Dosing and uses of Arsobal (melarsoprol)
African Trypanosomiasis (Sleeping Sickness)
Investigational drug
Not commercially available in US; however, available as treatment IND from CDC; 800-CDC-INFO (800-232-4636)
2-3.6 mg/kg/day IV x3 days
After 1 week: 3.6 mg/kg/day IV x3 days
Repeat again after 10-21 days: 3.6 mg/kg/day
Pediatric dosage forms and strengths
African Trypanosomiasis (Sleeping Sickness)
Investigational drug
Not commercially available in US; however, available as treatment IND from CDC; 800-CDC-INFO (800-232-4636)
18-25 mg/kg total over 1 month
Initial 0.36 mg/kg IV
Incr gradually to 3.6 mg/kg IV at intervals of 1-5 days for total of 9-10 doses
Arsobal (melarsoprol) adverse (side) effects
Frequency not defined
Hypertension
Myocardial damage
Encephalopathy
Peripheral neuropathy
Colic
Vomiting
Albuminuria
Herxheimer-type reaction
Warnings
Contraindications
Glucose-6-phosphate dehydrogenase (G6PD) deficiency, hypersensitivity
Pregnancy and lactation
Pregnancy category: no studies conducted
Lactation: not known if excreted in breast milk
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Arsobal (melarsoprol)
Distribution: crosses blood-brain barrier
Vd: 100 L/kg
Half-life: mean terminal elimination: 35 hr
Excreted: urine
Mechanism of action
Inhibits synthesis of ATP - the energy required for survival of the parasite
