Busto U, Sellers E M
Pharmacy Department, Addiction Research Foundation, Toronto, Ontario, Canada.
J Subst Abuse Treat. 1991;8(1-2):29-33. doi: 10.1016/0740-5472(91)90024-5.
Benzodiazepines, which are among the safest and most effective drugs, possess all the characteristic of abuseable compounds. Although there appear to be differences in potency among compounds and variations in sensitivity among individuals, benzodiazepines have clear reinforcing properties. Tolerance to the depressant effects of benzodiazepines is rapid, but tolerance to the anxiolytic effects develops slowly and to a limited extent. Although abusers use very high doses, most long-term users persist at daily doses in the low therapeutic range (10-20 mg of diazepam or its equivalent) without dose escalation. Physical dependence is a risk associated with long-term use, even at therapeutic doses. The withdrawal syndrome is mild at low doses. Continued self-administration of low therapeutic doses is maintained to alleviate withdrawal symptoms. The advances in the recent understanding of the molecular biology of the benzodiazepine receptor gives hope to the development of new anxiolytic compounds with less dependence liability than the present ones.
苯二氮䓬类药物是最安全、最有效的药物之一,具有所有可滥用化合物的特征。尽管不同化合物之间似乎存在效力差异,个体之间的敏感性也有所不同,但苯二氮䓬类药物具有明显的强化特性。对苯二氮䓬类药物的抑制作用耐受性发展迅速,但对其抗焦虑作用的耐受性发展缓慢且程度有限。尽管滥用者使用非常高的剂量,但大多数长期使用者的每日剂量仍维持在低治疗范围内(10 - 20毫克地西泮或其等效剂量),且剂量没有增加。即使在治疗剂量下,身体依赖也是长期使用相关的风险。低剂量时戒断综合征较轻。持续自我服用低治疗剂量是为了缓解戒断症状。最近对苯二氮䓬受体分子生物学的认识进展为开发比现有药物依赖性更小的新型抗焦虑化合物带来了希望。