Atovaquone-proguanil

General

• Type: Antimalarial
• Dosage Forms: tablet
• Dosage Strengths: 62.5mg/25mg, 250mg/100mg
• Routes of Administration: PO
• 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

• Hypersensitivity reaction
• Stevens-Johnson Syndrome
• Erythema multiforme
• Photosensitivity
• Hepatotoxicity
• Neutropenia
• Anemia
• Pancytopenia

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