Olmesartan

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Olmesartan
Clinical data
Trade namesBenicar
Other namesOlmesartan medoxomil
AHFS/Drugs.comMonograph
MedlinePlusa603006
License data
diuretics)
C09DB02 (WHO) (with amlodipine)
Legal status
Legal status
Pharmacokinetic data
Bioavailability26%
MetabolismLiver (cannot be removed by hemodialysis)
Elimination half-life13 hours
ExcretionKidney 40%, bile duct 60%
Identifiers
  • (5-methyl-2-oxo-2H-1,3-dioxol-4-yl)methyl 4-(2-hydroxypropan-2-yl)-2-propyl-1-({4-[2-(2H-1,2,3,4-tetrazol-5-yl)phenyl]phenyl}methyl)-1H-imidazole-5-carboxylate
JSmol)
  • CCCc1nc(c(n1Cc2ccc(cc2)c3ccccc3c4[nH]nnn4)C(=O)OCc5c(oc(=O)o5)C)C(C)(C)O
  • InChI=1S/C29H30N6O6/c1-5-8-23-30-25(29(3,4)38)24(27(36)39-16-22-17(2)40-28(37)41-22)35(23)15-18-11-13-19(14-12-18)20-9-6-7-10-21(20)26-31-33-34-32-26/h6-7,9-14,38H,5,8,15-16H2,1-4H3,(H,31,32,33,34) checkY
  • Key:UQGKUQLKSCSZGY-UHFFFAOYSA-N checkY
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Olmesartan, sold under the brand name Benicar among others, is a

olmesartan/amlodipine.[2]

Common side effects include dizziness,

angiotensin II.[2]

It was patented in 1991 and came into medical use in 2002.

generic medication.[5] In 2021, it was the 126th most commonly prescribed medication in the United States, with more than 4 million prescriptions.[6][7]

Medical uses

In the United States, olmesartan is

indicated for the treatment of hypertension in people aged six years of age and older to lower blood pressure.[1]

Olmesartan is used for the treatment of hypertension. It may be used alone or in combination with other antihypertensive agents.[8] The US Food and Drug Administration (FDA) has determined that the benefits of olmesartan continue to outweigh its potential risks when used for the treatment of people with high blood pressure according to the drug label.[9]

Contraindications

biliary obstruction. Another major contraindication is pregnancy; reports in the scientific literature reveal fetal malformations for pregnant women taking sartan-derived drugs.[10]

Adverse effects

The incidence of adverse effects with olmesartan is reported as similar to placebo; the only adverse effect that occurred in >1% of patients treated with it and more frequently than placebo was

serum creatinine or blood urea nitrogen have been reported. There has been no long-term use of olmesartan medoxomil in patients with unilateral or bilateral renal artery stenosis, but similar results may be expected.[1]

Chemistry

An ester

hydrolyzed to its active acid form.[13] The metabolites in this process are carbon dioxide and 2,3-dione.[citation needed
]

History

See also: Discovery and development of angiotensin receptor blockers

It was patented in 1991 and came into medical use in 2002.[4]

Society and culture

Brand names

Olmesartan and Sevikar HCT combined is marketed worldwide by Daiichi Sankyo, in India by Abbott Healthcare Pvt. Ltd. under the trade name WinBP, by Zydus Cadila under the trade name Olmy, by Ranbaxy Laboratories Ltd. under the trade name Olvance, Olsar by Unichem Laboratories and in Canada by Schering-Plough as Olmetec. The marketing rights to the brand names Benicar, Benicar HCT, Azor, and Tribenzor in the United States were transferred from Daiichi Sankyo to Cosette in January 2022.[14]

Several preparations containing olmesartan and other antihypertensives are available. Teva Pharmaceuticals produces a formulation containing olmesartan,

olmesartan medoxomil with hydrochlorothiazide
. Benitec H, another medication containing olmesartan medoxomil and hydrochlorothiazide, is marketed by GlaxoSmithKline in India.

Research

Olmesartan has demonstrated potential benefits in reducing the progression of atherosclerotic buildup in arteries. In large randomized placebo-controlled or active drug-controlled studies conducted in participants with hypertension, stable angina, or type 2 diabetes, long-term treatment with olmesartan has been shown to reduce the levels of markers of vascular inflammation.[16] This effect was also observed in a high-cholesterol primate test model.[17]

References

  1. ^ a b c d "Benicar- olmesartan medoxomil tablet, film coated". DailyMed. 7 September 2022. Retrieved 14 April 2023.
  2. ^ a b c d e f "Olmesartan Medoxomil Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 3 March 2019.
  3. ^ "Olmesartan Pregnancy and Breastfeeding Warnings". Drugs.com. Retrieved 3 March 2019.
  4. ^
    ISBN 9783527607495
    .
  5. ISBN 9780857113382
    .
  6. ^ "The Top 300 of 2021". ClinCalc. Archived from the original on 15 January 2024. Retrieved 14 January 2024.
  7. ^ "Olmesartan - Drug Usage Statistics". ClinCalc. Retrieved 14 January 2024.
  8. ^ "Benicar (olmesartan medoxomil)". RxList Inc. 5 July 2007. Retrieved 22 July 2010.
  9. ^ "FDA Alert: Benicar (olmesartan): Ongoing Safety Review". Drugs.com. Retrieved 27 June 2013.
  10. S2CID 260206339
    .
  11. S2CID 20614874
    .
  12. PMID 22728033
    .
  13. PMID 17692338
    .
  14. ^ "Cosette Pharmaceuticals Acquires Rights to Eight Branded Products from Daiichi Sankyo". Cosette Pharma (Press release). 18 January 2022. Retrieved 14 April 2023.
  15. ^ "OLMESARTAN MEDOXOMIL, AMLODIPINE AND HYDROCHLOROTHIAZIDE – olmesartan medoxomil, amlodipine and hydrochlorothiazide tablet, film coated". DailyMed. U.S. National Library of Medicine.
  16. PMID 30358114
    .
  17. S2CID 23755806
    .
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