健康受试者静脉注射和口服布罗替唑仑后的药代动力学
Pharmacokinetics of brotizolam in healthy subjects following intravenous and oral administration.
作者信息
Jochemsen R, Wesselman J G, Hermans J, van Boxtel C J, Breimer D D
出版信息
Br J Clin Pharmacol. 1983;16 Suppl 2(Suppl 2):285S-290S. doi: 10.1111/j.1365-2125.1983.tb02302.x.
Abstract
Pharmacokinetics and bioavailability of brotizolam after i.v. and oral administration were studied in healthy young volunteers. Kinetic parameters after i.v. administration were: volume of distribution 0.66 +/- 0.19 1/kg, total plasma clearance 113 +/- 28 ml/min, distribution half-life 11 +/- 6 min, and elimination half-life 4.8 +/- 1.4 h (mean values +/- s.d.). Kinetic parameters after oral administration were: absorption lag-time 8 +/- 12 min, absorption half-life 10 +/- 11 min, and elimination half-life 5.1 +/- 1.2 h (mean values +/- s.d.). Bioavailability of brotizolam was 70 +/- 22% when calculated by comparing oral and intravenous area-under-curve values, corrected for intra-individual half-life differences. An alternative calculation method, which is relatively independent of large clearance variations, provided a bioavailability of 70 +/- 24% (range: 47-117%).
摘要
在健康年轻志愿者中研究了静脉注射和口服布替唑仑后的药代动力学和生物利用度。静脉注射后的动力学参数为：分布容积0.66±0.19升/千克，总血浆清除率113±28毫升/分钟，分布半衰期11±6分钟，消除半衰期4.8±1.4小时（均值±标准差）。口服后的动力学参数为：吸收滞后时间8±12分钟，吸收半衰期10±11分钟，消除半衰期5.1±1.2小时（均值±标准差）。通过比较口服和静脉注射的曲线下面积值并校正个体内半衰期差异来计算，布替唑仑的生物利用度为70±22%。一种相对独立于较大清除率变化的替代计算方法得出的生物利用度为70±24%（范围：47 - 117%）。
相似文献
1
Pharmacokinetics of brotizolam in healthy subjects following intravenous and oral administration.健康受试者静脉注射和口服布罗替唑仑后的药代动力学
Br J Clin Pharmacol. 1983;16 Suppl 2(Suppl 2):285S-290S. doi: 10.1111/j.1365-2125.1983.tb02302.x.
2
Pharmacokinetics of brotizolam in the elderly.溴替唑仑在老年人中的药代动力学。
Br J Clin Pharmacol. 1983;16 Suppl 2(Suppl 2):299S-307S. doi: 10.1111/j.1365-2125.1983.tb02304.x.
3
Comparative pharmacokinetics of brotizolam and triazolam in healthy subjects.健康受试者中溴替唑仑和三唑仑的比较药代动力学
Br J Clin Pharmacol. 1983;16 Suppl 2(Suppl 2):291S-297S. doi: 10.1111/j.1365-2125.1983.tb02303.x.
4
Pharmacokinetics and metabolism of brotizolam in humans.溴替唑仑在人体中的药代动力学与代谢
Br J Clin Pharmacol. 1983;16 Suppl 2(Suppl 2):279S-283S. doi: 10.1111/j.1365-2125.1983.tb02301.x.
5
Pharmacokinetics of oral brotizolam in patients with liver cirrhosis.肝硬化患者口服溴替唑仑的药代动力学
Br J Clin Pharmacol. 1983;16 Suppl 2(Suppl 2):315S-322S. doi: 10.1111/j.1365-2125.1983.tb02306.x.
6
Pharmacokinetics of brotizolam in renal failure.溴替唑仑在肾衰竭中的药代动力学。
Br J Clin Pharmacol. 1983;16 Suppl 2(Suppl 2):309S-313S. doi: 10.1111/j.1365-2125.1983.tb02305.x.
7
Pharmacokinetics and metabolism of brotizolam in animals.溴替唑仑在动物体内的药代动力学与代谢
Br J Clin Pharmacol. 1983;16 Suppl 2(Suppl 2):261S-266S. doi: 10.1111/j.1365-2125.1983.tb02298.x.
8
Pilot pharmacokinetic study of brotizolam, a thienodiazepine hypnotic, using electron-capture gas-liquid chromatography.使用电子捕获气液色谱法对噻吩二氮卓类催眠药溴替唑仑进行的初步药代动力学研究。
Sleep. 1983;6(1):72-6. doi: 10.1093/sleep/6.1.72.
9
Inhibition of the metabolism of brotizolam by erythromycin in humans: in vivo evidence for the involvement of CYP3A4 in brotizolam metabolism.红霉素对人体中溴替唑仑代谢的抑制作用：CYP3A4参与溴替唑仑代谢的体内证据。
Br J Clin Pharmacol. 2005 Aug;60(2):172-5. doi: 10.1111/j.1365-2125.2005.02380.x.
10
Elimination of brotizolam in elderly patients after multiple doses.多次给药后老年患者中溴替唑仑的消除情况。
Eur J Clin Pharmacol. 1986;31(2):243-5. doi: 10.1007/BF00606668.
引用本文的文献
1
An explorative approach to understanding individual differences in driving performance and neurocognition in long-term benzodiazepine users.探索长期使用苯二氮䓬类药物的个体在驾驶表现和神经认知方面差异的方法。
Hum Psychopharmacol. 2021 Jul;36(4):e2778. doi: 10.1002/hup.2778. Epub 2021 Feb 6.
