krisman

More specific for liver test compared to AST, value normally increased in liver disease. Normally elevated during myocardial infarction, liver and muscle injury. Increase in bile duct obstruction, liver disease and Pagets disease of bone. Elevated with prostate carcinoma. Increase in renal dysfunction, G.I. bleeding, dehydration and high protein intake. Increase in renal failure. Decrease in renal failure. Values may increase by I.M. injection, myocardial infarction and acute psychotic episodes. Isoenzyme CK-MM in skeletal muscles; CK-MB in myocardial; CK-BB in brain. Increase in chronic alcoholics. Increased LDL or decreased HDL may increase the risk for atherosclerosis.

2.

AST (SGOT)

0 to 35 U/L

3.

Alkaline phosphate

30 to 120 U/L

4. 5.

Acid phosphatase BUN

0 to 5.5 U/L 8 to 18 mg/dl

6. 7. 8.

Creatinine Creatinine clearance Creatinine kinase

0.6 to 1.2 mg/dl 80 to 120 ml/min 0 to 150 U/L

9. 10.

GGT Cholesterol

0 to 30 U/L Total < 200 mg/dl LDL < 130 mg/dl HDL > 50 mg/dl < 160 mg/dl

11. 12.

Triglycerides Bilirubin Total Direct

Increased by alcohol and saturated fats.

0.1 to 1 mg/dl 0 to 0.2 mg/dl 3.5 to 5 mEq/L

Increased with hemolysis, cholestatic, liver injury.

13.

Potassium

Increased by renal dysfunction, acidosis, burns, and hemolysis. Decreased by diuretics, alkalosis, vomiting and severe diarrhea. Value may elevate in hypertension.

14.

Sodium

135 to 147 mEq/L

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Laboratory Tests 15. Calcium Normal Units 4.4 to 5.1 mEq/L Comments

Krisman

Regulated by body skeletal redistribution, parathyroid hormone, vitamin D and calcitonin. Decreased by malabsorption, severe diarrhea, alcoholism, pancreatitis, diuretics and hyperaldosteronism; increased by renal failure. Increased with renal dysfunction, hypervitaminosis D, and hypoparathyroidism. Decreased with excess aluminum antacids, malabsorption, renal losses. Decreased by G.I. loss of chloride-rich fluid due to vomiting, diarrhea, G.I. suction, intestinal fistulas and overdiuresis. Increased in diabetes or by adrenal corticosteroids.

16.

Magnesium

1.6 to 2.4 mEq/L

17.

Phosphate

2.5 to 5 mg/dl

18.

Chloride

95 to 105 mEq/L

19.

Glucose

70 to 110 mg/dl

20.

Uric acid

2 to 7 mg/dL

Increased in gout, neoplastic, or myeloproliferative disorder.

21.

ESR Male Female 0 to 20 mm/hr 0 to 30 mm/hr Increased with inflammation, infection, neoplasms, connective tissues disorders, pregnancy and nephritis.

22.

HCT (Hematocrit) Male Female 39% to 49% 33% to 43% Decreased with anemias, bleeding, hemolysis and overhydration. Increased with polycythemia, chronic hypoxia, dehydration.

23.

Hemoglobin Male Female 14 to 18 gm/dL 11.5 to 15.5 gm/dl 26 to 34 < 26 > 34 Similar to hematocrit.

24.

MCH

It measures weight of hemoglobin in average RBC. Hypochromic anemia. Hyperchromic anemia.

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Laboratory Tests 25. MCHC Normal Units 31 to 37 Comments

Krisman

< 31 > 37

It also measures concentration of hemoglobin in average RBC. It decreases in hypochromia or in iron deficiency. Hypochromic anemia. Hyperchromic anemia.

26.

MCV

80 to 100 < 80 > 100

Normal values between 80 to 100. Value < 80 indicates iron deficiency anemia (microcytic). Value > 100 indicates vitamin B12 or folic acid deficiency anemia. < 150,000 indicates thrombocytopenia or increased risk of bleeding.

27.

Platelets

150,000 to 300,000/mm3 0.1% to 2.4% > 2.4% < 0.1%

28.

Reticulocytes

Blood loss, hemolytic anemia. Polychromasia.

29.

RBC Men Women 4.3 to 5.9 million/mm3 3.5 to 5 million/mm3

30.

WBC

4000 to 11,000/mm3

It consist of neutrophils, lymphocytes, monocytes, eosinophils, and basophils. Indicates bacterial infections.

> 11,000

31.

Neutrophils Lymphocytes Monocytes Eosinophils Basophils

54 to 62% 25 to 33% 3 to 7% 1 to 3% < 1%

Neutrophils increase during bacterial or fungal infections. Eosinophils increase with allergies and parasitic infections.

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Reference Guide for the Pharmacy Licensing Exam Theory-Third Edition 57-Dementia

Krisman

Definition: Alzheimers disease is a progressive form of dementia that occurs in middle age or later, characterized by loss of short-term memory, deterioration in behavior and intellectual performance, confusion, and slowness of thought. The damage to the cholinergic pathway in the brain may be responsible for this. A. Reversible cholinesterase inhibitors: Cognex Exelon Aricept Razadyne Razadyne ER B. = = = = = Tacrine Rivastigmine Donepezil Galantamine Galantamine

N-methyl-D-aspartate receptor antagonist (NMDA): Namenda = Memantine

A. M/A:

Reversible cholinesterase inhibitors: These agents reversibly inhibit the metabolism of acetylcholine by temporarily inhibiting enzyme cholinesterase. Cognex (Tacrine), Exelon (Rivastigmine), Razadyne (Galantamine) and Aricept (Donepezil) are indicated for the treatment of mild to moderate dementia of the Alzheimers type. Cognex (Tacrine) therapy is associated with severe hepatic toxicity. This can be prevented by regularly monitoring the serum transaminase level (specially ALT). It is available in capsule form. Ulcers, neutropenia and seizures have been reported with Cognex (Tacrine) therapy. Weight loss and anorexia are principal side effects of Exelon (Rivastigmine). Patients should be watched for signs and symptoms of anorexia. G.I. ulcers, bleeding, seizure and anesthesia are also reported with Exelon (Rivastigmine) therapy. It is available in capsule and oral solution forms. Razadyne (Galantamine) has been associated with nausea, vomiting, anorexia and weight loss, and syncope. It is available in tablet and oral solution forms. The principal advantage of Aricept (Donepezil) is its once single-daily dosage regimen. This is especially important since patients have dementia. Aricept (Donepezil) has the longest half-life about 70 hours among all the currently available dementia agents. Therefore, its use requires great caution in patients with impaired liver and renal functions. It is available in tablet dosage form.

