ABSTRACT

Introduction .................................................................................................................................... 132 Antibacterial Agents ...................................................................................................................... 132

Inhibition of Cell Wall Synthesis ........................................................................................ 132 Drugs that Inhibit Cell Wall Biosynthetic Enzymes................................................ 132 Drugs that Bind to Carrier Molecules...................................................................... 133 Drugs that Combine with Cell Wall Precursors ...................................................... 133 Drugs that Inhibit Enzymatic Polymerization and Attachment of New

Peptidoglycan to Cell Wall (β-Lactams) .................................................... 134 Interference with Cytoplasmic Membrane Integrity .......................................................... 136

Drugs that Disorganize the Cytoplasmic Membrane .............................................. 136 Drugs that Produce Pores in Membranes ................................................................ 136

Inhibition of Nucleic Acid Synthesis .................................................................................. 137 Inhibitors of DNA Replication ................................................................................. 137 Inhibitors of RNA Polymerase: Rifamycins (Rifampin and Rifaximin) ................. 137

Inhibition of Ribosome Function and Protein Synthesis .................................................... 138 Inhibitors of 30S Ribosomal Subunits ..................................................................... 138 Inhibitors of 50S Ribosomal Subunits ..................................................................... 138

Inhibition of Synthesis of Essential Small Molecules ........................................................ 140 Inhibitors of Dihydropteroate Synthetase ................................................................ 140 Inhibitors of Dihydrofolate Reductase ..................................................................... 140

Antimycobacterial Agents ............................................................................................................. 140 Inhibition of Cell Wall Synthesis ........................................................................................ 140

Isoniazid (Isonicotinic Acid Hydrazide, INH) ........................................................ 140 Cycloserine .............................................................................................................. 140 Ethambutol ............................................................................................................... 141

Interference with Cytoplasmic Membrane Function: Pyrazinamide ................................. 141 Inhibition of Nucleic Acid Synthesis .................................................................................. 141

Rifamycins: Rifampin, Rifabutin, and Rifapentine ................................................. 141 Fluoroquinolones as Antimycobacterial Agents ...................................................... 141

Inhibition of Protein Synthesis ........................................................................................... 141 Aminoglycosides: Streptomycin and Amikacin ...................................................... 141

Antifungal Agents .......................................................................................................................... 141 Inhibition of Cell Wall Synthesis ........................................................................................ 141

Echinocandins: Caspofungin, Micafungin, and Anidulafungin ............................. 141 Interference with Membrane Integrity ............................................................................... 142

Polyenes: Amphotericin B and Nystatin .................................................................. 142 Azole Antifungal Drugs .......................................................................................... 142 Allylamines: Terbinane ......................................................................................... 143

Since the previous edition of this Handbook, many new antibiotics have been developed and are now on the market or undergoing clinical trials. There are many compounds with antimicrobial activity. This chapter, however, attempts to summarize current information about, and working models for, the mechanisms of action only of antimicrobial agents that are in clinical use or in advanced stages of investigation, or that illustrate important points or are used in laboratory research. This chapter also provides references to more extensive information.