Aliskiren.

Purpose: The pharmacology, bioavailability and pharmacokinetics, clinical efficacy, adverse effects and toxicity, drug interactions, and dosage and administration of aliskiren as well as safety and economic issues related to its use are reviewed.

Summary: Aliskiren is the first of a new class of antihypertensive agents, direct renin inhibitors, that act by blocking the rate- limiting step of the renin-angiotensin- aldosterone system (RAAS). It was approved by the Food and Drug Administration in 2007 for use as monotherapy or in combination with other antihypertensives. Clinical studies comparing aliskiren monotherapy with placebo indicated a dose-dependent reduction in both systolic and diastolic blood pressure (BP). Greater reductions in BP have been achieved when aliskiren was used in combination with hydrochlorothiazide or an angiotensin-receptor blocker. The most common adverse effects reported in clinical trials were headache, fatigue, dizziness, diarrhea, and nasopharyngitis. Aliskiren has not been studied in patients with moderate renal dysfunction; as a RAAS-acting drug, it should be prescribed for such patients only with caution.

Conclusion: Aliskiren at a dosage of 150 or 300 mg daily may be a good option for control of mild-to-moderate hypertension in patients with or without diabetes in whom first-line antihypertensives have failed to adequately control BP; comparative studies with other antihypertensives are needed to determine which patients can most benefit from aliskiren therapy.