Penicillin-binding proteins: Penicillinsalso inactivate numerous proteins on the bacterial cell membrane. Consequently, they are inactive against organisms devoid of this structure, such as mycobacteria, protozoa, fungi, and viruses. Penicillinsare only effective against rapidly growing organisms that synthesize a Peptidoglycan cell wall. These drugs are bactericidal and work in a time-dependent fashion. Cell lysis can then occur, either through osmotic pressure or through the activation of autolysins. Mechanism of action The penicillins interfere with the last step of bacterial cell wall Synthesis (transpeptidationor cross-linkage), resulting in exposure of the osmotically less stable membrane. The nature of this side chain affects the antimicrobial spectrum, stability to stomach acid, cross hypersensitivity, and susceptibility to bacterial degradativeenzymes (β-lactamases). Membersof this family differ from one another in the R substituent attached to the 6-aminopenicillanic acid residue. PENICILLINS The penicillins are among the most widely effective and the least toxic drugs known. The most important members of this group of drugs are the β-lactamantibiotics, vancomycin, and daptomycin. They have little or no effect on bacteria that are not growing and dividing. Inhibitors of cell wall synthesis require actively proliferating microorganisms. The cell wall is composed of a polymer called peptidoglycan that consists of glycan units joined to each other by peptide cross-links. Some antimicrobial drugs selectively interfere with synthesis of the bacterial cell wall-a structure that mammalian cells do not possess.
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