Product Information
Registration Status: ActiveOLMETEC TABLET 40MG is approved to be sold in Singapore with effective from 2004-07-19. It is marketed by PFIZER PTE LTD, with the registration number of SIN13018P.
This product contains Olmesartan 40mg in the form of TABLET, FILM-COATED. It is approved for ORAL use.
This product is manufactured by DAIICHI SANKYO EUROPE GmbH in GERMANY.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
Olmesartan is an antihypertensive agent, which belongs to the class of medications called angiotensin II receptor blockers. It is indicated for the treatment of high blood pressure and is marketed under the name Olmetec®. The FDA label includes a black-box warning of injury and death to the fetus, so women of child-bearing age need to be warned and take the necessary precautions. Olmesartan is also contraindicated in diabetes mellitus patients taking aliskiren.
Indication
For the treatment of hypertension.
Mechanism of Action
Olmesartan is an ARB that selectively inhibits the binding of angiotensin II to AT1, which is found in many tissues such as vascular smooth muscle and the adrenal glands. This effectively inhibits the AT1-mediated vasoconstrictive and aldosterone-secreting effects of angiotensin II and results in a decrease in vascular resistance and blood pressure. Olmesartan is selective for AT1 and has a 12,500 times greater affinity for AT1 than the AT2 receptor. Also unlike the well-known ARB losartan, olmesartan does not have an active metabolite or possess uricosuric effects.
Pharmacokinetics
- Absorption
- Bioavailability is about 26%. Food does not affect the bioavailability of olmesartan.
- Distribution
- The volume of distribution is 17 L and olmesartan poorly crosses the blood brain barrier.
- Metabolism
- 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.
- Elimination
Clearance
* Total plasma cl=1.3 L/h * Renal cl=0.6 L/h
Toxicity
The main symptoms of overdose include low blood pressure and fast heartbeat.
Active Ingredient/Synonyms
4-(1-hydroxy-1-methylethyl)-2-propyl-1-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1H-imidazole-5-carboxylic acid | 4-(hydroxy-1-methylethyl)-2-propyl-1-{[2'-(1H-tetrazol-5-yl)-1,1'-biphenyl-4-yl]methyl}-1H-imidazole-5-carboxylic acid | Olmesartan |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.