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Atovaquone–Proguanil

Brand: Malarone
Antimalarial Mitochondrial ETC inhibitor + DHFR inhibitor

Chemistry

Molecular Formula Atovaquone: C22H19ClO3, Proguanil: C11H16ClN5
Structure
structure

Pharmacokinetics

Half-life 48 hours
Clearance Route hepatic
Active Metabolites Cycloguanil (active metabolite of proguanil)
Notes Half-life: Atovaquone 2–3 days; Proguanil 12–20 h. Must be taken with fatty food to improve absorption.

⚠️ Safety & Warnings

Severity: Moderate

Adverse Effects:
Abdominal pain, nausea, vomiting, headache, elevated liver enzymes, mouth ulcers (due to proguanil). Rare: hallucinations.

Contraindications:
Severe renal impairment (CrCl <30 mL/min)

Precautions:
Take with fatty food to improve absorption; avoid in pregnancy unless no alternatives; monitor LFT in hepatic disease.