Пиронаридин

Химические свойства

solid

Антимикробная активность

Pyronaridine is active against the asexual erythrocytic stage of P. falciparum with little or no activity against gametocytes or the hepatic stage. In-vitro blood schizonticide activities are in the range of 0.001–0.03 mg/L, showing a moderate correlation to chloroquine resistance. However, this correlation varies between studies and does not seem to be clinically significant. It is also active against P. vivax, P. ovale and P. malariae. Antagonistic interactions with artemisinins were reported in vitro, but synergy with artesunate has been observed in rodent models.

Приобретенная устойчивость

Decreasing in-vitro sensitivity has been observed in China.

Фармацевтические приложения

An aza-aminoacridine formulated for oral use. A Mannichbase derivative of mepacrine.

Фармакокине?тика

Peak plasma concentrations are reached after 3–14 h depending upon the formulation; there is also considerable interindividual variation. Elimination half-lives of 63–190 h have been reported, again dependent upon the formulation.

Клиническое использование

Treatment of uncomplicated P. falciparum and P. vivax malaria
A fixed-dose combination with artesunate (Pyramax) is being developed for uncomplicated P. falciparum and P. vivax malaria.

Побочные эффекты

It is well tolerated and no outstanding toxic effects have been reported.