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1、磺胺与复方磺胺甲噁唑(Sulfonamides & Cotrimoxazole),北京协和医学院基础学院药理学系 郭 磊,2,History,Mechanism of action,Antibacteral spectrum-Broad, bacteriostatic,Gram-negative,Gram-positive,Others,Nocardia spp,Meningococcus,Escherichia coli,Streptococcus spp,Pneumococcus,S. aureus,Salmonella,Some protozoa,Chlamydia trachomati
2、s,P. jirovecii,T. gondii,5,nearly complete absorption, never given s.c or i.m,A,wide, PPB-10-95%, cross placenta & BBB, CSF conc = Plasma conc,D,acetylation, metabolite inactive but toxic.,M,less soluble in acidic urine, precipitate- crystalluria,E,Pharmacokinetics,6,Preparations and Clinical Uses,O
3、ral absorbable agents Sulfamethoxazole(磺胺甲噁唑) Sulfadiazine (磺胺嘧啶) Sulfadoxine(磺胺多辛),Oral nonabsorbable agents Sulfasalazine(柳氮磺胺吡啶),Topical agents Sulfacetamide(磺胺醋酰) Mafenide(甲磺米隆),UTI, Parasitic diseases (combined with other antimicrobials)- malaria, toxoplasmosis, PCP,ulcerative colitis, enteriti
4、s, other IBD,Ophthalemic, infections of burn and wound,7,Adverse effects,Crystalluria & renal toxicity,Hypersensitivity: rashes, stevens-johnson syndrome, drug fever,Hemolytic anemia (in G6PD def),Sulfonamides increase the risk of kernicterus in newborns,Cotrimoxazole (TMP-SMZ),Combination of trimet
5、hoprim + sulfamethoxazole,9,p-aminobenzoic acid,Dihydrofolic acid,Tetrahydrofolic acid,Dihydrofolate synthetase,Dihydrofolate reductase,Thymidine,Purines,Methionine,DNA,Mechanism of action,Urinary tract infections. Bacterial respiratory tract infections. Pneumocystis jirovicii (carinii) pneumonia (PCP),Therapeutic uses,Adverse effects,Stevens-Johnson综合征,17,Summary,Folate antagonists,18,Thanks!,
