melarsoprol

Introduction

Arsenical.

Indications

• Trypanosoma brucei-rhodesiense
• stage II, abnormal CSF or stage I who fail suramin &/or pentamidine
• because of toxicity, never the 1st agent for treatment of stage I

Dosage

• three courses of treatment each 3 days in duration
  • #1: 2-3.6 mg/kg/day IV divided TID
  • #2: (1 week later) 3.6 mg/kg/day IV divided TID
  • #3: (10-21 days later) 3.6 mg/kg/day IV divided TID

Adverse effects

(highly toxic)

• reactive encephalopathy 18%
  • high fever
  • headache
  • tremor
  • impaired speech
  • seizures
  • coma
  • death
• extravasation of drug produces intense local reactions
• vomiting
• abdominal pain
• nephrotoxicity
• myocardial damage

More general terms

• antiprotozoal agent

Additional terms

• arsenic [As]
• Trypanosoma brucei-rhodesiense

Database

• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=10311