Esophageal cancer chemotherapy drug presentation Lomustine

By | March 20, 2012

Lomustine introduction, Lomustine (Lomustine), other name: Cyclohexyl nitrite gills, Luo nitrogen mustard, chloroethyl cyclohexyl nitrite gills, Romo Division D, Kalomoh nitrogen mustard, referred to as CCNU. Chemical name 1 – (2 – chloroethyl) -3 cyclohexyl burn a base -1 nitroso pay attention, the formula Cg H16 C1N3 020.
Properties: yellow or yellowish powder, insoluble in water, the water solubility of less than five ten thousandths, slightly soluble in ethanol, heat instability.
Esophageal cancer chemotherapy Lomustine experimental study synthesis of the drug in 1963. It is the product of degradation in vivo could partially block the thymus slightly Wan Xi mixed types of nuclear DNA, RNA and protein synthesis inhibition. Animal experiments showed that it had similar effects with BCNU on mouse L615 and L1210, Walker carcinosarcoma 256 in rats significantly inhibited. Glioma of the brain C57BL mice inoculated by the intraperitoneal injection of CCNU could significantly prolong the survival time. Dogs and monkeys on the main toxicity of reversible bone marrow suppression, expressed as white blood cells and thrombocytopenia, anemia, lymph node atrophy, gastrointestinal bleeding, vomiting, liver damage and delay, even after the last administration can still occur aminotransferase 1 month , the sudden increase in alkaline phosphatase.
Lomustine introduction, cell kinetics studies have shown that similar general melted its agents, acting on the proliferating cells in each period and non-proliferating cells. In the G1 S phase boundary of S phase cells or the most sensitive to inhibition of G2 period was stronger than BCNU. Although the effect of the drug has melted, but generally no cross-resistance melted agent. Kang general agent resistant Hodgkin's disease is still valid. And VCR (vincristine), PCB (C kappa umbilical) and no cross-resistance to anti-metabolism drugs, but there is cross-resistance with BCNU.
Lomustine introduction, the drug soluble strong after oral administration of a rapidly through the blood brain barrier into the cerebrospinal fluid, the drug concentration in cerebrospinal fluid after a few minutes for the blood concentration of 50%. CCNU rapidly absorbed after oral administration, plasma half-life of 15min, the rapid metabolism in the liver, and its metabolites by human intestinal bile row, the formation of enterohepatic circulation, thus lasting effect, the biological transport, the drugs mainly excreted by the kidneys.

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