Hollister L E, Conley F K, Britt R H, Shuer L
JAMA. 1981 Oct 2;246(14):1568-70.
Plasma concentrations of diazepam and its major active metabolite nordiazepam were measured in 108 neurosurgical patients taking diazepam in doses of 5 to 40 mg/day for periods from one month to 16 years. Diazepam was used for relief of pain or muscle spasm, or anxiety and sleeplessness associated with these two symptoms, and was considered to be beneficial by 83% of the patients, although use of other drugs confounded this evaluation. Concentrations of total diazepam-nordiazepam ranged from 0 to 2,584 ng/mL, with nordiazepam being the predominant metabolite. "Low" concentrations (less than 250 ng/mL) were found in 35 of the 108 patients, with 19 having concentrations lower than 100 ng/mL. "High" concentrations (greater than 900 ng/mL) were found in 20 patients and did not occur more frequently than in other studies of long-term diazepam ingestion. Even with long-term use, diazepam seemed to retain its efficacy and did not lead to any clear-cut abuse.
对108例神经外科患者的血浆地西泮及其主要活性代谢产物去甲地西泮浓度进行了测定,这些患者服用地西泮的剂量为5至40毫克/天,服用时间从1个月至16年不等。地西泮用于缓解疼痛或肌肉痉挛,或与这两种症状相关的焦虑和失眠,83%的患者认为其有益,尽管使用其他药物使这一评估受到干扰。地西泮-去甲地西泮的总浓度范围为0至2584纳克/毫升,其中去甲地西泮是主要代谢产物。108例患者中有35例的浓度为“低”(低于250纳克/毫升),其中19例浓度低于100纳克/毫升。20例患者的浓度为“高”(高于900纳克/毫升),其发生频率并不高于其他长期服用地西泮的研究。即使长期使用,地西泮似乎仍保持其疗效,且未导致任何明显的滥用情况。