* *

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Common Adverse reactions: * * * * * Nausea and vomiting Anorexia and weight loss GI ulcer and bleeding Seizure and syncope Bradycardia and sick sinus syndrome Drug * * * * Tacrine Rivastigmine Galantamine Donepezil Dose 10 mg po q.i.d. 1.5 mg po b.i.d. 4 mg po b.i.d. 5 to 10 mg po q.d. Dosage from

Krisman

Capsule Capsule, oral solution Tablet, oral solution, capsule ER Tablet

Namenda = Memantine M/A: Namenda (Memantine) is an NMDA receptor antagonist. Persistent activation of the central nervous system NMDA receptors by the excitatory amino acid glutamate normally causes signs and symptoms of Alzheimers disease. Namenda (Memantine) binds to these NMDA receptors. The recommended therapeutic dose of Namenda (Memantine) is 5 to 10 mg once daily. It is available in tablet dosage form. Dizziness, confusion, headache, constipation, coughing and hypertension are principal side effects of the drug.

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58-TUBERCULOSIS

Krisman

Definition: It is an infectious disease caused by the bacillus of Mycobacterium tuberculosis and Mycobacterium leprae, and is characterized by the formation of nodular lesions. A. First-line treatment: Isoniazid Rifampin Pyrazinamide Streptomycin Ethambutol B. Second-line treatment Cycloserine = Ethionamide = Capreomycin = Kanamycin = Ciprofloxacin = Ofloxacin = Levofloxacin = Sparfloxacin = P-amino-salicylic acid = Rifabutin = Rifapentine = C. Combination agents Pyrazinamide + Isoniazid + Rifampin Isoniazid = INH M/A: It inhibits the synthesis of mycolic acids, an essential component of the bacterial cell wall of M.tuberculosis organisms. The recommended therapeutic dose of Isoniazid is 300 mg per day as a single dose or 900 mg two to three times weekly. It is available as 300 mg of oral strength (tablet). The prolonged use of Isoniazid may cause vitamin B6 (Pyridoxine) deficiency and peripheral neuritis. Patients should be supplemented with vitamin B6 during therapy. Severe and fatal hepatitis is the principal side effect of Isoniazid. Patients should be regularly checked for hepatic enzymes (specifically AST and ALT). Optic neuritis, peripheral neuropathy, convulsion, jaundice, fever and skin rash are reported side effects of the drug. = Rifater Seromycin Trecator-SC Capastat Kantrex Cipro Floxin Levaquin Zagam Paser Mycobutin Priftin = = = = = Isoniazid (INH), Nydrazid Rifadin, Rimactane Pyrazinamide (PZA) Streptomycin Myambutol

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Rifadin, Rimactane = Rifampin M/A: *

Krisman

Rifampin inhibits DNA-dependent RNA polymerase activity in susceptible microorganisms. It is indicated for the treatment of all forms of tuberculosis and symptomatic carries of N. meningitidis to eliminate meningococci from the nasopharynx. A three drug regimen (Isoniazid, Rifampin and Pyrazinamide) is recommended in the initial phase of therapy. The recommended therapeutic dose of the drug is 10 mg/kg in a single daily administration, not to exceed 600 mg per day. It is available as 150 and 300 mg of oral strength (capsule) and powder for injection. Hepatotoxicity and hyperbilirubinemia are principal side effects of the drug. It may cause a orange to yellow discoloration of the urine.

Pyrazinamide = PZA M/A: Pyrazinamide is a pyrazine analog of nicotinamide. It exerts the bacteriostatic as well as bactericidal effects against M. tuberculosis. It is indicated for the initial treatment of active tuberculosis. The recommended therapeutic dose of PZA is 15 to 30 mg/kg once daily (not to exceed 2 gm/day). It is available as 500 mg of oral strength (tablet). It inhibits renal excretion of urates and therefore it should be carefully prescribed to patients suffering from gout. Hepatotoxicity, hyperuricemia, nausea, vomiting, and interstitial nephritis are reported side effects of the drug.

* *

Streptomycin = Streptomycin M/A: * It is a bactericidal antibiotic that interferes with protein synthesis of M. tuberculosis. The recommended therapeutic dose of the drug is 15 mg/kg via intramuscular route. It is available as a lyophilized cake for intramuscular administration. Severe nephrotoxicity, ototoxicity, and neurotoxicity are major side effects of the drug. Creatinine clearance (CrCl) should be monitored regularly to check the renal function of patients. The simultaneous administration of ethacrynic acid, furosemide, and mannitol should be strictly avoided to prevent the nephro and ototoxic effects of Streptomycin. Vestibular ototoxicity (nausea, vomiting and vertigo), cochlear ototoxicity (deafness), rash, fever, muscle weakness and renal toxicity are reported side effects of the drug.

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Myambutol = Ethambutol M/A:

Krisman

It impairs the cell metabolism of mycobacterium bacilli, arrests the multiplication and causes cell death. The recommended therapeutic dose of Ethambutol is 15 mg/kg as a single oral dose, once every 24 hours. It is available as 100 mg and 400 mg of oral strength (tablets). Patients should be watched for renal and liver function impairment. Ethambutol may have adverse effects on vision. Patients should be regularly checked for visual activity. Aluminum salts or aluminum containing antacids may reduce the absorption of the drug. Simultaneous administration should be avoided. Dermatitis, nausea, vomiting, abdominal pain and precipitation of gout are reported side effects of the drug.

* *

Seromycin = Cycloserine M/A: * It inhibits cell wall synthesis of M.tuberculosis. It is indicated for the treatment of active pulmonary and extrapulmonary tuberculosis, and UTI caused by E.coli. The recommended dose of drug is 250 mg by mouth twice daily. Convulsions, anxiety and tremor are principal neurotoxic effects of the drug. This can be prevented by adding pyridoxine (vitamin B6) to the therapeutic regimen. Somnolence, headache, confusion, skin rash and hyperirritability are also reported with the drug.

* *

Trecator = Ethionamide M/A: * * It has bacteriostatic and bactericidal effects against M.tuberculosis. It is indicated for the treatment of active tuberculosis. The recommended therapeutic dose of the drug is 15 to 20 mg/kg/day once daily with a maximum dose up to 1 gm/day. Hepatotoxicity is reported. Patients should be regularly checked for liver enzyme elevation. Depression, drowsiness, peripheral neuritis and peripheral neuropathy, blurred vision, diplopia, and liver toxicity are reported side effects of the drug. Vitamin B6 should be given to prevent peripheral neuropathy and neuritis.

