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Review of Pharmacology - 9E (2015)

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Autacoids<br />

16. Ans. (b) Dangerous ventricular arrhythmias can occur (Ref: KDT 6/e p158)<br />

Ketoconazole, erythromycin and clarithromycin are potent inhibitors <strong>of</strong> microsomal enzymes. Astemizole, terfenadine<br />

and cisapride are the drugs that can block cardiac K + channels at high concentration. If administered along with microsomal<br />

enzyme inhibitors, these drugs can result in torsades de pointes, a serious polymorphic ventricular tachycardia.<br />

17. Ans. (c) It does not block cardiac K + channels (Ref: KDT 6/e p158)<br />

Fex<strong>of</strong>enadine is an active metabolite <strong>of</strong> terfenadine. It lacks K + channel blocking property, therefore is devoid <strong>of</strong> arrhythmogenic<br />

potential. It is available as a separate second generation H 1<br />

blocking agent.<br />

18. Ans. (d) Azelastine (Ref: KDT 6/e p159)<br />

19. Ans. (c) 5-HT 3<br />

(Ref: KDT 6/e p163)<br />

All serotonin receptors are G-protein coupled receptors except 5-HT 3<br />

, which is an inotropic receptor.<br />

20. Ans. (a) 5-HT 1A<br />

(Ref: KDT 6/e p163)<br />

21. Ans. (b) Serotonin 5-HT 3<br />

receptor (Ref: KDT 6/e p163)<br />

22. Ans. (d) Tegaserod (Ref: KDT 6/e p654)<br />

Both cisapride and tegaserod are selective 5HT 4<br />

agonists useful in the treatment <strong>of</strong> GERD. Cisapride possesses cardiac K +<br />

channel blocking activity and can lead to torsades de pointes. Tegaserod is devoid <strong>of</strong> this adverse effect. However, tegaserod<br />

has recently been withdrawn due to increased risk <strong>of</strong> MI and stroke.<br />

23. Ans. (b) Adrenaline (Ref: KDT 6/e p129)<br />

• Adrenaline is a physiological antagonist <strong>of</strong> histamine. It reverses bronchoconstriction caused by histamine. Ranitidine<br />

is an H 2<br />

antagonist that decreases gastric acid secretion but has no effect on smooth muscles.<br />

24. Ans. (c) Common cold (Ref: KDT 6/e p160)<br />

In this condition, excessive secretions (like rhinorrhoea) are due to cholinergic overactivity. First generation antihistaminics<br />

possess anticholinergic property and therefore are effective for common cold. On the other hand, second generation<br />

agents (lacking anticholinergic actions) are ineffective.<br />

25. Ans. (d) Treatment <strong>of</strong> these patients with erythromycin, a macrolide antibiotic (Ref: KDT 6/e p158)<br />

Astemizole and terfenadine are metabolized by microsomal enzymes. Erythromycin inhibits these enzymes and raises the<br />

plasma concentration <strong>of</strong> these drugs. At high levels, these agents block cardiac K + channels leading to arrhythmias.<br />

26. Ans. (d) Cinnarizine (Ref: KDT 6/e p156)<br />

27. Ans. (b) 5HT 2<br />

antagonist (Ref: KDT 6/e p167)<br />

28. Ans. (a) Chlorpheniramine (Ref: KDT 6/e p156-157)<br />

29. Ans. (a) Ketoconazole (Ref: KDT 6/e p763)<br />

30. Ans. (b) Lanreotide (Ref: KDT 6/e p166-167)<br />

Lanreotide is a somatostatin analog used in acromegaly.<br />

31. Ans. (c) Diphenhydramine (Ref: Katzung 11/e p278)<br />

Diphenhydramine and promethazine have maximum anti-cholinergic activity and maximum ability to cross the blood brain barrier<br />

and are thus most effective in motion sickness.<br />

32. Ans. (a) Antiemetic (Ref: KDT 6/e p646)<br />

33. Ans. (d) Terfenadine (Ref: KDT 6/e p158)<br />

34. Ans. (a) Gastroesophageal reflux disease (Ref: KDT 6/e p645)<br />

35. Ans. (d) Decreasing IP 3<br />

in stomach (Ref: KDT 6/e p153)<br />

36. Ans. (a) Dihydroergotamine (Katzung 11/e p289)<br />

This is a classical sign <strong>of</strong> ergot induced vasoconstriction. Dihydroergotamine can be used for acute attack <strong>of</strong> migraine and<br />

can result in these symptoms. Due to their vasoconstricing potential, ergot alkaloids are contra-indicated in a patient with<br />

peripheral vascular disease. These may also lead to development <strong>of</strong> gangrene.<br />

37. Ans. (d) Levetiracetam (Ref: Katzung 11/e p283)<br />

Prophylaxis <strong>of</strong> migraine is required if the attacks are frequent (>2-3 per month). The drugs useful for prophylaxis are:<br />

General Autacoids <strong>Pharmacology</strong><br />

• Propanolol is the most commonly used drug for prophylaxis <strong>of</strong> migraine attacks. Timolol, atenolol, metoprolol<br />

and nadolol can also be used but the drugs with ISA (e.g. pindolol) are ineffective.<br />

• Calcium channel blockers like flunarizine (also blocks Na + channels) is also effective<br />

139<br />

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