新型抗过敏药英文版.pptx

单击此处编辑母版标题样式,单击此处编辑母版文本样式,第二级,第三级,第四级,第五级,2016-11-10,0,抗过敏药,Antiallergic drug,我在花粉的刺激下脓包成堆,Flower?,你在春天的花朵里自拍纷飞,Content,:,1.Allergy disease and histamine,2.The development of antiallergic drug,3.New allergy medicine-Olopatadine Hydrochloride,4.T,he chemical structure,5.,Structure-activity relationship,(SAR),6.S,tudy on toxicity and side effect,7.Indications,8.S,ynthetic route,9.Prospects,10.,How to choose the allergy medicine,?,1.Allergy disease and histamine,W,hen body has been stimulated by the antigenic substances,it may be cause the tissue damage or physical disorders,namely pathological immune response to diseases.,H,istamine in inflammation and allergic diseases,p,lay an important role in physi,-,ological,histamine of proinflammatory and immune adjustment is by three kind,-,s of histamine H,1,H,2,H,3,.,Histamine is the most important medium allergic disease,.,2.The development of antiallergic drug,Antiallergic drugs are also called antihistamines,with the continuous development of pharmacology,antihistamines have been developed to six categories nearly hundred kinds of varieties.,3.New allergy medicine-Olopatadine Hydrochloride,Olopatadine,as a new kind of relatively high selectivity antiallergic,Concorde,F,ermentation by Japan listed company development and antiallergic,successively on the market in Europe,America,Japan and other countries.,4.T,he chemical structure,11-(,反,)-3-,二甲胺基丙烯,-6,11-,二氢苯骈,b,e,氧杂卓,-2-,乙酸 盐酸,Structure-activity relationship,(SAR):,1.,烯基碳和氮原子间相隔2个碳原子最佳,延长或缩短碳链对H,1,受体的亲和力减弱;氮原子上以二甲基取代抑制支气管哮喘作用最强,以二乙基取代抑制作用减弱,以吗琳和哌啶取代活性消失。,2.分子中梭基是必要的官能团,梭基和二苯骈氧卓环之间以亚甲基相连,抗过敏活性最强,但适当延长或缩短连接基团对H,1,受体的亲和力变化影响不大。,3.二苯骈氧卓环也是必要的,开环化合物失去所有的活性。,4.反式异构体比顺式体对H,1,受体的亲和力强,但它对M,1,受体亲和力也强,副作用多。,6.S,tudy on toxicity and side effect,:,Preclinical and clinical studies have sh,o,wn,:,no anticholine,r,gic side effects,;,does not lead to cataracts and eye symptoms of nerve damage,;,no antigenicity and allergic reaction,but lar,-,ge doses,;,pregnant women with fetal development or after the birth of a babys growth and lead to weight loss or developmental delays,so pregnant women and nursing mothers ban.,7.Indications:,Oral treatment:,Allergic rhinitis,skin irritations,pleomorphic exudative erythema and urticaria,Eye drops,:,Allergic conjunctivitis,D,osage form,:,T,ablets:5,mg/tablet,Eye drops,:1%,eye drops,8.S,ynthetic route,:,According to the chemical structural formul,a and,inverse synthetic analysis,a reasonable mode of fracture in the double bond,by carbonyl build double bond,.,Olopatadine Hydrochloride have certain effect to common variety of allergic conjunctivitis,at the same time have less adverse reaction.,9.Prospects:,Olopatadine Hydrochloride,have strong antagonism effect,to H,1,receptor,also inhibit mast cells release of inflammatory mediators,.In recent years,some new usages just like nasal spray and so on are under the researching.,Therefore,the research and development the los he will produce good economic benefit and social benefit.,10.,How to choose the allergy medicine,?,Antiallergic selection principle,:,1.Consult a physician before using this drug,.,2.,Find the allergen,.,3.Pay attention to medicine,taking time.,4.,Moderate,drug,dosage,.,5.Unfavorable combination in take allergy drugs at the same time,.,6.,Be careful of combining with Chinese medicine and western medicine.,R,eferences,:,1,薛建英.,新型抗过敏药盐酸奥洛他定的合成工艺研究M,2 王金龙,陈孝治.H,1,受体拮抗剂及其研究的新进展J,中国药房,1999,10(3):140,3,李莹,张潇等,.,过敏性结膜炎的流行病学及奥洛他定滴眼液开放性 多中心治疗的初步效果,J Ophthalmol CHN,2008(17):166-170,4,博恩,.,如何选用抗过敏药,J,中国中医药报 2010,(5),5,Kyosuke Satake,JunichiIkeda et.,Olopatadine hydrochloride suppresses hot flashes induced by topical treatment with tacrolimus ointment in ratsJ European Journal of Pharmacology,Volume 765,2015(10):402-405,6,B.Mortemousque,T.Bourcier,M.Khairallah et.,Comparison of preservative-free ketotifen fumarate and preserved olopatadine hydrochloride eye drops in the treatment of moderate to severe seasonal allergic conjunctivitisJ Journal Franais dOphtalmologie,2014(1):1-8,7,Saki Matsui,Hiroyuki Murota,Emi Ono et.,Olopatadine hydrochloride restores histamine-induced impaired sweatingJ Journal of Dermatological Science,2014(6):260-261,Thank you!,