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Capastat = Capreomycin *

Krisman

It is indicated for the treatment of pulmonary infections caused by capreomycin-susceptible strains of M tuberculosis. The recommended therapeutic dose of the drug is 1 gm daily via I.M. or I.V. for two to four months, followed by 1 gm two to three times weekly. Ototoxicity, nephrotoxicity, neuromuscular blockage and hypokalemia are principal side effects of the drug. Tinnitus, vertigo, pain and bleeding at the injection sites are also reported.

Paser = Para-Aminosalicylate Sodium M/A: * * * It has bacteriostatic action against M. tuberculosis. It is indicated for the treatment of tuberculosis in combination with other active agents. The recommended therapeutic dose of the drug is 4 gm by mouth three times a day. Hepatitis, rash and crystalluria are principal side effects of the drug. Fever, nausea, vomiting, diarrhea, abdominal pain, hypoglycemia and optic neuritis are also reported.

Priftin = Rifapentine M/A: * * * It inhibits DNA-dependent RNA polymerase activity in susceptible microorganisms. It is indicated for the treatment of pulmonary tuberculosis. The recommended therapeutic dose of Rifapentine is 600 mg (four 150 mg tablets) twice weekly. Rifapentine may cause a red-orange discoloration of body tissues or fluids. Rash, hyperbilirubinemia, proteinuria, hyperuricemia, and an increase in ALT and AST are reported side effects of the drug.

Mycobutin = Rifabutin M/A: * It inhibits DNA-dependent RNA polymerase activity in susceptible microorganisms. It is indicated for the prevention of disseminated Mycobacterium avium complex (MAC) in patients with advanced HIV infection. The recommended therapeutic dose of the drug is 300 mg once daily. It can also be taken in two divided doses. It is classified as an enzyme inducer drug. Neutropenia and thrombocytopenia are reported side effects of the drug. It may cause the discoloration of urine. Abdominal pain, headache, diarrhea, vomiting, rash, and an increased AST and ALT are also reported with the drug.

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Reference Guide for the Pharmacy Licensing Exam Theory-Third Edition 59-Multiple Sclerosis

Krisman

Definition: It is a chronic disease of the nervous system affecting young and middle-aged adults. The myelin sheaths surrounding nerves in the brain and spinal cord are damaged, which affect the function of the nervous system. The course of illness is characterized by recurrent relapses followed by remissions. The disease affects the different parts of the brain and spinal cord. Signs & symptoms: * * * Weakness, rapid involuntary movement of eyes (nystagmus) Numbness, unsteadiness in a limb, shaky movement of limbs (ataxia) Diplopia, defects in speech pronunciations (dysarthria)

Useful tests: * MRI of the brain or cervical cord.

Classification of drugs: A. * Corticosteroids: A high dose of prednisone (60 mg to 80 mg) should be given for 1 week followed by, a tapering dose. I.V Methylprednisolone in a dose of 1 gm for 3 days may be helpful in certain extents. Immunosuppressive agents: Immunosuppressive agents such as Azathioprine (Imuran) and Cyclophosphamide (Cytoxan) may help to prevent the progression of the disease to a certain extent. Muscle relaxants:

B. *

Lioresal = Baclofen M/A: It hyperpolarizes fibers to reduce impulse transmission. It appears to reduce transmission of impulses from the spinal cord to skeletal muscles. It is indicated for the treatment of spasticity caused by multiple sclerosis. The recommended therapeutic dose is 20 mg three times a day. Seizure and CNS depression are major adverse effects associated with this drug. Drowsiness, dizziness, seizure, headache, hypotension and blurred vision are also reported. Abrupt discontinuation of intrathecal baclofen may produce high fever, rebound muscle spasticity and rigidity, multiple organ-system failure, rhabdomyolysis and even death.

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Dantrium = Dantrolene Na

Krisman

M/A: It acts directly on skeletal muscles to interfere with intracellular calcium movement by decreasing excitation and contraction coupling. * It is indicated for the treatment of spasticity resulting from spinal cord injury, stroke, cerebral palsy, and multiple sclerosis. The recommended dose of the drug is 100 mg twice a day to four times a day. Seizure and hepatitis are major complications of therapy. The symptoms of hepatitis are reported in patients taking greater than 800 mg per day of the drug. Patients should be regularly checked for liver enzyme elevation. Drowsiness, dizziness, weakness, constipation, diplopia and taste alteration are also reported. Immunomodulators: Interferon Beta-1a Interferon Beta-1b Glatiramer acetate Interferon Beta * * Rebif, Avonex and Betaseron are indicated for the treatment of multiple sclerosis. The recommended therapeutic dose of Rebif is 44 mcg S.C. three times/week, for Avonex it is 30 mcg I.M. once a week. The recommended dose of Betaseron should be 0.25 mg via S.C. every other day. Seizure, severe depression, flu-like syndrome and cardiac toxicities are principal side effects of interferon Beta. Inflammation at the injection site, pain, asthenia, chills, hemorrhage, migraines and syncope are also reported with the therapy. = = = Rebif, Avonex Betaseron Copaxone

Copaxone = Glatiramer acetate * Copaxone is indicated for the reduction of the frequency of relapses in patients with relapsingremitting multiple sclerosis. The recommended therapeutic dose of Copaxone is 20 mg per day via subcutaneously. Vasodilation, injection site reaction, chest pain, asthenia, anxiety and hypertonia are reported side effects of the drug. Cytotoxic Agents: Mitoxantrone = M/A: Novantrone

Mitoxantrone is a potent inhibitor of the enzyme Topoisomerase. This enzyme is responsible for uncoiling and repairing damaged DNA. It is indicated for the treatment of multiple sclerosis and advanced hormone reflectory prostate cancer.

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*

Krisman

The recommended therapeutic dose of drug for multiple sclerosis is 12 mg/m2,via short I.V. infusion every three months. It should be administered via slow free flowing I..V infusion. It must not be administered via S.C., I.M. or intra-arterial route. The administration via these routes may cause severe local tissue damage. Mitoxantrone is highly cardiotoxic especially with cumulative doses. Patients should be regularly checked for cardiac function. High doses of Mitoxantrone may cause severe myelosuppression especially leukemia. The WBC should be closely monitored. Monoclonal Antibody Tysabri = Natalizumab

Tysabri (Natalizumab) is classified as a recombinant humanized monoclonal antibody. It is indicated for the treatment of multiple sclerosis. The recommended dose is 300 mg IV infusions every 4 weeks. Headache, fatigue, UTI, depression, rash, and arthralgia are reported side effects of the drug.

* *

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Reference Guide for the Pharmacy Licensing Exam Theory-Third Edition 60-Muscle Relaxants

Krisman

A.

