Swift C G, Swift M R, Hamley J, Stevenson I H, Crooks J
Age Ageing. 1984 Nov;13(6):335-43. doi: 10.1093/ageing/13.6.335.
The outcome of long-term benzodiazepine hypnotic therapy has been investigated in a group of elderly patients in the community; 220 receiving nitrazepam and 33 flurazepam. The estimated duration of therapy was as long as 15 years in some cases. More than half were taking doses greater than 5 mg and 15 mg, respectively, the majority on a regular nightly basis in accordance with the instructions on containers. The plasma concentrations of nitrazepam and the active desalkyl metabolite of flurazepam correlated positively with weight-related dose. In the case of desalkyl-flurazepam, but not nitrazepam, the levels were substantially higher than those previously reported in young individuals. There was sustained patient satisfaction with the effectiveness of the hypnotics and, despite the high plasma levels, little subjective or objective evidence of unwanted sedation, confusion or unsteadiness. The findings of the survey suggest the development of both pharmacodynamic tolerance to the unwanted sedative effects of these drugs and a degree of dependence in long-term recipients.
对一组社区老年患者进行了长期苯二氮䓬类催眠药治疗效果的调查；220人服用硝西泮，33人服用氟西泮。在某些情况下，估计治疗持续时间长达15年。超过一半的患者分别服用剂量大于5毫克和15毫克的药物，大多数患者按照药品包装说明每晚规律服药。硝西泮的血浆浓度以及氟西泮的活性去烷基代谢物浓度与体重相关剂量呈正相关。就去烷基氟西泮而言，而非硝西泮，其血药浓度显著高于此前报道的年轻人的血药浓度。患者对催眠药的有效性持续满意，尽管血药浓度较高，但几乎没有主观或客观证据表明存在不必要的镇静、意识模糊或步态不稳。该调查结果表明，长期服用这些药物的患者对其不良镇静作用产生了药效学耐受性，并出现了一定程度的依赖性。
