Needle problem drug

Melarsoprol usually is slowly administered intravenously through a fine needle, even though it is absorbed from the gastrointestinal tract. Because it is very irritating, care should be taken not to infiltrate surrounding tissue. Adequate trypanocidal concentrations appear in the CSF, whereas pentamidine does not penetrate the CSF. Melarsoprol is, therefore, the agent of choice in the treatment of T. brucei rhodesiense, which rapidly invades the CNS, as well as for meningoencephalitis caused by T. brucei gambiense. The host readily oxidizes melarsoprol to a relatively nontoxic, pentavalent arsenic compound. The drug has a very short half-life and is rapidly excreted in urine Melarsoprol is given parenterally because it causes gastrointestinal irritation; it may also cause a reactive encephalopathy that can be fatal.