Suramin

Suramin is widely used as a macrofilaricide in human onchocerciasis, and its action on microfilariae also is considerable. It also is useful in the treatment of the he-molymphatic stage of African trypanosomiasis. Early treatment of the infection with suramin clears try-panosomes from the blood and lymphatics within 30 minutes and keeps them clear for approximately 3 months. Suramin inhibits a number of filarial enzymes involved with carbohydrate metabolism as well as the production of adenosine triphosphate (ATP). It is 35 times more inhibitory to the dihydrofolate reductase of O. volvulus than to the same enzyme in human tissue. It is a potent inhibitor of reverse transcriptase, the DNA polymerase of retroviruses, and also has some effects on the infective and cytopathic effects of HIV. It is being evaluated as an anticancer drug, reducing pain and delaying progression in hormone-refractory prostate cancer. Its most significant toxicity has been the development of severe polyradiculoneuropathy.

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