Linezolid

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Contents

Introduction

An n'th line antibiotic effective against gram positive organisms including MRSA and VRE, but with considerable toxicity.

Clinical Use

Active against gram positive organisms, and also mycobacteria and nocardia. Good penetration of bones, also penetrates into CSF.

Indications

  • Used in infections caused by methicillin or vancomycin resistant staphylococci/enterococci
  • Other serious Gram-positive bacterial infections resistant to conventional treatment

(Initiate in hospital after consultation with relevant specialist CSM guidance)

Administration

Has both oral and IV forms.

Clinical Issues

For all drugs with monoamine oxidase inhibitor properties the most important interaction with food or drugs is life threatening serotonin syndrome especially with other drugs that inhibit the re-uptake of serotonin or increase monoamine concentrations by other means. This happens with all type A inhibitors and at high dose with selegiline or linezolid. It classically occurs with blue cheese, and drugs including:

  • Tricyclic antidepressants (TCAs)
  • Selective serotonin re-uptake inhibitors (SSRIs)
  • Pethidine, tramadol and some other narcotic analgesics
  • Over the counter cough medicines
  • Anti-migraine drugs,
  • Weight reduction agents
  • Anti-emetics
  • Drugs of abuse and herbal products

Opioids

While most, if not all manufactures advise to avoid, serious interaction has not yet been reported for some opioids such as buprenorphine. Pethidine and tramadol are definitely contraindicated as case reports of serotonin syndrome exist. The interaction can be either: The interaction between MAOIs and narcotic analgesics are:

>>>Category:Monoamine oxidase inhibitors

Contra-indications

  • Delirium
  • Bipolar disorder ("manic depression")
  • Schizophrenia
  • Pregnancy
  • As for MAOIs
    • Uncontrolled hypertension
    • Phaeochromocytoma, Carcinoid tumour
    • Thyrotoxicosis
    • Mania

Cautions and Interactions

No dose adjustments required for hepatic/renal impairment unless severe.

  • Special care for interactions as for MAOIs
  • Severe optic atrophy in prolonged use (> 28 days)
  • Needs haematological monitoring (weekly)
    • Special care if
      • Treatment > 10 days;
      • Pre-existing myelosuppression;
      • If other drugs with risk myleosuppression
      • Severe renal failure.

Side effects

  • Thrombocytopenia
  • Anaemia
  • Leucopenia
  • Pancytopenia
  • Optic atrophy

Special advice

Pharmacology

It inhibits ribosomal protein synthesis (by inhibiting formation of the initiation complex).