PHARMACOLOGY: GIVE REASONS QUESTIONS

MYASTHENIA GRAVIS 1. Edrophonium better used in diagnosis MG while neostigmine better in treatment? GLAUCOMA 1. Atropine and atropine like drugs contraindicated in case of glaucoma? Produce mydriasis n narrowing angleof filtration Decrease drainage of aqueous humour & increase IOP Dipivefrin eye drop are preferred to adrenaline treatment for open angle glaucoma? more stable and lipophilic-passes easily through cornea produce VC decrease aqueos formation -> increase drainage of aqueous humor Prodrug as it converted to adrenaline can be used in small concentration Timolol eye drops are contraindicated in patient with chest problem treated for glaucoma? GOUT 1. In treatment of gout, we must use large dose of probenecid (above1g). LD - block active reabsorption of uric acid in proximal convoluted tubule increase amount of urate eliminated. SD - reverse occurs Aspirin small dose is contraindicated in gout.

Neostigmine :: long duration of action :: can be taken orally Edrophonium :: rapid onset and short duration of action :: more specific on skeletal ms no colic 2. Atropine must be added before neostigmine in treatment in MG. Atropine produce initial bradycardia followed by tachycardia If atropine is given after neostigmine bradycardia produce by atropine will potentiate bradycardia produce by neostigmine cardiac arrest Aminoglycosides are contraindicated in MG patient.

2.

2.

Small dose of aspirin depress uric acid secretion by PCT resulting in uricacid retention. 3. Thiazide diuretics are contraindicated in gout.

3.

Decrease uric acid excretion due competitive inhibition of tubular transport of organic acid. 4. Tea and coffee are allowed in gout.

3.

Timolol is non selective BB decrease all cardiac properties HF 4. Guanithidine are combined with adrenaline in treatment of open angle glaucoma?

Aminoglycosides increase neuromuscular blocking properties 4. Neostigmine used in treatment of curare poisoning while contraindicated in succinylcholine poisoning. Neostigmne antagonize action of curare Neostigmine prolonged apnea produce by succinylcholine toxicity-delayed recovery from depolarized tissue Gallamine is contraindicated in thyrotoxic patient

Metaboilize into methyl-uric acid which are soluble and not precipitate in joints. 5. Probenecid is used with penicilin in treatment of some bacterial infection.

Produce miosis increase drainage decrease IOP 5. Pilocarpine is used in angle closure glaucoma

Probenecid renal tubular reabsorption of uric acid retention of penicillin (increase duration of activity and affectivity)

Produce miosis , no twitches , decrease IOP but lacrimination

5.

Gallamine cause tachycardia due to cardiac M2 blockage and NA release

PHARMACOLOGY: GIVE REASONS QUESTIONS

GENERAL ANESTHESIA 1. 2. Hyoscine is used as a pre anesthetic medication. To counteract the vagal effects that may occur during anesthesa and surgery. CNS depression and amnesia - less anesthetic is needed Stimulate respiration center Strong anti-secretory No tachycardia Nitrous oxide is not used in anemic patient. 3. MAO inhibitor are contraindicated in aged cheese. 3. DEPRESSION 1. TCAs contraindicated in senile enlarged prostate. EPILEPSY 1. Phenytoin should not used in young female.

TCAs has atropine like action produce urine retention 2. Lithium is used in prophylaxis of tardive dyskinesia induced by antipsychotic drugs.

Lead to gingival hyperplasia, coarsening of facial features, and hirsutism (Hydontoin faces) 2. Despite of effectiveness of trimethadione in managing petit mal epilepsy,it's rare used clinically. Its not controlled by or tolerate other agents Precipitate grand mal seizure Valproic acid and phenytoin are contraindicated during pregnancy

Prevent development of dopamine supersensitivity

Cause megaloblasticanemia due to depression of methionine synthetasewhichutilize vitamin B12 as coenzyme 3. Halothane is avoided in thyrotoxic patient

Cause cheese reaction due to high conc. of tyramine reach noradrenergic neurons and release NA in large amounts hypertensive crisis 4. Imipramine is indicated for nocturnal enuresis.

Teratogenic - Valproic acid neural tube defect Phenytoin cleft palate 4. Phenytoin is causing megaloblasticanemia, osteomalacia, coarsening of facial features and hyperglycemia.

