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Drugs
Erschienen in: Drugs 1/2005

01.01.2005 | Review Article

Piperaquine

A Resurgent Antimalarial Drug

verfasst von: Prof Timothy M. E. Davis, Te-Yu Hung, Ing-Kye Sim, Harin A. Karunajeewa, Kenneth F. Ilett

Erschienen in: Drugs | Ausgabe 1/2005

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Abstract

Piperaquine is a bisquinoline antimalarial drug that was first synthesised in the 1960s, and used extensively in China and Indochina as prophylaxis and treatment during the next 20 years. A number of Chinese research groups documented that it was at least as effective as, and better tolerated than, chloroquine against falciparum and vivax malaria, but no pharmacokinetic characterisation was undertaken. With the development of piperaquine-resistant strains of Plasmodium falciparum and the emergence of the artemisinin derivatives, its use declined during the 1980s.
However, during the next decade, piperaquine was rediscovered by Chinese scientists as one of a number of compounds suitable for combination with an artemisinin derivative. The rationale for such artemisinin combination therapies (ACTs) was to provide an inexpensive, short-course treatment regimen with a high cure rate and good tolerability that would reduce transmission and protect against the development of parasite resistance. This approach has now been endorsed by the WHO.
Piperaquine-based ACT began as China-Vietnam 4 (CV4®: dihydroartemisinin [DHA], trimethoprim, piperaquine phosphate and primaquine phosphate), which was followed by CV8® (the same components as CV4 but in increased quantities), Artecom® (in which primaquine was omitted) and Artekin® or Duo-Cotecxin® (DHA and piperaquine phosphate only). Recent Indochinese studies have confirmed the excellent clinical efficacy of piperaquine-DHA combinations (28-day cure rates >95%), and have demonstrated that currently recommended regimens are not associated with significant cardiotoxicity or other adverse effects.
The pharmacokinetic properties of piperaquine have also been characterised recently, revealing that it is a highly lipid-soluble drug with a large volume of distribution at steady state/bioavailability, long elimination half-life and a clearance that is markedly higher in children than in adults. The tolerability, efficacy, pharmacokinetic profile and low cost of piperaquine make it a promising partner drug for use as part of an ACT.
Fußnoten
1
The use of trade names is for product identification purposes only and does not imply endorsement.
 
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Metadaten
Titel
Piperaquine
A Resurgent Antimalarial Drug
verfasst von
Prof Timothy M. E. Davis
Te-Yu Hung
Ing-Kye Sim
Harin A. Karunajeewa
Kenneth F. Ilett
Publikationsdatum
01.01.2005
Verlag
Springer International Publishing
Erschienen in
Drugs / Ausgabe 1/2005
Print ISSN: 0012-6667
Elektronische ISSN: 1179-1950
DOI
https://doi.org/10.2165/00003495-200565010-00004

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