Filaricidal effect of mefloquine on adults and microfilariae of Brugia patei and Brugia malayi.
Mefloquine, DL-erythro-2,8-bis(trifluoromethyl)-alpha-(2-piperidyl)-4-quinoline methanolhydrochloride, a recently developed antimalarial drug shows filaricidal activity against larval and adult stages of Brugia patei and B. malayi maintained "in vitro". In the concentration range of 10 to 2 microM mefloquine paralysed and killed the filarial worms within 10 h and 3 d, respectively. The lethal effect of mefloquine treatment on larval and adult worms was shown by loss of motility as well as by decrease of lactate excretion by adults. Chloroquine at a concentration of 10 microM did not affect motility and survival of microfilariae and adults of B. patei. Addition of serum to the cultivation medium abolished the filaricidal effect, possibly due to the tight binding of mefloquine to serum proteins, thereby affecting the uptake of the drug into the parasite.
D000818:Animals; D000871:Anthelmintics / Q000494:pharmacology*; D001798:Blood Proteins / Q000378:metabolism; D002009:Brugia / Q000187:drug effects*; D002738:Chloroquine / Q000494:pharmacology; D005369:Filaricides / Q000378:metabolism / Q000494:pharmacology*; D015767:Mefloquine; D008842:Microfilariae / Q000187:drug effects; D011804:Quinolines / Q000378:metabolism / Q000494:pharmacology*
D000871:Anthelmintics; D001798:Blood Proteins; D005369:Filaricides; D011804:Quinolines; D002738:Chloroquine; D015767:Mefloquine