Cardiotoxic Stage1: increase vagal tone bradycardia and heart block Stage2: sensitize heart to catecholamine arrythmia Stage3: direct myocardial depression 4. Halothane is contraindicated in cirrhotic patient

Produce atropine like action (contraction of internal sphincter) urine retention 5. Fluoxetine is contraindicated with MAO inhibitor

Fluoxetine is SSRi producing serotonin syndrome.

Due to disorder of metabolism and decrease insulin secretion 5. Ethosuximide is drug of choice in petit mal epilepsy Highly efficacious and safe Block T type calcium ch of primary afferent

Hepatotoxic - halothane partially metabolize by liver forming tri-fluoro acetic acid (hepatotoxic subs.) 5. Thiopentone not suitable to maintain anesthesia

Short duration of action due to redistribution

PHARMACOLOGY: GIVE REASONS QUESTIONS

PARKINSONISM 1. Dopamine itself can't be used in ttt of Parkinsonism Dopamine cannot pass BBB 2. Carvidopa is used in combination with levodopa Carvidopa inhibit peripheral decarboxylase enz lead to high amount L-dopa can pass to CNS Prevent large amount L-dopa metabolized in gout 3. Vit B6 should not be used in patient receiving levodopa therapy 3. Ipratropium is not used in acute attack of asthma. Has slower onset 1-2 hours Used in chronic obstructive pulmonary disease (COPD) 4. Aspirin is contraindicated in bronchial asthma. 4. Avoid pirenzipine in narrow angle glaucoma BRONCHIAL ASTHMA 1. IV administration of theophylline should be slow. To avoid velocity reaction: Tachycardia and arrhythmia - may be fatal Severe hypotension and syncope Headache, nervousness, insomnia, convulsion 2. Atropine is antimuscarinic but not used in treatment of asthma. ACID PEPTIC DISEASE 1. 2. Ranitidine is more preferable than cimitidine in treatment of peptic ulcer. No hepatic microsomal inhibition No anti androgenic action No increase in prolactin Not pass BBB no CNS effects in elderly It is necessary in treatment of peptic ulcer to eradicate the helicobacter pylori?

Produce excessive dryness of sputum, become more tenacious and difficult to expectorate

Yes because 99% of peptic ulcer are cause by infection of H.pylori. 3. Avoid cimitidine in old age patients?

Vit B6 reduces anti-parkinsonism effect due to increase peripheral metabolism of L-dopa 4. Phenothiazines can develop iatrogenic parkinsonism

Cimitidine cause mental confusion in elderly

Blocks dopamine receptor in basal ganglia 5. Only less than 5% of levodopa can pass BBB 95% metabolize by peripheral decarboxylase enzyme to dopamine (not pass BBB) part of levodopa metabolize by peripheral COMT to 3-D methyl dopa 5% is converted by central decarboxylase enzyme to dopamine in CNS

Aspirin inhibit cyclooxygenase (COX) enzyme and no effect on lipooxygenase enzyme (LOX) production of leukotriens bronchoconstriction 5. Morphine is contraindicated in bronchial asthma.

Increase IOP due to mydriasis and cycloplegia 5. Pregnant female should not use misoprostol as a treatment of peptic ulcer?

Morphine caused Inhibition of cough reflex Bronchoconstriction release histamine Inhibition respiratory centre

Lead to uterine contraction resulting in bleeding or abortion

PHARMACOLOGY: GIVE REASONS QUESTIONS

HEART FAILURE 5. 1. Digitalis producebradycardia and prolong P.R interval. Direct action of digitalis on AVN lead to: decrease AVN conductivity prolongation of refractory period may decrease sensitivity of SAN and AVN to catecholamine Vagal action of digitalis lead to: Sensitization of baroreceptor in aortic arch and carotid body reflex stimulation to vagal centre Sensitize SAN to Acetylcholine Inhibit Bainbridge reflex Digitalis has vechronotropic effect(bradycardia) Digitalis is used in managing congestive heart failure. +ve inotropic increase COP& -vecronotropicdecrease HR Decrease venous congestion Morphine is used in treatment of acute pulmonary edema. VD decrease VR and preload Sedate respiration, sedate patient Decrease sympathetic VD decrease PR and after load Digitalis is contraindicated in myocardial ischemia and diphthereticmyocarditis. -myocardial ischemia produce exhaustion of energy stores digitalis depends on energyarrythmia -diptheric myocarditis produce weak myocardium digitalis has +ve inotropic rupture of cardiac ms 5. Prolonged use of Na nitroprusside may be dangerous. Ntroprusside liberate cyanide in RBCs and endothelium acidosis, arrhythmia and death. Cyanide in liver gives thiocyanate delirium and psychosis.

