Leonard Michael Z, Kangas Brian D
Harvard Medical School, McLean Hospital, Belmont, Massachusetts, USA.
Behav Pharmacol. 2020 Apr;31(2&3):168-173. doi: 10.1097/FBP.0000000000000542.
Developing effective analgesics with fewer unwanted side effects is a pressing concern. Due to a lack of effective nonopioid options currently available, an alternative approach termed opioid-sparing evaluates the ability of a coadministered drug to reduce the amount of opioid needed to produce an antinociceptive effect. Opioids and benzodiazepines are often coprescribed. Although this approach is theoretically rational given the prevalent comorbidity of chronic pain and anxiety, it also has inherent risks of respiratory depression, which is likely responsible for the substantial percentage of fatal opioid overdoses that have involved benzodiazepines. Moreover, there have been no clinical trials to support the effectiveness of this drug combination nor has there been corroborative preclinical evidence using traditional animal models of nociception. The present studies examined the prescription µ-opioid analgesic oxycodone (0.003-0.1 mg/kg) and the prototypical benzodiazepine anxiolytic diazepam (0.03-1.0 mg/kg), alone and in combination, using an animal model of pain that examines the restoration of conflict-related operant behavior as evidence of analgesia. Results documented significant dose-related increases in thermal threshold following oxycodone treatment. Diazepam treatment alone did not produce significant antinociception. In combination, diazepam pretreatment shifted oxycodone functions upward in a dose-dependent manner, but the additive effects were limited to a narrow dose range. In addition, combinations of diazepam and oxycodone at higher doses abolished responding. Taken together, though intriguing, these findings do not provide sufficient evidence that coadministration of an anxiolytic will result in clinically relevant opioid-sparing for pain management, especially when considering the inherent risks of this drug class combination.
开发副作用更少的有效镇痛药是一个紧迫的问题。由于目前缺乏有效的非阿片类药物选择,一种称为阿片类药物节省的替代方法评估了联合使用的药物减少产生抗伤害感受作用所需阿片类药物量的能力。阿片类药物和苯二氮䓬类药物经常联合处方。尽管考虑到慢性疼痛和焦虑的普遍共病,这种方法在理论上是合理的,但它也有呼吸抑制的内在风险,这可能是涉及苯二氮䓬类药物的大量致命阿片类药物过量的原因。此外,尚无临床试验支持这种药物组合的有效性,也没有使用传统伤害感受动物模型的佐证性临床前证据。本研究使用一种疼痛动物模型,单独和联合使用处方μ-阿片类镇痛药羟考酮(0.003-0.1mg/kg)和典型的苯二氮䓬类抗焦虑药地西泮(0.03-1.0mg/kg),该模型通过检查与冲突相关的操作性行为的恢复作为镇痛的证据。结果表明,羟考酮治疗后热阈值有显著的剂量相关增加。单独使用地西泮治疗未产生显著的抗伤害感受作用。联合使用时,地西泮预处理以剂量依赖的方式使羟考酮的作用向上转移,但相加作用仅限于狭窄的剂量范围。此外,较高剂量的地西泮和羟考酮组合会消除反应。综上所述,尽管这些发现很有趣,但它们并没有提供足够的证据表明联合使用抗焦虑药会在临床上产生与疼痛管理相关的阿片类药物节省效果,尤其是考虑到这类药物组合的内在风险时。