Atovaquone

Administration

• Type: Antimicrobial (active against Pneumocystis jirovecii, Babesiosis, Toxoplasmosis, Malaria)
• Dosage Forms: tablet, oral suspion
• Dosage Strengths: tablet: 250mg; oral suspension: 750mg/5mL
• Routes of Administration: PO
• Common Trade Names: Mepron

Adult Dosing

• Babesiosis: 750mg PO q12h + azithromycin
• Toxoplasma encephalitis, HIV+: 1500mg daily + leucovorin +/- pyrimethamine
• PCP pneumonia (2nd line): 1500mg daily
• Malaria prophylaxis:

Pediatric Dosing

• Babesiosis: 20mg/kg q12h (max 750mg/dose) + azithromycin
• PCP pneumonia (2nd line)
  • >13yo, HIV- : 1500mg daily
  • Adolescents, HIV+: 1500mg daily +/- leucovorin, +/- pyrimethamine
  • 1-3mo, 2-13yo, HIV+: 30 mg/kg PO daily
  • 4-24mo, HIV+: 45mg/kg PO daily
• Malaria prophylaxis: 250mg + 100mg proguanil daily
• Malaria falciparum/vivax treatment: 1000mg + proguanil 400mg daily

Special Populations

• Pregnancy Rating: C
• Lactation risk: Infant risk cannot be ruled out
• Renal dosing: atovaquone/proguanil contraindicated in severe renal failure for malaria prophylaxis, otherwise no adjustment
• Hepatic dosing: no adjustment

Contraindications

• Allergy to class/drug

Adverse Reactions

Serious

• SJS, erythema multiforme
• Methemoglobinemia
• Hepatitis, liver failure

Common

• Nausea/vomiting, diarrhea
• Rash
• Headache, insomnia
• Fever
• Cough, rhinitis

Pharmacology

• Half-life: 2.2-3.2 days
• Metabolism: undergoes enterohepatic recirculation
• Excretion: Fecal

Mechanism of Action

• Unclear mechanism; structurally similar to ubiquonone, which inhibits cytochromal electron transport in Plasmodia species