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特拉唑嗪药理学研究进展

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特拉唑嗪是一种新型抗高血压药物,作为哌唑嗪的类似物,具有选择性阻滞突触后α1-肾上腺受体的作用,可松弛血管平滑肌,控制血压;与哌唑嗪相比,特拉唑嗪具有降压作用较为缓和,作用时间长且线性量效关系良好的优点.欧美等地区的广泛临床研究表明,特拉唑嗪是一种长效的抗高血压新药,优于哌唑嗪.同时,特拉唑嗪可松弛前列腺和膀胱颈部的肌肉,使小便更顺畅,用于治疗良性前列腺疾病;在神经退行性疾病中(例如帕金森病、肌萎缩侧索硬化、阿尔茨海默病、多系统萎缩症等),特拉唑嗪能结合并激活磷酸甘油酸激酶1(PGK1),通过增强PGK1活性和促进糖酵解来保护神经元;特拉唑嗪与部分胃肠道疾病、创伤后应激障碍症、多汗症以及脑卒中的治疗也有一定的关系.本文介绍了特拉唑嗪的基本概况、药代动力学特征、临床应用及药理作用,为今后特拉唑嗪的研究提供参考.
Advances in the pharmacological study of terazosin
Terazosin(TZ)is a novel antihypertensive drug.As an analogue of prazosin,terazosin can selectively block the postsynaptic α1-adrenal receptor,relax the vascular smooth muscle,and control the blood pressure.Compared with prazosin,terazosin has a more moderate antihypertensive effect with a long action time and a good linear dose-effect relationship.Many studies in Europe and the United States have shown that it is a long-acting new antihypertensive drug,superior to prazosin.At the same time,terazosin can relax the muscles of the prostate and bladder neck,and facilitate urinationsuiable for benign prostate diseases.In neurodegenerative diseases(Parkinson's disease,amyotrophic lateral sclerosis,Alzheimer's disease,multisystem atrophy,etc.),terazosin binds and activates PGK1,protects the neurons by enhancing PGK1 activity and promoting glycolysis.Recent studies have linked terazosin to the treatment of some gastrointestinal disorders,post-traumatic stress disorder,hyperhidrosis,and stroke.This paper reviewed the basic situation,pharmacokinetics,clinical application and pharmacological action of terazosin to provide reference for its future research.

terazosinpharmacologyresearch progresspharmacokinetics

李玫、陶彦华、仇念壮、张雨琼、杨武斌、张雪辉、徐晓燕

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山东第一医科大学药理学研究所,山东 泰安 271016

菏泽市曹县职业教育中等专业学校,山东 菏泽 274400

特拉唑嗪 药理学 研究进展 药代动力学

泰安市科技发展计划

2018NS0173

2024

中南药学
湖南省药学会

中南药学

CSTPCD
影响因子:0.736
ISSN:1672-2981
年,卷(期):2024.22(4)
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