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ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS › ANTIPROTOZOALS › ANTIMALARIALS › Artemisinin and derivatives, combinations
artemisinin and naphthoquine
P01BF08
Forms & Strengths
- Fixed-dose combination tablet: artemisinin 100 mg + naphthoquine phosphate 40 mg
Adult Dosing
- Uncomplicated Plasmodium falciparum malaria: Total adult dose is typically 4 tablets (400 mg artemisinin / 160 mg naphthoquine) administered as a single dose or divided over 2 days depending on regional protocol
Pediatric Dosing
- Pediatric dosing is weight-based for uncomplicated malaria, following specific national guidelines or trial protocols due to the fixed-dose ratio
Indications
- Treatment of uncomplicated Plasmodium falciparum malaria
Mechanism of Action
- Artemisinin: Endoperoxide moiety is cleaved by intraparasitic heme, generating free radicals that alkylate and damage parasite macromolecules
- Naphthoquine: 4-aminoquinoline derivative that likely inhibits hemozoin polymerization, leading to toxic heme accumulation within the parasite
Contraindications
- Known hypersensitivity to artemisinin derivatives or naphthoquine (or other 4-aminoquinolines)
- Severe hepatic or renal impairment
- History of prolonged QT interval or cardiac arrhythmias
Adverse Reactions
- Transient dizziness
- Nausea and vomiting
- Abdominal pain
- Asymptomatic and reversible QT prolongation
- Transient neutropenia or elevated liver transaminases
Drug Interactions
- Avoid co-administration with other drugs known to prolong the QT interval (e.g., antiarrhythmics, macrolides, antipsychotics)
- Potential risk of altered plasma concentrations when used with strong CYP3A4 inducers or inhibitors due to hepatic metabolism of components
Curated Content: Needs Vetting Before Put to Clinical Use