Generic
Aliskiren
2 brands available in the market
At a glance
Aliskiren is a direct renin inhibitor used for the treatment of hypertension (high blood pressure). It relaxes blood vessels, lowers blood pressure, and reduces the risk of heart attack and stroke.
Description
Aliskiren is an orally active, potent, non-peptide and selective direct renin inhibitor used in the management of hypertension. By inhibiting the enzyme renin, it prevents conversion of angiotensinogen into angiotensin I and therefore inhibits subsequent production of angiotensin II and aldosterone. Unlike ACE inhibitors and angiotensin II receptor antagonists which cause a compensatory rise in plasma renin activity, treatment with aliskiren decreases plasma renin activity and concentrations of angiotensin I, angiotensin II and aldosterone.
Indications
Hypertension (high blood pressure).
Therapeutic class
Direct Renin Inhibitor
Pharmacological class
Antihypertensive (Renin Inhibitor)
Pharmacology
Aliskiren directly inhibits the enzyme renin at the first step of the renin-angiotensin system (RAS). It prevents the conversion of angiotensinogen to angiotensin I, resulting in decreased levels of angiotensin II and aldosterone. This leads to vasodilation, reduced peripheral vascular resistance, and decreased blood pressure. Unlike other RAS inhibitors, aliskiren decreases rather than increases plasma renin activity.
Mechanism of action
Aliskiren directly inhibits the renin enzyme, preventing the conversion of angiotensinogen to angiotensin I. This reduces angiotensin II (a potent vasoconstrictor) and aldosterone levels, causing vasodilation and decreased blood pressure.
Dosage
Adults: 150-300 mg once daily, with or without food (but consistently).
Maximum dose: 300 mg once daily.
Special populations:
- Caution in severe heart failure, sodium or volume depletion
- Discontinue if severe and persistent diarrhea occurs
- Discontinue as soon as possible when pregnancy is detected
Administration
May be taken with or without food, but take consistently (with or without meals).
Avoid taking with high-fat meals.
Swallow tablet whole; do not crush or chew.
Missed dose
If you miss a dose, take it as soon as you remember. If it is almost time for your next dose, skip the missed dose and continue with your regular schedule. Do not double the dose.
Side effects
Common side effects:
- Diarrhea
- Dizziness
- Joint pain
- Increased blood potassium levels
Precautions & warnings
- Highly unsafe during pregnancy (may cause fetal injury or death)
- Caution in severe heart failure, sodium/volume depletion
- Discontinue if severe and persistent diarrhea occurs
- Caution in patients with history of angioedema
- Contraindicated in severe renal impairment
- Avoid concomitant use with ACE inhibitors or ARBs in patients with diabetes and renal impairment
- Caution while driving (may cause dizziness)
Contraindications
- Hypersensitivity to aliskiren
- Pregnancy
- Severe renal impairment
- History of angioedema
- Concomitant use with ACE inhibitors or ARBs in patients with diabetes and renal impairment (GFR <60 mL/min)
- Concomitant use with cyclosporine, itraconazole, quinidine
Drug interactions
- Cyclosporine, itraconazole, quinidine: Concomitant use is contraindicated
- ACE inhibitors or ARBs: Avoid concomitant use in patients with diabetes and renal impairment
- Potassium supplements or potassium-sparing diuretics: Risk of hyperkalemia
- NSAIDs: May reduce renal function
Food interactions
- Alcohol: May cause excessive drowsiness; avoid
- High-fat meals: May reduce aliskiren absorption; avoid
Use in pregnancy
Pregnancy Category: D
Aliskiren is highly unsafe during pregnancy. It affects the renin-angiotensin system causing oligohydramnios, which may result in fetal injury and/or death. Discontinue as soon as pregnancy is detected.
Pregnancy Category: D — always consult a doctor before taking during pregnancy.
Use in lactation
It is not known whether aliskiren is excreted in human milk; use is not recommended.
Pediatric use
Safety and efficacy in children have not been established.
Pregnancy Category: C (1st trimester), D (2nd & 3rd trimesters).
Geriatric use
No dose adjustment needed for elderly patients, but renal function monitoring is required.
Renal / hepatic impairment
- Renal impairment: Caution required; dose adjustment may be needed. Monitor serum creatinine and potassium regularly. Contraindicated in severe renal impairment.
- Hepatic impairment: Caution in severe liver disease; dose adjustment may be needed. No dose adjustment recommended in mild to moderate liver disease.
Overdose effects
Overdose symptoms: significant hypotension, dizziness, electrolyte imbalance. Treatment: symptomatic and supportive measures.
Storage conditions
Store below 30°C in a cool and dry place, protected from light. Keep out of reach of children.
Chemical structure
C₃₀H₅₃N₃O₆