Piperaquine – A Resurgent, Effective Anti-malarial

As part of recent Research, Piperaquine Phosphate is said to be a new effective antimalarial. It is defined as a bisquinoline antimalarial drug that was first synthesised in the 1960s, and used extensively in China and Indochina for prophylaxis and treatment of malaria. 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 at that time. With the development and emergence of the artemisinin derivatives, its use declined during the 1980s.

However, during the next decades, piperaquine was rediscovered by Chinese scientists as one of a number of compounds suitable for combination with an artemisinin derivative. The rational 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 in China-Vietnam as CV4®: and Artecom (dihydroartemisinin (DHA), trimethoprim, piperaquine phosphate), which was followed by CV8® (the same components as CV4 but including primaquine), Artekin®, Duo-Cotexcin® and recently WAIPA ( in Nigeria) (containing DHA and piperaquine phosphate). Recent 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.

This piperaquine and Dihydroartemisinin Combination that was recently introduced in Nigeria, known as WAIPA® was acclamined by health professionals in the country as one of the most effective anti-malarial. It was well tolerated compared to other ACT’s in Nigeria.