2
Effect of itraconazole on the pharmacokinetics and pharmacodynamics of a single oral dose of brotizolam.伊曲康唑对单次口服剂量溴替唑仑药代动力学和药效学的影响。
Br J Clin Pharmacol. 2004 Nov;58(5):476-81. doi: 10.1111/j.1365-2125.2004.02208.x.
3
Pharmacokinetics of oral brotizolam in patients with liver cirrhosis.肝硬化患者口服溴替唑仑的药代动力学
Br J Clin Pharmacol. 1983;16 Suppl 2(Suppl 2):315S-322S. doi: 10.1111/j.1365-2125.1983.tb02306.x.
4
Pharmacokinetics of brotizolam in the elderly.溴替唑仑在老年人中的药代动力学。
Br J Clin Pharmacol. 1983;16 Suppl 2(Suppl 2):299S-307S. doi: 10.1111/j.1365-2125.1983.tb02304.x.
5
Brotizolam as a pre-operative hypnotic.溴替唑仑作为术前催眠药。
Br J Clin Pharmacol. 1983;16 Suppl 2(Suppl 2):419S-423S. doi: 10.1111/j.1365-2125.1983.tb02322.x.
6
Comparative studies on the efficacy of brotizolam and nitrazepam: a multi-centre study.溴替唑仑与硝西泮疗效的比较研究：一项多中心研究。
Br J Clin Pharmacol. 1983;16 Suppl 2(Suppl 2):403S-406S. doi: 10.1111/j.1365-2125.1983.tb02317.x.
7
Efficacy and tolerance: comparative studies with brotizolam and flunitrazepam.疗效与耐受性：溴替唑仑与氟硝西泮的对比研究。
Br J Clin Pharmacol. 1983;16 Suppl 2(Suppl 2):397S-401S. doi: 10.1111/j.1365-2125.1983.tb02316.x.
8
Tolerance studies with brotizolam in hospitalized patients.住院患者中溴替唑仑的耐受性研究。
Br J Clin Pharmacol. 1983;16 Suppl 2(Suppl 2):385S-389S. doi: 10.1111/j.1365-2125.1983.tb02314.x.
9
Comparative pharmacokinetics of brotizolam and triazolam in healthy subjects.健康受试者中溴替唑仑和三唑仑的比较药代动力学
Br J Clin Pharmacol. 1983;16 Suppl 2(Suppl 2):291S-297S. doi: 10.1111/j.1365-2125.1983.tb02303.x.
10
Kinetic and dynamic interaction of brotizolam and ethanol.溴替唑仑与乙醇的动力学和动态相互作用。
Br J Clin Pharmacol. 1986 Feb;21(2):197-204. doi: 10.1111/j.1365-2125.1986.tb05175.x.
本文引用的文献
1
Studies on sleep and performance with a triazolo-1, 4-thienodiazepine (brotizolam).关于三唑并-1,4-噻二氮䓬（溴替唑仑）对睡眠及工作表现影响的研究。
Br J Clin Pharmacol. 1980 Jul;10(1):75-81. doi: 10.1111/j.1365-2125.1980.tb00504.x.
2
Diazepam disposition determinants.地西泮处置的决定因素。
Clin Pharmacol Ther. 1980 Mar;27(3):301-12. doi: 10.1038/clpt.1980.40.
3
Disposition of intravenous diazepam in young men and women.静脉注射地西泮在年轻男性和女性中的处置情况。
Eur J Clin Pharmacol. 1981;20(3):207-13. doi: 10.1007/BF00544599.
4
[Pharmacokinetics of midazolam after i.v. administration (author's transl)].静脉注射咪达唑仑后的药代动力学（作者译）
Arzneimittelforschung. 1981;31(12a):2202-5.
5
Pharmacokinetics and bioavailability of intravenous, oral, and rectal nitrazepam in humans.硝西泮在人体中的静脉注射、口服及直肠给药的药代动力学和生物利用度
J Pharmacokinet Biopharm. 1982 Jun;10(3):231-45. doi: 10.1007/BF01059259.
6
Comparative pharmacokinetics of brotizolam and triazolam in healthy subjects.健康受试者中溴替唑仑和三唑仑的比较药代动力学
Br J Clin Pharmacol. 1983;16 Suppl 2(Suppl 2):291S-297S. doi: 10.1111/j.1365-2125.1983.tb02303.x.
7
Effect of age and gender on disposition of temazepam.
J Pharm Sci. 1981 Oct;70(10):1104-7. doi: 10.1002/jps.2600701004.
8
Triazolam: a review of its pharmacological properties and therapeutic efficacy in patients with insomnia.三唑仑：失眠患者的药理特性及治疗效果综述
Drugs. 1981 Aug;22(2):81-110. doi: 10.2165/00003495-198122020-00001.
9
Automated gas chromatography for studies of midazolam pharmacokinetics.用于咪达唑仑药代动力学研究的自动气相色谱法。
Anesthesiology. 1981 Aug;55(2):176-9. doi: 10.1097/00000542-198108000-00014.
10
Assay of triazolam in plasma by capillary gas chromatography.采用毛细管气相色谱法测定血浆中三唑仑的含量。
J Chromatogr. 1981 May 8;223(2):438-44. doi: 10.1016/s0378-4347(00)80119-x.
Zotero 插件