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Quick Review to Pharmacology for Screening Test

1. Pharmacology can be defined as the study of substances that interact with living

systems through chemical processes, especially by binding to regulatory molecules and

activating or inhibiting normal body processes. These substances may be chemicals

administered to achieve a beneficial therapeutic effect on some process within the

patient or for their toxic effects on regulatory processes in parasites infecting the

patient.
2. Medical pharmacology, which is often defined as the science of substances used to

prevent, diagnose, and treat disease.

3. Toxicology is the branch of pharmacology that deals with the undesirable effects of

chemicals on living systems, from individual cells to humans to complex ecosystems.

4. Pharmacogenomics (or pharmacogenetics) is the study of the genetic variations that

cause differences in drug response among individuals or populations. Future clinicians

may screen every patient for a variety of such differences before prescribing a drug.
5. Non Polar, Lipid Soluble, Non Ionized drugs easily cross membranes.
6. Low pH favors acidic drugs, High pH favors basic drugs.
7. Large Vd means Large Half Life.
8. Areas with only sympathetic innervation : Adrenal Medula, Kidney, Pilomotor muscles,

Sweat Glands.
9. Areas with only parasympathetic innervation : lacrimal Glands.
10. Acetylcholine :↓in heart rate and cardiac output, ↓ in blood pressure by production of

NO, ↑ Salivation, ↑ GIT motility & Tone, ↑ Bronchial Secreations, Bronchospasm,

Urinary expulsion, Miosis.

11. Renin inhibitors are represented by aliskiren.
12. Aliskiren is considered a peptidomimetic amide hydrolysis transition state analog that

results in a high affinity interaction with renin. Its actions on preventing the production

of angiotensin I cause a decrease in circulating angiotensin II and subsequent lowering

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in aldosterone. The loss of both aldosterone and angiotensin II leads to significant

decreases in peripheral vascular resistance and systemic blood pressure.

13. Currently, aliskiren is used as a second-line therapy for the management of

hypertension.
14. Renin is an aspartate protease that catalyzes the rate-limiting conversion of

angiotensinogen to angiotensin I.
15. Loop diuretics are

Anthranilic acid derivatives with a sulfonamide substituent

 furosemide ,
 bumetanide
 torsemide

Or an aryloxyacetic acid without a sulfonamide substituent

 ethacrynic acid
16. Potassium-sparing diuretics include
 amiloride
 triamterene
 spironolactone
 eplerenone
17. Cytokines are a group of secreted proteins that cause a signaling response to infl uence

cell function in other cells.

18. Interleukins (ILs) are cytokines released by white cells and other cell types in response

to antigen and other stimulation whose function is primarily to regulate the immune

system.
19. A lymphokine is a cytokine produced by a lymphocyte. ILs 2-6 and TNF- are examples of

lymphokines.
20. Phase I metabolites are often somewhat more polar than their parents. With the

exception of acetylated and methylated metabolites.

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21. Phase II metabolites are much more polar than their parents. Thus, phase I

metabolites are more likely to retain some lipid solubility and are more likely to cross

cellular membranes.
22. It is unusual for a single metabolite to be excreted for a given drug. Most drugs yield a

mixture of metabolites. Because of the high polarity and subsequent high excretion of

phase II metabolites, they are not likely to undergo further metabolism.

23. Phase I metabolites, on the other hand, are less polar and are very likely to undergo

further phase II metabolic reactions.

24. Because of the types of functional groups present, aspirin may undergo a number of

different metabolic reactions. These include hydroxylation of the aromatic nucleus,

conjugation of the carboxyl group with glycine, conjugation of the carboxyl group with

glucuronic acid with the formation of an ester glucuronide, hydrolysis of the acetate

ester, and conjugation of the phenol group (resulting from hydrolysis of the acetate

ester) with glucuronic acid to form an ether glucuronide.

25. Sulfasalazine has both anti-infl ammatory and antibacterial activity when converted to

aminosalicylic acid and sulfapyridine in the body. This reaction occurs by reductive

cleavage of the “azo” linkage contained in the sulfasalazine molecule and is catalyzed

in the intestine by bacterial azoreductase. This is a form of site-specific delivery because

the intact drug is not absorbed from the stomach or upper intestine and reaches the

colon, where it is metabolized. Sulfasalazine is one of a few drugs that are effective for

the treatment of ulcerative colitis.

