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"Emetine"
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Status:
US Previously Marketed
First marketed in 1914
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Emetine is a principal alkaloid of ipecac, isolated from the ground roots of Uragoga ipecacuanha. Early use of emetine was in the form of oral administration of the extract of ipecac root, or ipecacuanha. This extract contains several, including cephaeline, and others. The identification of emetine as a more potent agent improved the treatment of amoebiasis. While the use of emetine still caused nausea, it was more effective than the crude extract of ipecac root. Additionally, emetine could be administered hypodermically which still produced nausea, but not to the degree experienced in oral administration. Emetine dihydrochloride hydrate is used in the laboratory to block protein synthesis in eukaryotic cells. It does this by binding to the 40S subunit of the ribosome. Emetine induces hypotension by blocking adrenoreceptors. Also, emetine was identified as a specific inhibitor of HIF-2α protein stability and transcriptional activity. Heavy or over usage of emetine can carry the risk of developing proximal myopathy and/or cardiomyopathy.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ABSOLUTE)
Oral dehydroemetine dihydrochloride (+/-) (Mebadin) was found useful both as a tissue and contact amoebicide. It is much less toxic and more active than emetine and can be given in larger doses and for longer periods with safety. Owing to the quick excretion, repeat courses can be given at short intervals, as necessary, without danger. No serious side effects were noted particularly with the oral form and it was far better tolerated by children, who received relatively higher dosage than most adults. The only contra-indication is for patients with manifest decompensation of vital organs, or fevers. Mebadin injection and Mebadin tablets are discontinued products.
