新型抗过敏药英文版

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 histamine2.The development of antiallergic drug3.New allergy medicine-Olopatadine Hydrochloride4.The chemical structure5.Structure-activity relationship(SAR)6.Study on toxicity and side effect7.Indications8.Synthetic route9.Prospects10.How to choose the allergy medicine?,1.Allergy disease and histamine,When body has been stimulated by the antigenic substances, it may be cause the tissue damage or physical disorders, namely pathological immune response to diseases.Histamine in inflammation and allergic diseases play an important role in physi-ological, histamine of proinflammatory and immune adjustment is by three kind-s of histamine H1,H2, H3.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.,The first generation of antiallergic drug,The first generation of histamine H1 receptor antagonist has strong central nervous calming and choline fighting effects.,The second generation of antiallergic drug,The advantages of second generation antiallergic:(1)better clinical curative effect (2)long-term effect(3)no side effect to central nervous system (4)no resisting choline effect(5)eutherapeutic to asthma (6)good tolerabilitySlightly CNS effect:Sleepinessheadache whet the appetite and side effect to cardiovascular system,3.New allergy medicine-Olopatadine Hydrochloride,Olopatadine as a new kind of relatively high selectivity antiallergic, Concorde Fermentation by Japan listed company development and antiallergic, successively on the market in Europe, America, Japan and other countries.,4.The 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H1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H1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H1受体的亲和力强,但它对M1受体亲和力也强,副作用多。,6.Study on toxicity and side effect:,Preclinical and clinical studies have shown:no anticholinergic 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 urticariaEye drops:Allergic conjunctivitisDosage form:Tablets:5 mg/tabletEye drops:1% eye drops,8.Synthetic route:,According to the chemical structural formula 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 H1 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.,References:,1 薛建英. 新型抗过敏药盐酸奥洛他定的合成工艺研究M2 王金龙,陈孝治. H1受体拮抗剂及其研究的新进展J,中国药房,1999,10(3):1403 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):166-1704 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): 402-4056B. 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 conjuncti