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QuickView for olmesartan (compound)


PubChem Substance
Name: olmesartan
PubChem Substance ID: 707351
Synonyms:
Benicar; Votum; DE-092; Olmetec; Olmesartan; Olmesartan medoximil; Olmesartan medoxomil
DrugBank
Identification
Name: olmesartan
Name (isomeric): DB00275
Drug Type: small molecule
Synonyms:
DE-092; Olmesartan medoximil; Olmesartan medoxomil
Brand: Olmetec, Benicar, Votum, Benicar HCT
Category: Angiotensin II Type 1 Receptor Blockers, Antihypertensive Agents
CAS number: 144689-63-4
Pharmacology
Indication: For the treatment of hypertension.
Pharmacology:
Olmesartan, a specific angiotensin II type 1 antagonist, is used alone or with other antihypertensive agents to treat hypertension. Unlike the angiotensin receptor antagonist losartan, olmesartan does not have an active metabolite or possess uricosuric effects. Blockade of the angiotensin II receptor inhibits the negative regulatory feedback of ang...
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Mechanism of Action:
Angiotensin II is formed from angiotensin I in a reaction catalyzed by angiotensin converting enzyme (ACE, kininase II). Angiotensin II is the principal pressor agent of the renin-angiotensin system, with effects that include vasoconstriction, stimulation of synthesis and release of aldosterone, cardiac stimulation and renal reabsorption of sodium....
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Absorption: Bioavailability is about 26%. Food does not affect the bioavailability of olmesartan.
Protein binding: Highly bound to plasma proteins (99%) and does not penetrate red blood cells.
Biotransformation: Olmesartan is rapidly and completely bioactivated by ester hydrolysis to olmesartan during absorption from the gastrointestinal tract. There is virtually no further metabolism of olmesartan.
Half Life: Approximately 13 hours
Clearance: Total plasma cl=1.3 L/h Renal cl=0.6 L/h
Toxicity: Symptoms of overdose include dehydration (dry mouth, excessive thirst, muscle pain or cramps, nausea and vomiting, weakness), dizziness, low blood pressure, and slow or irregular heartbeat.
Affected organisms: Humans and other mammals
Interactions
Food interaction:
Food does not affect the bioavailability of olmesartan.
Drug interaction:
TobramycinIncreased risk of nephrotoxicity
TrandolaprilThe angiotensin II receptor blocker, Olmesartan, may increase the adverse effects of Trandolapril.
TreprostinilAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
DrospirenoneIncreased risk of hyperkalemia

Targets


Transporters