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莫比可抑制白三烯释放:一种可能的临床优势。

Inhibition of leukotriene release by mofebutazone: a possible clinical advantage.

作者信息

Khayyal M T, el-Khatib A S, el-Ghazaly M, Hatem A

机构信息

Department of Pharmacology, Faculty of Pharmacy Cairo University, Egypt.

出版信息

Int J Clin Pharmacol Res. 1993;13(5):255-61.

PMID:8200720
Abstract

The isolated perfused lung preparation from actively sensitized guinea-pigs was used; after it was challenged with antigen, mediators such as histamine, prostaglandins and leukotrienes were released into the lung effluent. It was found that treatment of the perfused lungs before and during challenge with mofebutazone (10 micrograms/ml) inhibited the immunological release of prostaglandins as well as leukotrienes. Phenylbutazone, on the other hand, at the same dose level inhibited the release of prostaglandins, whereas the release of leukotrienes was much less affected by the drug. Histamine release was not altered by either drug. When clinically mofebutazone tablets (300 mg) were given as an analgesic twice daily for 15 days to a number of asthmatic volunteers including 3 aspirin-sensitive individuals, there was no increase in the incidence or intensity of the asthmatic attacks, even in the aspirin-sensitive patients. Pulmonary ventilatory functions which showed a certain obstructive pattern were not worsened by the treatment and even tended to be somewhat improved.

摘要

使用来自主动致敏豚鼠的离体灌流肺制备物;在用抗原攻击后,组胺、前列腺素和白三烯等介质释放到肺流出物中。发现用莫比丁酮(10微克/毫升)在攻击前和攻击期间处理灌流肺,可抑制前列腺素以及白三烯的免疫释放。另一方面,保泰松在相同剂量水平下抑制前列腺素的释放,而白三烯的释放受该药物的影响小得多。两种药物均未改变组胺的释放。当给包括3名阿司匹林敏感个体在内的多名哮喘志愿者每天两次服用临床剂量的莫比丁酮片(300毫克)作为镇痛药,持续15天时,即使在阿司匹林敏感患者中,哮喘发作的发生率或严重程度也没有增加。显示出一定阻塞模式的肺通气功能并未因治疗而恶化,甚至有改善的趋势。

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