Centrally acting muscular analgesics: Flexeril , Amrix Norflex Norgesic Parafon Forte DSC Robaxin Skelaxin Soma Soma comp Soma comp/codeine = = = = = = = = = Cyclobenzaprine Orphenadrine Orphenadrine + Aspirin + Caffeine Chlorzoxazone Methocarbamol Metaxalone Carisoprodol Carisoprodol + Aspirin Carisoprodol + Aspirin + Codeine

B.

Directly acting muscular analgesics: Dantrium = Dantrolene sodium

C.

Centrally acting alpha-2 adrenergic agonists: Zanaflex = Tizanidine

D.

Benzodiazepine Valium = Diazepam

A. *

Centrally acting muscular analgesics: Flexeril (Cyclobenzaprine) and Norflex (Orphenadrine) possess anticholinergic side effects such as drowsiness, dry mouth, tachycardia, palpitation, constipation, increased intraocular pressure of the eyes and urinary retention, therefore it should be carefully prescribed to patients suffering from urinary retention and close-angle glaucoma. Flexeril (Cyclobenzaprine) may also produce arrhythmia, tachycardia and conduction abnormalities. Patients should be watched for signs and symptoms of arrhythmia. Amrix is an extended release capsule formation of Cyclobenzaprine. The recommended therapeutic dose of the drug is 15mg to 30mg qd. Therapy longer than 2-3 weeks is not recommended. The simultaneous administration of Ultram (Tramadol) with Flexeril (Cyclobenzaprine) may increase the risk of seizure. Concurrent use is strictly prohibited. Confusion, anxiety and tremor are reported when Norflex (Orphenadrine) is given with Darvon (Propoxyphene). Concurrent use should be avoided. Severe and fatal hepatotoxicity has been reported with use of Parafon forte (Chlorzoxazone). Patients should be regularly checked for liver function impairment.

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*

Krisman

Skelaxin (Metaxalone) may cause drug induced hemolytic anemia. A WBC should be done regularly when patients are treated with this drug. Therapeutic use of centrally acting muscular analgesics:

Acute and painful musculoskeletal conditions. Common adverse effects:

* * * * * * *

Anticholinergic side effects Drowsiness Dizziness Hypotension Constipation Lightheadedness Nausea and vomiting Drug Cyclobenzaprine Orphenadrine Chlorzoxazone Methocarbamol Metaxalone Carisoprodol Dosage 5 mg po t.i.d 100 mg po bid 500 mg po tid /q.i.d. 1500 mg po q.i.d. for 2-3 days, followed by 1000 mg po q.i.d. 800 mg po tid/q.i.d. 350 mg po tid and hs Dosage forms Tablet, capsule ER Tablet ER, injection Tablet Tablet, injection Tablet Tablet

B.

Directly acting muscular analgesics:

Dantrium = Dantrolene sodium M/A: It acts directly on skeletal muscles to interfere with intracellular calcium movement by decreasing excitation and contraction coupling. * It is indicated for the treatment of spasticity resulting from spinal cord injury, stroke, cerebral palsy, and multiple sclerosis. The recommended dose of the drug is 100 mg, twice a day to four times a day. Seizure and hepatitis are major complications of therapy. The symptoms of hepatitis are reported in patients taking greater than 800 mg per day of the drug. Patients should be regularly checked for liver enzyme elevation. Drowsiness, dizziness, weakness, constipation, diplopia and taste alteration are reported side effects of the drug.

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C. Centrally acting alpha-2 adrenergic agonists:

Krisman

Zanaflex = Tizanidine M/A: * It stimulates alpha-2 adrenergic receptors. It is indicated for short-term treatment of spasticity. The recommended dose of the drug is 4 mg by mouth every 6 to 8 hours. It may cause hypotension and QT interval prolongation, therefore it should be carefully prescribed to patients with cardiac abnormality. Dry mouth, somnolence, asthenia, urinary frequency, flu-like syndrome and rhinitis are also reported. Benzodiazepine

D.

Valium= Diazepam * * It is classified as a benzodiazepine. It is useful as an adjunct therapy in skeletal muscle spasm. The recommended therapeutic dose of Valium (Diazepam) for muscle spasm is 5 to 10 mg I.M./I.V., repeated in 3 to 4 hours if needed, or a dose of 2 to 10 mg po tid/q.i.d.. Drowsiness, dizziness, fatigue, restlessness, constipation and ataxia are reported side effects of the drug.

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Important Cancer-Related Definitions:

Krisman

Mycosis fungoides: A type of non-Hodgkins lymphoma that first appears on the skin. Also called cutaneous T-cell lymphoma. Multiple myeloma: A malignancy of plasma cells (a form of lymphocyte) that typically involves multiple sites within the bone morrow and secretes all or part of a monoclonal antibody. Also called plasma cell myeloma. Neuroblastoma: A leading childhood form of cancer that arises in the adrenal gland or in tissue in the nervous system that is related to the adrenal gland. Neuroblastoma is the most common solid tumor outside the brain in infants and children. It is often present at birth but usually is not detected until later in infancy or childhood.. The most common symptoms are the result of pressure by the tumor or bone pain from metastases. Protruding eyes and dark circles around the eyes are common and are caused by cancer that has spread to the area behind the eye. Neuroblastomas may compress the spinal cord, causing paralysis. Adenocarcinoma: A cancer that develops in the lining or inner surface of an organ. More than 95 percent of prostate cancers are adenocarcinoma. Retinoblastoma: A malignant eye tumor in children, usually under age 5, that arises in cells in the developing retina containing cancer-predisposing mutations in both copies of the gene RB1. The most common sign of retinoblastoma (RB) is a white pupillary reflex to light (leucoria). Strabismus (a lazy eye) is the second most common sign. Squamous cell carcinoma: Cancer that begins in squamous cells thin, flat cells that look like fish scales under the microscope. Squamous cells are found in the tissue that forms the surface of the skin, the lining of hollow organs of the body, and the passages of the respiratory and digestive tracts. Squamous cell carcinomas may arise in any of these tissues. The word squamous came from the Latin squama meaning the scale of a fish or serpent. Pleural effusion: Excess fluid between the two membranes that envelop the lungs. These membranes are called the visceral and parietal pleurae. The visceral pleura wraps around the lung while the parietal pleura lines the inner chest wall. There is normally a small quantity (about 3 to 4 teaspoons) of fluid that is spread thinly over the visceral and parietal pleurae and acts as a lubricant between the two membranes. Any significant increase in the quantity of pleural fluid is a pleural effusion. Hemolytic uremic syndrome: A condition characterized by the breakup of red blood cells (hemolysis) and kidney failure. Hairy Cell Leukemia: A form of chronic leukemia in which malignant B-lymphocytes (a type of white blood cell) are seen in the bone marrow, spleen and peripheral blood; when viewed under the microscope, these cells appear to be covered with tiny hair-like projections. Hairy cell leukemia represents 2% of all leukemia. Melanoma: The most dangerous form of skin cancer, a malignancy of the melanocyte, the cell that produces pigment in the skin. Melanoma is most common in people with fair skin, but can occur in people with all skin colors. Most melanomas present as a dark, mole-like spot that spreads and, unlike a mole, has an irregular border. The tendency toward melanoma may be inherited, and the risk increases with overexposure to the sun and sunburn.

