Atovaquone-proguanil

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General

  • Type: Antimalarial
  • Dosage Forms: PO (62.5mg/25mg, 250mg/100mg)
  • Common Trade Names: Malarone

Adult Dosing

Malaria prophylaxis

  • 250mg/100mg PO QD
    • Start 1-2 days prior to possible exposure
    • Continue 7 days after possible exposure

Malaria treatment

  • 1000mg/400mg PO QD x 3 days
  • Not for severe, complicated or cerebral malaria
  • See CDC Recommendations for complete dosing/recommendations

Pediatric Dosing

Malaria prophylaxis

  • For all dosing regimins
    • Start 1-2 days prior to possible exposure
    • Continue 7 days after possible exposure

5-8 kg

  • 31.25mg/12.5mg PO QD

9-10 kg

  • 46.9mg/18.7mg PO QD

11-20 kg

  • 62.5mg/25mg PO QD

21-30 kg

  • 125mg/50mg PO QD

31-40 kg

  • 187.5mg/75mg PO QD

>40 kg

  • See adult dosing

Malaria treatment

  • Not for severe, complicated or cerebral malaria
  • See CDC Recommendations for complete dosing/recommendations

5-8 kg

  • 125mg/50mg PO QD x 3 days

9-10 kg

  • 187.5mg/75mg PO QD x 3 days

11-20 kg

  • 250mg/100mg QD x 3 days

21-30 kg

  • 500mg/200mg PO QD x 3 days

31-40 kg

  • 750mg/300mg PO QD x 3 days

>40 kg

  • See adult dosing

Special Populations

  • Pregnancy Rating: C
  • Lactation: Safety unknown; caution advised
  • Renal Dosing: Adult and Pediatric
    • CrCl>30: No adjustment
    • CrCl<30
      • Contraindicated for malaria prophylaxis
      • Risk/benefit analysis for malaria treatment
  • Hepatic Dosing: Adult and Pediatric
    • Undefined for severe impairment otherwise no adjustment

Contraindications

  • Allergy to class/drug
  • CrCl <30
  • Caution
    • CrCl<30 for treatment
    • Persistent severe diarrhea/vomiting

Adverse Reactions

Serious

Common

  • Elevated LFTs
  • Abdominal pain
  • Headache
  • Nausea/Vomiting
  • Cough
  • Diarrhea
  • Asthenia
  • Vivid dreams
  • Oral ulcers
  • Anorexia
  • Dizziness
  • Gastritis
  • Pruritus
  • Insomnia

Pharmacology

  • Half-life: 12-21 hours
  • Metabolism:
    • Atovaquone
      • CYP450
    • Proguanil
      • liver; CYP450
  • Excretion: feces and urine
  • Mechanism of Action:
    • Atovaquone
      • bacteriostatic or bactericidal
    • Proguanil
      • Inhibits parasite dihydofolate

Administration

  • Give with food or milk
  • If vomiting occurs within 1 hour repeat dose

See Also

Malaria

References

  • Epocrates