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化疗中通常因为细胞毒药物狭窄的治疗指标限制而无法给予足够的剂量,这主要是由于这些药物不能对正常细胞和肿瘤细胞作出区别。损害正常细胞的毒性作用可能影响病人的生命质量。应用化学保护剂使化疗药物特定失活的方法已经被广泛探讨。它是通过减少对正常组织可能的剂量限制性毒性来改善细胞毒药物的治疗作用。严格来说,化学保护剂必须做到不影响化疗药物的疗效并且没有干扰化疗实施的毒性。 第一个化学保护剂是亚叶酸(甲酰四氢叶酸),它被用来克服氨甲蝶呤诱发的毒性。随着顺铂、烷化剂和蒽环霉素损害正常组织机理的阐明,人们已经构想出一些特定药物并在临床中进行考察,其目的是减少化疗药物对正常组织的毒性。实验证明含硫的亲核化合物和金属螯合物具有较
Chemotherapy is often due to restrictions on the treatment of cytotoxic drugs can not be given sufficient dose, mainly because these drugs can not distinguish between normal cells and tumor cells. The toxic effects of damage to normal cells may affect the patient’s quality of life. The use of chemoprotectants to specifically inactivate chemotherapeutic drugs has been extensively explored. It improves the therapeutic effect of cytotoxic drugs by reducing the potential dose-limiting toxicity to normal tissues. Strictly speaking, the chemoprotectant must not affect the efficacy of chemotherapy drugs and does not interfere with the toxicity of chemotherapy. The first chemoprotectant is leucovorin (leucovorin), which is used to overcome methotrexate-induced toxicity. With the elucidation of the mechanism by which cisplatin, alkylating agents and anthracyclines impair normal tissues, some specific drugs have been conceived and investigated clinically to reduce the toxicity of chemotherapeutic drugs to normal tissues. Experiments show that sulfur-containing nucleophilic compounds and metal chelates have more