抗生素英文课件精品 BETA LACTAM ANTIBIOTICS AND OTHER CELL WALL SYNTHESIS INHIBITORS教程文件.ppt

BETA LACTAM ANTIBIOTICS AND OTHER CELL WALL SYNTHESIS INHIBITORSMa. Shiela Cano-Guiking, M.D.;;PENICILLINS I. CLASSIFICATION A. Penicillinase Resistant ( Antistaphylococcal Penicillins) 1. Methicillin ( Staphcillin)2. Nafcillin (Unipen, Nafcil, Nallpen)3. Isoxazolyl penicillins a. Oxacillin  b. Cloxacillin c. Dicloxacillin d. Flucloxacillin  ;B. Penicillinase-Susceptible 1. Narrow-Spectrum a. Benzylpenicillin – Penicillin G b. Phenoxymethyl penicillin – Penicillin V 2. Extended Spectrum A. Aminopenicillins a.1 Ampicillin a.2 Esters a.2.1. Bacampicillin a.2.2. Pivampicillin a.2.3. Talampicillin a.3. Amoxicillin ;;Mechanisms of Action: Specific: inhibit the last step in the peptidoglycan synthesis of  the cell wall Underlying:  1. inhibition of transpeptidase enzymes2. activation of penicillin binding proteins (PBPs)3. activation of autolysins (murein hydrolases) ;;;;;;;- cannot penetrate the blood-brain barrier; but 50% of the plasma concentration can pass through in the presence of inflammation:  Probenecid and certain organic acids can inhibit transfer from cerebrospinal fluid (CSF) to blood stream; may lead to increase CSF level. - Metabolized by the liver to penicillanic/penicillenic acid; penicillamine, penicilloic acid and other penicilloyl derivatives (allergenic metabolites) - Excreted primarily by the kidneys (90% tubular secretion, 10% glomerular filtration) small amount through bile and feces, sputum and milk; renal excretion inhibited by probenecid;E. Adverse Effects: 1. Hypersensitivity reactions most common adverse effects - cause the highest incidence of antibiotic allergy a. major antigenic determinant- penicilloyl metabolite skin testing( penicilloyl polylysine (PPL) ) b. Signs and symptoms: - varied skin rashes and purpuric