Chemical Properties
solid
Definition
ChEBI: Pyronaridine is an aminoquinoline.
Antimicrobial activity
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.
Acquired resistance
Decreasing in-vitro sensitivity has been observed in China.
Pharmaceutical Applications
An aza-aminoacridine formulated for oral use. A Mannichbase
derivative of mepacrine.
Pharmacokinetics
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.
Clinical Use
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.
Side effects
It is well tolerated and no outstanding toxic effects have been
reported.
