Linezolid: Difference between revisions
From IDWiki
No edit summary |
No edit summary |
||
| Line 16: | Line 16: | ||
* Linezolid 600 mg PO/IV q12h |
* Linezolid 600 mg PO/IV q12h |
||
== |
=== Renal Dosing === |
||
* No adjustment needed |
|||
== Safety == |
|||
=== Adverse Drug Reactions === |
|||
* [[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 |
||
** Ideally hold SSRIs when starting linezolid |
** Ideally hold SSRIs when starting linezolid |
||
* 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) |
||
** More common with prolonged use, e.g. after 2 weeks |
** 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%)<ref>Lan Z, Ahmad N, Baghaei P, Barkane L, Benedetti A, Brode SK, Brust JCM, Campbell JR, Chang VWL, Falzon D, Guglielmetti L, Isaakidis P, Kempker RR, Kipiani M, Kuksa L, Lange C, Laniado-Laborín R, Nahid P, Rodrigues D, Singla R, Udwadia ZF, Menzies D; Collaborative Group for the Meta-Analysis of Individual Patient Data in MDR-TB treatment 2017. Drug-associated adverse events in the treatment of multidrug-resistant tuberculosis: an individual patient data meta-analysis. Lancet Respir Med. 2020 Apr;8(4):383-394. doi: [https://doi.org/10.1016/S2213-2600(20)30047-3 10.1016/S2213-2600(20)30047-3]. Epub 2020 Mar 17. PMID: 32192585; PMCID: [https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7384398/ PMC7384398].</ref> |
|||
* About 15% of patients had to permanently discontinue due to adverse effects |
|||
* Risk of adverse reactions increases with time<ref>Migliori GB, Eker B, Richardson MD, Sotgiu G, Zellweger JP, Skrahina A, Ortmann J, Girardi E, Hoffmann H, Besozzi G, Bevilacqua N, Kirsten D, Centis R, Lange C; TBNET Study Group. A retrospective TBNET assessment of linezolid safety, tolerability and efficacy in multidrug-resistant tuberculosis. Eur Respir J. 2009 Aug;34(2):387-93. doi: [https://doi.org/10.1183/09031936.00009509 10.1183/09031936.00009509]. Epub 2009 Mar 12. PMID: [https://pubmed.ncbi.nlm.nih.gov/19282348/ 19282348].</ref> |
|||
** <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) |
|||
[[Category:Antibiotics]] |
[[Category:Antibiotics]] |
||
Revision as of 18:13, 18 September 2022
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 time[2]
- <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)
- ↑ Lan Z, Ahmad N, Baghaei P, Barkane L, Benedetti A, Brode SK, Brust JCM, Campbell JR, Chang VWL, Falzon D, Guglielmetti L, Isaakidis P, Kempker RR, Kipiani M, Kuksa L, Lange C, Laniado-Laborín R, Nahid P, Rodrigues D, Singla R, Udwadia ZF, Menzies D; Collaborative Group for the Meta-Analysis of Individual Patient Data in MDR-TB treatment 2017. Drug-associated adverse events in the treatment of multidrug-resistant tuberculosis: an individual patient data meta-analysis. Lancet Respir Med. 2020 Apr;8(4):383-394. doi: 10.1016/S2213-2600(20)30047-3. Epub 2020 Mar 17. PMID: 32192585; PMCID: PMC7384398.
- ↑ Migliori GB, Eker B, Richardson MD, Sotgiu G, Zellweger JP, Skrahina A, Ortmann J, Girardi E, Hoffmann H, Besozzi G, Bevilacqua N, Kirsten D, Centis R, Lange C; TBNET Study Group. A retrospective TBNET assessment of linezolid safety, tolerability and efficacy in multidrug-resistant tuberculosis. Eur Respir J. 2009 Aug;34(2):387-93. doi: 10.1183/09031936.00009509. Epub 2009 Mar 12. PMID: 19282348.
