Pyronaridine Struktur

Pyronaridine

Bezeichnung:Pyronaridine

Englisch Name:Pyronaridine

CBNumberCB01179619

SummenformelC29H32ClN5O2

Molgewicht518.05

Pyronaridine physikalisch-chemischer Eigenschaften

Siedepunkt	621.3±55.0 °C(Predicted)
Dichte	1.356±0.06 g/cm3 (20℃ 760 Torr)
Brechungsindex	1.5650 (estimate)
Löslichkeit	DMSO (Slightly), Water (Slightly)
Aggregatzustand	Solid
pka	8.20±0.50(Predicted)
Farbe	Light Yellow to Orange
Stabilität	Incompatible with strong oxidizing agents.
CAS Datenbank	74847-35-1

Pyronaridine Chemische Eigenschaften,Einsatz,Produktion Methoden

Chemische Eigenschaften
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.
Pharmazeutische Anwendungen
An aza-aminoacridine formulated for oral use. A Mannichbase derivative of mepacrine.
Pharmakokinetik
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.
Nebenwirkungen
It is well tolerated and no outstanding toxic effects have been reported.