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Docetaxel

已有 1796 次阅读 2014-8-29 10:54 |系统分类:论文交流

Docetaxel for Paclitaxel antineoplastic, by interfering with mitosis and the sky split between microtubule network necessary for cell function of the anti-tumor effect. Docetaxel binds to free tubulin and promoting tubulin assembly into stable microtubules while inhibiting their depolymerization, resulting in loss of a fixed normal function of microtubules generation and microtubules to inhibit cell mitosis. Docetaxel in combination with microtubules does not alter the number of raw silk, which is the most current spindle different clinical applications of drug toxicity. Toxicology Genetic toxicity: in CHO-K1 cells and chromosome aberration test in mouse bone marrow micronucleus test, Docetaxel showing cause faulting, but in the Ames test and the CHO / HGPRT gene mutation test in no mutagenic effect. Reproductive toxicity: In rats intravenously Docetaxel 0.3mg / kg (translated by body surface area, which is about the recommended clinical dose 1/50), no effects on fertility damage, but can cause testicular weight. The results with rats and dogs 10 cycles (administered once every 21 days for 6 months) repeated dose test results correlated; intravenous dose in rats and dogs were 5mg / kg and 0.375mg / kg when (according to body surface area conversion, equivalent to about a third of the recommended clinical dose and fifteenth respectively), showing that testicular atrophy and degeneration, increase the number of rats administered at low doses also showed a similar effect.

Docetaxel use during pregnancy can cause fetal damage. Rats and rabbits during organogenesis were given Docetaxel≥0.3mg / kg / day and 0.03mg / kg / day (converted by the body surface area, equivalent to the recommended daily dose clinical 1/50 and 300th, respectively), showing that embryo toxicity and fetal toxicity (manifested as intrauterine death, fetal absorption increased fetal weight loss and delayed ossification). More doses can also cause maternal toxicity. There are no adequate and strictly controlled clinical research data in pregnant women. If the patient is in the FDA pregnancy, during pregnancy or in the FDA should be told that the potential hazards and potential hazards of aborted fetuses. Women of childbearing potential should avoid using this treatment during pregnancy. Docetaxel is unclear whether excreted in human milk. Given that many drugs can be excreted in human milk, and Docetaxel may cause serious adverse reactions in nursing infants, mothers should stop breastfeeding before using this product.




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