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Gynecomastia: Excessive development of the male breasts.

Krisman

Oligospermia: Fewer sperm than normal. Azoospermia, by contrast, means absolutely no sperm at all. Interstitial pneumonia: It is inflammation of the lung that involves the meshwork of lung tissue (alveolar septa) rather than the air spaces (alveoli). The word interstitial is pertaining to being between things, especially between things that are normally closely spaced. The word interstitial comes from the Latin interstitium, which was derived from inter meaning between and sistere meaning to stand to stand between. Endometriosis: In endometriosis, cells that normally grow inside the uterus (womb) instead grow outside the uterus. Sarcoma: One of a group of tumors usually arising from connective tissue. Most sarcomas are malignant. Many types are named after the type of cell, tissue, or structure involved, as in angiosarcoma, chondrosarcoma, fibrosarcoma, liposarcoma, and osteosarcoma. Refractory: Not yielding (at least not yielding readily) to treatment. Acute lymphoblastic leukemia: An acute (sudden onset), rapidly progressing form of leukemia that is characterized by the presence in the blood and bone marrow of large numbers of unusually immature white blood cells destined to become lymphocytes. Acute lymphoblastic leukemia is also called acute lymphocytic leukemia and is abbreviated ALL. Ubiquitin: It is a highly conserved small regulatory protein that is ubiquitous in eukaryotes. Ubiquitination (or Ubiquitylation) refers to the post-translational modification of a protein by the covalent attachment (via an isopeptide bond) of one or more ubiquitin monomers. The most prominent function of Ubiquitin is labeling proteins for proteasomal degradation. Proteasomes: They are large protein complexes inside all eukaryotes and archaea, as well as in some bacteria. In eukaryotes, they are located in the nucleus and the cytoplasm. The main function of the proteasome is to degrade unneeded or damaged proteins by proteolysis, a chemical reaction that breaks peptide bonds. Enzymes that carry out such reactions are called proteases. Proteasomes are a major mechanism by which cells regulate the concentration of particular proteins and degrade misfolded proteins. The degradation process yields peptides of about seven to eight amino acids long, which can then be further degraded into amino acids and used in synthesizing new proteins. Proteins are tagged for degradation by a small protein called ubiquitin. The tagging reaction is catalyzed by enzymes called ubiquitin ligases. Once a protein is tagged with a single ubiquitin molecule, this is a signal to other ligases to attach additional ubiquitin molecules. The result is a polyubiquitin chain that is bound by the proteasome, allowing it to degrade the tagged protein. Hemoptysis: Spitting up blood or blood-tinged sputum. Abscess: A local accumulation of pus anywhere in the body. Androgen ablation: Treatment designed to suppress or block the production of male hormones.

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Mechanism of actions of antineoplastic agents: *

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Alkylating agents: An alkylating antineoplastic agent is an alkylating agent that attaches an alkyl group to DNA. Since cancer cells generally divide more rapidly than do healthy cells, they are more sensitive to DNA damage; alkylating agents are used clinically to treat a variety of tumors. Anthracyclins: Anthracyclins inhibit DNA and RNA synthesis by intercalating between base pairs of the DNA/RNA strand, thus preventing the replication of rapidly-growing cancer cells. They also create iron-mediated free oxygen radicals that damage the DNA and cell membranes. Methotrexate: Methotrexate competitively and reversibly inhibits dihydrofolate reductase (DHFR), an enzyme that is part of the folate synthesis metabolic pathway. The affinity of methotrexate for DHFR is about one thousand-fold that of folate for DHFR. Dihydrofolate reductase catalyses the conversion of dihydrofolate to the active tetrahydrofolate (folic acid) Folic acid is needed for the de novo synthesis of the nucleoside thymidine, required for DNA synthesis. Therefore, Methotrexate inhibits the synthesis of DNA, RNA, thymidylates, and proteins. Methotrexate acts specifically during DNA and RNA synthesis, therefore it is cytotoxic during the S-phase of the cell cycle. Logically, it therefore has a greater toxic effect on rapidly dividing cells (such as malignant and myeloid cells, and GI and oral mucosa) that replicate their DNA more frequently. Thus, it inhibits the growth and proliferation of non-cancerous cells as well. Lower doses of methotrexate have been shown to be very effective for the management of rheumatoid arthritis and psoriasis. In these cases, inhibition of dihydrofolate reductase (DHFR) is not thought to be the main mechanism, rather the inhibition of enzymes involved in purine metabolism, leading to accumulation of adenosine, or the inhibition of T-cell activation and suppression of intercellular adhesion molecule expression by T-cells. Gemcitabine (Gemzar): Gemcitabine inhibits thymidylate synthetase, leading to inhibition of DNA synthesis and cell death. Gemcitabine is a prodrug so activity occurs as a result of intracellular conversion to two active metabolites, gemcitabine diphosphate and gemcitabine triphosphate, by deoxycytidine kinase. Gemcitabine diphosphate inhibits ribonucleotide reductase, the enzyme responsible for catalyzing synthesis of deoxynucleoside triphosphates required for DNA synthesis. Gemcitabine triphosphate (diflurorodeoxycytidine triphosphate) competes with endogenous deoxynucleoside triphosphates for incorporation into DNA. Capecitabine (Xeloda): Capecitabine is rapidly converted into 5-fluorouracil in the GI tract. Both normal and tumor cells metabolize 5-FU to 5-fluoro-2-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP). These metabolites cause cell injury by two different mechanisms. First, FdUMP and the folate cofactor N5-10-methylene-tetrahydrofolate bind to thymidylate synthase (TS) to form a covalently bound ternary complex. This binding inhibits the formation of thymidylate from 2-deoxyuridylate. Thymidylate is the necessary precursor of thymidine triphosphate, which is essential for the synthesis of DNA, so that a deficiency of this compound can inhibit cell division. Second, nuclear transcriptional enzymes can mistakenly incorporate FUTP in place of uridine triphosphate (UTP) during the synthesis of RNA. This metabolic error can interfere with RNA processing and protein synthesis.