26. The chloramphenicol molecule contains an aromatic nucleus,
 which would be subject to hydroxylation;
 a nitro group that is subject to reduction;
 an amide group that is subject to liver hydrolysis;
 And alcohol groups that are subject to glucuronidation.

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27. Of all the enzyme systems responsible for these reactions, the system responsible for

glucuronidation is developed poorly in premature infants and infants up to

approximately 6 to 8 weeks of age.

28. By definition, prodrugs are inactive or very weakly active molecules that require in vivo

activation to the parent molecule.

29. Phase II drug-metabolizing enzymes are commonly called transferase enzymes because

they transfer a biomolecule from an activated cofactor to a target functional group.

Phase II enzymes include glucuronosyltransferase, sulfotransferase, N-acyltransferase,

glutathione-S-transferase, N-acetyltransferase, and methyltransferase.

30. CYP450 is the most common phase I enzyme.
31. Levodopa is not associated with agranulocytosis.
32. Due to venodilatory actions, prazosin is associated with postural or orthostatic

hypotension.
33. Pilocarpine acts directly at the muscarinic receptor.
34. Dipivefrin eventually activates alpha 2-receptors.
35. Dipivefrin is diacetylated epinephrine, which is readily metabolized to epinephrine to

activate alpha 2-receptors on the ciliary body to reduce the production of aqueous

humor.
36. Timolol blocks Beta-receptors.
37. Echothiophate inhibits the metabolism of ACh, indirectly increasing levels of the

endogenous neurotransmitter.
38. Tamsulosin is an alpha 1A-selective antagonist that may be used in place of finasteride

to treat benign prostatic hypertrophy (BPH).

39. Clozapine, although therapeutically defined as a general antipsychotic, is used almost

exclusively in the treatment of schizophrenia.

40. Calcium-channel blockers
 Block the slow inward current carried by calcium during phase 2 of the cardiac

action potential.
 They dilate peripheral arterioles and reduce total peripheral resistance.
 They are useful in treating vasospastic angina.
 adverse effects include bradycardia, dry cough and edema

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41. The termination of heparin activity by protamine sulfate is the result of an acid–base

interaction.
42. Digoxin may be useful in treating CHF.
43. ACE inhibitors will cause
 Birth defects and fetal demise if taken during the second and third trimesters of

pregnancy.
44. Autacoids are classified as substances that are released at or near their site of action

and have a short duration of activity.

45. Autacoids, such as prostaglandins, leukotrienes, kallidin, bradykinin, serotonin, and

histamine, have varied structures and physiological activities that are modulated by

several different drugs.

46. PGs are derivatives of prostanoic acid, a 20-carbon fatty acid containing a 5-carbon ring.
47. Serotonin, in addition to being a neurotransmitter, is also an autacoid with various

effects, including vasoconstriction and platelet aggregation.

48. Serotonin (5-hydroxytryptamine, 5-HT) is a bioamine that is synthesized from the

amino acid tryptophan by a two-step enzymatic process catalyzed by tryptophan

hydroxylase and L-amino acid decarboxylase.

49. Histamine is a bioamine derived principally from dietary histidine, which is

decarboxylated by L -histidine decarboxylase.

50. Aspirin is the acetyl ester of salicylic acid or a salicylate member of the NSAIDs.
51. Diclofenac is an example of an acetic acid derivative,
52. Ibuprofen is an example of a propionic acid.
53. Meclofenamate sodium is an example of an N-arylanthranilic acid or fenamic acid.
54. Meloxicam is an example of an enolic acid derivative or an oxicam.
55. There are three sources of drug information: (clinical MCQ)
 journals/clinical trials (primary sources),
 indexing and abstracting services (secondary sources),
 Textbook and databases (tertiary sources).
56. Clinical toxicology. Focuses on the effects of substances in patients caused by accidental

poisonings or intentional overdoses of medications, drugs of abuse, household products,

or various other chemicals.

