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Pharmacology

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Cardiovascular Systems

Question
38 out of 84
 

Which is NOT a prodrug (DNB Dec 2010)



A Losartan
B Enalapril

C Hydralazine
D Lisinopril

Ans. D Lisinopril (Ref: BG Katzung, pp-182, 11th Edition, 2009)

a. Prodrug is a drug that is inactive until when given orally.

b. Metabolic conversion in liver is needed.

c. Some drugs can be labeled both as drug and prodrugs. So this term may be labeled ‘loosely’.

d. Like flucytosine forms 5-flurouracil and both of them are labeled as prodrugs.

e. Lisinopril is a lysing derivative of enalapril.

f. It is a drug and does not contain sulfhydryl group like its derivative.

g. As a result, dysguesia with these two drugs is lower than that of a drug that contains SH group i.e. captopril.

h. Losartan is a long acting antihypertensive that block AT1 receptors of Angiotensin-II class.

i. The drug forms a long acting active metabolite named irbisartan. It is eliminated by bile and does modification in renal failure therefore is not needed.

j. Importantly, the drug has uricosuric activity and therefore, it is the preferred antihypertensive for patients with gout with hypertension.

k. Losartan should be stopped 24 hours before surgery as the drug can increase bleeding tendency. Zoxazolamine is a muscle relaxant with uricosuric activity, while ticrinofen is a thiazide diuretic with uricosuric property.

l. Fenofibrate, a lipid-lowering drug may also have some degree of uricosuric action.

[Mnemonics: All ACEI are prodrug except CL (Casual Leave) Lisinopril & Captopril ]

Cardiovascular Systems Flashcard List

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