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, vomiting (↑ in children), nausea.
Neuro: dizziness, vertigo, fatigue, neuropsychiatric symptoms.
Therapeutic Classification: antimalarials
Pharmacologic Classification: quinine analogues
Absorption: Well absorbed following oral administration.
Distribution: Extensive tissue distribution including parasitized erythrocytes.
Protein Binding: 98%.
Metabolism/Excretion: Extensively metabolized by the liver primarily by the CYP3A4 isoenzyme; metabolites do not have antimalarial activity. Excreted mostly in bile and feces as metabolites. Small amounts excreted in urine.
Half-life: 2–4 wk.
20 kg): Mild to moderate malaria: 20–25 mg/kg (may be split into two doses 6–8 hr apart, if vomiting occurs, all or part of the dose may be repeated); patients with acute P. vivax should also be subsequently treated with an 8-aminoquinoline; prophylaxis: 5 mg/kg once weekly (for patients >45 kg: use one 250 mg tablet, if 30–45 kg: use ¾ tablet, if 20–30 kg: use ½ tablet) beginning one wk before arrival in endemic area (sooner if concurrent medications decrease tolerance) and continued for 4 wk after returning.