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CARDIOVASCULAR SYSTEM › AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM › OTHER AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM › Renin-inhibitors
aliskiren and amlodipine
C09XA53
Forms & Strengths
- Aliskiren/amlodipine 150 mg/5 mg oral tablet
- Aliskiren/amlodipine 150 mg/10 mg oral tablet
- Aliskiren/amlodipine 300 mg/5 mg oral tablet
- Aliskiren/amlodipine 300 mg/10 mg oral tablet
Adult Dosing
- Hypertension: One tablet once daily
- Titrate dose based on clinical response up to max dose of 300 mg/10 mg daily
- Initial therapy not recommended; typically used when patients are already controlled on individual components
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established
Indications
- Treatment of hypertension, to lower blood pressure
- May be used as initial therapy in patients likely to need multiple drugs to achieve blood pressure goals
- Replacement therapy in patients stabilized on individual agents
Mechanism of Action
- Aliskiren is a direct renin inhibitor (DRI), binding to the S3BP binding pocket of renin and blocking the rate-limiting step of the renin-angiotensin-aldosterone system (RAAS) conversion of angiotensinogen to angiotensin I
- Amlodipine is a dihydropyridine calcium channel blocker (CCB) that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle, causing peripheral vasodilation
Contraindications
- Concomitant use with ACE inhibitors or ARBs in patients with diabetes mellitus or renal impairment (eGFR < 60 mL/min/1.73m2)
- History of angioedema with aliskiren
- Pregnancy (second and third trimesters)
- Hypersensitivity to aliskiren, amlodipine, or any component of the formulation
Adverse Reactions
- Peripheral edema
- Dizziness
- Headache
- Fatigue
- Hyperkalemia (especially in patients with renal impairment or diabetes)
- Hypotension
- Diarrhea
Drug Interactions
- ACE inhibitors, ARBs, or potassium-sparing diuretics: increased risk of hyperkalemia, renal impairment, and hypotension
- CYP3A4 inhibitors (e.g., ketoconazole, ritonavir): may increase amlodipine plasma concentrations
- CYP3A4 inducers (e.g., rifampin, St. John's wort): may decrease amlodipine plasma concentrations
- Ciclosporin or itraconazole: significantly increases plasma concentrations of aliskiren; co-administration is not recommended
- NSAIDs: may decrease antihypertensive effect and increase risk of renal impairment
Curated Content: Needs Vetting Before Put to Clinical Use