CAJ | 학술논문

组胺与组胺受体结合后引发以组胺为主的炎性介质释放,导致变态反应性疾病的发生.H1受体拮抗剂是抗组胺药物之一,可阻断组胺与Hl受体结合,从而抑制组胺发挥其生物学效应.Hl受体拮抗剂主要用于治疗由组胺释放诱发的变态反应性疾病.第一代抗组胺药作用时间短,有明显的镇静作用.第二代抗组胺药药效与第一代相近或强于第一代,作用时间长,无明显的中枢镇静作用,但有心脏毒性,故新药的研究成为热点.
조알여조알수체결합후인발이조알위주적염성개질석방,도치변태반응성질병적발생.H1수체길항제시항조알약물지일,가조단조알여Hl수체결합,종이억제조알발휘기생물학효응.Hl수체길항제주요용우치료유조알석방유발적변태반응성질병.제일대항조알약작용시간단,유명현적진정작용.제이대항조알약약효여제일대상근혹강우제일대,작용시간장,무명현적중추진정작용,단유심장독성,고신약적연구성위열점.
The binding of histamine to its receptors can induce the release of inflammatory mediators predominated by histamine followed by the development of allergic diseases.H1-receptor antagonists,as a kind of antihistamine,can inhibit the biological effects of histamine by blocking its binding to H1 receptor,and are mainly used to treat allergic diseases which are induced by the release of histamine.First-generation antihistamines have a short duration of action and an obvious sedative effect on central nervous system.Compared with first-generation antihistamines,second-generation antihistamines show a similar or stronger efficacy,longer duration of action and less sedative effects.However,cardiac toxicity has been observed in second-generation antihistamines,which has warranted the development of new antihistamine agents.