5-HT3受体拮抗剂预防化疗所致的恶心和呕吐。药理学和临床疗效的比较。
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Gregory再保险Ettinger DS
5-HT3受体拮抗剂预防化疗所致的恶心和呕吐。药理学和临床疗效的比较。
药。1998年2月,55 (2):173 - 89。
- PubMed ID
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9506240 (在PubMed]
- 文摘
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在1980年代中期发现血清素(5 -羟色胺;5)至少部分负责生产化疗所致恶心和呕吐。因此意识到5 -羟色胺与5 -羟色胺受体封锁5-HT3受体拮抗剂可抑制化疗所致恶心和呕吐。5-HT3拮抗剂具有不同的化学结构和受体结合亲和力。Granisetron dolasetron及其主要代谢物是纯5-HT3拮抗剂,而联合和tropisetron薄弱5-HT4受体拮抗剂。联合也被证明在其他5 -羟色胺受体和绑定到μ阿片受体。granisetron的半衰期,tropisetron和dolasetron活性代谢物2到3倍的时间比联合。这些观察最初建议将需要更频繁的联合政府;不过,它现在已经表明受体封锁不与消除半衰期和所有5-HT3拮抗剂可以有效地管理每天一次。临床试验进行直接比较5-HT3拮抗剂。 To compare these studies, it is necessary to assess trial design, including known risk factors for the development of chemotherapy-induced nausea and vomiting, and response criteria. Stratification for risk factors, use of strict efficacy criteria and randomisation to a blinded trial using an appropriate comparative regimen are essential for a well designed antiemetic trial. Comparative clinical trials using various doses, routes and regimens of administration have been conducted with 5-HT3 antagonists. Despite some trial design shortcomings, most of the studies show equal efficacy between the agents, especially in moderately emetogenic chemotherapy and mild, infrequently occurring adverse effects. The addition of steroids also appears to improve outcome. However, since many doses and regimens of ondansetron were used, further study is needed to determine the optimal regimen. The efficacy of 5-HT3 antagonists in controlling delayed nausea and vomiting from chemotherapy is less well studied. Further, there is no good scientific rationale for the use of 5-HT3 antagonists in controlling delayed nausea and vomiting since serotonin has not been shown to be released during the delayed phase. In fact, most studies show no benefit or modest benefit of 5-HT3 antagonists over placebo. Because the 5-HT3 antagonists perform similarly in the clinical setting, pharmacological differences do not seem to translate into therapeutic differences. There is also no appreciable difference in the incidence or severity of adverse effects among the 5-HT3 antagonists. Determination of clinical use may then be driven by cost.