Melarsoprol

Melarsoprol is a medication used in the treatment of African trypanosomiasis, also known as sleeping sickness. It is specifically used for late stage Trypanosoma brucei gambiense or Trypanosoma brucei rhodesiense, when the disease has invaded the central nervous system. Melarsoprol is given by injection into a vein.

Medical Uses

Melarsoprol is used in the treatment of late stage African trypanosomiasis, when the disease has invaded the central nervous system. It is effective against both Trypanosoma brucei gambiense and Trypanosoma brucei rhodesiense.

Side Effects

The use of melarsoprol can result in a number of side effects, including fever, nausea, vomiting, headache, and pain in the joints. More serious side effects can include high blood pressure, rapid heart rate, and the so-called "reactive encephalopathy", which can lead to coma and death.

Mechanism of Action

Melarsoprol works by inhibiting the enzyme pyruvate kinase, which is essential for the survival of the trypanosomes. This leads to a decrease in ATP production, causing cell death.

History

Melarsoprol was first synthesized in 1949. It is one of the few treatments available for late stage African trypanosomiasis, and despite its toxicity, it remains the only effective treatment for this stage of the disease.

External Links

• WHO Model List of Essential Medicines
• Drugs.com Monograph

Melarsoprol Resources
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