Antibacterial Agents

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Abstract
Antimicrobial chemotherapy has played a vital role in the treatment of human infectious diseases since the discovery of penicillin in the 1920s. Hundreds of antimicrobial agents have been developed or synthesized to date, and a broad number and variety of agents are currently available for clinical use. However, the sheer numbers and continuing development of agents make it difficult for clinicians to keep up with progress in the field. This chapter provides an overview of the antibacterial agents currently marketed in the United States, with major emphasis on their mechanisms of action, spectra of activity, important pharmacologic parameters, and toxicities. The major antibacterial action of penicillins is derived from their ability to inhibit a number of bacterial enzymes, namely penicillin-binding proteins (PBPs), that are essential for peptidoglycan synthesis. Cephalosporins are generally very well tolerated. The monobactams are β-lactams with various side chains affixed to a monocyclic nucleus. Since the first aminoglycoside, streptomycin, was introduced, this class of antibiotic has played a vital role in the treatment of serious gram-negative infections. The currently available aminoglycosides are derived from Micromonospora spp. or from Streptomyces spp. Tetracyclines are broad-spectrum bacteriostatic antibiotics with the hydronaphthacene nucleus, which contains four fused rings. Glycylcyclines are a group of semisynthetic tetracycline derivatives containing a glycylamido substitution at position 9. Streptogramins are natural cyclic peptides produced by Streptomyces spp. They are a unique class of antibiotics in which each member is a combination of at least two structurally unrelated components, groups A and B streptogramins.

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