Dolasetron。回顾其药理学和治疗潜在的管理化疗引起的恶心和呕吐,放疗或手术。

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贝尔福杰,果阿吉隆坡

Dolasetron。回顾其药理学和治疗潜在的管理化疗引起的恶心和呕吐,放疗或手术。

药。1997年8月,54 (2):273 - 98。

PubMed ID
9257083 (在PubMed
]
文摘

Dolasetron (Dolasetron甲磺酸盐)是一个pseudopelletierine-derived 5-HT3拮抗剂最近成为可供临床使用。它正迅速在体内转化成积极的主要代谢物,hydrodolasetron,似乎主要负责其药理作用。在临床试验中,单一的静脉注射或口服剂量的dolasetron是有效预防急性化疗所致恶心、呕吐(CINV)。静脉注射剂量为1.8毫克/公斤实现完全抑制呕吐在大约50%的患者接受高度emetogenic cisplatin-containing在大约60 - 80%的病人接受化疗和适度emetogenic化疗。在后一种设置,口服200毫克剂量的实现类似的响应率。在比较研究中,静脉注射dolasetron 1.8毫克/公斤是有效的静脉granisetron 3毫克或联合32毫克高度emetogenic化疗后,和口服200毫克dolasetron相当于多个口服剂量的联合(3或4剂8毫克)后适度emetogenic化疗。Dolasetron 1.8毫克/公斤优于胃复安在预防呕吐引起的高剂量顺铂化疗或适度emetogenic高危组。Dolasetron还显示效果在预防radiotherapy-induced恶心和呕吐(RINV)的初步研究。单一静脉或口服dolasetron剂量范围从12.5到100毫克和25 - 200毫克,分别明显比安慰剂更有效预防术后恶心呕吐(PONV)的女外科病人。50毫克静脉注射剂量是有效预防PONV出现集团联合4毫克。 Intravenously administered dolasetron was also effective in treating established PONV, although complete suppression of vomiting was achieved in < 40% of patients. Dolasetron has a tolerability profile characteristic of this class of compounds, with headache, dizziness and diarrhoea being the most commonly occurring adverse events in clinical trials. Diarrhoea is not thought to be related to dolasetron administration, being experienced mostly by patients receiving chemotherapy. Dolasetron and other 5-HT3 receptor antagonists have been associated with minor changes in ECG intervals, but these generally do not appear to be clinically important. Thus, available evidence suggests that dolasetron will provide an alternative to other 5-HT3 receptor antagonists for the management of CINV and PONV. Further studies are required to determine whether it offers any advantages over other agents in these settings and to determine the optimum dosage for preventing RINV.

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药物
药物靶点
药物 目标 类 生物 药理作用 行动
Dolasetron 5 -羟色胺受体3 蛋白质 人类
是的
拮抗剂
 细节