4-[(7-クロロ-2-メトキシベンゾ[b]-1,5-ナフチリジン-10-イル)アミノ]-2,6-ビス(1-ピロリジニルメチル)フェノール 化学特性,用途語,生産方法
化学的特性
solid
抗菌性
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.
獲得抵抗性
Decreasing in-vitro sensitivity has been observed in China.
応用例（製薬）
An aza-aminoacridine formulated for oral use. A Mannichbase
derivative of mepacrine.
薬物動態学
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.
臨床応用
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.
副作用
It is well tolerated and no outstanding toxic effects have been
reported.
4-[(7-クロロ-2-メトキシベンゾ[b]-1,5-ナフチリジン-10-イル)アミノ]-2,6-ビス(1-ピロリジニルメチル)フェノール 上流と下流の製品情報
原材料
準備製品