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两种异构体麻黄碱和曲普利啶对人体中枢神经系统的影响及其相互作用。

Effects on the human central nervous system of two isomers of ephedrine and triprolidine, and their interaction.

机构信息

Department of Clinical Pharmacology, Wellcome Research Laboratories, Langley Court, Beckenham, Kent.

出版信息

Br J Clin Pharmacol. 1974 Feb;1(1):71-8. doi: 10.1111/j.1365-2125.1974.tb00209.x.

DOI:10.1111/j.1365-2125.1974.tb00209.x
PMID:22454872
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1402412/
Abstract

1 D(-)ephedrine is four times as potent as L(+)pseudoephedrine in producing both tachycardia and a rise in systolic blood pressure. No changes in diastolic blood pressure occurred in 12 subjects with doses of up to D(-)ephedrine (50 mg) and L(+)pseudoephedrine (180 mg). 2 Significant evidence of stimulation of the central nervous system occurred only after D(-)ephedrine in that tapping rates were increased and subjects could reliably detect that they had received an active drug. While mean performance rates in an auditory vigilance test were higher following both ephedrine isomers these changes were not significant. 3 Impairment of both tapping rates and auditory vigilance occurred following triprolidine in another group of 12 subjects. The effect was generally related to dose of antihistamine given and lasted up to 7.25 hours. Subjective effects were reliably recognized by subjects following all treatments containing triprolidine (2.5 mg or more) for up to 4.75 hours. Using analogue lines for self rating the subjective effects following triprolidine indicated both mental and physical impairment differing significantly from scores after lactose and L(+)pseudoephedrine (60 mg). 4 Combination of triprolidine (2.5 mg) and L(+)pseudoephedrine (60 mg) produced effects similar to triprolidine alone on both subjective measures and the auditory vigilance test. It is suggested that these objective tests and subjective scales could be used to measure effects on the central nervous system produced by antihistamines together with similar drugs, and their interaction with other compounds administered concurrently.

摘要

1 D(-)麻黄碱在引起心动过速和收缩压升高方面的效力是 L(+)伪麻黄碱的四倍。在 12 名受试者中,给予 D(-)麻黄碱(50mg)和 L(+)伪麻黄碱(180mg)的剂量高达 D(-)麻黄碱时,舒张压没有变化。

2 只有在给予 D(-)麻黄碱后,中枢神经系统才会受到明显的刺激,因为敲击率增加,并且受试者可以可靠地检测到他们已经接受了活性药物。虽然在听觉警戒测试中,两种麻黄碱异构体的平均表现率更高,但这些变化并不显著。

3 在另一组 12 名受试者中,给予曲普利啶后,敲击率和听觉警戒均受到损害。这种影响通常与给予的抗组胺药剂量有关,持续时间长达 7.25 小时。在服用含有曲普利啶(2.5mg 或更多)的所有药物长达 4.75 小时后,受试者可靠地识别出了所有的主观效应。使用模拟线进行自我评分,曲普利啶引起的主观效应表明,精神和身体损害与乳糖和 L(+)伪麻黄碱(60mg)后的评分有显著差异。

4 曲普利啶(2.5mg)和 L(+)伪麻黄碱(60mg)的联合使用对主观测量和听觉警戒测试的影响与曲普利啶单独使用相似。因此,这些客观测试和主观量表可以用于测量抗组胺药与其他类似药物联合使用对中枢神经系统的影响,以及它们与同时给予的其他化合物的相互作用。

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本文引用的文献

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A PHARMACOLOGICAL STUDY OF THE EPHEDRINE ISOMERS.麻黄碱异构体的药理学研究
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Some neuropharmacological properties of the ephedrine isomers.麻黄碱异构体的一些神经药理学特性。
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