Atovaquone
Brand names: Wellvone, Malarone (combined with proguanil)
Atovaquone is an oral antiprotozoal and antifungal agent used mainly for the treatment and prevention of Pneumocystis jirovecii pneumonia in patients who cannot tolerate co-trimoxazole, and for toxoplasmosis.
Adult dose
Dose adjustments
eMC §4.2: not specifically studied in patients with significant hepatic or renal impairment. If it is necessary to treat such patients, caution is advised and administration should be closely monitored; no numeric dose adjustment is stated. The benzyl alcohol content means it should be used with caution in liver or kidney impairment because of the risk of accumulation and toxicity (metabolic acidosis). US labelling §5.2: closely monitor patients with severe hepatic impairment following administration - cases of cholestatic hepatitis, elevated liver enzymes and fatal liver failure have been reported.
Dose auto-extracted from UK Summary of Product Characteristics (SPC) via the eMC; US FDA prescribing information (openFDA / DailyMed) — cross-check; US labelling may differ from UK — not yet clinician-verified. Always confirm against the product SmPC and your local formulary before prescribing.
Contraindications
- Known hypersensitivity to atovaquone or to any of the excipients (eMC §4.3)
- US labelling additionally: patients who develop or have a history of hypersensitivity reactions (e.g. angioedema, bronchospasm, throat tightness, urticaria) to atovaquone or any component of the oral suspension
Side effects
- Very common: nausea
- Very common: rash, pruritus
- Common: diarrhoea, vomiting
- Common: headache, insomnia, fever
- Common: anaemia, neutropenia, hyponatraemia
- Common: elevated liver enzyme levels; hypersensitivity reactions including angioedema, bronchospasm and throat tightness
- Not known: erythema multiforme, Stevens-Johnson syndrome
Interactions
- Rifampicin or rifabutin - concomitant administration is NOT recommended (reduces atovaquone concentrations)
- Tetracycline - reduces atovaquone concentrations; patients receiving concurrent tetracycline should be closely monitored for loss of atovaquone efficacy
- Metoclopramide - concurrent use is not recommended; another antiemetic treatment should be given
- Efavirenz or boosted protease inhibitors - concomitant administration should be avoided whenever possible
- Etoposide - atovaquone can increase the levels of etoposide and its metabolite
- Indinavir (US labelling) - reduces indinavir trough concentrations; use caution and monitor for loss of indinavir efficacy
Clinical monograph
How it works
It selectively inhibits the parasite cytochrome bc1 complex of the mitochondrial electron transport chain, disrupting pyrimidine biosynthesis and energy production.
Prescribing in practice
- Absorption is poor and highly dependent on fat, so atovaquone must be taken with a fatty meal to achieve adequate plasma concentrations and treatment efficacy, particularly important in patients with diarrhoea or malabsorption.
- It is generally less effective than co-trimoxazole for Pneumocystis pneumonia, so it is reserved for those intolerant of first-line therapy.
- Concurrent rifampicin and certain other agents can substantially lower atovaquone levels and reduce efficacy.
Monitoring
Monitor clinical response and tolerability, with attention to whether the drug is being taken with food to ensure adequate absorption.
Counselling the patient
- Always take this medicine with food, ideally something containing fat, to help it work.
- Continue prophylaxis for as long as advised even when you feel well.
- Report persistent diarrhoea or vomiting, which may reduce how well the drug is absorbed.
Evidence & guidelines
Atovaquone is recommended in UK guidance as an alternative agent for Pneumocystis jirovecii pneumonia prophylaxis and treatment in patients intolerant of co-trimoxazole.
Reference: BHIVA HIV Guidelines; PHE Malaria Guidelines; NICE Malaria Prevention Guidance; IDSA PCP Guidelines; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. The structured dose values shown have been reviewed by a clinician. Monograph status: clinician-reviewed (2026-07-04).
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