Linezolid: Difference between revisions
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* Linezolid 600 mg PO/IV q12h |
* Linezolid 600 mg PO/IV q12h |
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== |
=== Renal Dosing === |
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* No adjustment needed |
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== Safety == |
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=== Adverse Drug Reactions === |
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* [[Adverse drug reaction::Serotonin syndrome|Serotonin syndrome]] when taken concurrently with certain psychiatric medications |
* [[Adverse drug reaction::Serotonin syndrome|Serotonin syndrome]] when taken concurrently with certain psychiatric medications |
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** Ideally hold SSRIs when starting linezolid |
** Ideally hold SSRIs when starting linezolid |
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* Cytopenias, including [[Adverse drug reaction::Thrombocytopenia|thrombocytopenia]] (most common), [[Adverse drug reaction::anemia]], and [[Adverse drug reaction::leukopenia]] (least common) |
* Cytopenias, including [[Adverse drug reaction::Thrombocytopenia|thrombocytopenia]] (most common), [[Adverse drug reaction::anemia]], and [[Adverse drug reaction::leukopenia]] (least common) |
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** More common with prolonged use, e.g. after 2 weeks |
** More common with prolonged use, e.g. after 2 weeks |
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** Likely more common with higher dose (600 mg versus 300 mg) |
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==== Long-Term Use ==== |
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* The generally-recommended maximum therapy is 28 days |
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* However, linezolid is used in the treatment for [[MDR-TB]] in much longer courses |
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* The most common adverse effects were [[peripheral neuropathy]] (64%), myelosuppression (22%), optic neuritis (5%), GI effects (2%), and rash (2%)[[CiteRef::lan2020dr]] |
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* About 15% of patients had to permanently discontinue due to adverse effects |
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* Risk of adverse reactions increases with time[[CiteRef::migliori2009a]] |
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** <10% at 2 weeks (for higher, standard dose) |
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** 12% at 4 weeks |
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** 20% at 8 weeks |
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** 40% at 16 weeks |
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** 55% at 32 weeks |
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=== Drug-Drug Interactions === |
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* Coadminitration with rifampin decreases AUC and peak by 32 and 21%, respectively |
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* Increases warfarin INR |
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* Weak, reversible, nonselective MAO inhibitor, leading to a risk of serotonin syndrome if coadministered with other MAOIs (and may SSRIs) |
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[[Category:Antibiotics]] |
[[Category:Antibiotics]] |
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Latest revision as of 17:05, 27 September 2024
Background
- Oxazolidinone antibiotic
Mechanism of Action
- Inhibits the 50S ribosome of Gram-positive bacteria
Spectrum of Activity
- Active against Gram-positive bacteria
- Not active against Gram-negative bacteria
Dosing
- Linezolid 600 mg PO/IV q12h
Renal Dosing
- No adjustment needed
Safety
Adverse Drug Reactions
- Serotonin syndrome when taken concurrently with certain psychiatric medications
- Ideally hold SSRIs when starting linezolid
- Cytopenias, including thrombocytopenia (most common), anemia, and leukopenia (least common)
- More common with prolonged use, e.g. after 2 weeks
- Likely more common with higher dose (600 mg versus 300 mg)
Long-Term Use
- The generally-recommended maximum therapy is 28 days
- However, linezolid is used in the treatment for MDR-TB in much longer courses
- The most common adverse effects were peripheral neuropathy (64%), myelosuppression (22%), optic neuritis (5%), GI effects (2%), and rash (2%)1
- About 15% of patients had to permanently discontinue due to adverse effects
- Risk of adverse reactions increases with time2
- <10% at 2 weeks (for higher, standard dose)
- 12% at 4 weeks
- 20% at 8 weeks
- 40% at 16 weeks
- 55% at 32 weeks
Drug-Drug Interactions
- Coadminitration with rifampin decreases AUC and peak by 32 and 21%, respectively
- Increases warfarin INR
- Weak, reversible, nonselective MAO inhibitor, leading to a risk of serotonin syndrome if coadministered with other MAOIs (and may SSRIs)
References
- ^ Zhiyi Lan, Nafees Ahmad, Parvaneh Baghaei, Linda Barkane, Andrea Benedetti, Sarah K Brode, James C M Brust, Jonathon R Campbell, Vicky Wai Lai Chang, Dennis Falzon, Lorenzo Guglielmetti, Petros Isaakidis, Russell R Kempker, Maia Kipiani, Liga Kuksa, Christoph Lange, Rafael Laniado-Laborín, Payam Nahid, Denise Rodrigues, Rupak Singla, Zarir F Udwadia, Dick Menzies, N Ahmad, P Baghaei, L Barkane, A Benedetti, SK Brode, JCM Brust, JR Campbell, VWL Chang, D Falzon, L Guglielmetti, P Isaakidis, RR Kempker, M Kipiani, L Kuksa, Z Lan, C Lange, R Laniado-Laborín, P Nahid, D Rodrigues, R Singla, ZF Udwadia, D Menzies. Drug-associated adverse events in the treatment of multidrug-resistant tuberculosis: an individual patient data meta-analysis. The Lancet Respiratory Medicine. 2020;8(4):383-394. doi:10.1016/s2213-2600(20)30047-3.
- ^ G. B. Migliori, B. Eker, M. D. Richardson, G. Sotgiu, J-P. Zellweger, A. Skrahina, J. Ortmann, E. Girardi, H. Hoffmann, G. Besozzi, N. Bevilacqua, D. Kirsten, R. Centis, C. Lange. A retrospective TBNET assessment of linezolid safety, tolerability and efficacy in multidrug-resistant tuberculosis. European Respiratory Journal. 2009;34(2):387-393. doi:10.1183/09031936.00009509.