HYPERTENSION 1. Captopril is contraindicated in 2 and 3 trimester of pregnancy -Decrease amount of amniotic fluid) deformity - cause fetal hypotension, renal failure, malformation and death. 2. Diuretic should be added to methyl dopa in treatment of hypertension
nd rd

ANGINA PECTORIS 1. Non selective -blockers are contraindicated in variant angina.

Lead to severe VC due to block of 2 receptor 2. Nifedipine may aggravate myocardial ischemia.

2.

Because nifedipine cause reflex tachycardia, increased oxygen need. And by decrease of coronary perfusion. 3. Diltiazem is contraindicated in heart failure.

To antagonize compensatory salt and water retention. 3. -blockers must be added to hydralazine in treatment of hypertension

3.

Decrease all cardiac properties mostly ve inotropic 4. Verapamil should not be given with -blockers in treatment of angina.

Hydralazine produce arterial VD leads to compensatory sympathetic stimulation (tachycardia and angina) -blockers is added to antagonize tachycardia and angina. (symp. stimulation) 4. Sudden stop of clonidine therapy is contraindicated. Clonidine therapy decrease adrenergic nerve supply to all tissue upregulation of & receptor s stop suddenly lead to increase adrenergic neurotransmission, lead to severe hypertension.

4.

Digitalis is used in treatment of atrial arrhythmia and contraindicated in ventricular arrhythmia. Atrial arrhythmia: -to protect ventricle from high rate of atrium by decrease conductivity in AV system both direct and vagal effect Ventricle arrhythmia: -increase automaticity in purkinjefiberarrythmia

Verapamil and -blockers decrease all cardiac properties mostly vedromotropicsevere HB. 5. Nitrate therapy should never be stopped suddenly.

Nitrate will cause coronary dependence after long exposure. Sudden withdrawal will causes severe angina or even infarction.

PHARMACOLOGY: GIVE REASONS QUESTIONS

ARRYTHMIA 1. Quinidine is contraindicated in old atrial fibrillation SHOCK 1. Dopamine is useful in many types of shock? Hypovolemic, cardiogenic, septic shock . Dopamine leads to: -renal vasodilatation with increase in renal blood flow and urine volume -improves microcirculation of vital organ +ve inotropic effect lead to increase in COP 2. Adrenaline is life saving in anaphylactic shock but may be a bad choice in hypovolemic shock? Adrenaline is physiological antagonist of histamine. Also produce VC leading to decrease angioedema and has bronchodilator effect. Adrenaline in hypovolemic shock causes VC of renal blood vessel decrease RBF that transform reversible shock to irreversible shock. Alcohols , sedatives, head down position are avoided in management of shock? Depress CNS and causes cutaneous VD increase heat loss Depress CNS especially VMC -allow visceral to press on diaphragm ?difficulty in respiration Dobutamine is superior than dopamine in treatment of cardiogenic shock? Dobutamine is B1 agonist and has no dopaminergic action like dopamine +veinotopic and +vedromotropic Minimal tachycardia and minimal change in PR Morphine is use in neurogenic and cardiogenic shock? Pain kiler, veinodilator (VR lung congestion in pulmonary edema) Relieve anxiety, cerebral and coronary blood flow HYPERLIPOPROTEINEMIA 1. Dont use cholestyramine in patients treated by digitalis

To avoid embolic manifestation. Old AF stasis of blood formation mural thrombi Quinidine restores normal sinus rhythm in atrial fibrillation complete contraction of atria dislodgment of mural thrombus 2. In atrial flutter and recent atrial fibrillation, pretreatment with digitalis before quinidine?

Cholestyramine bind digitalis, decrease their absorption, decrease activity of digitalis. So digitalis must be given 1 or 2H after / before cholestyramine to ensure complete absorption. 2. Oral anticoagulant is contraindicated with fibrates. Clofibrate is HME inhibitor, inhibit metabolism of oral anticoagulants, potentiat their effect. Also potentiate effect of anticoagulant because fibrate displace oral anticoagulant from plasma protein binding sites. With hepatic dysfunction patient,gemfibrozil is better to be avoided?

