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Table 7.5 Drugs that inhibit bacterial cell wall synthesis

[Drugs that i]nteract directly with penicillin-binding protein (PBPs) and inhibit transpeptidase activity

Drug class Specific drugs Natural or semisynthetic Spectrum of activity
Penicillins Penicillin G, penicillin V Natural Narrow-spectrum against gram-positive and a few gram-negative bacteria
Ampicillin, amoxicillin Semisynthetic Narrow-spectrum against gram-positive bacteria but with increased gram-negative spectrum
Methicillin Semisynthetic Narrow-spectrum against gram-positive bacteria only, including strains producing penicillinase
Cephalosporins Cephalosporin C Natural Narrow-spectrum similar to penicillin but with increased gram-negative spectrum
First-generation cephalosporins Semisynthetic Narrow-spectrum similar to cephalosporin C
Second-generation cephalosporins Semisynthetic Narrow-spectrum but with increased gram-negative spectrum compared with first generation
Third- and fourth-generation cephalosporins Semisynthetic Broad-spectrum against gram-positive and gram-negative bacteria, including some β-lactamase producers
Fifth-generation cephalosporins Semisynthetic Broad-spectrum against gram-positive and gram-negative bacteria, including MRSA
Monobactams Aztreonam Semisynthetic Narrow-spectrum against gram-negative bacteria, including some β-lactamase producers
Carbapenems Imipenem, meropenem, doripenem Semisynthetic Broadest spectrum of the β-lactams against gram-positive and gram-negative bacteria, including many β-lactamase producers

Large molecules that bind to the peptide chain of peptidoglycan subunits, blocking transglycosylation and transpeptidation

Drug class Specific drugs Natural or semisynthetic Spectrum of activity
Glycopeptides Vancomycin Natural Narrow spectrum against gram-positive bacteria only, including multidrug-resistant strains

Block transport peptidoglycan subunits across cytoplasmic membrane

Drug class Specific drugs Natural or semisynthetic Spectrum of activity
Bacitracin Bacitracin Natural Broad-spectrum against gram-positive and gram-negative bacteria

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