Product Information
Registration Status: ActiveMEFLOTAS TABLET 250mg is approved to be sold in Singapore with effective from 2002-03-15. It is marketed by APOTHECA MARKETING PTE LTD, with the registration number of SIN11848P.
This product contains Mefloquine 250mg in the form of TABLET. It is approved for ORAL use.
This product is manufactured by INTAS PHARMACEUTICALS LTD in INDIA.
It is a Pharmacy Only Medicine that can be obtained from a pharmacist at a retail pharmacy.
Description
A phospholipid-interacting antimalarial drug (antimalarials). It is very effective against plasmodium falciparum with very few side effects. [PubChem]
Indication
For the treatment of mild to moderate acute malaria caused by Mefloquineuine-susceptible strains of Plasmodium falciparum (both chloroquine-susceptible and resistant strains) or by Plasmodium vivax. Also for the prophylaxis of Plasmodium falciparum and Plasmodium vivax malaria infections, including prophylaxis of chloroquine-resistant strains of Plasmodium falciparum.
Mechanism of Action
Mefloquine has been found to produce swelling of the Plasmodium falciparum food vacuoles. It may act by forming toxic complexes with free heme that damage membranes and interact with other plasmodial components.
Pharmacokinetics
- Absorption
- Well absorbed from the gastrointestinal tract. The presence of food significantly enhances the rate and extent of absorption.
- Distribution
- * 20 L/kg [healthy adults]
- Metabolism
- Hepatic. Two metabolites have been identified in humans. The main metabolite, 2,8-bis-trifluoromethyl-4-quinoline carboxylic acid, is inactive against Plasmodium falciparum. The second metabolite, an alcohol, is present in minute quantities.
- Elimination
Clearance
* 30 mL/min
Toxicity
Oral, rat: LD50 = 880 mg/kg. Symptoms of overdose include nausea, vomiting, and weight loss.
Active Ingredient/Synonyms
[(R*,S*)-2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol | alpha-2-Piperidinyl-2,8-bis(trifluoromethyl)-4-quinolinemethanol | Mefloquin | Mefloquina | Méfloquine | Mefloquine | Mefloquinum | Mefloquine |
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.