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ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS › ANTIPROTOZOALS › ANTIMALARIALS › Aminoquinolines
tafenoquine
P01BA07
Adult Dosing
- Radical cure of Plasmodium vivax malaria: 300 mg single dose administered with chloroquine
- Malaria prophylaxis: 200 mg daily for 3 days, then 200 mg once weekly
Pediatric Dosing
- Safety and efficacy not established in pediatric patients aged <16 years (malaria prophylaxis)
- Safety and efficacy not established in pediatric patients aged <2 years (P. vivax radical cure)
Indications
- Radical cure (prevention of relapse) of Plasmodium vivax malaria in patients aged >=2 years
- Prophylaxis of malaria in patients aged >=16 years
Mechanism of Action
- 8-aminoquinoline antimalarial agent that targets the intramitochondrial parasite and produces reactive oxygen species, leading to disruption of parasite function and eradication of latent liver hypnozoites of Plasmodium vivax
Contraindications
- G6PD deficiency or unknown G6PD status due to risk of hemolytic anemia
- Breastfeeding an infant with G6PD deficiency or unknown G6PD status
- Hypersensitivity to tafenoquine or other 8-aminoquinolines
Adverse Reactions
- Hemolytic anemia in G6PD-deficient patients
- Methemoglobinemia
- Nausea, vomiting, diarrhea, headache
- Dizziness
- Elevated liver enzymes
- Psychiatric symptoms (e.g., anxiety, depression, psychotic symptoms in rare cases)
Drug Interactions
- Substrates of OCT2 and MATE1 transporters (may increase concentrations of co-administered drugs like dofetilide)
- Avoid concurrent administration with strong CYP1A2 or P-gp inhibitors/inducers where applicable
- Additive risk of hemolysis with other oxidant drugs
Curated Content: Needs Vetting Before Put to Clinical Use