ABSTRACT

Piperaquine (PQP) is a bis-4amino-quinoline schizonticidal anti-malarial drug first synthesized simultaneously in both China and France in the 1960s (Figure 172.1) (Chen et al., 1989; Piperaquine, 2004). Because of its relative potency and tolerability, from 1979 it superseded chloroquine (CQ) as the anti-malarial recommended by the Chinese national malaria control program. The equivalent of 140 million adult treatment doses were subsequently manufactured and distributed, including as population-wide mass drug administration. The subsequent development of PQP-resistant strains of Plasmodium falciparum led to a diminution of its use in the 1980s (Tran et al., 2004). However, since 1990, it has been “rediscovered” and repurposed as a component of short-course artemisinin-based combination therapies (ACTs) formulated to minimize selection pressure for resistance and to achieve high cure rates without significant side effects. ACTs are now considered the standard of care for the management of uncomplicated (nonsevere) malaria due to P. falciparum in most contexts (WHO, 2015). Chemical structure of piperaquine phosphate (l,3-bis[l-{7-chloro-4′quinolyl}-4′piperazinyl] phosphate). https://s3-euw1-ap-pe-df-pch-content-public-p.s3.eu-west-1.amazonaws.com/9781315152110/08d8042d-9481-4a8d-8c27-9bd589f6de6b/content/fig172_1.tif" xmlns:xlink="https://www.w3.org/1999/xlink"/>