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ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS › ANTIPROTOZOALS › ANTIMALARIALS › Artemisinin and derivatives, combinations
artesunate, sulfalene and pyrimethamine
P01BF04
Forms & Strengths
- Fixed-dose combination tablet: artesunate / sulfalene / pyrimethamine (varying regional strengths, commonly artesunate 100mg / sulfalene 500mg / pyrimethamine 25mg)
Adult Dosing
- Uncomplicated Plasmodium falciparum malaria: Administered as a 3-day course
- Typical regimen: Total dose based on local guidelines, often 4 mg/kg/day artesunate component once daily for 3 days combined with single or multi-day sulfalene-pyrimethamine doses according to national treatment protocols
Pediatric Dosing
- Uncomplicated malaria in children: Weight-based dosing over 3 consecutive days
- Must follow exact national malaria treatment guidelines based on weight bands to ensure adequate artesunate and antifolate exposure without toxicity
Indications
- Treatment of acute uncomplicated Plasmodium falciparum malaria in endemic regions
- Reduction of transmission through blood-stage parasite clearance and gametocidal activity of artesunate combined with longer-acting partner drugs
Mechanism of Action
- Artesunate: Endoperoxide moiety is cleaved by intraparasitic iron, generating free radicals that damage parasite macromolecules
- Sulfalene: Inhibits dihydropteroate synthase (DHPS), blocking bacterial/parasitic folate synthesis
- Pyrimethamine: Inhibits dihydrofolate reductase (DHFR), synergizing with sulfalene to halt nucleic acid synthesis
Contraindications
- Known hypersensitivity to artesunate, artemisinin derivatives, sulfalene, pyrimethamine, or any sulfonamide
- History of sulfonamide-induced immune thrombocytopenia or severe cutaneous adverse reactions
- Severe hepatic or renal impairment where elimination of components is significantly compromised
- First trimester of pregnancy (where alternative first-line agents are preferred per WHO guidelines, unless no options exist)
Adverse Reactions
- Common: Headache, dizziness, nausea, vomiting, abdominal pain, asthenia
- Hematologic: Transient reticulocytopenia, neutropenia, anemia
- Hepatic: Transient elevations in transaminases
- Severe (sulfonamide/pyrimethamine components): Hypersensitivity reactions, Stevens-Johnson syndrome, toxic epidermal necrolysis, severe hematologic toxicities (agranulocytosis, megaloblastic anemia)
Drug Interactions
- Antifols (e.g., methotrexate, trimethoprim-sulfamethoxazole): Increased risk of bone marrow suppression and folate deficiency
- CYP2A6 and CYP2C19 substrates/inhibitors: Potential pharmacokinetic interactions with the artesunate component
- Highly protein-bound drugs: Sulfalene may displace or be displaced, potentially altering free fraction concentrations
- QT-prolonging agents: Use with caution due to additive cardiac conduction risks
Curated Content: Needs Vetting Before Put to Clinical Use