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Aliskiren (ah LIS ker in; Tekturna – Novartis), the first direct renin inhibitor, has been approved by the FDA for treatment of hypertension. It is indicated for oral use either as monotherapy or in combination with other antihypertensive agents.
MECHANISM OF ACTION — Renin catalyzes the cleavage of angiotensinogen to form angiotensin I, the first and rate-limiting step of the renin-angiotensinaldosterone system (RAAS). Aliskiren binds renin, leading to reduced levels of angiotensin I, angiotensin II and aldosterone.
All drugs that inhibit RAAS, including aliskiren, can cause a compensatory increase in plasma renin concentrations (PRC), but unlike angiotensin converting enzyme (ACE) inhibitors and angiotensin receptor blockers (ARBs), aliskiren does not appear to increase plasma renin activity (PRA) because it binds renin with high affinity in plasma.1,2 In one pharmacokinetic... more