57. Intoxication. Toxicity associated with any chemical substance.
58. Poisoning. A clinical toxicity secondary to accidental exposure.

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59. Overdose. An intentional exposure with the intent of causing self-injury or death.
60. Toxidromes. A group of signs, symptoms, and laboratory findings that suggest a specific

ingestion.
61. Thermal sterilization involves the use of either moist or dry heat.
62. Moist-heat sterilization is the most widely used and reliable sterilization method.
 Microorganisms are destroyed by cellular protein coagulation.
 The objects to be sterilized are exposed to saturated steam under 1 atmosphere

pressure at a minimum temperature of 121°C for at least 20 to 60 mins.

 An autoclave is commonly used for moist-heat sterilization.
 Because it does not require as high a temperature, moist-heat sterilization

causes less product and equipment damage compared to dry-heat sterilization.

63. Dry-heat sterilization is appropriate for materials that cannot withstand moist-heat

sterilization. Objects are subjected to a temperature of at least 160°C for 120 mins (if

higher temperatures can be used, less exposure time is required).

64. Chemical (gas) sterilization is used to sterilize surfaces and porous materials (e.g.,

surgical dressings) that other sterilization methods may damage.

 In this method, ethylene oxide is used generally in combination with heat and

moisture.
 Residual gas must be allowed to dissipate aft er sterilization and before use of the

sterile product.
65. Pregnancy tests detect pregnancy by the presence in the urine of human chorionic

gonadotropin (hCG), which is secreted after fertilization. Many pregnancy test kits can

detect hCG 1 day after missed menses. False-positive results can occur if the patient

takes the test too early, is taking fertility medications (e.g., hCG), or has ovarian cysts. If a

patient uses a household container or a waxed cup to collect urine, it may affect the test

results. Patients should be referred to the appropriate health care provider if they

receive a positive result or two negative results 7 days apart and have not had menses.
66. Milrinone lactate and amrinone lactate are classified as inotropic agents. They are

used only parenterally for the short-term treatment of congestive heart failure (CHF).

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They produce a positive inotropic effect (ie, they increase the force of cardiac

contraction) and they produce vasodilation.

67. Latanoprost is a prostaglandin F2a analog that is used as an ophthalmic solution to

reduce intraocular pressure by increasing the outflow of aqueous humor from the eye.
68. Alteplase and reteplase are tissue plasminogen activators prepared by recombinant

DNA technology. They are administered intravenously in order to lyse thrombi in

patients with acute myocardial infarction.

69. Colestipol is an anion exchange resin that binds bile acids in the intestine, causing them

to be removed in the feces.

70. Minoxidil is a direct-acting peripheral vasodilator. Because of its potential for producing

a number of serious adverse effects, minoxidil is not a first-choice antihypertensive

agent. Its ability to produce excess hair growth (hirsutism, hypertrichosis) has led to its

topical use for the treatment of alopecia.

71. Magnesium-containing antacids (eg, magnesium hydroxide) may cause diarrhea

because of their saline cathartic action on the GI tract. They may also cause

hypermagnesemia in renal failure patients.

72. Acarbose and miglitol are both alpha-glucosidase inhibitors. Since they act to reduce

the GI absorption of carbohydrates, they are best taken three times a day with the first

bite of each main meal.

73. The autonomic nervous system consists of two major branches: the sympathetic

(adrenergic) branch and the parasympathetic (cholinergic) branch. Each branch utilizes

different neurotransmitters. For example, the sympathetic branch utilizes

norepinephrine, whereas the parasympathetic branch utilizes acetylcholine.

74. Acetazolamide is a carbonic anhydrase inhibitor
 used clinically in the treatment of chronic open-angle glaucoma
 As well as secondary glaucoma.
 It is also used for treatment of edema caused by congestive heart failure
 or drug use, or associated with certain forms of epilepsy.

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75. Thiazide diuretics such as hydrochlorothiazide increase the renal excretion of sodium,

chloride, and potassium while decreasing the excretion of calcium and uric acid.
76. Dalteparin sodium is a low molecular-weight heparin derivative used in preventing or

treating thromboembolic complications following surgery or ischemic complications of

unstable angina and MI.

