Piperaquine phosphate

Piperaquine is a bisquinoline antimalarial agent, often as a partner antimalarial for artemisinin drug-based combination therapy (ACT)[1][2].

Research Areas >> Infection

Piperaquine (10-90 mg/kg; a single i.p.) decreases parasitemia at all of the doses tested in mice[1]. Piperaquine (90 mg/kg; a single i.p.) exhibits the t1/2, apparent clearance, and apparent volume of distribution 17.8 days, 33.5 mg•h/L, 1.55 L/h/kg, and 956 L/kg, respectively, in healthy mice and 16.1 days, 27.3 mg•h/L, 1.9 L/h/kg, and 1,059 L/kg in malaria-infected mice[1]. Animal Model: Male BALB/c mice (7 to 8 weeks) are inoculated with Plasmodium berghei parasites[1] Dosage: 0, 10, 30, 90 mg/kg Administration: A single i.p. administration Result: The median survival time was 10 days at dose of 10 mg/kg. The median survival time was 54 days at dose of 30 mg/kg. All mice were active and alert and had stable body weights throughout the course of the study at dose of 90 mg/kg. Animal Model: Male Swiss mice (6 weeks old)[1] Dosage: 90 mg/kg (Pharmacokinetic Analysis) Administration: A single i.p. administration Result: t1/2=17.8 d; AUC=33.5 mg•h/L; apparent clearance=1.55 L/h/kg; apparent volume of distribution=956 L/kg.

[1]. Moore BR, et, al. Pharmacokinetics and pharmacodynamics of piperaquine in a murine malaria model. Antimicrob Agents Chemother. 2008 Jan; 52(1): 306-11.

[2]. Davis TME, et, al. Piperaquine: a resurgent antimalarial drug. Drugs. 2005; 65(1): 75-87.