Irbesartan

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Irbesartan
Irbesartan skeletal.svg
Clinical data
Trade names Avapro
AHFS/Drugs.com Monograph
MedlinePlus a698009
License data
Pregnancy
category
  • AU: D
Routes of
administration
Oral
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only)
  • UK: POM (Prescription only)
  • US: ℞-only
Pharmacokinetic data
Bioavailability 60–80%
Protein binding ~90%
Metabolism Hepatic (CYP2C9)
Biological half-life 11–15 hours
Excretion Renal 20%, faecal 65%
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
ECHA InfoCard 100.119.966
Chemical and physical data
Formula C25H28N6O
Molar mass 428.53 g/mol
3D model (JSmol)
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Irbesartan (INN) /ɜːrbəˈsɑːrtən/ is an angiotensin II receptor antagonist used mainly for the treatment of hypertension. It was developed by Sanofi Research (now part of Sanofi-Aventis). It is jointly marketed by Sanofi-Aventis and Bristol-Myers Squibb under the trade names Aprovel, Karvea, and Avapro.

Clinical use[edit]

Indications[edit]

As with all angiotensin II receptor antagonists, irbesartan is indicated for the treatment of hypertension. It may also delay progression of diabetic nephropathy and is also indicated for the reduction of renal disease progression in patients with type 2 diabetes,[1] hypertension and microalbuminuria (>30 mg/24 hours) or proteinuria (>900 mg/24 hours).[2]

Combination with diuretic[edit]

Irbesartan is also available in a combination formulation with a low-dose thiazide diuretic, invariably hydrochlorothiazide, to achieve an additive antihypertensive effect. Irbesartan/hydrochlorothiazide combination preparations are marketed under similar trade names to irbesartan preparations.

Heart failure[edit]

I-PRESERVE, a large randomized trial following 4100+ men and women with heart failure and normal ejection fraction (>=45%) over 4+ years found no improvement in study outcomes or survival with irbesartan as compared to placebo.[3]

See also[edit]

References[edit]

  1. ^ Lewis EJ, Hunsicker LG, Clarke WR, Berl T, Pohl MA, Lewis JB, Ritz E, Atkins RC, Rohde R, Raz I, Collaborative Study Group. (2001). "Renoprotective effect of the angiotensin-receptor antagonist irbesartan in patients with nephropathy due to type 2 diabetes". N Engl J Med. 345 (12): 851–60. PMID 11565517. doi:10.1056/NEJMoa011303. 
  2. ^ Rossi S, editor. Australian Medicines Handbook 2006. Adelaide: Australian Medicines Handbook; 2006. ISBN 0-9757919-2-3
  3. ^ Massie BM, Carson PE, McMurray JJ, Komajda M, McKelvie R, Zile MR, Anderson S, Donovan M, Iverson E, Staiger C, Ptaszynska A (December 2008). "Irbesartan in patients with heart failure and preserved ejection fraction". N. Engl. J. Med. 359 (23): 2456–67. PMID 19001508. doi:10.1056/NEJMoa0805450.