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*

Krisman

Cladribine (Leustatin): Cladribine is phosphorylated to its corresponding nucleotide CdATP, which accumulates and is incorporated into the DNA of cells such as lymphocytes. High levels of CdATP lead to DNA strand breaks, inhibition of DNA synthesis, and cell death. Cytarabine (Cytosar): Cytarabine acts through direct DNA damage and incorporation into DNA by blocking a key enzyme DNA polymerase. Mercaptopurine (Purinethol): Mercaptopurine competes with hypoxanthine and guanine for the enzyme hypoxanthine-guanine phosphoribosyltransferase (HGPRTase) and is itself converted to thioinosinic acid (TIMP). In addition, 6-methylthioinosinate (MTIMP) is formed by the methylation of TIMP. Both TIMP and MTIMP have been reported to inhibit glutamine-5phosphoribosylpyrophosphate amidotransferase the first enzyme unique to the de novo pathway for purine ribonucleotide synthesis. Thioguanine (Thioguanine): Thioguanine competes with hypoxanthine and guanine for the enzyme hypoxanthine-guanine phosphoribosyltransferase (HGPRTase) and is itself converted to 6-thioguanylic acid (TGMP). TGMP inhibits de novo purine biosynthesis by pseudo-feedback inhibition of glutamine-5-phosphoribosylpyrophosphate amidotransferase the first enzyme unique to the de novo pathway for purine ribonucleotide synthesis. Fludarabine (Fludara): Fludarabine appears to act by inhibiting DNA polymerase alpha, ribonucleotide reductase and DNA primase, thus inhibiting DNA synthesis. Fluorouracil (Efudex): In the anabolic pathway, Fluorouracil blocks the methylation reaction of deoxyuridylic acid to thymidylic acid. In this manner, fluorouracil interferes with the synthesis of deoxyribonucleic acid (DNA) and to a lesser extent inhibits the formation of ribonucleic acid (RNA). Since DNA and RNA are essential for cell division and growth, the effect of fluorouracil may be to create a thymine deficiency, which provokes unbalanced growth and death of the cell. The effects of DNA and RNA deprivation are most marked on those cells (cancer cells) that grow more rapidly and take up fluorouracil at a more rapid rate. Floxuridine (FUDR): When Floxuridine is given by rapid intra-arterial injection, it is apparently rapidly catabolized to 5-fluorouracil. Mechanism of action is similar to 5-fluorouracil. Hydroxyurea (Hydrea): Hydroxyurea causes an immediate inhibition of DNA synthesis by acting as a ribonucleotide reductase inhibitor, without interfering with the synthesis of ribonucleic acid or of protein. Nelarabine (Arranon): Nelarabine is a pro-drug of the deoxyguanosine. It inhibits DNA synthesis, which leads to a cells (cancer) death. Fluoxymesterone (Halotestin): Endogenous androgens are responsible for normal growth and development of the male sex organs and for maintenance of secondary sex characteristics. During exogenous administration of androgens, endogenous testosterone release is inhibited through feedback inhibition of pituitary luteinizing hormone (LH). With large doses of exogenous androgens, spermatogenesis may also be suppressed through feedback inhibition of pituitary follicle stimulating hormone (FSH). It is indicated for replacement therapy in conditions associated with symptoms of deficiency or absence of endogenous testosterone.

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*

Krisman

Flutamide (Eulexin): Flutamide exerts its antiandrogenic action by inhibiting androgen uptake and/or by inhibiting nuclear binding of androgen in target tissues, or both. Prostatic carcinoma is known to be androgen-sensitive; it responds to treatment that counteracts the effect of androgen and/or removes the source of androgen. Bicalutamide (Casodex): Bicalutamide is a non-steroidal antiandrogen. It competitively inhibits the action of androgens by binding to cytosol androgen receptors in the target tissue. Prostatic carcinoma is known to be androgen sensitive; it responds to treatment that counteracts the effect of androgen and/or removes the source of androgen. Nilutamide (Nilandron): Prostate cancer is known to be androgen-sensitive and responds to androgen ablation. Nilutamide blocks the effects of testosterone at the androgen receptor level. It also interacts with the androgen receptor and prevents the normal androgenic response. Tamoxifen (Nolvadex): Many breast cancers have estrogen receptors (ER), and the growth of these tumors can be stimulated by estrogen. Tamoxifen is a nonsteroidal agent that has demonstrated potent antiestrogenic properties. The antiestrogenic effects may be related to its ability to compete with estrogen for binding sites in target tissues such as breast. Therefore, it is useful for the treatment of breast cancer. Fulvestrant (Faslodex): Many breast cancers have estrogen receptors (ER), and the growth of these tumors can be stimulated by estrogen. Fulvestrant is an estrogen receptor antagonist that binds to the estrogen receptor in a competitive manner with affinity comparable to that of estradiol. Letrozole (Femara): The growth of some cancers of the breast is stimulated or maintained by estrogens. In postmenopausal women, estrogens are mainly derived from the action of the aromatase enzyme, which converts adrenal androgens (primarily androstenedione and testosterone) to estrone and estradiol. The suppression of estrogen biosynthesis in peripheral tissues and in the cancer tissue itself can therefore be achieved by specifically inhibiting the aromatase enzyme. Letrozole is a nonsteroidal competitive inhibitor of the aromatase enzyme system; it inhibits the conversion of androgens to estrogens. Anastrozole (Arimidex): Many breast cancers have estrogen receptors; growth of these tumors can be stimulated by estrogen. In postmenopausal women, estrogens are mainly derived from the action of the aromatase enzyme, which converts adrenal androgens (primarily androstenedione and testosterone) to estrone and estradiol. Anastrozole is a potent and selective non-steroidal aromatase inhibitor. It significantly lowers serum estradiol concentration. Exemestane (Aromasin): Breast cancer cell growth may be estrogen-dependent. Aromatase is the principal enzyme that converts androgens to estrogens both in pre- and postmenopausal women. While the main source of estrogen (primarily estradiol) is the ovary in premenopausal women, the principal source of circulating estrogens in postmenopausal women is from conversion of adrenal and ovarian androgens (androstenedione and testosterone) to estrogens (estrone and estradiol) by the aromatase enzyme in peripheral tissues. Estrogen deprivation through aromatase inhibition is an effective and selective treatment for some postmenopausal patients with hormone-dependent breast cancer. Exemestane is an irreversible, steroidal aromatase inactivator, structurally related to the natural substrate androstenedione.

