抗组胺药物应用进展

Advancement of antihistamine drugs application

抗组胺药物治疗过敏性疾病已广泛地应用于临床。由于第 1代抗组胺药物嗜睡的不良反应而影响了它的临床应用 ,2 0世纪 80年代后生产的第 2代抗组胺药物具有H1受体选择性高、无镇静作用与组胺作用分离等特点 ,称非镇静抗组胺药 (NSA)。但第 2代抗组胺药仍有一些不良反应 ,尤以心脏的毒性作用 ,这与抗组胺药物相互作用、药动学、以及药物的分子结构有关。 1997年新型抗组胺药物———非索非那定 (fexofenadine)问世 ,它是作用快、疗效高、相对安全低毒的抗组胺药。非索非那定的开发 ,为寻找既无中枢镇静作用 。

Antihistamine have already widely been used in clinic to cure allergic disease. Because first generation antihistamines have been shown to produce sedation side effect, their clinical use is influenced. Second generation antihistamines produced late in the 80's of 20 th have many characteristics, such as high selectivity of H 1 receptor, non sedation, and histamine isolation and so on. Thus second generation antihistamines are called non sedating antihistamines (NSA). However, Some of them also have adverse reaction, especially cardiotoxicity, which is related to antihistamines drugs interaction, pharmacokinetics and drug molecular structure. In 1997, fexofenadine, a new antihistamic drug, made an appearance. It is fast action, high effection, relative safety and low toxicant antihistamine. The exploitation of fexofenadine establishs new way to look for antihistamic drugs which have neigher sedating effects on the central nervous system nor cardiotoxicity.