Drugs>Antimicrobial Agents>

INDICATIONS

• Not FDA approved. Orphan Drug Status for use in treatment of metastatic hormone-refractory prostate cancer.

• First-line treatment of early hemolymphatic stage of African trypanosomiasis with normal CSF
• Salvage treatment of late stage African trypanosomiasis with CNS involvement in debilitated patients (limited efficacy).
• Infection by Onchocerca volvulus (second-line)
• Carcinoma of prostate (compassionate use)

FORMS

*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

• African trypanosomiasis, early hemolymphatic stage with normal CSF: 1 gram IV on days 1, 3, 7, 14, and 21.
• African trypanosomiasis, late stage with CNS involvement, in debilitated patients: 200 mg IV daily for 2 to 4 days before starting melarsoprol 18 mg. If cannot tolerate melarsoprol, alternative: tryparsamide (30 mg/kg every 5 days for a total of 12 injections) and suramin (10 mg/kg IV every 5 days also for a total of 12 injections); may be repeated after 1 month.
• Onchocerciasis: 1 gm of a 10% solution administered by slow IV injection (at weekly intervals) for 5 wks; usually given after a 23-day course of diethylcarbamazine as alternative to ivermectin.
• NOTE: Test dose of 100 to 200 mg IV should be given to detect toxic drug reactions

RENAL DOSING

ADVERSE DRUG REACTIONS

• Before initiating suramin therapy, 100-200 mg test dose recommended for adults (10-20 mg test dose for children) because severe toxic reactions may occur. Incidence (0.1-0.3%)

• Anaphylactoid reaction, Mazzotti reaction (inflammatory response to rapid destruction of microfilaria in the cutaneous tissues).
• Nausea, vomiting, stomatitis, diarrhea, and abdominal pain
• Renal toxicity, albuminuria, proteinuria, hematuria and acute renal failure.

• Immediate reaction (nausea, vomiting, shock, and loss of consciousness).
• Erythema multiforme, keratoacanthoma, exfoliative dermatitis, and toxic epidermal necrolysis.
• Adrenal insufficiency
• Anemia, leukopenia, agranulocytosis, thrombocytopenia, neutropenia, and coagulopathy.
• Ototoxicity
• ASL/ALT elevation.

DRUG INTERACTIONS

• Drug interactions with PIs and NNRTIs unlikely.

SPECTRUM

• Trypanosoma brucei gambiense; Trypanosoma brucei rhodesiense; Onchocerca volvulus

PHARMACOLOGY

Pharmacology

COMMENTS

Basis for Recommendations

• African trypanosomiasis (sleeping sickness); http://www.who.int/mediacentre/factsheets/fs259/en/ ;
  Rating: Basis for recommendation
  Comments:WHO recommendations
  
  

REFERENCED WITHIN THIS GUIDE

• Melarsoprol