(精选)Antimicrobial Drugs一教学课件.pptVIP

Antimicrobial Drugs;Antimicrobial Drugs;Historical Perspective;1928 – Fleming discovered penicillin, produced by Penicillium. 1940 – Howard Florey and Ernst Chain performed first clinical trials of penicillin.;Properties of an ideal antibiotic;Major genera that produce clinically useful antibiotics ;Major targets of antimicrobial activity;Major targets of antimicrobial activity;Penicillin Natural penicillins Semisynthetic penicillins Penicilinase-resistant penicillins Extended-spectrum penicillins Penicillins + ?-lactamase inhibitors Carbapenems Monobactam ;Antibacterial Antibiotics Inhibitors of Cell Wall Synthesis;Chloramphenicol Broad spectrum Binds 50S subunit, inhibits peptide bond formation Aminoglycosides Streptomycin, neomycin, gentamycin Broad spectrum Changes shape of 30S subunit;Tetracyclines Broad spectrum Interferes with tRNA attachment Macrolides Gram-positives Binds 50S, prevents translocation Erythromycin Gram-positives Binds 50S, prevents translocation;Disk-Diffusion Test;Definitions;Broth Dilution Test;A variety of mutations can lead to antibiotic resistance. Mechanisms of antibiotic resistance 1. Enzymatic destruction of drug 2. Prevention of penetration of drug 3. Alteration of drugs target site 4. Rapid ejection of the drug Resistance genes are often on plasmids or transposons that can be transferred between bacteria.;Misuse of antibiotics selects for resistance mutants. Misuse includes: Using outdated, weakened antibiotics Using antibiotics for the common cold and other inappropriate conditions Use of antibiotics in animal feed Failure to complete the prescribed regimen Using someone elses leftover prescription;Figure 20.20;Synergism occurs when the effect of two drugs together is greater than the effect of either alone. Antagonism occurs when the effect of two drugs together is less than the effect of either alone.;Effects of Combinations of Drugs;Antimicrobial peptides Broad spectrum antibiotics from plants and animals Squalamine (shark