← Search & browse all drugs
CARDIOVASCULAR SYSTEM › AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM › OTHER AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM › Renin-inhibitors
aliskiren
C09XA02
Forms & Strengths
- Oral tablets: 150 mg
- Oral tablets: 300 mg
Adult Dosing
- Hypertension: Initial 150 mg once daily, may increase to 300 mg once daily as needed and tolerated
- Maximum recommended dose: 300 mg once daily
Pediatric Dosing
- Safety and efficacy in pediatric patients < 18 years of age have not been established
Indications
- Treatment of hypertension to lower blood pressure in adults
- May be used alone or in combination with other antihypertensive agents
Mechanism of Action
- Direct renin inhibitor that binds to the S3sp binding pocket of human renin
- Blocks the rate-limiting step of the renin-angiotensin-aldosterone system (RAAS) by converting angiotensinogen to angiotensin I
Contraindications
- Concomitant use with ACE inhibitors or angiotensin receptor blockers (ARBs) in patients with diabetes mellitus
- Hypersensitivity to aliskiren or any component of the formulation
- Pregnancy (second and third trimesters)
Adverse Reactions
- Hypotension
- Hyperkalemia
- Diarrhea
- Dizziness
- Headache
- Nasopharyngitis
- Angioedema
Drug Interactions
- ACE inhibitors or ARBs: Increased risk of renal impairment, hyperkalemia, and hypotension (contraindicated in diabetes)
- CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, cyclosporine): May increase plasma concentrations of aliskiren
- Potassium-sparing diuretics, potassium supplements, or salt substitutes containing potassium: Increased risk of severe hyperkalemia
- Nonsteroidal anti-inflammatory drugs (NSAIDs): May reduce the antihypertensive effect and increase the risk of renal impairment
Curated Content: Needs Vetting Before Put to Clinical Use