Melarsoprol
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| Trade names | Arsobal |
| AHFS/Drugs.com | Micromedex Detailed Consumer Information |
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IV |
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| Pharmacokinetic data | |
| Biological half-life | 35 hours |
| Excretion | Kidney |
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| Synonyms | Mel B, Melarsen Oxide-BAL |
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| ChEMBL | |
| ECHA InfoCard | 100.007.086 |
| Chemical and physical data | |
| Formula | C12H15AsN6OS2 |
| Molar mass | 398.341 g/mol |
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Melarsoprol is a medication used for the treatment of sleeping sickness (African trypanosomiasis). It is specifically used for second-stage disease caused by Trypanosoma brucei rhodesiense when the central nervous system is involved. For Trypanosoma brucei gambiense, the medication eflornithine is usually preferred. It is given by injection into a vein.
Melarsoprol has a high number of side effects. Common side effects include brain dysfunction, numbness, rashes, and kidney and liver problems. In those with glucose-6-phosphate dehydrogenase (G6PD) deficiency, red blood cell breakdown may occur. It has not been studied in pregnancy. It works by blocking pyruvate kinase, an enzyme required for the parasite to make adenosine triphosphate.
Melarsoprol has been used medically since 1949. It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system. In regions of the world where the disease is common, melarsoprol is provided for free by the World Health Organization. It is not commercially available in Canada or the United States. In the United States, it may be obtained from the Centers for Disease Control and Prevention, while in Canada it is available from Health Canada.
People diagnosed with trypanosome-caused disease should be treated with an anti-trypanosomal. Treatment is based on stage, 1 or 2, and parasite,T. b. rhodesiense or T. b. gambiense. In stage 1 disease, trypanosomes are present only in the peripheral circulation. In stage 2 disease, trypanosomes have crossed the blood brain barrier and are present in the central nervous system.
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