摘要
肿瘤放化疗中致吐机制及传递神经递质的多样性、治疗药物药理特点的多样性决定了临床药物选择的多样性,且同类药物间也存在用药特点的差异性。肿瘤放化疗所致的呕吐,其形成呕吐反射的神经递质主要为多巴胺、乙酰胆碱、组胺、5-羟色胺(5-HT3)和神经激肽(NK1)。近年来,临床使用的药物主要为5-HT3受体拮抗剂和NK1受体拮抗剂。5-HT3受体拮抗剂类药物作用机制大致相同,其差异性主要体现在与受体的作用方式、亲和力、量效曲线关系和药代动力学特征及药物代谢酶的差异。阿瑞吡坦为2003年被美国FDA批准上市的第一个NK1受体拮抗剂,与5-HT3受体拮抗剂、地塞米松合用被列为高致吐化疗和延迟性呕吐的标准药物治疗方案。2006年,ASCO修订委员会颁布了新版肿瘤患者止吐药应用指南,该指南中把止吐药物定位为:1)较高治疗指数药物;2)较低治疗指数药物;3)辅助药物。对肿瘤化疗高度、中度致吐的止吐治疗中,均将上述较高指数的3类药物联合或组合应用。对低度止吐的化疗方案,则适当使用辅助药物。
The mechanism of emetic and the transitive neurotransmitter and the therapeutic drugs are diversity, and the same kind drugs have different characteristics. The neurotransmitters of emetic are included： dopamine, acetylcholine, histamine, 5-hydroxytryptamine, neurokinin. The mainly drugs used in clinical are 5-hydroxytryptamine-3 （5-HT3） serotonin receptor antagonists and neurokinin-1 receptor antagonist. The mechanism of 5-HT3 antagonists are similar, their differences are the mode of action and affinity with receptors, the potency and pharmaceutical characteristics. Aprepitant is the first NK1 receptor antagonist approved by FDA. The three-drug combination of 5-HT3 serotonin receptor antagonist, dexamethasone and aprepitant are recommended before chemotherapy of high emetic risk. American Society of Clinical Oneology Guideline for Antiemetics in Oncology was updated in 2006. According to the guideline, the antiemetic agents are divided into three kinds： 1 ）highest therapeutic index drugs; 2）lower therapeutic index drugs; 3）adjunctive drugs. For patients with high or moderate emetic risk, the three-drug combination is recommended. For patients with low emetic risk, the adjunctive drugs can be used.
出处
《中华肿瘤防治杂志》
CAS
2007年第21期1675-1678,共4页
Chinese Journal of Cancer Prevention and Treatment
关键词
肿瘤/治疗
肿瘤/药物疗法
止吐药
综述文献
neoplasms/therapy
neoplasms/drug therapy
antiemeties
review literature
