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Chapter 41: Protein Synthesis Inhibitors and Miscellaneous Antibacterial Agents

INTRODUCTION

This chapter will be most useful after having a basic understanding of the material in Chapter 55, Protein Synthesis Inhibitors and Miscellaneous Antibacterial Agents in Goodman & Gilman’s The Pharmacological Basis of Therapeutics, 12th Edition. In addition to the material presented here Chapter 55 contains:

  • Table 55-2 which provides information about the activity of most of the antibacterial agents covered in this chapter against key gram-positive pathogens

LEARNING OBJECTIVES

  • Understand the mechanisms of action and resistance of tetracyclines, macrolides, vancomycin, linezolid, daptomycin, and quinupristin/dalfopristin

  • Describe the unique toxicities of antibiotics that are inhibitors of bacterial protein synthesis

  • Describe the uses and untoward reactions of vancomycin

  • Identify the drug–drug interactions that occur with some of these antibiotics

  • Understand how linezolid, daptomycin, and quinupristin/dalfopristin are used to treat methicillin-resistant and vancomycin-resistant organisms

DRUGS INCLUDED IN THIS CHAPTER

  • Azithromycin (ZITHROMAX)

  • Bacitracin

  • Chloramphenicol

  • Clarithromycin (BIAXIN, others)

  • Clindamycin (CLEOCIN PHOSPHATE, others)

  • Daptomycin (CUBICIN)

  • Doxycycline

  • Erythromycin

  • Linezolid (ZYVOX)

  • Mupirocin (BACTROBAN)

  • Polymyxin

  • Quinupristin/dalfopristin (SYNERCID)

  • Spectinomycin

  • Teicoplanin

  • Telithromycin (KETEX)

  • Tetracycline

  • Tigecycline

  • Vancomycin (VANCOCIN)

MECHANISMS OF ACTION AND RESISTANCE OF PROTEIN SYNTHESIS INHIBITORS
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MECHANISMS OF ACTION AND RESISTANCE OF PROTEIN SYNTHESIS INHIBITORS
...
DRUGS MECHANISM OF ACTION MECHANISM OF RESISTANCE
Tetracycline, Doxycycline, Tigecycline Inhibition of protein synthesis by binding to the 30S bacterial ribosome subunit (see Figure 41-1)

Decreased bacterial cell accumulation of tetracycline

Bacterial production of a ribosomal protection protein that displaces drug from its target

Enzymatic destruction of drug
Chloramphenicol Inhibition of protein synthesis by binding to the 50S bacterial ribosome subunit (see Figure 41-2) Bacterial production of acetyltransferase that inactivates the drug
Erythromycin, Clarithromycin, Telithromycin, Azithromycin Inhibition of protein synthesis by binding to the 50S bacterial ribosome subunit (see Figure 41-3)

Enhanced efflux from bacterial cell

Ribosomal protection by production of methylase enzymes

Hydrolysis by esterases

Mutation of 50S ribosomal protein
Clindamycin Inhibition of protein synthesis by binding to the 50S bacterial ribosome subunit

Ribosomal protection by constitutively produced methylase enzyme

Altered metabolism
Quinupristin/Dalfopristin Inhibition of protein synthesis by binding to the 50S bacterial ribosome subunit

Production of methylase enzyme that prevents binding to target

Production of acetyltransferase that inactivates the drug

Enhanced efflux from bacterial cell
Linezolid Inhibition of protein synthesis by binding to the 50S bacterial ribosome subunit to prevent formation of larger ribosomal complex Point mutations in rRNA
Spectinomycin Inhibition of protein synthesis by binding to the 30S bacterial ribosome subunit

Mutations in rRNA

Modifications of the drug by adenyltransferase
Polymyxin As surface-active agents, polymyxins interact with phospholipids and disrupt bacterial cell wall Resistance is rare
Vancomycin, Teicoplanin Inhibit cell wall synthesis by binding to D-alanyl-D-alanine terminus of cell wall precursor units (see Figure 41-4) Bacterial alteration of drug target
Daptomycin Binds to bacterial membranes resulting in depolarization, loss of membrane potential and cell death Not fully characterized
Bacitracin

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