Primaquine: Report From CDC Expert Meeting on Malaria Chemoprophylaxis I

Abstract

Primaquine phosphate has been used for preventing relapse of Plasmodium vivax and P. ovale malaria since the early 1950s, based on its ability to kill latent (hypnozoite) and developing liver stages of these parasites. There are three uses for primaquine in malaria: radical cure of established infection with P. vivax or P. ovale malaria; presumptive anti-relapse therapy (PART; terminal prophylaxis) in persons with extensive exposure to these parasites; and primary prophylaxis against all malaria species. All persons for whom primaquine is being considered must have a glucose-6-phosphate dehydrogenase (G6PD) enzyme level checked before use, and persons who have a deficiency of G6PD must not take primaquine for prophylaxis or PART. The recommended adult dose for PART based on clinical trials and expert opinion is 30 mg base daily for 14 days, started on return from a malarious region and overlapping with a blood schizonticide. The adult dose for primary prophylaxis is 30 mg daily begun 1 day before travel and continued for 7 days after return. This review will examine the evidence for these recommendations.

Gametocitemia en malaria por Plasmodium falciparum tratada con amodiaquina o artesunato

“…Con el enfoque de quimioprofilaxis antipalúdica primaria con primaquina hemos hecho recientemente dos revisiones (20,38) y con el enfoque anterior más la "profilaxis terminal" conocemos otra (39).…”

Diagnosis and Treatment of Plasmodium vivax Malaria

“…102 In an attempt to reduce potential toxicity, the WHO guidelines for the radical cure of vivax malaria currently recommends the use of a daily dose of 0.25 mg/kg/day (3.5 mg/kg total dose) PQ taken with food once daily for 14 days, coadministered with CQ or ACT depending on CQ sensitivity in the region. 103 In southeast Asia and Oceania, the same guidelines recommend a higher daily dose of 0.5 mg/kg (7.0 mg/kg total dose) in view of the high risk of relapses.…”

Primaquine dipeptide derivatives bearing an imidazolidin-4-one moiety at the N-terminus as potential antimalarial prodrugs

“…However, primaquine presents a short plasma half-life (ca. 6 h) [6,7], as a result of its rapid oxidative deamination to the inactive metabolite carboxyprimaquine 2 (Scheme 1) [8][9][10][11][12]. Blood toxicity, in particular the ability of primaquine to induce oxidation of oxyhemoglobin to methemoglobin, has been also a source of concern [13].…”