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曲普利啶与赛克利嗪对人体组胺(H1)拮抗作用、主观效应及性能测试的比较。

A comparison of triprolidine and cyclizine on histamine (H1) antagonism, subjective effects and performance tests in man.

作者信息

Hamilton M, Bush M, Bye C, Peck A W

出版信息

Br J Clin Pharmacol. 1982 Mar;13(3):441-4. doi: 10.1111/j.1365-2125.1982.tb01399.x.

DOI:10.1111/j.1365-2125.1982.tb01399.x
PMID:6120718
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1402101/
Abstract

1 The effects of triprolidine and cyclizine on the histamine skin response, performance tests and subjective effects were examined in a controlled, double-blind study in eight healthy volunteers. 2 Triprolidine was considerably more potent that cyclizine in inhibiting the skin response to histamine. Significant inhibition of flare size occurred at 1, 2 an 4 h after triprolidine 2.5 mg. A smaller but significant reduction occurred at 2 and 4 h after cyclizine 100 mg but not after the 50 mg dose. 3 Cyclizine 100 mg produced a significant increase in reaction time at 4.5 h compared with lactose. Smaller though non significant increases followed triprolidine and cyclizine 50 mg. 4 Subjective effects were seen only after cyclizine 100 mg when subjects were significantly more drowsy, feeble, muzzy, lethargic and dreamy than after lactose dummy. No significant changes followed triprolidine 2.5 mg or cyclizine 50 mg. 5 It was concluded that while cyclizine has antihistamine properties, these are weak compared with triprolidine, and are not seen with doses sufficiently low to avoid central nervous system impairment.

摘要
  1. 在一项针对8名健康志愿者的对照双盲研究中,考察了曲普利啶和赛克利嗪对组胺皮肤反应、性能测试及主观效应的影响。2. 曲普利啶在抑制皮肤对组胺的反应方面比赛克利嗪效力强得多。2.5毫克曲普利啶给药后1小时、2小时和4小时,光斑大小出现显著抑制。100毫克赛克利嗪给药后2小时和4小时光斑大小有较小但显著的减小,但50毫克剂量给药后未出现此现象。3. 与乳糖相比,100毫克赛克利嗪在4.5小时时使反应时间显著延长。50毫克曲普利啶和50毫克赛克利嗪给药后反应时间虽有较小延长但不显著。4. 仅在给予100毫克赛克利嗪后出现主观效应,此时受试者比服用乳糖安慰剂后明显更困倦、虚弱、迷糊、慵懒和多梦。2.5毫克曲普利啶或50毫克赛克利嗪给药后未出现显著变化。5. 得出的结论是,虽然赛克利嗪具有抗组胺特性,但与曲普利啶相比这些特性较弱,且在剂量足够低以避免中枢神经系统损害时未观察到这些特性。

相似文献

1
A comparison of triprolidine and cyclizine on histamine (H1) antagonism, subjective effects and performance tests in man.曲普利啶与赛克利嗪对人体组胺(H1)拮抗作用、主观效应及性能测试的比较。
Br J Clin Pharmacol. 1982 Mar;13(3):441-4. doi: 10.1111/j.1365-2125.1982.tb01399.x.
2
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Eur J Clin Pharmacol. 1975 Aug 14;8(6):455-63. doi: 10.1007/BF00562321.
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Clin Pharmacol Ther. 1985 Oct;38(4):381-6. doi: 10.1038/clpt.1985.191.
5
Effects of two antihistamine drugs on actual driving performance.两种抗组胺药物对实际驾驶性能的影响。
Br Med J (Clin Res Ed). 1984 Jan 28;288(6413):281-2. doi: 10.1136/bmj.288.6413.281.
6
Effect of the antihistamines, brompheniramine maleate and triprolidine hydrochloride, on performance in man.抗组胺药马来酸溴苯那敏和盐酸曲普利啶对人体行为表现的影响。
Br J Clin Pharmacol. 1979 Oct;8(4):321-4. doi: 10.1111/j.1365-2125.1979.tb04712.x.
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Performance studies with the H1-histamine receptor antagonists, astemizole and terfenadine.使用H1组胺受体拮抗剂阿司咪唑和特非那定的性能研究。
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Effects of triprolidine and dipipanone in the cold induced pain test, and the central nervous system of healthy volunteers.曲普利啶和二苯哌己酮在冷诱导疼痛试验中的作用以及对健康志愿者中枢神经系统的影响。
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The effects of single and repeated administration of ebastine on cognition and psychomotor performance in comparison to triprolidine and placebo in healthy volunteers.与曲普利啶和安慰剂相比,依巴斯汀单次及重复给药对健康志愿者认知和精神运动表现的影响。
Curr Med Res Opin. 2001;17(4):273-81.
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Br J Clin Pharmacol. 1993 Jul;36(1):67-70. doi: 10.1111/j.1365-2125.1993.tb05894.x.

引用本文的文献

1
Effects of triprolidine and dipipanone in the cold induced pain test, and the central nervous system of healthy volunteers.曲普利啶和二苯哌己酮在冷诱导疼痛试验中的作用以及对健康志愿者中枢神经系统的影响。
Br J Clin Pharmacol. 1987 Jul;24(1):43-50. doi: 10.1111/j.1365-2125.1987.tb03134.x.
2
Behavioural effects of histamine and its antagonists: a review.组胺及其拮抗剂的行为效应:综述
Psychopharmacology (Berl). 1988;95(1):1-14. doi: 10.1007/BF00212757.

本文引用的文献

1
Pharmacologic properties of cyclizine hydrochloride (marezine).盐酸赛克利嗪(晕海宁)的药理特性
J Pharmacol Exp Ther. 1954 Nov;112(3):297-305.
2
The action of sedatives on brain stem oculomotor systems in man.镇静剂对人类脑干动眼系统的作用。
Neuropharmacology. 1971 Mar;10(21):181-91. doi: 10.1016/0028-3908(71)90039-6.
3
The effects of nitrous oxide on the human auditory evoked response.氧化亚氮对人体听觉诱发反应的影响。
Psychopharmacologia. 1969;16(2):115-27. doi: 10.1007/BF00403614.
4
(--)-Hyoscine and cyclizine as motion sickness remedies.(-)-东莨菪碱和茶苯海明作为晕动病治疗药物。
Br J Pharmacol Chemother. 1967 Aug;30(3):463-9. doi: 10.1111/j.1476-5381.1967.tb02152.x.
5
The evaluation of histamine antagonists in man.组胺拮抗剂在人体中的评估。
Eur J Clin Pharmacol. 1971 Sep;3(4):215-20. doi: 10.1007/BF00565009.
6
A comparison of triprolidine and clemastine on histamine antagonism and performance tests in man: implications for the mechanism of drug induced drowsiness.曲普利啶与氯马斯汀对人体组胺拮抗作用及行为测试的比较:对药物所致嗜睡机制的启示
Eur J Clin Pharmacol. 1975 Aug 14;8(6):455-63. doi: 10.1007/BF00562321.
7
Two doses of triprolidine for treatment of allergic rhinitis.两剂曲普利啶治疗变应性鼻炎。
Ann Allergy. 1979 May;42(5):330-2.