primaquine is an approved drug (FDA (1952))
Compound class:
Synthetic organic
Comment: Primaquine is a synthetic, 8-aminoquinoline derivative that has potent antimalarial activity.
The approved drug is a racemic mixture and we show the chemical structure without stereochemistry to represent the mixture. The non-isomeric structure is also represented in the PubChem, ChEMBL and ChEBI entries listed in the links table below, while the two enantiomers forming the racemate are represented by PubChem CID 3044368 and PubChem CID 3044369. The marketed formulations contain primaquine phosphate (PubChem CID 6135). The Malaria tab on this ligand page provides additional curator comments of relevance to the Guide to MALARIA PHARMACOLOGY. Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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No information available. |
Summary of Clinical Use |
Primaquine has a broad spectrum of antimalarial activity and has a number of uses: primary prophylaxis against all Plasmodium species, terminal prophylaxis for P. vivax and P. ovale exposure, and as a radical cure (in combination with an effective blood stage schizonticide) after P. vivax or P. ovale clinical disease [2]. In addition, a recent WHO policy update, recommends the use of primaquine as a gametocytocide to reduce P. falciparum malaria transmission from human to mosquito host. Testing for glucose-6-phosphate dehydrogenase (G6PD) deficiency is required before administration because primaquine causes haemolysis in genetically sensitive individuals [3]. |
Pharmacokinetics |
Elimination |
Primaquine has a terminal half-life for elimination in the 2-12 hour range [2]. |
External links |
For extended ADME data see the following: Drugs.com |