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Piperaquine

Antimalarial

Also known as Piperaquine phosphate, Piperaquine tetraphosphate

Antimalarial
CDSCO approvedSchedule H
EXCRETION
not curated
INTERACTIONS
none in our sources
PREGNANCY
Toxicity in animal studies with artemether. Manufacturer advises use only if potential benefit outweighs risk.
FDA category + note

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

Treatment of uncomplicated falciparum malariapartner drug in act, e.g., dihydroartemisinin-piperaquine for uncomplicated malariauncomplicated CQ-resistant falciparum malaria (as part of ACT)Uncomplicated falciparum malaria (in fixed dose combination with dihydroartemisinin or arterolane)Mass prophylaxis/treatment of malaria (historically in China, replaced CQ)

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

Onset
2 h after a single dose
Half-life
Long half-life
Protein binding
Large volume of distribution
Metabolism
Primary isoenzyme CYP3A4

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

Common
Abdominal painAppetite decreasedArthralgiaAstheniaCoughDiarrhoeaDizzinessGait abnormalHeadacheMovement disordersMyalgiaNauseaPalpitationsQT interval prolongationSensation abnormalSkin reactionsSleep disordersVomiting
Serious
  • Angioedema
  • Arrhythmias (implied by contraindications)
  • Sudden death (implied by contraindications)
  • Rashes (rare)

Pregnancy & lactation

Pregnancy

Toxicity in animal studies with artemether. Manufacturer advises use only if potential benefit outweighs risk.

Lactation

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