Irbesartan

Irbesartan, sold under the trade name Avapro among others, is a medication used to treat high blood pressure, heart failure, and diabetic kidney disease.[1] It is a reasonable initial treatment for high blood pressure.[1] It is taken by mouth.[1] Versions are available as the combination irbesartan/hydrochlorothiazide.[1]

Irbesartan
Clinical data
Pronunciation/ɜːrbəˈsɑːrtən/
Trade namesAvapro, others
AHFS/Drugs.comMonograph
MedlinePlusa698009
License data
Pregnancy
category
  • AU: D
    Routes of
    administration    		By mouth
    ATC code
    Legal status
    Legal status
    • AU: S4 (Prescription only)
    • UK: POM (Prescription only)
    • US: ℞-only
    Pharmacokinetic data
    Bioavailability60% to 80%
    Protein binding~90%
    MetabolismLiver (CYP2C9)
    Elimination half-life11 h to 15 h
    ExcretionKidney 20%, faecal 65%
    Identifiers
    CAS Number
    PubChem CID
    IUPHAR/BPS
    DrugBank
    ChemSpider
    UNII
    KEGG
    ChEBI
    ChEMBL
    CompTox Dashboard (EPA)
    ECHA InfoCard100.119.966
    Chemical and physical data
    FormulaC25H28N6O
    Molar mass428.53 g/mol g·mol−1
    3D model (JSmol)
      (verify)

    Common side effects include dizziness, diarrhea, feeling tired, muscle pain, and heartburn.[1][2] Serious side effects may include kidney problems, low blood pressure, and angioedema.[1] Use in pregnancy may harm the baby and use when breastfeeding is not recommended.[3] It is an angiotensin II receptor antagonist and works by blocking the effects of angiotensin II.[1]

    Irbesartan was patented in 1990 and approved for medical use in 1997.[4] It is available as a generic medication.[2] A month supply in the United Kingdom costs the NHS less than two pounds as of 2019.[2] In the United States the wholesale cost of this amount is about six dollars.[5] In 2016, it was the 171st most prescribed medication in the United States, with more than 3.6 million prescriptions.[6]

    Medical uses

    As with all angiotensin II receptor antagonists, irbesartan is used 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,[7] hypertension and microalbuminuria (>30 mg/24 h) or proteinuria (>900 mg/24 h).[8]

    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.

    Society and culture

    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.

    References
    1. "Irbesartan Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 3 March 2019.
    2. British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 175. ISBN 9780857113382.
    3. "Irbesartan Pregnancy and Breastfeeding Warnings". Drugs.com. Retrieved 3 March 2019.
    4. Fischer, Jnos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 470. ISBN 9783527607495.
    5. "NADAC as of 2019-02-27". Centers for Medicare and Medicaid Services. Retrieved 3 March 2019.
    6. "The Top 300 of 2019". clincalc.com. Retrieved 26 February 2019.
    7. 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" (PDF). N Engl J Med. 345 (12): 851–60. doi:10.1056/NEJMoa011303. hdl:2445/122787. PMID 11565517.
    8. Rossi S, editor. Australian Medicines Handbook 2006. Adelaide: Australian Medicines Handbook; 2006. ISBN 0-9757919-2-3
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