8-aminoquinoline antimalarial indicated for radical cure (prevention of relapse) of Plasmodium vivax malaria in patients ≥ 16 years receiving chloroquine for acute P. vivax infection.
Also known as: Krintafel
DailyMed approved label (KRINTAFEL, tafenoquine succinate; setID 5cf989d5-36f5-4561-a30b-9fcb9deb6b6a).
DailyMed approved label (KRINTAFEL, tafenoquine succinate; setID 5cf989d5-36f5-4561-a30b-9fcb9deb6b6a).
Tafenoquine + metformin: tafenoquine increases metformin exposure (OCT2/MATE substrate) — monitor for toxicity.
The FDA tafenoquine label documents that co-administration with OCT2/MATE transporter substrates (e.g., dofetilide, metformin) should be avoided; if unavoidable, monitor for related toxicities and consider dose reduction (section 7.1). Metformin depends on tubular secretion via OCT2 and MATE for its elimination; inhibition of these transporters by tafenoquine raises metformin plasma concentrations. The clinical risk is metformin toxicity — gastrointestinal symptoms, renal function and, in rare cases, lactic acidosis, especially if renal impairment already exists. As tafenoquine is used in a short regimen (single dose in malaria prophylaxis), the ideal is to avoid the combination on the day of administration; if unavoidable, monitor and consider adjustment.
Tafenoquine + metformin: tafenoquine inhibits OCT2/MATE and increases metformin exposure — avoid the combination.
The FDA tafenoquine label documents: "Avoid co-administration with drugs that are substrates of organic cation transporter-2 (OCT2) or multidrug and toxin extrusion (MATE) transporters (e.g., dofetilide, metformin). If coadministration cannot be avoided, monitor for drug-related toxicities and consider dosage reduction" (7.1). Metformin is an OCT2/MATE substrate — tafenoquine inhibits these transporters and raises its levels.
Monitor renal function, gastrointestinal symptoms and signs of lactic acidosis (rare) during the combination.
Lactic acidosis, severe gastrointestinal symptoms or worsening renal function with the combination.
Avoid the combination whenever possible; if unavoidable, monitor for metformin toxicity signs and consider dose reduction.
DailyMed/FDA (NIH/NLM) — approved Tafenoquine label (ARAKODA, section 7.1): https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=299e49d8-470f-4779-a010-4a1ee0e0c6cd ; approved Metformin label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=34496b43-05a2-45fb-a769-52b12e099341
Alcohol may worsen the psychiatric effects (insomnia, anxiety, abnormal dreams) of tafenoquine; limit intake.
Limit alcohol intake during treatment.
DailyMed/FDA (NIH/NLM) — approved Tafenoquine label (KRINTAFEL): https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=5cf989d5-36f5-4561-a30b-9fcb9deb6b6a
Tafenoquine can be taken with or without food; taking with food reduces gastrointestinal discomfort.
Take with food if gastric discomfort occurs.
DailyMed/FDA (NIH/NLM) — approved Tafenoquine label (KRINTAFEL): https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=5cf989d5-36f5-4561-a30b-9fcb9deb6b6a
Tafenoquine causes psychiatric effects (insomnia, anxiety, depression, abnormal dreams); use with caution in patients with psychiatric disease.
Monitor psychiatric symptoms; stop with severe symptoms.
DailyMed/FDA (NIH/NLM) — approved Tafenoquine label (KRINTAFEL): https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=5cf989d5-36f5-4561-a30b-9fcb9deb6b6a
Tafenoquine causes severe haemolysis in patients with G6PD deficiency; it is contraindicated in deficiency or when G6PD status is unknown.
Mandatory G6PD screening before prescribing; contraindicated in deficiency or unknown status.
DailyMed/FDA (NIH/NLM) — approved Tafenoquine label (KRINTAFEL): https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=5cf989d5-36f5-4561-a30b-9fcb9deb6b6a
Tafenoquine is contraindicated in pregnancy: the fetal G6PD status is unknown and there is a risk of severe fetal haemolysis.
Contraindicated in pregnancy; postpone radical cure until after delivery.
Contraindicated in breastfeeding if the infant is G6PD deficient or of unknown status.
Advise effective contraception during treatment.
DailyMed/FDA (NIH/NLM) — approved Tafenoquine label (KRINTAFEL): https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=5cf989d5-36f5-4561-a30b-9fcb9deb6b6a
Clinical and educational support tool. The information does not replace a medical prescription or the opinion of a qualified healthcare professional.
8-aminoquinoline antimalarial active against liver hypnozoites of P. vivax; does not prolong the QTc interval to a clinically relevant extent even at a cumulative dose of 1,200 mg (4x the maximum recommended dose).
Mechanism similar to other 8-aminoquinolines: inhibition of mitochondrial function and oxidative stress in dormant liver stages of the parasite, preventing relapse.
Maximum plasma concentrations generally 12–15 hours after oral administration; food increases plasma AUC.
Extensively metabolized; elimination is slow (long half-life), allowing single-dose administration.
Elimination half-life of ~15 days.
Medicines from the same therapeutic group (ATC classification) or the same pharmacological class.