Quinidine may increase AV conduction by atropine like action, lead to paradoxical ventricular tachycardia. Pre-treatment by digitalis to decrease AV conduction (vagal & direct effect), prevent paradoxical ventricular tachycardia. 3. Verapamil and digoxin are better avoided in WPW. -worsen condition as increase conduction in accessory pathway 4. Amiodarone has many side effect -bind to all tissue -longerhalf life (10-100 days) 5. Adenosine is preferable in terminating supraventricular tachycardia Due to high efficacy (90-95%) and very short duration of action (15 sec) cAMP induced Ca influx slow AV conduction, prolong RP + Activate K channel

3.

3.

Because it is extensively metabolized in liver. 4. Statins may be used in combination with bile acid resin in hyeprlipidemicpatients?

Statins decrease cholesterol, correct possible increase TG and VLDL produce by bile acid binding resin. 5. Niacin is contraindicated in gout.

4.

Niacin produce hyperuricemia

5.

PHARMACOLOGY: GIVE REASONS QUESTIONS

DEEP VEIN THROMBOSIS 1. Warfarin is contraindicated in pregnancy. HYPERTHYROIDISM 1. Effect of thioamide appear after a latent period from 1-2 weeks. DIABETES MELLITUS 1. Oral hypoglycemic drugs are not beneficial in type I DM? Oral hypoglycemic act on cell of pancreas to secrete insulin but type 1 has no functional cell of pancreas. (absolute insulin deficiency) 2. -blockers,sulfonamides , diazoxide are contraindicated in diabetic patient? -blockers - Decrease insulin release hyperglycemia - If patient develop hypoglycemia mask sign of hypoglycemia liketremors, tachycardia and anxiety Sulphonamide have similar structure to sulphonylurea which may displace it from plasma protein bindingsevere hypoglycemia Diazoxide is K+ ch opener-hyperpolarize-suppress B-cell of pancreas- decrease insulin release 3. Protamine zinc insulin cant be mixed with soluble insulin in same syringe while,isophane insulin can be mixed? -bcoz protamine is highly alkaline solution ?precipitation of soluble insulin -isophane insulin is neutral insulin ?doesnt precipitate soluble insulin

Warfarin passes placental barrier and produce teratogenicity. 2. Enoxaparin is better than unfractionated heparin.

Till exhaustion of thyroid hormone in colloid of thyroid gland 2. Iodide therapy never combined with ionic inhibitor in treatment of hyperthyroidism

Enoxaparin: 3. Has high affinity to anti thrombin III Minimal effect in platelet aggregation Minimal effect in lipoprotein lipase activity Minimal bleeding tendency Has longer half life Thrombolytics are contraindicated in active tuberculosis.

Can cause exacerbation of thyrotoxicosis. 3. Radioactive iodine is contraindicated in childhood, during pregnancy and lactation. During pregnancy & lactation damage of fetal & infant thyroid During childhood hypothyroidism and high chances of malignancy Propanalol is drug of choice of -blocker in sympatomatic treatment of hyperthyroidism. No ISA (intrinsic sympathetic activity) Protects heart from tachycardia, angina, and arrhythmia Can pass BBB and prevent anxiety, tremors of hyperthyroidism Decrease conversion of T4 to T3 (active) Iodide therapy used 7-10 days before subtotal thyroidectomy.

Thrombolytislyse fibrous tissues that surrounding the lesion leading to reactivation and dissemination. 4. The dose of warfarin should be reduced when aspirin is concomitantly used.

4. 5.

Aspirin increase potency of oral anticoagulant by inhibit platelet aggregation and function. 5. Tissue plasminogen activity activator is better than streptokinase. Selectively activate fibrin bound plasminogen at site of thrombus no systemic fibrinolysis &depletion of plasma fibrinogen. More effective and fast acting. Non-antigenic, can be given in cases of upper respiratory infection by streptococci.

4.

Decrease size and vascularity of thyroid gland. More than 15 days, relapse of hyperthyroidism can occur (due to TSH)

Sometimes evening dose of insulin must be reduced? -some patient when taking proper insulin dose develop excess hyperglycemia ?activation of counter regulatory hormone (glucagon,GH,cortisol) ?all act overnight ?hypoglycemia 5. Biguanides cause lactic acidosis?Increase peripheral glucose uptake and anaerobic glycolysis excessive lactic acid production