Comparison of the rate of elimination of racemic 2-dehydroemetine (Ro 1-9334) and of natural emetine in animals
Schwartz, D.E.; Rieder, J.
Bulletin de la Societe de Pathologie Exotique et de Ses Filiales 54: 38-48
1961
ISSN/ISBN: 0037-9085 PMID: 13749080 Document Number: 8574
The rate of disappearance of 2-dehydro-emetine and emetine in laboratory animais has been compared. Each animal received the drug as a single parenteral dose of 5 mg./kg. body weight. At varions times after its application the drug remaining in the body was measured by a new spectrofluorimetric method. Determinations were made: in blood plasma after intraarterial administration to rabbits, in the entire body and separately in the liver and in the heart after intraperitoneal injection into guinea pigsThe following results were obtained:. The rate of disappearance of 2-dehydro-emetine and emetine from blood plasma is very nearly the same. It is rapid during the first 30 minutes after the injection but slows down and becomes more constant in the following hours. 2. 2-dehydro-emetine disappears from the entire body and from the liver more than twice as fast as emetine. The following half-life periods were determined: Entire body: emetine=5,27 days. (after removal of fur and paws) 2-dehydro-emetine=2,22 days. Liner : emetine=4,16 days. 2-dehydro-emetine=1,72 day. The concentration of the drug in the entire body and in the liver is lowered, in the case of 2-dehydro-emetine after 12 days in the case of emetine after 30 days, nearly to the limit of sensitivity of the method. 3. 2-dehydro-emetine and emetine are both found in high concentration in the liver. 4. No particularly high concentration of either preparation was found in the heart. Our results lead to the conclusion that, following the application of equal doses, 2-dehydro-emetine because of its higher rate of elimination, will constantly be present in the organs at a lower concentration than emetine. This could explain the better tolerance observed with 2-dehydro-emetine.
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