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Tafenoquine

8-Aminoquinoline antimalarial (radical cure) · Antimalarial

START
Radical cure: 300 mg PO single dose with food (after CQ/CQ-eq course); prophylaxis 200 mg/day x3 then weekly
TYPICAL MAX
300 mg single dose (radical cure)
STOP IF
Severe haemolysis / symptomatic methaemoglobinaemia / hypersensitivity
WATCH
G6PD quantitative testing BEFORE dosing; Hb / urine colour; psychiatric
CDSCO approvedSchedule HATC P01BA07
Dose laddermg/d
200prophylaxis300radical cure
Renal dose adjustmenteGFR mL/min/1.73m²
FULLStandard dosing30CAUTIONLimited data — caution90

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours
4hONSET13hPEAK2w1wDURATION
ONSET
4h · absorption
PEAK
13h · Tmax
2w · t½ ~14 d
DURATION
1w · weekly
EXCRETION
Mainly biliary/faecal; minor renal
route + CYP
INTERACTIONS
5 major
SEVERE in our sources
PREGNANCY
Contraindicated (limited data; theoretical fetal haemolysis if fetus G6PD-deficient).
FDA category + note
Top interactionssee all 6
  • DofetilideSevereDatabaseDDInter
  • Nitrous AcidSevereDatabaseDDInter
  • PrilocaineSevereDatabaseDDInter
  • Methaemoglobin Inducing DrugsSevereDatabaseKimi deep-research + Cla

Mechanism

8-aminoquinoline with active metabolites that produce reactive oxygen species lethal to Plasmodium hypnozoites in the liver — provides radical cure of P. vivax / P. ovale relapsing malaria; activity against hepatic and erythrocytic stages.

Indications

Radical cure of Plasmodium vivax malaria (after chloroquine treatment of the acute infection, in G6PD-normal adults)Prophylaxis of malaria (alternative to mefloquine/atovaquone-proguanil for travellers)

Dosing

Adult
Radical cure: 300 mg PO single dose (after chloroquine course). Prophylaxis: 200 mg PO once daily for 3 days starting 3 days before travel, then 200 mg once weekly while in malarious area, then 200 mg once 7 days after leaving.
Pediatric
≥16 y: as adult; <16 not established.
Renal adjustment
Not studied in severe renal impairment.
Hepatic adjustment
Not studied in moderate–severe impairment.
Geriatric
Limited data.
Max dose
300 mg single dose (radical cure); 200 mg/day or 200 mg/week (prophylaxis)

Pharmacokinetics

Onset
Hypnozoite kill over days
Peak effect
~12–15 h (Tmax with food)
Duration
~weeks (long terminal half-life supports weekly dosing)
Half-life
~14–15 days
Bioavailability
Increased ~50% with food
Protein binding
>99%
Metabolism
Hepatic CYP2D6 minor, plus other CYPs
Excretion
Mainly biliary/faecal; minor renal

Contraindications

  • G6PD deficiency (severe haemolysis risk; quantitative testing required)
  • Severe hypersensitivity
  • Caution: psychiatric disorders, breastfeeding G6PD-deficient infants

Side effects

Common
Nausea/vomitingHeadacheDizzinessMethaemoglobinaemia (asymptomatic)Decreased haemoglobin
Serious
  • Severe haemolytic anaemia (G6PD-deficient)
  • Symptomatic methaemoglobinaemia (esp. NADH-MetHb-reductase deficiency)
  • Psychiatric events (anxiety, abnormal dreams)
  • Hypersensitivity / SJS

Pregnancy & lactation

Pregnancy

Contraindicated (limited data; theoretical fetal haemolysis if fetus G6PD-deficient).

Lactation

Avoid breastfeeding G6PD-deficient infants; otherwise weigh risk.

Drug interactions

Dofetilide
Severe
Database

Clinical effect not specified

Source: DDInter

Nitrous Acid
Severe
Database

Clinical effect not specified

Source: DDInter

Prilocaine
Severe
Database

Clinical effect not specified

Source: DDInter

Methaemoglobin Inducing Drugs
Severe
Database

Additive methaemoglobinaemia

Avoid combination

Source: Kimi deep-research + Cla

Other 8 Aminoquinolines
Severe
Database

Duplicate therapy + additive haemolysis

Do not co-administer

Source: Kimi deep-research + Cla

Oct2
Moderate
Database

Tafenoquine inhibits OCT2 / MATE

Monitor metformin levels / clinical effect

Source: Kimi deep-research + Cla

6 additional low-confidence interactions hidden — those rows lack a documented mechanism or management plan in our sources.

Related guidelines

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Sources: KD Tripathi 7e, Goodman & Gilman 14e, Harrison 22e, Katzung·Verified: 2026-05-20 · House clinical team·Cockpit curated: 2026-05-20