The penicillins.

Abstract:

:The penicillin family of antibiotics remains an important part of our antimicrobial armamentarium. In general, these agents have bactericidal activity, excellent distribution throughout the body, low toxicity, and efficacy against infections caused by susceptible bacteria. The initial introduction of aqueous penicillin G for treatment of streptococcal and staphylococcal infections was an important pharmacologic landmark. The emergence of penicillinase-producing Staphylococcus aureus prompted the development of the penicillinase-resistant penicillins (for example, methicillin, oxacillin, and nafcillin), in which an acyl side chain prevented disruption of the beta-lactamase ring. Subsequently, the aminopenicillins (ampicillin, amoxicillin, and bacampicillin) were developed because of the need for gram-negative antimicrobial activity. Their spectrum initially included Escherichia coli, Proteus mirabilis, Shigella, Salmonella, Listeria, Haemophilus, and Neisseria. The search for a penicillin with additional antimicrobial activity against the Enterobacteriaceae and Pseudomonas aeruginosa led to the development of the carboxypenicillins (carbenicillin and ticarcillin) and the ureidopenicillins (mezlocillin, azlocillin, and piperacillin). Finally, the combination of a beta-lactamase inhibitor (clavulanic acid, sulbactam, or tazobactam) and an aminopenicillin, ticarcillin, or piperacillin has further extended their antibacterial spectra by inhibiting certain beta-lactamases (non-group 1) of resistant bacteria. The development of an ideal penicillin that is rapidly bactericidal, nonsensitizing, nontoxic, bioavailable, and resistant to beta-lactamases and that has a high affinity for penicillin-binding proteins remains the goal.

journal_name

Mayo Clin Proc

journal_title

Mayo Clinic proceedings

authors

Wright AJ

doi

10.4065/74.3.290

keywords:

subject

Has Abstract

pub_date

1999-03-01 00:00:00

pages

290-307

issue

3

eissn

0025-6196

issn

1942-5546

pii

S0025-6196(11)63867-6

journal_volume

74

pub_type

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