Piperaquine
Antimalarial
Also known as Piperaquine phosphate, Piperaquine tetraphosphate
Mechanism
Piperaquine is a bisquinoline antimalarial that accumulates in the parasite digestive food vacuole, where it inhibits heme polymerization to hemozoin — a mechanism shared with chloroquine. However, its bisquinoline structure retains activity against many chloroquine-resistant Plasmodium falciparum strains. Its extremely long elimination half-life (2-3 weeks) provides prolonged post-treatment prophylaxis, and it is used in fixed-dose combination with dihydroartemisinin as a WHO-recommended artemisinin combination therapy (ACT).
Indications
Dosing
- Adult
- Adult (body-weight 40 kg and above): 320 mg (as Piperaquine phosphate, 1 tablet) once daily for 3 days
- Pediatric
- Child 6 months–17 years (body-weight 7–12 kg): 0.5 tablet once daily for 3 days, max. 2 courses in 12 months; second course given at least 2 months after first course. Child 6 months–17 years (body-weight 13–23 kg): 1 tablet once daily for 3 days, max. Child 6 months–17 years (body-weight 24–35 kg): 2 tablets once daily for 3 days, max.
- Renal adjustment
- Manufacturer advises caution in severe impairment. Monitor ECG and plasma potassium concentration.
- Hepatic adjustment
- Manufacturer advises caution in severe impairment (no information available)—monitor ECG and plasma potassium concentration.
Pharmacokinetics
Contraindications
- Family history of congenital QT interval prolongation
- Family history of sudden death
- History of arrhythmias
- History of clinically relevant bradycardia
- History of congestive heart failure accompanied by reduced left ventricular ejection fraction
- Acute porphyrias
- Electrolyte disturbances
Side effects
- Angioedema
- Arrhythmias (implied by contraindications)
- Sudden death (implied by contraindications)
- Rashes (rare)
Pregnancy & lactation
Toxicity in animal studies with artemether. Manufacturer advises use only if potential benefit outweighs risk.
Manufacturer advises avoid breastfeeding for at least 1 week after last dose. Present in milk in animal studies.
Related guidelines
Other Antimalarial drugs
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Sources: KD Tripathi 7e, Goodman & Gilman 14e, Katzung·Verified: 2026-05-13 · House clinical team