29216-28-2
29216-28-2 結構式
基本信息
甲喹吩嗪
MEQUITAZINE
10-(1-Azabicyclo[2.2.2]oct-3-ylmethyl)-10H-phenothiazine
10-(3-Quinuclidinylmethyl)phenothiazine
Butix
Instotal
LM 209
Mequitazina
Metaplexan
Mircol
Phenothiazine, 10-(3-quinuclidinylmethyl)-
Primalan
Vigigan
Virginan
Zesulan
10H-Phenothiazine, 10-(1-azabicyclo[2.2.2]oct-3-ylmethyl)- (9CI)
Nipolazin
NSC 303612
Phenothiazine, 10-(3-quinuclidinylmethyl)- (8CI)
Quitadrill
物理化學性質(zhì)
常見問題列表
美喹他嗪(mequitazine)由法國Aventis公司研發(fā)，商品名為Primalan，于1976年在法國上市，目前已在20多個國家銷售。美喹他嗪為選擇性H1受體拮抗劑，是無中樞鎮(zhèn)靜和抗膽堿能作用的長效抗組胺藥，對外周H1受體有選擇性拮抗作用，能抑制肥大細胞脫顆粒，調(diào)節(jié)迷走神經(jīng)緊張性，從而阻止慢性過敏癥狀的發(fā)展。本品尚有輕度抗膽堿能作用。臨床用于常年性及季節(jié)性過敏性皮炎、急慢性蕁麻疹、過敏性結膜炎、蟲咬性水腫、哮喘、各種皮膚瘙癢、濕疹等。
美喹他嗪口服吸收快，6h達峰值，t1/2為18h。口服后38h從體內(nèi)清除，不易通過血-腦脊液屏障。體內(nèi)分布廣，血管滲透性高。肝內(nèi)代謝，經(jīng)膽汁排出體外。
甲喹吩嗪不能與單胺氧化酶抑制劑同用。與中樞抑制藥(如中樞鎮(zhèn)靜藥和鎮(zhèn)靜藥)合用，可使中樞抑制作用加強。
Mequitazine is a potent H 1 -receptors selective antihistaminic drug widely studied and used for allergic disorders such as hay fever and urticaria. Mequitazine demonstrates significant bactericidal effects against all the tested clinical isolates including Ps. aeruginosa . Its effect against the Gram-positive isolates is more pronounced.
Mequitazine and clemizole antagonize the effect of histamine in guinea-pig ileum competitively. Mequitazine at 10 7 produces a parallel shift of the dose-response curve to acetylcholine in the rat duodenum. Mequitazine at highest concentration shows anticholinergic activity. Mequitazine inhibits contractile responses to KCl, phenylephrine (PE), 5-hydroxytryptamine (5-HT), and Ca 2+ in rat aorta.