Kimura E, Niimi S, Watanabe A, Akiyama M, Tanaka T
Dept. of Obstetrics and Gynecology, Jikei University School of Medicine, Japan.
Gan To Kagaku Ryoho. 1996 Mar;23(4):477-81.
Azasetron, a selective 5-HT3 receptor antagonist, has been previously shown to be highly effective in the prophylaxis of nausea and vomiting induced by anticancer drugs and is widely used in the clinical setting in Japan. In order to improve the antiemetic effect of azasetron, we designed a continuous intravenous infusion method of this drug and compared the antiemetic effect of this method with that of standard bolus intravenous injection on nausea and vomiting associated with anticancer drugs including 75 mg/m2 cisplatin (CDDP). A continuous group is intravenous bolus injection of 2.5 mg azasetron followed by 7.5 mg continuous intravenous infusion for 24 hrs, and a bolus group is intravenous bolus injection of 10 mg azasetron. The inhibitory effect on nausea of the continuous group was significantly superior to those of the bolus group on day 3 and 4 (p < 0.05) and inhibitory effect on vomiting of the continuous group was significantly superior to those of bolus group on day 2 (p < 0.05). No adverse effects were observed in either group of this study. From these data, continuous intravenous infusion of azasetron was considered to be highly effective in prophylaxis of nausea and vomiting induced by anticancer drugs.
阿扎司琼是一种选择性5 - HT3受体拮抗剂，此前已证明其在预防抗癌药物引起的恶心和呕吐方面非常有效，在日本临床上广泛使用。为了提高阿扎司琼的止吐效果，我们设计了该药物的持续静脉输注方法，并将该方法与标准静脉推注法对包括75 mg/m2顺铂（CDDP）在内的抗癌药物相关恶心和呕吐的止吐效果进行了比较。持续组为静脉推注2.5 mg阿扎司琼，随后24小时持续静脉输注7.5 mg，推注组为静脉推注10 mg阿扎司琼。持续组在第3天和第4天对恶心的抑制作用显著优于推注组（p < 0.05），持续组在第2天对呕吐的抑制作用显著优于推注组（p < 0.05）。本研究两组均未观察到不良反应。根据这些数据，阿扎司琼持续静脉输注被认为在预防抗癌药物引起的恶心和呕吐方面非常有效。
