Contraindicated in:
Use Cautiously in:
Prophylaxis of Malaria
EENT: visual difficulties.
GI: abdominal pain, oral ulcers.
Treatment of Malaria
CNS: headache, dizziness, weakness.
Derm: pruritus (↑ in children), photosensitivity.
GI: abdominal pain, diarrhea, nausea, vomiting, anorexia, ↑ liver enzymes.
Hemat: neutropenia.
Neuro: dizziness, dreams, headache, insomnia.
Drug-Drug:
(Generic available)
Prevention of Malaria
Treatment of Malaria
Absorption: Atovaquone — variably absorbed following oral administration, food enhances absorption; Proguanil — well absorbed following oral administration.
Distribution: Proguanil — enters breast milk in small quantities.
Protein Binding: Atovaquone — >99%.
Metabolism/Excretion: Atovaquone — undergoes enterohepatic recycling, >94% eliminated unchanged in feces; Proguanil — metabolized mostly by the CYP2C19 enzyme system and is converted to cycloguanil, the pharmacologically active metabolite.
Half-life: Atovaquone — adults: 2–3 days, children: 1–2 days Cycloguanil — Adults: 8.3 hr, elderly: 14.9 hr.
(blood levels)
| ROUTE | ONSET | PEAK | DURATION |
|---|---|---|---|
| atovaquone PO | unknown | 1–8 hr; 24–96 hr† | 24 hr |
| proguanil PO | unknown | unknown | 24 hr |
NDC Code*