上海交通大学：《药理学 Pharmacology》课程教学资源（讲义课件）氨基糖苷类、多粘菌素类、大环内酯类等 Aminoglycosides（氨基糖苷类）, Macrolides（大环内酯类）and others

上游充通大 SHANGHAI JIAO TONG UNIVERSITY Aminoglycosides(氨基糖苷类)， Macrolides(大环内酯类)and others 2011.12 1B三S

Aminoglycosides（氨基糖苷类）, Macrolides（大环内酯类）and others 2011.12

上游充通大 Aminoglycosides(氦基糖苷类) SHANGHAI JIAO TONG UNIVERSITY Tuberculosis,still severe infection now 1882，Heinrich Hermann Robert Koch discovered M.tuberculosis（结核分枝杆菌) 1940's,Merck supported S.A.Waksman's lab, Rutgers university,NJ 1940,actinomycin(放线菌素)，toxic 1942,streptothricin（链丝菌素)，still toxic ④1942，Albert Schatz,PhD student

Aminoglycosides（氨基糖苷类） Tuberculosis, still severe infection now 1882, Heinrich Hermann Robert Koch discovered M. tuberculosis （结核分枝杆菌） 1940’s, Merck supported S.A. Waksman’s lab, Rutgers university, NJ 1940, actinomycin（放线菌素）, toxic 1942, streptothricin （链丝菌素），still toxic 1942, Albert Schatz, PhD student

上游充通大 Aminoglycosides(氨基糖苷类) SHANGHAI JIAO TONG UNIVERSITY 1943.6 returned from army 0ct19,1943, HO OH streptomycin isolated Ho 一NH2 1944,Mayo clinic HO HN-CH3 OH NH2 1946,graduated and 一NH2 patent left in Rutgers H2N 1947,succeeded in TB treatment Streptomycin(链霉素) Law suit 1952,Nobel Prize to Waksman

Aminoglycosides（氨基糖苷类） 1943.6 returned from army Oct 19, 1943， streptomycin isolated 1944, Mayo clinic 1946, graduated and patent left in Rutgers 1947, succeeded in TB treatment Law suit 1952, Nobel Prize to Waksman Streptomycin（链霉素）

上游充通大 SHANGHAI JIAO TONG UNIVERSIT The Nobel Prize in Physiology or Medicine 1952 "for his discovery of streptomycin,the first antibiotic effective against tuberculosis" Selman Abraham Waksman

上游充通大 Individual aminoglycosides SHANGHAI JIAO TONG UNIVERSITY © Streptomycin(链霉素) © Gentamycin（庆大霉素) Amikacin（氨苄卡星) Tobramycin(妥布霉素) ©Netilmycin(奈替米星)

Individual aminoglycosides Streptomycin（链霉素） Gentamycin（庆大霉素） Amikacin（氨苄卡星） Tobramycin（妥布霉素） Netilmycin（奈替米星）

上游充通大 aminoglycosides SHANGHAI JIAO TONG UNIVERSITY Common characters: Potent effect on Gram-bacteria,including Pseudomonas,Mycobacterium tuberculosis Ineffective against anaerobic bacteria Not absorbed orally Untoward effects:>5 days;high dose;elderly;renal insufficiency ototoxicity(2%-10%):vertigo(眩晕)，ataxia(共 济失调)，loss of banlance nephrotoxicity (6%-10%) neuromuscular blocking (co-administered with general analgesics or muscle relaxants)

aminoglycosides Common characters: ü Potent effect on Gram- bacteria, including Pseudomonas, Mycobacterium tuberculosis ü Ineffective against anaerobic bacteria ü Not absorbed orally ü Untoward effects: >5 days; high dose; elderly; renal insufficiency ototoxicity（2％-10％）: vertigo（眩晕）, ataxia（共 济失调）, loss of banlance nephrotoxicity（6％-10％） neuromuscular blocking (co-administered with general analgesics or muscle relaxants)

上泽充通大学 Toxicity SHANGHAI JIAO TONG UNIVERSITY Their undesirable side effects:severe ototoxicity and nephrotoxicity. 18 of 21 actress showing "qianshou guanyin"were caused deafness by aminoglycosides

Toxicity Their undesirable side effects: severe ototoxicity and nephrotoxicity. 18 of 21 actress showing “qianshou guanyin” were caused deafness by aminoglycosides

上游充通大 SHANGHAI JIAO TONG UNIVERSITY A B C 78 9 10 11 2 3 12 4 5

上游充通大 SHANGHAI JIAO TONG UNIVERSITY anterior canal 小囊 Nerve Utricle 球囊 Saccule posterior canal horizontal canal Cochlea 耳蜗 水平半规管

耳蜗 球囊 小囊 水平半规管

上泽充通大学 SHANGHAI JIAO TONG UNIVERSITY 血管纹 Stria vascularis 前庭阶 Scala vestibuli 44 Scala media 中阶；蜗管 Ductus cochlearis 2b Limulus 6 10 Scala tympani 鼓阶

前庭阶 血管纹 鼓阶 中阶；蜗管