Abstract:
:Ethanol aggravates benzodiazepine-induced central nervous depression by pharmacokinetic and/or pharmacodynamic interactions and Ro 15-1788 reverses promptly the hypnotic effects of benzodiazepines. We therefore studied the acute effects of Ro 15-1788 on the ethanol-induced sedation in six healthy male subjects. Subsequently to an oral loading dose (0.54 g ethanol kg-1) ethanol was infused for 4 h (0.15 g ethanol kg-1 h-1) and steady state blood levels between 0.9 to 1.2 g l-1 were reached within 2 h. At steady state and during the elimination phase of ethanol an intravenous bolus of 0.5 mg Ro 15-1788 or placebo was administered in a randomized, double-blind crossover fashion. The marked sedative effects of ethanol as assessed by visual analogue scales (2 to 6 fold increase in the sedation index), and choice reaction time (25 to 40% prolongation) were not affected by Ro 15-1788. However, the pharmaco-EEG indicated that Ro 15-1788 seems to reverse transiently the ethanol-induced changes in total alpha, delta, and slow alpha bands. There was no pharmacokinetic interaction between both agents since elimination of Ro 15-1788 (t1/2 = 1.2 +/- 0.7 h) and of ethanol (0.17 +/- 0.02 g l-1 h-1) were in good agreement with control values. Thus, it could be concluded that Ro 15-1788 might affect for a short while the action of ethanol by interfering with the benzodiazepine receptors.
journal_name
Br J Clin Pharmacoljournal_title
British journal of clinical pharmacologyauthors
Klotz U,Ziegler G,Rosenkranz B,Mikus Gdoi
10.1111/j.1365-2125.1986.tb02929.xsubject
Has Abstractpub_date
1986-11-01 00:00:00pages
513-20issue
5eissn
0306-5251issn
1365-2125journal_volume
22pub_type
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journal_title:British journal of clinical pharmacology
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journal_title:British journal of clinical pharmacology
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journal_title:British journal of clinical pharmacology
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doi:10.1111/j.1365-2125.1986.tb05199.x
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pub_type: 临床试验,杂志文章
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journal_title:British journal of clinical pharmacology
pub_type: 杂志文章,多中心研究
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pub_type: 临床试验,杂志文章,随机对照试验
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pub_type: 临床试验,杂志文章
doi:10.1111/j.1365-2125.1982.tb01870.x
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pub_type: 临床试验,杂志文章,随机对照试验
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journal_title:British journal of clinical pharmacology
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pub_type: 临床试验,杂志文章,随机对照试验
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journal_title:British journal of clinical pharmacology
pub_type: 临床试验,杂志文章,随机对照试验
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journal_title:British journal of clinical pharmacology
pub_type: 临床试验,杂志文章,随机对照试验
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