Mefloquine hydrochloride

Описание

Mefloquine hydrochloride is an erythrocytic schizonticide useful, in combination with sulfadoxine and pyrimethamine, in the prophylaxis and treatment of malaria. Administered once weekly, the combination is effective against pathogens resistant to other agents.

Химические свойства

White Solid

Использование

Mefloquine Hydrochloride (Polymorph Form E) is a polymorphic form of Mefloquine Hydrochloride (M207055), a quinoline methanol antimalarial agent.

Общее описание

Certified pharmaceutical secondary standards for application in quality control provide pharma laboratories and manufacturers with a convenient and cost-effective alternative to pharmacopeia primary standards

Клиническое использование

The newest of the 4-aminoquinolines,mefloquine, is marketed as the R,S-isomer. It was developedin the 1960s as part of the U.S. Army’s WalterReed Institute for Medical Research antimalarial researchprogram. It differs significantly from the other agents in this class by having two trifluromethyl moieties at positions2’ and 8' and no electronegative substituents at eitherpositions 6' (quinine) or 7' (chloroquine). Mefloquine alsodiffers from chloroquine and its analogs by being a schizonticide acting before the parasite canenter the erythrocyte. There is some evidence that it acts byraising the pH in the parasite’s vesicles interfering with itsability to process heme. Mefloquine-resistant strains ofP. falciparum have appeared. Relapse can occur with acuteP. vivax that has been treated with mefloquine because thedrug does not eliminate the hepatic phase of this species,which can reinfect the liver.
Mefloquine is teratogenic in rats, mice, and rabbits. Thereis an FDA-required warning that this drug can cause exacerbatemental disorders and is contraindicated in patients withactive depression, a recent history of depression, generalizedanxiety disorder, psychosis, schizophrenia, and other majorpsychiatric disorders or a history of convulsions.