Active Ingredients: 250 mg Atovaquone and 100 mg Proguanil Hydrochloride per tablet
Form: Tablets
Manufacturer: GlaxoSmithKline Inc.
Indications and Clinical Use
Prevention of Malaria: Indicated for the prophylaxis of Plasmodium falciparum malaria, including areas where chloroquine resistance has been reported.
Treatment of Malaria: Indicated for the treatment of acute, uncomplicated P. falciparum malaria.
Mechanism of Action
Atovaquone: Inhibits mitochondrial electron transport in P. falciparum.
Proguanil: Inhibits dihydrofolate reductase, disrupting DNA synthesis and replication.
Pharmacokinetics
Absorption: Atovaquone absorption increases with dietary fat. Proguanil is rapidly absorbed regardless of food intake.
Distribution: Atovaquone is highly protein-bound, and proguanil is moderately protein-bound.
Metabolism: Atovaquone is not significantly metabolized; proguanil is metabolized to cycloguanil.
Elimination: Atovaquone is eliminated in feces; proguanil and its metabolites are excreted in urine.
Adult Dosage:
Prevention: 1 tablet daily (250 mg atovaquone + 100 mg proguanil) with fatty food or milky drink, starting one day before entering a malaria-endemic area, during exposure, and for 7 days after leaving.
Treatment: 4 tablets once daily for 3 days with fatty food or milky drink.
Pediatric Dosage:
Prevention:
< 11 kg: Weight-based dose daily (specific doses provided in the document).
11–20 kg: 1 pediatric tablet daily.
20–30 kg: 2 pediatric tablets daily.
30–40 kg: 3 pediatric tablets daily.
40 kg: 1 adult tablet daily.
Treatment:
Weight-based dose once daily for 3 days with fatty food or milky drink (specific doses provided in the document).
Advantage:
Causal prophylaxis, only need to continue for 7 days after exposure.
Disadvantage:
Daily dosing required for prophylaxis.
Contraindications
Known hypersensitivity to atovaquone or proguanil hydrochloride.
Severe renal impairment (creatinine clearance <30 mL/min).
Warnings and Precautions
Hypersensitivity Reactions: Rare, but include angioedema and anaphylaxis.
Severe Malaria: Not evaluated for cerebral malaria or severe malaria manifestations.
Gastrointestinal Absorption: Absorption may be reduced in patients with diarrhea or vomiting.
Seizures and Psychiatric Symptoms: Use with caution in patients with a history of epilepsy or psychiatric illness.
Pregnancy and Breastfeeding: Use only if the potential benefit justifies the potential risk.
