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ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS › ANTIPROTOZOALS › ANTIMALARIALS › Biguanides
proguanil and atovaquone
P01BB51
Forms & Strengths
- Atovaquone 250 mg / Proguanil hydrochloride 100 mg adult tablets
- Atovaquone 62.5 mg / Proguanil hydrochloride 25 mg pediatric tablets
Adult Dosing
- Malaria prophylaxis: 1 tablet daily starting 1-2 days before travel, during travel, and for 7 days after leaving the malaria-endemic area
- Malaria treatment: 4 tablets (total atovaquone 1000 mg/proguanil 400 mg) once daily for 3 consecutive days
Pediatric Dosing
- Prophylaxis/Treatment weight-based dosing (daily for 3 days for treatment, or during/after travel for prophylaxis):
- 11-20 kg: 1 pediatric tablet daily
- 21-30 kg: 2 pediatric tablets daily
- 31-40 kg: 3 pediatric tablets daily
- Greater than 40 kg: 1 adult tablet daily
Indications
- Prevention of Plasmodium falciparum malaria
- Treatment of acute, uncomplicated Plasmodium falciparum malaria
Mechanism of Action
- Atovaquone selectively inhibits parasite mitochondrial electron transport at the cytochrome bc1 complex
- Proguanil acts primarily via its metabolite cycloguanil, inhibiting Plasmodium dihydrofolate reductase and disrupting deoxythymidylate synthesis
Contraindications
- Known hypersensitivity to atovaquone, proguanil, or any component of the formulation
- Severe renal impairment (creatinine clearance <30 mL/min) for malaria prophylaxis
Adverse Reactions
- Headache
- Insomnia
- Nausea
- Vomiting
- Diarrhea
- Abdominal pain
- Elevated liver transaminases
- Pruritus
Drug Interactions
- Rifampin and rifabutin significantly decrease atovaquone plasma concentrations
- Tetracycline may decrease atovaquone plasma concentrations
- Metoclopramide may decrease absorption of atovaquone
- Warfarin effects may be potentiated by proguanil, increasing bleeding risk
Curated Content: Needs Vetting Before Put to Clinical Use