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Emetine.2hcl: Carcinogenic Potency Database potency.berkeley.edu |
Emetine is a drug used as both an anti-protozoal and to induce vomiting. It is produced from the ipecac root.
[edit] Early emetine-based preparationsEarly use of emetine was in the form of oral administration of the extract of ipecac root, or ipecacuanha. This extract was originally thought to contain only one alkaloid, emetine, but was found to contain several, including cephaeline, emetine, psychotrine and others. Although this therapy was reportedly successful, the extract caused vomiting in many patients which reduced its utility. In some cases, it was given with opioids to reduce nausea. Other suggestions to reduce nausea involved coating the drug to allow it to be released after digestion in the stomach. [1] [edit] Use of emetine as anti-amoebicThe identification of emetine as a more potent agent improved the treatment of amoebiasis. While 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. Although it is a potent anti-protozoal, the drug also can interfere with muscle contractions, leading to cardiac failure in some cases. Because of this, in some uses it is required to be administered in a hospital environment so that adverse events can be addressed. [edit] DehydroemetineMain article: dehydroemetine Dehydroemetine is a synthetically produced antiprotozoal agent similar to emetine in its anti-amoebic properties and structure (they differ only in a double bond next to the ethyl radical), but it produces fewer side effects. [edit] Use in blocking protein synthesisEmetine dihydrochloro 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 (Jimenez et al., Enzymatic and nonenzymatic translocation of yeast polysomes. Site of action of a number of inhibitors. Biochemistry, 1977 16;4727-4730). This can thus be used in the study of protein degradation in cells. [edit] Side EffectsHeavy/ overusage of emetine can carry the risk of developing proximal myopathy and/or cardiomyopathy. [edit] References
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