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Olmesartan, sold under the brand name Benicar among others, is a medication used to treat high blood pressure (hypertension). [ 1 ] [ 2 ] It is taken orally (swallowed by mouth). [ 2 ] Versions are available as the combination olmesartan/hydrochlorothiazide and olmesartan/amlodipine . [ 2 ]
Like olmesartan, the metabolism of the drug is unusual as it is a cascading prodrug. Candesartan has good bioavailibility and is the most potent by weight of the AT-1 receptor antagonists. It was patented in 1990 and approved for medical use in 1997. [2]
Olmesartan works by blocking the effects of angiotensin II while hydrochlorothiazide works by increasing the loss of sodium by the kidneys. [1] No generic version is available in the United States as of 2017. [2] In 2022, it was the 235th most commonly prescribed medication in the United States, with more than 1 million prescriptions. [4] [5]
Losartan, the first ARB. Angiotensin II receptor blockers (ARBs), formally angiotensin II receptor type 1 (AT 1) antagonists, [1] also known as angiotensin receptor blockers, [2] [3] angiotensin II receptor antagonists, or AT 1 receptor antagonists, are a group of pharmaceuticals that bind to and inhibit the angiotensin II receptor type 1 (AT 1) and thereby block the arteriolar contraction and ...
Telmisartan is, on the other hand, in part metabolized by glucuronidation and olmesartan is excreted as the unchanged drug. [23] Telmisartan is the only ARB that can cross the blood–brain barrier and can therefore inhibit centrally mediated effects of Ang II, contributing to even better blood pressure control. [1]
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Verapamil is also used in cell biology as an inhibitor of drug efflux pump proteins such as P-glycoprotein and other ABC transporter proteins. [ 45 ] [ 44 ] This is useful, as many tumor cell lines overexpress drug efflux pumps, limiting the effectiveness of cytotoxic drugs or fluorescent tags .