Pharmacology · Cardiovascular Drugs (Antihypertensives, Anti-Anginals, Heart Failure, Anti-Arrhythmics)

Among the following antihypertensive agents, which one is a direct renin inhibitor that acts at the first and rate-limiting step of the RAAS?

  • A Olmesartan
  • B Perindopril
  • C Eplerenone
  • D Aliskiren
Correct answer: D. Aliskiren

Explanation

Aliskiren is the only clinically approved direct renin inhibitor; it binds the active site of renin and prevents cleavage of angiotensinogen to angiotensin I, thereby inhibiting the RAAS at its very first enzymatic step. This results in reduced plasma renin activity and decreased Ang I and Ang II levels. Olmesartan is an ARB (blocks AT1 receptor), perindopril is an ACE inhibitor, and eplerenone is a selective mineralocorticoid receptor antagonist.

Reference: KD Tripathi, Essentials of Medical Pharmacology, 8th ed.

High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP

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