Product Information
Registration Status: ActiveISENTRESS 400MG TABLET is approved to be sold in Singapore with effective from 2008-05-11. It is marketed by MSD PHARMA (SINGAPORE) PTE LTD, with the registration number of SIN13568P.
This product contains Raltegravir 400mg in the form of TABLET, FILM-COATED. It is approved for ORAL use.
This product is manufactured by MSD International GmbH (Ballydine) in SINGAPORE,MSD INTERNATIONAL GMBH (SINGAPORE BRANCH) in IRELAND, andPT. Merck Sharp Dohme Pharma Tbk. (Primary and Secondary Packager) in INDONESIA REP OF.
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
Raltegravir is an antiretroviral drug produced by Merck & Co., used to treat HIV infection. It received approval by the U.S. Food and Drug Administration (FDA) on 12 October 2007, the first of a new class of HIV drugs, the integrase inhibitors, to receive such approval.
Indication
For the treatment of HIV-1 infection in conjunction with other antiretrovirals.
Mechanism of Action
Raltegravir targets integrase, an HIV enzyme that integrates the viral genetic material into human chromosomes, a critical step in the pathogenesis of HIV. The drug is metabolized away via glucuronidation.
Pharmacokinetics
- Absorption
- Absorbed from the gastrointestinal tract.
- Distribution
- Approximately 83% bound to human plasma protein and is minimally distributed into red blood cells (blood-to-plasma partitioning ratio of 0.6).
- Metabolism
- Hepatic (UGT1A1)
- Elimination
Clearance
The major mechanism of clearance of raltegravir in humans is glucuronidation mediated by UGT1A1, the renal clearance of unchanged drug is a minor pathway of elimination of raltegravir (9% of total dose).
Active Ingredient/Synonyms
Raltegravir | Raltegravir |
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.