77. Patients using metronidazole should avoid alcoholic beverages to avoid disulfiram-like

effects when the combination is used.

78. Allopurinol : purine analog that the ↓production of uric acid by competitively

inhibiting the last two steps in uric acid biosynthesis that are catalyzed by xanthine

oxidase.
 Used in treatment of primary hyperuricemia of gout and hyperuricemia

secondary to other conditions.

 Adverse: Hypersensitivity reactions, especially skin rashes
79. 1st Order Metabolism: the rate of drug metabolism is directly proportional to the

concentration of free drug. V= {V(max) x C} / K(m)

80. Zero Order: the rate of drug metabolism is independent of the concentration of free

drug. V= V(max).
81. Phase I reactions convert lipophilic molecules into more polar ones by introducing or

unmasking a polar functional group. i.e., Oxidation

82. Phase II: This phase consists of conjugation reactions. Conjugation reaction with an

endogenous substrate, such as glucuronic acid, sulfuric acid, acetic acid, or an amino

acid, results in polar, usually more water-soluble compounds that are most often

therapeutically inactive.
83. Senna is a widely used stimulant laxative. Its active ingredient is a group of sennosides, a

natural complex of anthraquinone glycosides. Taken orally, it causes evacuation of the

bowels within 8 to 10 hours.

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84. Bisacodyl, available as suppositories and enteric-coated tablets, is a potent stimulant of

the colon. It acts directly on nerve fibers in the mucosa of the colon. Adverse effects

include abdominal cramps and the potential for atonic colon with prolonged use.
85. Castor oil is broken down in the small intestine to ricinoleic acid, which is very irritating

to the gut, and promptly increases peristalsis. It should be avoided by pregnant patients,

because it may stimulate uterine contractions.

86. Chloramphenicol :
 50S.
 Only used as alternative to other Drugs.
 Gray baby Syndrome, GIT, Anemias
87. Griseofulvin requires treatment of 6 to 12 months in duration. Causes disruption of the

mitotic spindle and inhibition of fungal mitosis. Griseofulvin potentiates the intoxicating

effects of alcohol.
88. Opioid receptors
 Brainstem: Opioid receptors influence respiration, cough, nausea and vomiting,

blood pressure, pupillary diameter, and control of stomach secretions.

 Medial thalamus: This area mediates deep pain that is poorly localized and

emotionally influenced.
 Spinal cord: Receptors in the substantia gelatinosa are involved with the receipt

and integration of incoming sensory information, leading to the attenuation of

painful afferent stimuli.

 Hypothalamus: Receptors here affect neuroendocrine secretion.
 Limbic system: The greatest concentration of opiate receptors in the limbic

system is located in the amygdala. They probably do not exert analgesic action,

but they may influence emotional behavior.

 Periphery: Nerve fibers & their terminals. As in the CNS, they inhibit Ca2+-

dependent release of excitatory, proinflammatory substances (for example,

substance P) from these nerve endings.

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 Immune cells: Opioid-binding sites have also been found on immune cells. The

role of these receptors in nociception (response or sensitivity to painful stimuli)

has not been determined.

89. Antidotes
 Acetaminophen (Paracetamol)= N-Acetyl Cysteine ( Most-effective), Methionine,

Activated Charcoal(Universal Anti-Dote)

 Anti-cholinergics = Physostigmine
 Benzodiazepine = Flumazenil
 CO(Carbon mono-oxide)= Oxygen(+/- Hyperbaric chamber)
 Cyanide= Amyl Nitrite pearls, Sodium Nitrite, Sodium thiosulphate
 Digitalis= Digoxin Immune Fab (Digibind)
 Methanol/Ethylene glycol= Fumepizol
 Heparin= Protamine Sulphate
 Lead= Dimercapto-succinic acid
 Mercury/Arsenic/Gold= Dimercaprol
 Methemogobenemia, nitrates= Methylene Blue
 Opioids= Naloxone/Nalmafene/Naltroxone
 Organophosphates/Carbamates/Nerve Gases= Atropine/ Pralidoxime
 Cholroquine
 Diazepam

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