Aliskiren
- Atc Codes:C09XA02
- CAS Codes:173334-57-1#173334-58-2
- PHARMGKB ID:173334-57-1#173334-58-2
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Substrate of
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Enviage (d), Rasilez, Riprazo, Sprimeo, Tekturna (d); Belgium: Rasilez; Cyprus: Rasilez; Czech Republic: Enviage (d), Rasilez, Riprazo, Sprimeo, Tekturna (d); Denmark: Rasilez; Estonia: Enviage (d), Rasilez, Riprazo, Sprimeo; Finland: Rasilez; France: Rasilez; Germany: Enviage (d), Rasilez, Riprazo, Sprimeo, Tekturna (d); Greece: Enviage (d), Rasilez, Riprazo, Sprimeo, Tekturna (d); Hungary: Rasilez; Ireland: Rasilez; Italy: Rasilez; Latvia: Enviage (d), Rasilez, Riprazo, Sprimeo, Tekturna (d); Luxembourg: Enviage (d), Rasilez, Riprazo, Tekturna (d); Netherlands: Enviage (d), Rasilez, Riprazo, Sprimeo; Poland: Enviage (d), Rasilez, Riprazo, Sprimeo, Tekturna (d); Portugal: Enviage (d), Rasilez, Riprazo, Sprimeo, Tekturna (d); Romania: Enviage (d), Rasilez, Riprazo, Sprimeo, Tekturna (d); Slovakia: Enviage (d), Rasilez, Sprimeo, Riprazo, Tekturna (d); Spain: Rasilez, Sprimeo; Sweden: Enviage (d), Rasilez, Riprazo, Sprimeo; UK: Rasilez.
North America
Canada: Rasilez; USA: Tekturna.
Latin America
Argentina: Rasilez; Mexico: Rasilles.
Drug combinations
Aliskiren and Amlodipine
Aliskiren and Hydrochlorothiazide
Aliskiren and Valsartan
Aliskiren, Amlodipine and Hydrochlorothiazide
Chemistry
Aliskiren: C~30~H~53~N~3~O~6~. Mw: 551.76. (1) Benzeneoctanamide, δ-amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)-γ-hydroxy-4-methoxy-3-(3-methoxypropoxy)-α,ζ-bis(1-methylethyl)-, (αS, γS, δS, ζS)-; (2)(2S,4S,5S,7S)-5-Amino-N-(2-carbamoyl-2-methylpropyl)-4-hydroxy-2-isopropyl-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-8-methylnonamide. CAS-173334-57-1 (2005).
Aliskiren Fumarate: (C~30~H~53~N~3~O~6~)~2~ C~4~H~4~O~4~. Mw: 1219.59. (1) Benzeneoctanamide, δ-amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)-γ-hydroxy-4-methoxy-3-(3-methoxypropoxy)-α,ζ-bis(1-methylethyl)-, (αS, γS, δS, ζS)-, (2E)-2-butenedioate (2:1)(salt); (2) Bis(2S,4S,5S,7S)-5-amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-8-methyl-2-(1-methylethyl)nonanamide] (2E)-but-2-enedioate. CAS-173334-58-2 (2006).
Pharmacologic Category
Renin Inhibitors. (ATC-Code: C09XA02).
Mechanism of action
Blocks conversion of angiotensinogen to angiotensin I.
Therapeutic use
Treatment of hypertension.
Pregnancy and lactiation implications
Can cause injury and death to the developing fetus when used in the second and third trimesters. Should be discontinued as soon as possible once pregnancy is detected. Not recommended during lactation.
Unlabeled use
Treatment of persistent proteinuria in type 2 diabetes mellitus, hypertension, and nephropathy despite administration of optimized recommended renoprotective therapy (e.g. angiotensin II receptor blocker).
Contraindications
Hypersensitivity to aliskiren or any component of the formulation.
Warnings and precautions
Angioedema, hyperkalemia and hypotension (rarely) might occur. Caution in severe renal impairment or renal artery stenosis (bilateral or unilateral). Risk of interactions in patients taking strong inhibitors of P-glycoprotein (e.g. cyclosporine).