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*

Krisman

Leuprolide (Lupron): Leuprolide acetate, an LH-RH agonist, acts as a potent inhibitor of gonadotropin secretion when given continuously and in therapeutic doses. Administration of leuprolide acetate has resulted in inhibition of the growth of certain hormone-dependent tumors, as well as atrophy of the reproductive organs. Goserelin (Zoladex): Goserelin is a synthetic decapeptide analogue of LHRH. It acts as a potent inhibitor of pituitary gonadotropin secretion. Administration of Goserelin has resulted in inhibition of the growth of certain hormone-dependent tumors. Vinca alkaloids: They act by the inhibition of microtubule formation in the mitotic spindle, resulting in an arrest of dividing cells (cancer) at the metaphase stage. Docetaxel (Taxotere): Docetaxel is an antineoplastic agent that acts by disrupting the microtubular network in cells that is essential for mitotic and interphase cellular functions. Docetaxel binds to free tubulin and promotes the assembly of tubulin into stable microtubules while simultaneously inhibiting their disassembly. This leads to the production of microtubule bundles without normal function and to the stabilization of microtubules, which results in the inhibition of mitosis in cells. Etoposide (Vepesid, Etopophos): VePesid has been shown to cause metaphase arrest in chick fibroblasts. Its main effect, however, appears to be at the G 2 portion of the cell cycle in mammalian cells. It does not interfere with microtubular assembly. The predominant macromolecular effect of etoposide appears to be the induction of DNA strand breaks by an interaction with DNA topoisomerase II or the formation of free radicals. Paclitaxel (Taxol): Paclitaxel is a novel antimicrotubule agent that promotes the assembly of microtubules from tubulin dimers and stabilizes microtubules by preventing depolymerization. This stability results in the inhibition of the normal dynamic reorganization of the microtubule network that is essential for vital interphase and mitotic cellular functions. In addition, paclitaxel induces abnormal arrays or bundles of microtubules throughout the cell cycle and multiple asters of microtubules during mitosis. Teniposide (Vumon): Teniposide is a phase-specific cytotoxic drug, acting in the late S or early G2 phase of the cell cycle, thus preventing cells from entering mitosis. Teniposide causes dosedependent single- and double-stranded breaks in DNA and DNA-protein cross-links. The mechanism of action appears to be related to the inhibition of type II topoisomerase activity. The cytotoxic effects of teniposide are related to the relative number of double-stranded DNA breaks produced in cells. Irinotecan (Camptosar): Irinotecan is a derivative of camptothecin. Camptothecins interact specifically with the enzyme topoisomerase I, which relieves torsional strain in DNA by inducing reversible single-strand breaks. Irinotecan binds to the topoisomerase I-DNA complex and prevents religation of these single-strand breaks. The cytotoxicity of irinotecan is due to doublestrand DNA damage produced during DNA synthesis.

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*

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Protein tyrosine kinase inhibitor/inactivator: A tyrosine kinase is an enzyme that can transfer a phosphate group from ATP to a tyrosine residue in a protein. Tyrosine kinases are a subgroup of the larger class of protein kinases. Phosphorylation of proteins by kinases is an important mechanism in signal transduction for regulation of enzyme activity. Kinase inhibitors work by binding to the ATP binding site of bcr-abl and inhibiting the enzyme activity of the protein synthesis competitively. This lead to the death of cancer cells. Lenalidomide (Revlimid): Lenalidomide possesses antineoplastic, immunomodulatory and antiangiogenic properties. Lenalidomide inhibits the secretion of pro-inflammatory cytokines and increases the secretion of anti-inflammatory cytokines from peripheral blood mononuclear cells. Lenalidomide inhibits cell proliferation with varying effectiveness in some but not all cell lines. Of cell lines tested, lenalidomide was highly effective in inhibiting growth of a human B cell lymphoma. Monoclonal antibody CD20 blocker: A genetically engineered human monoclonal antibody directed against the CD20 antigen found on the surface of normal and malignant B lymphocytes. Vorinostat (Zolinza): Vorinostat inhibits the enzymatic activity of histone deacetylases. These enzymes catalyze the removal of acetyl groups from the lysine residues of proteins, including histones and transcription factors. Vorinostat causes the accumulation of acetylated histones and induces cell cycle arrest and/or apoptosis of some transformed cells. Pegaspargase (Oncaspar): Leukemic cells are unable to synthesize asparagine due to a lack of asparagine synthetase and are dependent on an exogenous source of asparagine for survival. Rapid depletion of asparagines, which results from treatment with the enzyme L-asparaginase (Pegaspargase), kills the leukemic cells. Normal cells, however, are less affected by the rapid depletion due to their ability to synthesize asparagine. This is an approach to therapy based on a specific metabolic defect in some leukemic cells that do not produce asparagine synthetase. Bortezomib (Velcade): Bortezomib is a reversible inhibitor of the chymotrypsinlike activity of the 26S proteasome in mammalian cells. The 26S proteasome is a large protein complex that degrades ubiquitinated proteins. The ubiquitinproteasome pathway plays an essential role in regulating the intracellular concentration of specific proteins, thereby maintaining homeostasis within cells. Inhibition of the 26S proteasome prevents this targeted proteolysis, which can affect multiple signaling cascades within the cell. This disruption of normal homeostatic mechanisms can lead to cell death. Bevacizumab (Avastin): Bevacizumab binds VEGF (Vascular endothelial growth factor) and prevents the interaction of VEGF to its receptors on the surface of endothelial cells. VEGF (vascular endothelial growth factor) is a substance made by cells that stimulates the formation of new blood vessels, a process called angiogenesis. VEGF also acts as a mitogen for vascular endothelial (vessel lining) cells, stimulating these cells to divide and multiply. By inhibiting VEGF binding to its receptor sites, anticancer action is produced. EGFR antagonists: EGFR antagonists bind specifically to the EGFR on both normal and tumor cells, and competitively inhibit the binding of epidermal growth factor (EGF) and other ligands to their receptor sites. This may result in inhibition of cell growth, induction of apoptosis (a form of cell death in which a programmed sequence of events leads to the elimination of cells without releasing harmful substances into the surrounding area) and decreased vascular endothelial growth factor (VEGF) production.

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Reference Guide for the Pharmacy Licensing Exam Theory-Third Edition Table-1
Name Diptheria H.Influenza Causative organism Corynebacterium diphtheria H.influenzae Recommended dose

Krisman

Adult dose, boost every 10 years. Most children have 3 to 4 doses between age 2 months to 15 months. 3 doses at 1 month, 6 to 12months old infant and for patients age 2 years to 18 years, while 2 doses every 6 months to 1 year apart for patients age more than 18 years. 3 doses at 1 to 2 months old infants and adults. 1 dose every year 2 MMR vaccine at 12-15 months of age and again at 4 to 6 years of age. It should be given to children aged 6 weeks to 7 months. It should be given at 2 months, 4 months, 12-18 months and at 4 to 6 years.

Hepatitis A

HAV

Hepatitis B

HBV

Influenza Measles, Mumps and Rubella Pertussis

Influenza Measles, Mumps and Rubella

B.Pertussis

Poliomyelitis

Polio virus

Pneumococcal Tetanus

S. pneumonia Clostridium tetani

1 dose 3 to 4 doses plus a booster every 10 years.

