Primaquine pharmacology in the context of CYP 2D6 pharmacogenomics: current state of the art

SR Marcsisin, G Reichard, BS Pybus - Pharmacology & therapeutics, 2016 - Elsevier
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 …

Tafenoquine: A Step toward Malaria Elimination: Published as part of the Biochemistry series “Biochemistry to Bedside”

KY Lu, ER Derbyshire - Biochemistry, 2020 - ACS Publications
There is a pressing need for compounds with broad-spectrum activity against malaria
parasites at various life cycle stages to achieve malaria elimination. However, this goal …

Metabolism of primaquine in normal human volunteers: investigation of phase I and phase II metabolites from plasma and urine using ultra-high performance liquid …

B Avula, BL Tekwani, ND Chaurasiya, P Fasinu… - Malaria journal, 2018 - Springer
Abstract Background Primaquine (PQ), an 8-aminoquinoline, is the only drug approved by
the United States Food and Drug Administration for radical cure and prevention of relapse in …

Primaquine pharmacokinetics in lactating women and breastfed infant exposures

ME Gilder, W Hanpithakphong… - Clinical Infectious …, 2018 - academic.oup.com
Background Primaquine is the only drug providing radical cure of Plasmodium vivax
malaria. It is not recommended for breastfeeding women as it causes hemolysis in glucose-6 …

Effects of MAO-A and CYP450 on primaquine metabolism in healthy volunteers

NM Ariffin, F Islahudin, E Kumolosasi… - Parasitology …, 2019 - Springer
Eliminating the Plasmodium vivax malaria parasite infection remains challenging. One of the
main problems is its capacity to form hypnozoites that potentially lead to recurrent infections …

Enantiospecific pharmacokinetics and drug–drug interactions of primaquine and blood-stage antimalarial drugs

K Chairat, P Jittamala… - Journal of …, 2018 - academic.oup.com
Objectives Characterization of the pharmacokinetic properties of the enantiomers of
primaquine and carboxyprimaquine following administration of racemic primaquine given …

Pathway-specific inhibition of primaquine metabolism by chloroquine/quinine

PS Fasinu, BL Tekwani, B Avula, ND Chaurasiya… - Malaria Journal, 2016 - Springer
Background There has been some evidence to suggest that the addition of chloroquine (CQ)
or quinine (QN) to 8-aminoquinoline (8-AQ) treatment regimens may increase the …

Formation primaquine-5, 6-orthoquinone, the putative active and toxic metabolite of primaquine via direct oxidation in human erythrocytes

PS Fasinu, NPD Nanayakkara, YH Wang… - Malaria Journal, 2019 - Springer
Background The activity and haemolytic toxicity associated with primaquine has been linked
to its reactive metabolites. The reactive metabolites are thought to be primarily formed …

Simultaneous and enantiospecific quantification of primaquine and carboxyprimaquine in human plasma using liquid chromatography-tandem mass spectrometry

W Hanpithakpong, NPJ Day, NJ White, J Tarning - Malaria Journal, 2022 - Springer
Background The enantiomers of the 8-aminoquinoline anti-malarial primaquine have
different pharmacological properties. Development of an analytical method for simultaneous …

Differential kinetic profiles and metabolism of primaquine enantiomers by human hepatocytes

PS Fasinu, B Avula, BL Tekwani, NPD Nanayakkara… - Malaria Journal, 2016 - Springer
Background The clinical utility of primaquine (PQ), used as a racemic mixture of two
enantiomers, is limited due to metabolism-linked hemolytic toxicity in individuals with genetic …