Oxalactams

Author: Prof. Dr. med. Peter Altmeyer

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Last updated on: 29.10.2020

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Synonym(s)

Beta-lactamase inhibitors

Definition
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A group of antibiotics which bind to β-lactamases and irreversibly inhibit their enzymatic activity (β-lactamase inhibitors) is counted among the oxalactams. Their inhibitory effect particularly affects plasmid-encoded β-lactamases. They have only a limited effect against chromosomally coded β-lactamases.

β lactamase inhibitors themselves have no antibacterial efficacy and must therefore always be combined with a β lactam antibiotic. By selectively suppressing β-lactamases they increase the potency of the combination partners and extend their spectrum of action by β-lactamase-producing germs such as staphylococci, Moraxella catarrhalis, Bacteroides fragilis, Haemophilus influenzae and many enterobacteria (Noguchi JK et al. 1988).

Classification
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Field of application/use
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Sulbactam can be freely combined with any β lactam antibiotic. Clavulanic acid and tazobactam on the other hand have solid combination partners(amoxicillin and piperacillin). The combination of tazobactam and piperacillin has the broadest spectrum of action of all penicillins. Penicillin-resistant pneumococci and MRSA germs do not become more sensitive to penicillins in these combinations.

Undesirable effects
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Gastrointestinal UAW:

Clavulanic acid/amoxicillin leads with a frequency of 1:15,000 -1:10,000 to hepatocellular toxic effects, which can lead to severe cholestatic hepatitis.

  • Symptoms of diarrhoea
  • severe diarrhoea ( pseudomembranous enterocolitis)

Dermatological UAW:

Haematological ADRs:

  • Eosinophilia

Nephrogenic UAWs:

  • Interstitial Nephritis (rare)

Note: Cystic fibrosis patients treated with piperacillin are more often affected by fever and exanthema.

Contraindication
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Pencillin allergy

Literature
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  1. Graefe KH et al (2016) Antibacterial agents. In: Graefe KH et al (Eds) Pharmacology and Toxicology. Georg Thieme Publisher Stuttgart S.578-579
  2. Noguchi JK et al (1988) Sulbactam: a beta-lactamase inhibitor. Clin Pharm 7:37-51.

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Last updated on: 29.10.2020