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 Guide Editors
 Editor In Chief
    Joel E. Gallant, MD, MPH

Pharmacology Editor
    Paul Pham, PharmD, BCPS

Zambia Guideline Team
   Peter Mwaba MMed PhD FRCP
   Alywn Mwinga MMed
   Isaac Zulu MMed MPH
   Velepie Mtonga MMed
   Albert Mwango MBChB
   Jabbin Mulwanda MMed FCS
 

 

 

Drugs>Antimicrobial Agents>
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Melarsoprol

Pham P and Bartlett JG
08-29-2008

Zambia Specific Information

  • Available formulation in Zambia: Melarsoprol injection: 3.6% solution, 5ml ampoule (180 mg of active compound).
  • Used in the treatment of African sleeping sickness (Gambian and Rhodesian trypanosomiasis) with neurologic involvement.
  • Second line treatment of early African sleeping sickness resistant to treatment with suramin.
  • Pre-treatment with suramin for 24-48 hours recommended in debilitated pts w/ high levels of parasitemia in order to reduce Jarisch-Herxheimer-like reaction.

REFERENCES

Zambia Information Author: Paul A. Pham, Pharm. D.

INDICATIONS

NON-FDA APPROVED USES

  • Late stage African sleeping sickness (Gambian and Rhodesian trypanosomiasis) with neurologic involvement.
  • Early stage African (Gambian and Rhodesian trypanosomiasis) sleeping sickness, resistant to treatment with suramin or pentamidine.

FORMS

brand 
name
 
generic 
Mfg 
brand 
forms
 
cost* 
Arsobal, Mel B and Melarson Oxide-BALAvailable from the CDC ( 404-639-3670 )--
-
-
-

*Prices represent cost per unit specified and are representative of "Average Wholesale Price" (AWP). AWP Prices were obtained and gathered by Lakshmi Vasist Pharm D using the Red Book, manufacturer's information, and the McKesson database.

^Dosage is indicated in mg unless otherwise noted.

USUAL ADULT DOSING

  • Late stage T. brucei gambiense: melarsoprol 3.6 mg/kg/day (up to 180 mg) on days 1, 2, 3, 11, 12, 13 and if CSF WBC>20, days 21, 22, 23. Pre-treatment with 1-2 doses of 4 mg/kg pentamidine 24-72h before 1st injection of melarsoprol to prevent Jarisch-Herxheimer-like reaction .
  • Late stage T. brucei rhodesiense: melarsoprol in mg/kd (day): 0.36mg/kg (day1), 0.72mg/kg (day2), 1.1 mg/kg (day3), 1.8mg/kg (day10,11,and 12), 2.2mg/kg (day19), 2.9mg/kg (day20), 3.6mg/kg (up to 180 mg)(day21,28,29,and 30). Pre-treatment with 2-3 doses of suramin (5,10,20 mg/kg) IV over 3-5 days before 1st injection of melarsoprol to prevent Jarisch-Herxheimer-like reaction .
  • Prevention of melarsoprol-induced encephalopathy: prednisolone 1 mg/kg up to 40 mg/day started 1-2 days before first dose of melarsoprol, continued to last dose, tapered over 3 days (30, 20, 10 mg).
  • Eflornithine is a more effective and better-tolerated for T. b. gambiense infections.

RENAL DOSING

DOSING FOR GLOMERULAR FILTRATION OF 50-80

Usual dose.

DOSING FOR GLOMERULAR FILTRATION OF 10-50

No data. Consider dose reduction.

DOSING FOR GLOMERULAR FILTRATION OF <10 ML/MIN

No data. Consider dose reduction.

DOSING IN HEMODIALYSIS

No data. Consider dose reduction.

DOSING IN PERITONEAL DIALYSIS

No data.

ADVERSE DRUG REACTIONS

COMMON

  • Encephalopathy (10-12% of patients, usually after day 3, and the start of the second course)
  • Phlebitis
  • Peripheral neuropathy
  • Jarisch-Herxheimer-like reaction (pre-treatment with suramin or pentamidine for 24-48 hours recommended in debilitated pts w/ high levels of parasitemia in order to reduce Jarisch-Herxheimer-like reaction)
OCCASIONAL

  • Rash
  • Hepatic dysfunction
  • Hypertension
  • Arthralgia
  • Hemolytic anemia
RARE

  • Shock

DRUG INTERACTIONS

None known

SPECTRUM

Trypanosoma brucei gambiense and Trypanosoma brucei rhodesiense

PHARMACOLOGY

Pharmacology

COMMENTS

Melarsoprol (Mel B, Arsobal), an investigational drug, is an arsenical compound with trypanosomicidal effects. It is indicated for the treatment of African sleeping sickness (Gambian and Rhodesian trypanosomiasis) with neurologic involvement and for the treatment of early African sleeping sickness that is resistant to treatment with suramin or pentamine.

REFERENCES

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