Atovaquone
MEPRON
What it isInhibitor of the parasite and fungal mitochondrial electron transport chain; PJP and babesiosis.
Why this oneIt treats and prevents Pneumocystis in sulfa allergy, which few alternatives do.
What limits itAbsorption depends heavily on fat, so it must be taken with a fatty meal. It is expensive and less effective than co-trimoxazole.
FDA-approved for
- Pneumocystis jirovecii pneumonia (1992)
- malaria prophylaxis with proguanil
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Prevention of Pneumocystis jirovecii pneumonia (PCP), TMP-SMX-intolerant | Adults & adolescents ≥13 yr | 1,500 mg (10 mL) QD with food | 1,500 mg QD with food | 1,500 mg/day |
| Treatment of mild-to-moderate PCP, TMP-SMX-intolerant | Adults & adolescents ≥13 yr | 750 mg (5 mL) BID with food ×21 days | 750 mg BID with food ×21 days | 1,500 mg/day |
Renal Undefined
Hepatic No adjustment stated; closely monitor patients with severe hepatic impairment (hepatotoxicity reported)
Instructions
- Administer with food — failure to take with food lowers plasma concentrations and may limit response
- Foil pouch: take entire contents (2 pouches for a 10-mL dose); bottle: shake gently before use
- Consider alternative therapy in patients unable to take with food or with GI disorders limiting absorption
Contraindications
- History of severe cutaneous adverse reaction (SJS, DRESS, EM) with atovaquone — must not be re-treated
Cautions
- Limited oral absorption — must be taken with food; GI disorders may cause suboptimal concentrations
- Hepatotoxicity: cholestatic hepatitis, elevated liver enzymes, and fatal liver failure reported
- Severe cutaneous adverse reactions (SJS, DRESS, erythema multiforme) — discontinue immediately if signs develop
- Not studied for severe PCP ((A-a)DO2 >45 mm Hg) or after TMP-SMX treatment failure
Adverse reactions
- Prevention: diarrhea, rash, headache, nausea, fever
- Treatment: rash (incl. maculopapular), nausea, diarrhea, headache, vomiting, fever
Pregnancy Insufficient human data; pregnant women with HIV and PCP are at increased risk of severe illness and maternal death
Lactation No data on presence in human milk (present in rat milk); for women with HIV, breastfeeding risks include HIV-1 transmission; weigh benefits and risks
NO BOXED WARNINGS
Principal riskAbsorption fails without a fatty meal
Cost, est. cash$10–$300/month
Generic entry2014
Classes and tags
Clinical profile
Legacy pregnancy categoryUnknown / historical label unavailable
Defining liabilityGenerally tolerated at therapeutic doses; clinically important risks are agent-specific and increase with interactions or organ impairment.
Mechanism of action: Atovaquone ballicule
