磺胺类药物及抗菌增效剂20min

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,History,2,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 trachomatis,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,Preparations and Clinical Uses,Oral absorbable agentsSulfamethoxazole(磺胺甲噁唑)Sulfadiazine (磺胺嘧啶) Sulfadoxine(磺胺多辛),6,Oral nonabsorbable agentsSulfasalazine(柳氮磺胺吡啶),Topical agentsSulfacetamide(磺胺醋酰)Mafenide(甲磺米隆),UTI, Parasitic diseases (combined with other antimicrobials)- malaria, toxoplasmosis, PCP,ulcerative colitis, enteritis, other IBD,Ophthalemic,infections of burn and wound,Adverse effects,7,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 trimethoprim + sulfamethoxazole,p-aminobenzoic acid,Dihydrofolic acid,Tetrahydrofolic acid,Dihydrofolate synthetase,Dihydrofolate reductase,Thymidine,Purines,Methionine,9,DNA,Mechanism of action,Urinary tract infections. Bacterial respiratory tract infections.Pneumocystis jirovicii (carinii) pneumonia (PCP),Therapeutic us