Bauer V, Buran L, Babul'ová A
Institute of Experimental Pharmacology, Slovak Academy of Sciences, Bratislava, Czechoslovakia.
Arch Int Pharmacodyn Ther. 1990 Mar-Apr;304:232-46.
The effect of stobadine on respiratory smooth muscles, blood pressure, heart rate and gastric acid secretion was studied and compared with the action of other antihistamines in vivo. Stobadine, as diphenhydramine, dithiadene and promethazine, but in contrast to cimetidine and ranitidine, prevented histamine from producing bronchospasm both after i.v. and oral administration. Based on the potency of its pharmacological action, diphenhydramine had a lower bioavailability after oral administration than the other antihistamines. Both cimetidine and ranitidine reduced the gastric acid secretion while stobadine was ineffective in this respect. None of the drugs studied antagonized histamine in reducing blood pressure, but all of them, with exception of promethazine and diphenhydramine, reduced mean arterial blood pressure. The results suggest that the action of stobadine on the respiratory and vascular smooth muscle effects is intermediate between that of diphenhydramine and dithiadene. In view of the minimal effect of stobadine on gastric acid secretion and its marked activity on airways, it is concluded that this drug predominantly acts on H1-receptors.
研究了司他定对呼吸道平滑肌、血压、心率和胃酸分泌的影响，并在体内将其与其他抗组胺药的作用进行了比较。司他定与苯海拉明、二硫氮卓和异丙嗪一样，但与西咪替丁和雷尼替丁不同，静脉注射和口服后均能防止组胺引起支气管痉挛。基于其药理作用的效力，苯海拉明口服后的生物利用度低于其他抗组胺药。西咪替丁和雷尼替丁均能减少胃酸分泌，而司他定在这方面无效。所研究的药物均未在降低血压方面拮抗组胺，但除异丙嗪和苯海拉明外，所有药物均能降低平均动脉血压。结果表明，司他定对呼吸道和血管平滑肌的作用介于苯海拉明和二硫氮卓之间。鉴于司他定对胃酸分泌的影响极小，而对气道有显著活性，得出结论：该药物主要作用于H1受体。
