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

References

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