Contraindicated in:
Use Cautiously in:
CV: arrhythmias (including sinus bradycardia, sinus arrhythmia, first degree AV block, abnormal T waves), ECG changes, syncope.
Derm: rash.
EENT: tinnitus.
GI: abdominal pain, diarrhea, nausea, vomiting (↑ in children).
Neuro: dizziness, fatigue, neuropsychiatric symptoms, vertigo.
Drug-Drug:
Absorption: Well absorbed following oral administration.
Distribution: Extensive tissue distribution including parasitized erythrocytes; crosses the placenta, minimal excretion in breast milk.
Protein Binding: 98%.
Metabolism/Excretion: Extensively metabolized by the liver (primarily by the CYP3A4 enzyme system), metabolites do not have antimalarial activity. Excreted mostly in bile and feces as metabolites. Small amounts excreted in urine.
Half-life: 24 wk.