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地西泮在成年癫痫患者中静脉注射、口服及直肠给药后的生物利用度。

Bioavailability of diazepam after intravenous, oral and rectal administration in adult epileptic patients.

作者信息

Dhillon S, Oxley J, Richens A

出版信息

Br J Clin Pharmacol. 1982 Mar;13(3):427-32. doi: 10.1111/j.1365-2125.1982.tb01397.x.

Abstract

1 The absorption of single doses of diazepam in six adult epileptic subjects following intravenous, oral and rectal administration were studied in order to evaluate the usefulness of the latter in emergency situations in the adult. 2 Diazepam tablets (Valium, Roche) and rectal solution (Valium solution for intravenous administration) produced similar peak serum concentrations after delays of 15-90 min. 3 Two suppository formulations showed statistically significant differences in absorption characteristics. 4 Serum diazepam levels above 400 ng ml-1 (suggested to be necessary for a satisfactory anticonvulsant effect) were reached in only a few subjects after rectal doses of 10-20 mg of solution, and then usually after a delay of over 2 h.

摘要
  1. 为评估直肠给药在成人紧急情况下的有效性,研究了六名成年癫痫患者静脉注射、口服和直肠给药后单剂量地西泮的吸收情况。2. 地西泮片(安定,罗氏公司)和直肠溶液(静脉注射用安定溶液)在延迟15 - 90分钟后产生相似的血清峰值浓度。3. 两种栓剂制剂在吸收特性上显示出统计学上的显著差异。4. 直肠给予10 - 20毫克溶液后,只有少数受试者的血清地西泮水平达到400纳克/毫升以上(据认为这是获得满意抗惊厥效果所必需的),而且通常是在延迟超过2小时之后。

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本文引用的文献

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Benzodiazepines in the treatment of epilepsy. A review.
Epilepsia. 1973 Sep;14(3):277-310. doi: 10.1111/j.1528-1157.1973.tb03965.x.
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Plasma levels of diazepam after parenteral and rectal administration in children.
Epilepsia. 1975 Jun;16(2):277-83. doi: 10.1111/j.1528-1157.1975.tb06058.x.
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Plasma diazepam levels after single dose oral and intramuscular administration.
Anaesthesia. 1975 Mar;30(2):164-9. doi: 10.1111/j.1365-2044.1975.tb00828.x.
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Blood levels of diazepam after single rectal administration in infants and children.
J Pediatr. 1978 Dec;93(6):1039-41. doi: 10.1016/s0022-3476(78)81254-2.

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