Robinson G M, Sellers E M, Janecek E
Clin Pharmacol Ther. 1981 Jul;30(1):71-6. doi: 10.1038/clpt.1981.129.
Although intravenous phenobarbital loading is effective in barbiturate withdrawal, controlled infusions of a drug are inconvenient. To develop a practical and more widely applicable method, oral loading doses of phenobarbital were given to 21 barbiturate addicts, whose estimated mean daily intake of barbiturates was 1 gm (range 0.5 to 4 gm). Twelve had a past or present history of barbiturate withdrawal seizures. Phenobarbital was given orally at a rate of 120 mg/hr until a predetermined clinical end point of phenobarbital effect was achieved. This end point was the presence of at least three of the following: nystagmus, drowsiness, ataxia, dysarthria, or emotional lability. The total phenobarbital loading dose (mean +/- SD) was 23.4 +/- 7.1 mg/kg, median phenobarbital concentration after loading was 35.9 mg/l (range 13.2 to 71.6 mg/l), and median half-life (t 1/2) of phenobarbital was 90 hr (range 38 to 240 hr). One patient with t 1/2 = 38 hr was given supplemental doses of phenobarbital. None developed seizures or other evidence of barbiturate withdrawal.
尽管静脉注射苯巴比妥负荷剂量对巴比妥类药物戒断有效,但药物的控制性输注并不方便。为了开发一种实用且更广泛适用的方法,对21名巴比妥类药物成瘾者给予口服苯巴比妥负荷剂量,这些成瘾者估计每日巴比妥类药物摄入量平均为1克(范围为0.5至4克)。其中12人有巴比妥类药物戒断性癫痫发作的既往史或现病史。以120毫克/小时的速率口服给予苯巴比妥,直到达到苯巴比妥效应的预定临床终点。该终点为至少出现以下三种情况:眼球震颤、嗜睡、共济失调、构音障碍或情绪不稳定。苯巴比妥总负荷剂量(平均值±标准差)为23.4±7.1毫克/千克,负荷后苯巴比妥浓度中位数为35.9毫克/升(范围为13.2至71.6毫克/升),苯巴比妥的半衰期(t1/2)中位数为90小时(范围为38至240小时)。一名t1/2 = 38小时的患者给予了苯巴比妥补充剂量。无一例出现癫痫发作或巴比妥类药物戒断的其他证据。