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ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS › ANTIPROTOZOALS › ANTIMALARIALS › Artemisinin and derivatives, plain
artenimol
P01BE05
Forms & Strengths
- Artenimol (Dihydroartemisinin) oral tablets: 40 mg
- Artenimol/Piperaquine combination tablets: 40 mg / 320 mg
Adult Dosing
- Uncomplicated Plasmodium falciparum malaria: 2 mg/kg/day once daily for 3 days in combination with an adequate partner drug
- Artenimol-piperaquine fixed-dose combination: 3 tablets (total artenimol 120 mg / piperaquine 960 mg) once daily for 3 consecutive days
Pediatric Dosing
- Children >= 6 months and weight >= 5 kg: Dosing based on weight bands using fixed-dose combination tablets once daily for 3 days
- Artenimol-piperaquine weight-based dosing: 5 to <8 kg: 0.5 tablet daily; 8 to <15 kg: 1 tablet daily; 15 to <24 kg: 1.5 tablets daily; 24 to <36 kg: 2 tablets daily; 36 to <60 kg: 3 tablets daily for 3 days
Indications
- Treatment of acute uncomplicated Plasmodium falciparum malaria
- Initial management of severe malaria when parenteral therapy is not immediately available (as part of artemisinin-based combination therapy)
Mechanism of Action
- Dihydroartemisinin is the active metabolite of all artemisinin compounds
- Acts as a blood schizonticide against asexual parasite forms
- Endoperoxide bridge interacts with intracellular iron to generate reactive oxygen species and free radicals, alkylating parasite macromolecules and inhibiting vital parasite functions
Contraindications
- Known hypersensitivity to artenimol, dihydroartemisinin, or any component of the formulation
- Severe malaria with vital organ dysfunction (when used as oral monotherapy)
- First trimester of pregnancy (where alternative effective treatments are available, per WHO guidelines)
- History of familial QT prolongation or concurrent administration of drugs that prolong the QT interval (specifically for partner drugs like piperaquine)
Adverse Reactions
- Headache
- Dizziness
- Asthenia
- Nausea
- Vomiting
- Anorexia
- Reticulocytopenia
- Transient transaminase elevations
- QT interval prolongation (primarily associated with combination partners like piperaquine)
Drug Interactions
- Strong CYP3A4 inhibitors (e.g., ketoconazole, ritonavir) may increase exposure to partner drugs like piperaquine, increasing the risk of QT prolongation
- Strong CYP3A4 inducers (e.g., rifampin, carbamazepine, St. John's wort) may decrease plasma concentrations of artemisinins and partner drugs, leading to treatment failure
- Drugs that prolong the QT interval (e.g., antiarrhythmics, macrolides, antipsychotics): increased risk of ventricular arrhythmias when co-administered with artemisinins combined with piperaquine
Curated Content: Needs Vetting Before Put to Clinical Use