Abstract：
:Primaquine is the only antimalarial drug available to clinicians for the treatment of relapsing forms of malaria. Primaquine development and usage dates back to the 1940s and has been administered to millions of individuals to treat and eliminate malaria infections. Primaquine therapy is not without disadvantages, however, as it can cause life threatening hemolysis in humans with glucose-6-phosphate dehydrogenase (G6PD) deficiency. In addition, the efficacy of primaquine against relapsing malaria was recently linked to CYP 2D6 mediated activation to an active metabolite, the structure of which has escaped definitive identification for over 75years. CYP 2D6 is highly polymorphic among various human populations adding further complexity to a comprehensive understanding of primaquine pharmacology. This review aims to discuss primaquine pharmacology in the context of state of the art understanding of CYP 2D6 mediated 8-aminoquinoline metabolic activation, and shed light on the current knowledge gaps of 8-aminoquinoline mechanistic understanding against relapsing malaria.
journal_name
Pharmacol Therjournal_title
Pharmacology & therapeuticsauthors
Marcsisin SR,Reichard G,Pybus BSdoi
10.1016/j.pharmthera.2016.03.011subject
Has Abstractpub_date
2016-05-01 00:00:00pages
1-10eissn
0163-7258issn
1879-016Xpii
S0163-7258(16)30019-5journal_volume
161pub_type
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