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Irbesartan

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Title: Irbesartan  
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Subject: Angiotensin II receptor antagonist, Sanofi, Antihypertensive drug, Discovery and development of angiotensin receptor blockers, Angiotensin II receptor antagonists
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Irbesartan

Irbesartan
Systematic (IUPAC) name
2-butyl-3-({4-[2-(2H-1,2,3,4-tetrazol-5-yl)phenyl]phenyl}methyl)-1,3-diazaspiro[4.4]non-1-en-4-one
Clinical data
Trade names Avapro
AHFS/Drugs.com
MedlinePlus
Licence data EMA:, US FDA:
Pregnancy
category
Legal status
  • S4 (Au), POM (UK), ℞-only (U.S.)
Routes of
administration
Oral
Pharmacokinetic data
Bioavailability 60–80%
Protein binding ~90%
Metabolism Hepatic (CYP2C9)
Biological half-life 11–15 hours
Excretion Renal 20%, faecal 65%
Identifiers
CAS Registry Number  Y
ATC code C09
PubChem CID:
IUPHAR/BPS
DrugBank  Y
ChemSpider  Y
UNII  Y
KEGG  Y
ChEBI  Y
ChEMBL  Y
Chemical data
Formula C25H28N6O
Molecular mass 428.53 g/mol
 Y   

Irbesartan (INN) 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.

Contents

  • Clinical use 1
    • Indications 1.1
    • Combination with diuretic 1.2
    • Heart failure 1.3
  • See also 2
  • References 3

Clinical use

Indications

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

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

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

References

  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.  
  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; Carson; McMurray; Komajda; McKelvie; Zile; Anderson; Donovan; Iverson; Staiger; Ptaszynska; i-Preserve (December 2008). "Irbesartan in patients with heart failure and preserved ejection fraction". N. Engl. J. Med. 359 (23): 2456–67.  


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