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癫痫患儿中司可巴比妥的直肠吸收与处置

Rectal absorption and disposition of secobarbital in epileptic children.

作者信息

Levine H L, Cohen M E, Duffner P K, Lacey D J, Karpynec R, Shen D D

出版信息

Pediatr Pharmacol (New York). 1982;2(1):33-8.

PMID:7110754
Abstract

The absorption and disposition of rectally administered secobarbital was studied in ten epileptic children, ages 2-13 yrs. Five subjects received secobarbital rectally in solution, and the other five received secobarbital suppositories. Concentration of secobarbital in serum was serially determined during 48 hrs after a single rectal dose of about 5 mg/kg. The rate of absorption of secobarbital, as measured by the time to reach peak serum concentration, was much more rapid from the solution than the suppository (0.92 +/- 0.47 hr vs 4.60 +/ 2.30 hr). The peak serum concentration of secobarbital in the solution group was consistently higher than in the suppository group (2.26 +/- 0.37 micrograms/ml vs 1.35 +/- 0.24 microgram/ml). None of the individual peak serum concentrations exceeded 3 micrograms/ml, which is well below the previously reported minimum toxic concentration of secobarbital (ie, 6 microgram/ml). The elimination half-life of secobarbital varied over a wide range, from 2.7 to 13.5 hr, and is, on the average, shorter than estimates previously reported for adult volunteers or poly-drug abusers. Also, the mean elimination half-life did not differ between the solution and the suppository groups. The extent of rectal absorption of secobarbital, as assessed by the area under the serum concentration time curve, was not significantly different between the solution and the suppository treatments. If rectal secobarbital is considered for treatment of prolonged seizure, a rectal solution may offer a more rapid and consistent onset of action than with the suppository preparation.

摘要

对10名年龄在2至13岁的癫痫儿童进行了直肠给药速可巴比妥的吸收和处置研究。5名受试者接受了速可巴比妥溶液直肠给药,另外5名接受了速可巴比妥栓剂给药。在单次直肠给予约5mg/kg剂量后的48小时内,连续测定血清中速可巴比妥的浓度。以达到血清峰值浓度的时间来衡量,速可巴比妥从溶液中的吸收速度比栓剂快得多(0.92±0.47小时对4.60±2.30小时)。溶液组中速可巴比妥的血清峰值浓度始终高于栓剂组(2.26±0.37微克/毫升对1.35±0.24微克/毫升)。个体血清峰值浓度均未超过3微克/毫升,远低于先前报道的速可巴比妥最低中毒浓度(即6微克/毫升)。速可巴比妥的消除半衰期在2.7至13.5小时的范围内变化很大,平均而言,比先前报道的成年志愿者或多药滥用者的估计值要短。此外,溶液组和栓剂组之间的平均消除半衰期没有差异。以血清浓度-时间曲线下面积评估,速可巴比妥的直肠吸收程度在溶液和栓剂治疗之间没有显著差异。如果考虑用直肠速可巴比妥治疗癫痫持续状态,直肠溶液可能比栓剂制剂起效更快且更一致。

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