Drug reference

Atovaquone

Antiprotozoal · Antipneumocystis agent

AntiprotozoalAntipneumocystis agent

CDSCO approved

EXCRETION

—

not curated

INTERACTIONS

6 major

SEVERE in our sources

PREGNANCY

Avoid (fetotoxicity and teratogenicity in animals) unless potential benefit outweighs risk.

FDA category + note

Top interactionssee all 10 →

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Mechanism

Atovaquone is an antiprotozoal agent that acts by inhibiting the parasite's mitochondrial electron transport chain. Specifically, it interferes with cytochrome b, disrupting electron transport. This action impairs ATP production and other vital metabolic processes, ultimately leading to the death of the organism.

Indications

Treatment of mild to moderate Pneumocystis jirovecii (Pneumocystis carinii) pneumonia in patients intolerant of co-trimoxazoleProphylaxis against pneumocystis pneumonia (unlicensed indication)malaria chemoprophylaxistreatment of uncomplicated p. falciparum malaria (fixed combination with proguanil)treatment of mild-to-moderate infections due to chloroquine- or sp-resistant p. falciparum malariatreatment of p. vivax malaria (followed by primaquine)Mild-moderate babesiosis (in combination with azithromycin)Toxoplasmosis (alternative regimen, less effective)prophylaxis (in combination with proguanil for travellers)Uncomplicated CQ-resistant P. falciparum (in fixed dose oral combination with proguanil, USA and some other countries, not India)Uncomplicated P. vivax malaria (in fixed dose oral combination with proguanil, USA and some other countries, not India)Prophylaxis for nonimmune travellers visiting endemic areas (in combination with proguanil)Opportunistic infections with P. jiroveci (second line drug)Opportunistic infections with T. gondii (second line drug)Alternative treatment for mild *P. jirovecii* pneumonia (PCP)Prophylaxis of *P. jirovecii* pneumonia (PCP)

Dosing

Adult: Treatment of mild to moderate Pneumocystis jirovecii (Pneumocystis carinii) pneumonia: 750 mg twice daily for 21 days, taken with food, particularly high fat food. Prophylaxis against pneumocystis pneumonia: 750 mg twice daily.
Pediatric: 5–8 kg: 2 pediatric tablets; 9–10 kg: 3 pediatric tablets; 11–20 kg: 1 adult tablet; 21–30 kg: 2 adult tablets; 31–40 kg: 3 adult tablets; >41 kg: 4 adult tablets. Daily dose to be taken for 3 consecutive days.
Renal adjustment: Manufacturer advises caution; monitor more closely in renal impairment.
Hepatic adjustment: Caution in mild to moderate hepatic impairment (risk of deterioration); avoid in severe impairment. Use with caution in significant impairment and monitor closely.
Geriatric: Caution in elderly.

Pharmacokinetics

Half-life

2 to 3 days (adults); 1 to 2 days (children)

Bioavailability

slow and variable, improves with fatty meal

Protein binding

more than 99% (plasma protein)

Excretion

bile (unchanged in feces)

Contraindications

Pregnancy (fetotoxicity and teratogenicity in animals)
Breast feeding
Severe hepatic impairment
children weighing less than 11 kg
pregnant women
lactating mothers
severe renal impairment (creatinine clearance <30 ml/min)
hypersensitivity to atovaquone or proguanil
Pregnancy

Side effects

Common

AnaemiaAngioedemaBronchospasmDiarrhoeaHeadacheHypersensitivityHyponatraemiaInsomniaNauseaNeutropeniaSkin reactionsThroat tightnessVomitingabdominal paindiarrhearashtransient elevations of serum transaminasetransient elevations of amylasecorneal deposits (similar to amiodarone)RashesFeverHepatitis

Serious