32.四环素和氯霉素——山东大学药理学英文课件.pptVIP

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32.四环素和氯霉素——山东大学药理学英文课件.ppt

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32.四环素和氯霉素——山东大学药理学英文课件

Commonly used Quinolones Nalidixic acid and pipemidic acid Used only in urinary tract infection Norfloxacin The least active in fluoroquinolones, F low No effects on mycoplasmas, chlamydiae, mycobaterium tuberculosis, legionella Urinary tract and intestinal tract infections Ciprofloxacin(悉复欢) The most active agent in fluoroquinolones against gram-negatives, particularly P. aeruginosa in vitro No effects on anaerobes Ofloxacin(泰利必妥） Improved quality in pharmacokinetics F 89% Effective on mycobateria, chlamydiae and some anaerobes Effective on resistant bacteria Second line agent for tuberculosis Levo-ofloxacin（可乐必妥,来立信） F 100% Superior activity against gram-positive organisms Effective on mycoplasma, legionella, chlamydia and anaerobes Lowest toxicity among fluoroquinolones Lomefloxacin: F 98% t ?= 7h To G+ and G-: Similar to ofloxacin To anaerobes: ofloxacin Photosensitivity C8-F Fleroxacin F 100%, t ?10h Higher activity than ciprofloxacin and ofloxacin (in vivo) Sparfloxacin Long-acting t ?16h Improved activity against G+ bacteria, anaerobes, mycobateria, mycoplasmas, chlamydiae Second line agent for tuberculosis Moxifloxacin fourth generation F 90% t ? 12~15h High activity on most G+ ,G-, anaerobes, mycobateria, mycoplasmas, chlamydiae Low toxicity Sulfonamides Sulfonamides Classification Used in systemic infections Short-acting: SIZ Medium-acting: SD, SMZ Long-acting: SMD Used in intestinal infections: sulfasalazine Topic sulfonamides: SD-Ag, SA-Na, SML Sulfonamides Antimicrobial activity Broad-spectrum bacteriostatic agents Both G+ and G- , chlamydiae trachomatis mycoplasm and some protozoa Mechanism of action Inhibit dihydropteroate synthetaseand block bacteria folic acid synthesis Sulfonamides Pharmacokinetics Metabolism: liver Excretion : kidney pH Sulfonamides Adverse effects Urinary tract disturbance: crystalluria, hematuria, obstruction Allergic reactions: fever, skin r