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Olmesartan

Catalog No. DB00275 Name DrugBank
CAS Number 144689-63-4 Website http://www.ualberta.ca/
M. F. C29H30N6O6 Telephone (780) 492-3111
M. W. 558.5851 Fax (780) 492-1071
Purity Email david.wishart@ualberta.ca
Storage Chembase ID: 160

SYNONYMS

IUPAC name
(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
IUPAC Traditional name
olmesartan
Brand Name
Olmetec
Votum
Benicar
Benicar HCT
Synonyms
Olmesartan medoxomil
Olmesartan medoximil
DE-092

DATABASE IDS

CAS Number 144689-63-4

PROPERTIES

Hydrophobicity(logP) 5.9

DETAILS

Description (English)
Item Information
Drug Groups approved; investigational
Description Olmesartan is an antihypertensive agent which belongs to the class of medicines called angiotensin II receptor antagonists. It acts rapidly to lower high blood pressure. It is marketed worldwide by Daiichi Sankyo, Ltd. and in the United States by Daiichi Sankyo, Inc. and Forest Laboratories.
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 angiotensin II on renin secretion, but the resulting increased plasma renin activity and circulating angiotensin II levels do not overcome the effect of olmesartan on blood pressure.
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
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.
Absorption Bioavailability is about 26%. Food does not affect the bioavailability of olmesartan.
Half Life Approximately 13 hours
Protein Binding Highly bound to plasma proteins (99%) and does not penetrate red blood cells.
Distribution * 17 L
Clearance * Total plasma cl=1.3 L/h
* Renal cl=0.6 L/h
External Links
Wikipedia
RxList
PDRhealth
Drugs.com

REFERENCES