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ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS › ANTIPROTOZOALS › ANTIMALARIALS › Artemisinin and derivatives, combinations
artesunate, sulfadoxine and pyrimethamine
P01BF09
Forms & Strengths
- Artesunate 50 mg / Sulfadoxine 250 mg / Pyrimethamine 12.5 mg tablets
Adult Dosing
- Artesunate: 4 mg/kg once daily for 3 days
- Sulfadoxine / Pyrimethamine: Single dose on day 1 (25 mg/kg sulfadoxine / 1.25 mg/kg pyrimethamine equivalents)
Pediatric Dosing
- Children >= 5 kg: Weight-based dosing matching adult mg/kg regimens once daily for 3 days for artesunate and single dose on day 1 for sulfadoxine-pyrimethamine
- Safety and efficacy not well established in infants under 5 kg
Indications
- Treatment of uncomplicated Plasmodium falciparum malaria in endemic areas
Mechanism of Action
- Artesunate: Produces free radicals via cleavage of endoperoxide bridge, alkylating parasite proteins
- Sulfadoxine: Inhibits dihydropteroate synthase, blocking folate synthesis
- Pyrimethamine: Inhibits dihydrofolate reductase, halting parasite DNA synthesis
Contraindications
- Known hypersensitivity to artesunate, sulfonamides, or pyrimethamine
- Severe hepatic or renal impairment
- History of sulfonamide-induced immune thrombocytopenia or Stevens-Johnson syndrome
- First trimester of pregnancy (due to potential teratogenicity of antifolates)
Adverse Reactions
- Dizziness
- Headache
- Nausea and vomiting
- Anorexia
- Asthenia
- Severe cutaneous adverse reactions (e.g., Stevens-Johnson syndrome, toxic epidermal necrolysis)
- Hematologic toxicities (leukopenia, thrombocytopenia, hemolytic anemia)
Drug Interactions
- Methotrexate: Increased risk of bone marrow suppression and hematologic toxicity
- Warfarin: Potential potentiation of bleeding risk
- CYP2A6 and CYP2C19 inhibitors/inducers: May alter artesunate metabolism
- Other sulfonamides or antifolates: Additive toxicity and adverse effects
Curated Content: Needs Vetting Before Put to Clinical Use