阿片类拮抗剂对苯二氮䓬类药物抗惊厥和催眠活性的影响。
Effects of opioid antagonists on anticonvulsant and hypnotic activity of benzodiazepines.
作者信息
Fidecka S, Langwiński R
机构信息
Department of Pharmacodynamics, Medical Academy, Lublin, Poland.
出版信息
Pol J Pharmacol. 1996 Jul-Aug;48(4):409-14.
The influence of naloxone and naltrexone on the hypnotic and protective efficacy of diazepam, chlordiazepoxide, clonazepam and estazolam against electroshock- and pentylenetetrazole-induced seizures was studied in mice. Naloxone and naltrexone significantly decreased the anticonvulsant effects of diazepam and estazolam, but they did not changed that of chlordiazepoxide and clonazepam in electroshock-induced tonic hindlimb extension. Protective effects of benzodiazepines against pentylenetetrazole-induced seizures were slightly diminished by naloxone and naltrexone (16 mg/kg). Opioid antagonists were able to reduce the duration of benzodiazepines-induced sleep at high dose (32 mg/kg) only. These findings suggest that the endogenous opioid system may participate in antiepileptic effects of benzodiazepines but not in their hypnotic activity.
在小鼠中研究了纳洛酮和纳曲酮对苯二氮䓬类药物（地西泮、氯氮䓬、氯硝西泮和艾司唑仑）抗电击和戊四氮诱发惊厥的催眠及保护作用的影响。纳洛酮和纳曲酮显著降低了地西泮和艾司唑仑的抗惊厥作用，但在电击诱发的强直性后肢伸展实验中，它们并未改变氯氮䓬和氯硝西泮的抗惊厥作用。纳洛酮和纳曲酮（16mg/kg）使苯二氮䓬类药物对戊四氮诱发惊厥的保护作用略有减弱。阿片类拮抗剂仅在高剂量（32mg/kg）时能够缩短苯二氮䓬类药物诱导的睡眠时间。这些发现表明内源性阿片系统可能参与苯二氮䓬类药物的抗癫痫作用，但不参与其催眠活性。
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