Olmesartan belongs to the angiotensin II receptor blocker (ARB) family of drugs, which also includes [telmisartan], [candesartan], [losartan], [valsartan], and [irbesartan]. ARBs selectively bind to angiotensin receptor 1 (AT1) and prevent the protein angiotensin II from binding and exerting its hypertensive effects, which include vasoconstriction, stimulation and synthesis of aldosterone and ADH, cardiac stimulation, and renal reabsorption of sodium, among others. Overall, olmesartan's physiologic effects lead to reduced blood pressure, lower aldosterone levels, reduced cardiac activity, and increased excretion of sodium. Olmesartan also affects the renin-angiotensin aldosterone system (RAAS), which plays an important role in hemostasis and regulation of kidney, vascular, and cardiac functions. Pharmacological blockade of RAAS via AT1 receptor blockade inhibits negative regulatory feedback within RAAS, which is a contributing factor to the pathogenesis and progression of cardiovascular disease, heart failure, and renal disease. In particular, heart failure is associated with chronic activation of RAAS, leading to inappropriate fluid retention, vasoconstriction, and ultimately a further decline in left ventricular function. ARBs have been shown to have a protective effect on the heart by improving cardiac function, reducing afterload, increasing cardiac output and preventing ventricular hypertrophy and remodelling.[A174154] By comparison, the angiotensin-converting enzyme inhibitor (ACEi) class of medications (which includes drugs such as [ramipril], [lisinopril], and [perindopril]) inhibit the conversion of angiotensin I to angiotensin II through inhibition of the ACE enzyme. However, this does not prevent the formation of all angiotensin II within the body. The angiotensin II receptor blocker (ARB) family of drugs unique in that it blocks all angiotensin II activity, regardless of where or how it was synthesized. Olmesartan is commonly used for the management of hypertension and Type 2 Diabetes-associated nephropathy, particularly in patients who are unable to tolerate ACE inhibitors. ARBs such as olmesartan have been shown in a number of large-scale clinical outcomes trials to improve cardiovascular outcomes including reducing risk of myocardial infarction, stroke, the progression of heart failure, and hospitalization.[A174124,A178153,A173869,A185324,A185327,A185333,A185342,A185345] Like other ARBs, olmesartan blockade of RAAS slows the progression of diabetic nephropathy due to its renoprotective effects.[A185906,A185909,A185912] Orally available olmesartan is produced as the prodrug olmesartan medoxomil which is rapidly converted _in vivo_ to the pharmacologically active olmesartan.[A175330] It was developed by Daiichi Sankyo Pharmaceuticals and approved in 2002.[A175345, L12882]
Olmesartan Medoxomil, Amlodipine and Hydrochlorothiazide 40/10/12.5 mg
Apo-olmesartan/hctz
Azor
OLMESARTAN MEDOXOMIL and HYDROCHLOROTHIAZIDE
Amlodipine and olmesartan Medoxomil
Auro-olmesartan
Ach-olmesartan Hctz
Gln-olmesartan Hctz
Teva-olmesartan/hctz
Auro-olmesartan Hctz
Ach-olmesartan
AMLODIPINE and OLMESARTAN medoxomil
Olmesartan Medoxomil / Hydrochlorothiazide
Med-olmesartan
Olmesartan/hctz
Olmetec Plus
Benicar
Olmesartan
Olmetec
Olmesartan Medoxomil/hctz
Amlodipine Besylate and Olmesartan Medoxomil
Benicar HCT
Apo-olmesartan
Amlodipine besylate and Olmesartran medoxomil
Olmesartan Medoxomil, Amlodipine and Hydrochlorothiazide
Olmesartan Medoxomil, Amlodipine and Hydrochlorothiazide 40/5/12.5 mg
Olmesartan Medoxomil, Amlodipine and Hydrochlorothiazide 40/10/25 mg
PMS-olmesartan-hctz
Olmesartan Medoxomil and Hydrochlorothiazide
Jamp-olmesartan Hctz
Ag-olmesartan Hctz
Ag-olmesartan
M-olmesartan
Olmesartan Medoxomil
Amlodipine besylate and Olmesartan medoxomil
Prz-olmesartan
Olmesartan Medoxomil, Amlodipine and Hydrochlorothiazide 20/5/12.5 mg
Indication
Olmesartan is indicated for the treatment of hypertension either alone or in combination with other antihypertensive agents.[F4709,F4712,A173869] Olmesartan is also used off-label for the management Type 2 Diabetes-associated nephropathy, heart failure, and post-myocardial infarction, particularly in patients who are unable to tolerate ACE inhibitors.[A178153,A185912,A185915] ARBs such as olmesartan have been shown in a number of large-scale clinical outcomes trials to improve cardiovascular outcomes including reducing risk of myocardial infarction, stroke, the progression of heart failure, and hospitalization.[A174124,A178153,A173869,A185324,A185327,A185333,A185342,A185345] Like other ARBs, olmesartan blockade of RAAS slows the progression of diabetic nephropathy due to its renoprotective effects.[A185906,A185909,A185912]
Categories
Agents Acting on the Renin-Angiotensin System
Agents causing hyperkalemia
Angiotensin 2 Receptor Blocker
Angiotensin II Antagonists and Calcium Channel Blockers
Angiotensin II receptor antagonists
Angiotensin II receptor blockers (ARBs) and calcium channel blockers
Angiotensin II receptor blockers (ARBs) and diuretics
Angiotensin II receptor blockers (ARBs), plain
Angiotensin Receptor Antagonists
Antihypertensive Agents
Antihypertensive Agents Indicated for Hypertension
Drug Info/Drug Targets: DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Knox C, Law V, Jewison
T, Liu P, Ly S, Frolkis A, Pon A, Banco K, Mak C, Neveu V, Djoumbou Y, Eisner R, Guo AC, Wishart DS.
Nucleic Acids Res. 2011 Jan; 39 (Database issue):D1035-41. | PMID:21059682
