Piperaquine

General information

Piperaquine is a synthetic 4-aminoquinoline with high blood schizonticidal activity, similar to that of chloroquine [ ]. It was developed in the 1960s by Shanghai Pharmaceutical Industry Research (China) and Rhone Poulenc (France) and has been combined with dihydroartemisinin (as Artekin™) to provide a cheap and reasonably well-tolerated, short-course treatment for P. falciparum , with a high cure rate against drug-resistant parasites. Artekin™ has been extensively used in controlled clinical trials in South-East Asia, with good results against chloroquine-resistant parasites. However, piperaquine has a long half-life (23 days), which is markedly different from that of dihydroartemisinin (1 hour); this discrepancy has raised concerns that such a combination might rapidly attract resistance [ ].

There is some evidence that piperaquine is active against chloroquine-resistant Plasmodium falciparum , but laboratory studies suggest a degree of cross-resistance. Piperaquine 600 mg/month was well tolerated. Reported adverse reactions included headache, dizziness, vomiting, and diarrhea.