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丁丙诺啡栓剂用于术后患者的临床评估——血浆浓度及对呼吸和循环系统的影响

[Clinical evaluation of buprenorphine suppositories in postoperative patients--plasma concentrations and effects on the respiratory and circulatory system].

作者信息

Tashiro C, Takenoshita M, Mori T, Yoshiya I, Terakawa N, Tanizawa O, Yonenobu S, Ono K, Yoshikawa K

出版信息

Masui. 1989 Feb;38(2):182-9.

PMID:2733136
Abstract

The plasma concentrations of buprenorphine were measured and blood gas analysis was done after administration of buprenorphine suppositories (0.2 and 0.4 mg) or its intramuscular injection (0.2mg) in postoperative patients. The C max for 0.4mg suppositories was comparable to that for 0.2mg injection, whereas the T max for suppositories was as large as about 2 hrs in contrast to 1.5 hrs for 0.2mg injection. The size of AUC was in the following order: 0.4mg suppositories greater than 0.2mg injection greater than 0.2mg suppositories. Neither notable increase in PaCO2 nor decrease in respiration rate was observed after administration of the suppositories, indicating that the formulation will not cause clinically significant respiratory depression. No significant changes were observed in blood pressure or pulse rate. Buprenorphine suppositories are considered to be safe for use in postoperative patients. Percent pain relief in the suppository group was smaller than that in the injection group. This appears to be due to a slower rate of increase in the plasma levels of buprenorphine after administration of suppositories than that after intramuscular injection. Therefore, it seems practical to give this drug to postoperative patients before the start of pain.

摘要

在术后患者中,给予丁丙诺啡栓剂(0.2毫克和0.4毫克)或其肌肉注射剂(0.2毫克)后,测量丁丙诺啡的血浆浓度并进行血气分析。0.4毫克栓剂的Cmax与0.2毫克注射剂相当,而栓剂的Tmax长达约2小时,相比之下,0.2毫克注射剂为1.5小时。AUC大小顺序如下:0.4毫克栓剂>0.2毫克注射剂>0.2毫克栓剂。给予栓剂后,未观察到PaCO2显著升高或呼吸频率降低,这表明该制剂不会引起临床上显著的呼吸抑制。血压或脉搏率未观察到显著变化。丁丙诺啡栓剂被认为对术后患者使用是安全的。栓剂组的疼痛缓解百分比低于注射组。这似乎是由于给予栓剂后丁丙诺啡血浆水平的升高速度比肌肉注射后慢。因此,在疼痛开始前给术后患者使用这种药物似乎是可行的。

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