My watch list
my.bionity.com  
Login  

Aliskiren



Aliskiren
Systematic (IUPAC) name
(2S,4S,5S,7S)-5-amino-N-(2-carbamoyl-2-methyl-
propyl)-4-hydroxy-7-{[4-methoxy-3-(3-methoxypropoxy)
phenyl]methyl}-8-methyl-2-propan-2-yl-nonanamide
Identifiers
CAS number 173334-57-1
ATC code C09XA02 C09XA52
PubChem 5493444
Chemical data
Formula C30H53N3O6 
Mol. mass 551.758 g/mol
Pharmacokinetic data
Bioavailability Low (approximately 2.5%)
Metabolism Hepatic, CYP3A4-mediated
Half life 24 hours
Excretion Renal
Therapeutic considerations
Pregnancy cat.

C in first trimester
D in second and third trimesters

Legal status

-only(US)

Routes Oral

Aliskiren (INN) is a first in class renin inhibitor co-developed by the Swiss pharmaceutical companies Novartis and Speedel.[1][2] It was approved by the U.S. Food and Drug Administration in 2007 for the treatment of hypertension.[3] The trade name for aliskiren is Tekturna in the USA, and Rasilez in the UK.

Additional recommended knowledge

Contents

Adverse effects

A rare adverse event was allergic swelling of the face, lips or tongue and difficulty breathing, side effects that are common with other drugs for hypertension that act directly on the renin-angiotensin system. [4]


Contraindications

As with ACE inhibitors, renin inhibitors should not be used in pregnancy, specifically the second and third trimesters, during which they will interfere with fetal kidney development and lead to oligohydramnios.

Aliskiren has not yet been evaluated in patients with significantly impaired renal function.

Drug Interactions

Minor substrate of CYP3A4:

References

  1. ^ Gradman A, Schmieder R, Lins R, Nussberger J, Chiang Y, Bedigian M (2005). "Aliskiren, a novel orally effective renin inhibitor, provides dose-dependent antihypertensive efficacy and placebo-like tolerability in hypertensive patients". Circulation 111 (8): 1012-8. PMID 15723979.
  2. ^ Straessen JA, Li Y, and Richart T (2006). "Oral Renin Inhibitors". Lancet 368 (9545): 1449-56. PMID 17055947.
  3. ^ "First Hypertension Drug to Inhibit Kidney Enzyme Approved", CBC, March 6, 2007. Retrieved on 2007-03-14. 
  4. ^ FDA approves renin inhibitor aliskiren for hypertension. RxDrug News (2007). Retrieved on 2007-12-02.
 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Aliskiren". A list of authors is available in Wikipedia.
Your browser is not current. Microsoft Internet Explorer 6.0 does not support some functions on Chemie.DE