Olmesartan

Overview

Olmesartan, sold under the brand name Benicar among others, is a medication used to treat high blood pressure (hypertension). It is taken orally (swallowed by mouth). Versions are available as the combination olmesartan/hydrochlorothiazide and olmesartan/amlodipine. It is available as a prodrug, olmesartan medoxomil.[1][2] WP

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

It was patented in 1991 and came into medical use in 2002. It is available as a generic medication. In 2023, it was the 96th most commonly prescribed medication in the United States, with more than 7 million prescriptions.[4–7] WP

Uses, dosage and effects

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] WP

Olmesartan is used for the treatment of hypertension. It may be used alone or in combination with other antihypertensive agents.[8] WP

Risks and side effects

Contraindications

Contraindications for treatment with olmesartan include biliary obstruction. Another major contraindication is pregnancy; reports in the scientific literature reveal fetal malformations for pregnant women taking sartan-derived drugs.[9] WP

Adverse effects

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.[10][11] WP

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 dizziness (3% vs 1%). Rarely, olmesartan can cause severe gastrointestinal issues called olmesartan-induced enteropathy. The symptoms, which include nausea, vomiting, diarrhea, weight loss, and electrolyte abnormalities, are common among those who have celiac disease. Recent studies suggested this form of sprue-like enteropathy could be caused by the inhibition of TGF-β, a polypeptide cytokine that maintains intestinal homeostasis. However, it is still unclear why this action was never observed with other ARBs. In studies of angiotensin II receptor antagonists such as olmesartan, patients with unilateral or bilateral renal artery stenosis have been reported to have increases in serum creatinine or blood urea nitrogen. 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][12][13] WP

Research

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. This effect was also observed in a high-cholesterol primate test model.[14][15] WP

History

History

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

Legal status

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.[16] WP

Several preparations containing olmesartan and other antihypertensives are available. Teva Pharmaceuticals produces a formulation containing olmesartan, amlodipine, and hydrochlorothiazide. Benicar HCT is the brand name of a medication containing olmesartan medoxomil with hydrochlorothiazide. Benitec H, another medication containing olmesartan medoxomil and hydrochlorothiazide, is marketed by GlaxoSmithKline in India.[17] WP⚠ Wikipedia itself has flagged this text: citation needed.

Chemistry

Formula

C29H30N6O6 PC

CAS number

144689-63-4 PC

Molar mass (g/mol)

558.6 PC

IUPAC name (computed by PubChem)

(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 5-(2-hydroxypropan-2-yl)-2-propyl-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazole-4-carboxylate PC

SMILES

CCCC1=NC(=C(N1CC2=CC=C(C=C2)C3=CC=CC=C3C4=NNN=N4)C(=O)OCC5=C(OC(=O)O5)C)C(C)(C)O PC

InChIKey

UQGKUQLKSCSZGY-UHFFFAOYSA-N PC

PubChem CID

130881

Harm reduction information

No harm reduction data is on file for this compound yet. That means no dose, timing or combination data from PsychonautWiki or TripSit. Please don't guess a dose from similar compounds. If you have taken it and feel unwell, contact emergency services or a poison control center.

User reports

Pop culture

No references added yet.

Sources

1. Journal / agency Benicar- olmesartan medoxomil tablet, film coated. 7 September 2022
2. Other Olmesartan Medoxomil Monograph for Professionals
3. Other Olmesartan Pregnancy and Breastfeeding Warnings
4. Other Fischer J, Ganellin CR. Analogue-based Drug Discovery. 2006
5. Other British national formulary: BNF 76. 2018
6. Other Top 300 of 2023
7. Other Olmesartan Drug Usage Statistics, United States, 2014 - 2023
8. Other Benicar (olmesartan medoxomil). 5 July 2007
9. Journal / agency Hünseler C, Paneitz A, Friedrich D, Lindner U, Oberthuer A, Körber F, Schmitt K, Welzing L, Müller A, Herkenrath P, Hoppe B, Gortner L, Roth B, Kattner E, Schaible T. Angiotensin II receptor blocker induced fetopathy: 7 cases. Klinische Padiatrie. January 2011. doi:10.1055/s-0030-1269895 · PMID 21271514
10. Other FDA Alert: Benicar (olmesartan): Ongoing Safety Review
11. Journal / agency FDA Drug Safety Communication: FDA review of cardiovascular risks for diabetics taking hypertension drug olmesartan not conclusive; label updates required. 24 June 2014
12. Journal / agency De Petris G, Caldero SG, Chen L, Xiao SY, Dhungel BM, Spizcka AJ, Lam-Himlin D. Histopathological changes in the gastrointestinal tract due to medications: an update for the surgical pathologist (part II of II). International Journal of Surgical Pathology. May 2014. doi:10.1177/1066896913502230 · PMID 24021900
13. Journal / agency Rubio-Tapia A, Herman ML, Ludvigsson JF, Kelly DG, Mangan TF, Wu TT, Murray JA. Severe spruelike enteropathy associated with olmesartan. Mayo Clinic Proceedings. August 2012. doi:10.1016/j.mayocp.2012.06.003 · PMID 22728033 · PMC3538487
14. Journal / agency Omboni S, Volpe M. Management of arterial hypertension with angiotensin receptor blockers: Current evidence and the role of olmesartan. Cardiovascular Therapeutics. December 2018. doi:10.1111/1755-5922.12471 · PMID 30358114 · PMC6587798
15. Journal / agency Miyazaki M, Takai S. Anti-atherosclerotic efficacy of olmesartan. Journal of Human Hypertension. May 2002. doi:10.1038/sj.jhh.1001393 · PMID 11967727
16. Other Cosette Pharmaceuticals Acquires Rights to Eight Branded Products from Daiichi Sankyo. 18 January 2022
17. Journal / agency OLMESARTAN MEDOXOMIL, AMLODIPINE AND HYDROCHLOROTHIAZIDE – olmesartan medoxomil, amlodipine and hydrochlorothiazide tablet, film coated

Text and values on this page are quoted from Wikipedia (CC BY-SA 4.0), PubChem (public domain). Each value links to the exact revision it came from.