Tafenoquine
Antimalarials
AntimalarialsPregnancy: contraindicated
Contraindicated in pregnancy because it may cause haemolysis in a G6PD-deficient fetus; a pregnancy test is done before use.
Long-acting 8-aminoquinoline, a single dose with chloroquine for P. vivax radical cure; G6PD must be shown normal first.
Quick facts
- Group
- Antimalarials
- Target
- Not fully known: like primaquine, acts on liver hypnozoites and gametocytes
- Used for
- Radical cure · Prophylaxis in travellers
- Key effects
- Nausea · Headache and dizziness · Insomnia
- Monitor
- Quantitative G6PD test before use
- ATC
- P01BA07
No doses: the clinician sets them by the current guideline.
Mechanism of action
A derivative of primaquine with presumably the same mechanism: oxidant metabolites kill the dormant liver forms (hypnozoites) of P. vivax and act on other stages. Its main difference is pharmacokinetic: it is absorbed slowly and eliminated over weeks, so one dose replaces a two-week primaquine course for radical cure. Like primaquine, it causes haemolysis in G6PD deficiency.
- Primaquine-like 8-aminoquinoline
- Kills P. vivax liver hypnozoites
- Very long half-life: one dose for radical cure
- Haemolysis if G6PD is deficient
Indications
- Radical cure (prevention of relapse) of P. vivax malaria, as a single dose together with chloroquine or hydroxychloroquine, in people aged 16 or older Malaria →
- Prophylaxis in travellers (a separate product, for up to six months) Malaria →
Adverse effects
Common
- Nausea, vomiting and diarrhoea
- Headache and dizziness
- Insomnia, anxiety, unusual dreams and mood changes
- Blurred vision or light sensitivity; vortex keratopathy
- Raised liver enzymes
Contraindications
- G6PD deficiency or unknown G6PD status
- Pregnancy
- Current or past psychosis or psychotic symptoms
- Hypersensitivity to tafenoquine or primaquine
Key interactions
- Chloroquine or hydroxychloroquine
- Required partner for radical cure; tafenoquine is used only with them in that indication
- Drugs that cause haemolysis or methaemoglobinaemia (e.g. dapsone, primaquine)
- Additive red-cell toxicity is expected, as with primaquine
What is monitored
- Quantitative G6PD test before use (qualitative tests can miss intermediate activity in women)
- Pregnancy test before use
- Haemoglobin and urine colour after the dose; effects can appear late because the drug persists
- Mood and behaviour changes
Administration and safety
- Oral, with food; tablets are swallowed whole, not split, chewed or crushed.
- Given on the first or second day of the chloroquine course.
- If vomiting occurs within an hour of the dose, the prescriber decides whether to repeat it.
- Two products exist for different uses (radical cure, prophylaxis): confirm which one is ordered.
Pregnancy and breastfeeding
Contraindicated in pregnancy because it may cause haemolysis in a G6PD-deficient fetus; a pregnancy test is done before use.
Nursing care
- Confirm a normal quantitative G6PD result and a negative pregnancy test before giving it.
- Ask about psychiatric history.
- Teaching: report dark urine, pallor, shortness of breath, blue-grey lips, yellow eyes or hallucinations, even weeks later.
- Contraception during treatment and for about three months after.
Pharmacokinetics
- Absorption
- Oral, slow (peak about half a day after dosing); taken with food
- Distribution
- Large volume of distribution
- Metabolism
- Not well characterised
- Elimination
- Low clearance, very slow elimination
- Half-life
- About 14 days
Test yourself
Think of the answer, then tap the question to see it.
What is the main advantage of tafenoquine over primaquine?
Its half-life of about two weeks lets a single dose replace a long primaquine course, which improves adherence.
What test is mandatory before tafenoquine, and why quantitative?
G6PD activity; quantitative tests are needed because qualitative tests can miss intermediate deficiency, which is common in heterozygous women.
With which drug is it given for P. vivax radical cure?
With chloroquine (or hydroxychloroquine), which treats the blood stage.
Connections
← Back to the class: Antimalarials
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: Tafenoquine: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2025); Malaria in the United States: Treatment Tables (Centers for Disease Control and Prevention (CDC), 2026).
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Representative model, for educational purposes only.