Table-2
Drugs with a prolonged half- life * * * * * * * Chlorpropamide Corgard Piroxicam Amiodarone Bromocriptine Azithromycin Clofazimine

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Table-3 Disulfiram reactions producing drugs * * * * * * * * * * * Metronidazole Chlorpropamide Cefotetan Cefoperazone Moxalactam Cefamandole Tolbutamide Acetohexamide Glyburide Glipizide Disulfiram

Krisman

Drugs precipitate disulfiram-like reactions with (Table-3) * * * * Alcohol Benadryl Elixir Digoxin Elixir Lanoxicap

Platelets aggregation inhibitors * * * * * * * * * Cefamandole Cefoperazone Moxalactam Cefotetan Plicamycin Ketorolac Aspirin Ticlid Plavix

Urine discoloration producing drugs * * * * * * * Phenazopyridine Senna Rifampin Rifapentine Phenolphthalein Levodopa Sulfasalazine

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Drugs that require a patient package insert * * * * * * * Isotretinoin Oral contraceptives Isoproterenol Ticlid Progesterone Estrogen Intrauterine devices

Krisman

Drugs contraindicated in pregnancy * * * * * * * * * * * * * Isotretinoin Ribavirin Tetracycline Chloramphenicol Sulfonamide Misoprostol Finasteride Methimazole Coumadin Metronidazole Valproic acid Lithium carbonate Alcohol

Drugs and their normal serum therapeutic concentration * * * * * * * * * * * * * Digoxin 0.7 to 1.4 Phenytoin 10 to 20 Amikacin 10 Carbamazepine 10 to 20 Gentamicin 2 Tobramycin 2 Fosphenytoin 10 to 20 Theophylline 10 to 20 Streptomycin 5 Digitoxin 09 to 25 Quinidine 02 to 06 Carbamazepine 04 to 12 Phenobarbital 10 to 40 ng/ml mcg/ml mcg/ml mcg/ml mcg/ml mcg/ml mcg/ml mcg/ml mcg/ml mcg/ml mcg/ml mcg/ml mcg/ml Primidone Vancomycin Lithium Valproic acid Haloperidol 04 to 12 mcg/ml 05 to 15 mcg/ml 0.6 to 1.2 mEq/L 40 to 100 mcg/ml 05 to 20 ng/ml

Drugs that cause photosensitivity reactions * * * * * * Accutane Micronase Retin-A Bactrim Carbamazepine Sulfonylureas * * * * * * Cipro DiaBeta Doxycycline Griseofulvin Methotrexate Noroxin * * * * * * Rheumatrex Sulfonamide Tetracycline Thiazide diuretic Tricyclic antidepressant Glucotrol

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Abbreviations * * * * * * * * * * * * * aa N and V a.c. p.c. a.d. a.s. a.u. q.d b.i.d. t.i.d q.i.d q.o.d pt. of each nausea and vomiting before meals after meals right ear left ear both ears or each ear daily twice daily three times daily four times daily every other day pint * * * * * * * * * * * * * D.A.W. gtt a.m. p.m. h.s o.d. o.s. o.u. o2 p.o. pr q.6h prn

Krisman

dispense as written drop morning evening at bed time right eye left eye both eyes or each eye both eyes by mouth per rectum every 6 hours as needed

Drugs that cause enzyme induction * * * * * * * * Rifampin Carbamazepine Phenobarbital Troglitazone Phenytoin Nicotine Omeprazole Rifabutin

Drugs that cause enzyme inhibition * * * * * * Cipro Cimetidine Erythromycin Fluvoxamine Ketoconazole Nelfinavir * * Clopidogrel Ritonavir

Stool discolor producing drugs Drug Rifampin Phenolphthalein Pyrinium Antacid Kao-pectin Iron salt Warfarin Color Red orange Red Red White Black Black brown Black

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Drugs that need to be stored in the refrigerator Calcimar Xalatan (opthalamic solution) Viroptic (opthalamic solution) Opthetic (opthalamic solution) Fluorocaine (opthalamic solution) Occusert Pilo Phospholine Iodine (opthalamic solution) Erythromycin Ethyl Succinate Suspension Promethazine suppository Fosphenytoin (Injection) Bicillin-LA (Injection) Mose (Injection) Harvix-A (Injection) Neupogen (Injection) Thyrolar Mycostatin pastilles Fortovase capsules Norvir Capsules Calcitonin Salmon (Injection, nasal spray) Bacid (dietary supplement) Lactinex (dietary supplement) Sterile Bacitracin powder Diltiazem injection Pepcid injection Urokinase Sus-Phrine (injection) Dornase-alpha Tetanus Toxoid Hepatitis-A MMR vaccine Pancrelipase supplement products Ku-Zyme-HP Viokase Creon Cotazym Ilozyme Festal Wycillin (Injection) Bicillin ( Injection) Permapen (Injection) Intron-A (Injection) Epogen (Injection) Neupogen (Injection) Hyperstat (Injection) Sandostatin (Injection) Novolin (Injection) Humulin (Injection) Regranex ( Cream )

Krisman

Drugs that should not be used by patients with Belladonna alkaloids or Phenobarbital allergy Barbidonna Kinesed Spasmophen Donnapine Hyosophen Spaslin Spasmolin Relaxadon Malatal

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Drugs available in Depot preparation Haloperidol Decanoate Fluphenazine Decanoate Methylprednisolone Medroxyprogesterone Estradiol Leuprolide = = = = = = Haldol Prolixin Depo Medrol Depo Provera Depo Estradiol Lupron Depot

Krisman

Drugs that should not be used by patients with Sulfonamide allergy Sulfonamide Oral sulfonylurea Thiazide diuretic Diazoxide Celebrex Dapsone

Drugs that should not be used by patients with TCA allergy Tricyclic antidepressant Carbamazepine Cyclobenzaprine Seizure producing drugs * * * * * * Tramadol Bupropion Meperidine Chlorpromazine Clozapine Sodium phosphate

Drugs that are available in Transdermal dosage form Name of Drug Climara Catapres Estradiol Nitrodur Transdermal nitro Deponit Nicoderm Prostep Habitrol Nicotrol Duragesic Transderm scop Oxytrol Neupro Emsam Flector Need to change Once a week Once a week Twice a week Applied in morning and remove in the evening Applied in morning and remove in the evening Applied in morning and remove in the evening Every 24 hours Every 24 hours Every 24 hours Applied upon awakening and remove at bed time Every 72 hours Every 72 hours Twice a week Once a day Once every 24-hour Apply one patch to painful area bid

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