pharmacopeia
GET
/api/v1/drug/linezolid
2D structure
N-[[(5S)-3-(3-fluoro-4-morpholin-4-ylphenyl)-2-oxo-1,3-oxazolidin-5-yl]methyl]acetamide
SMILES CC(=O)NC[C@H]1CN(C(=O)O1)C2=CC(=C(C=C2)N3CCOCC3)F
InChIKey TYZROVQLWOKYKF-ZDUSSCGKSA-N

Mechanism of action

Sourced from openFDA

Linezolid is an antibacterial drug [see Microbiology ( 12.4 )] .

Monoamine OxidaseProtein Synthesis

Indications

Sourced from openFDA
  • Linezolid for Oral Suspension is an oxazolidinone-class antibacterial indicated in adults and children for the treatment of the following infections caused by susceptible Gram-positive bacteria: Nosocomial pneumonia ( 1.1 ); Community-acquired pneumonia ( 1. 2); Complicated skin and skin structure infections, including diabetic foot infections, without concomitant osteomyelitis ( 1.ICD-10: J18.9

Contraindications

Sourced from openFDA
  • • Known hypersensitivity to linezolid or any of the other product components. ( 4.1 ) • Patients taking any monoamine oxidase inhibitors (MAOI) or within two weeks of taking an MAOI.contraindicated

Dosage & administration

Sourced from openFDA

Dosage, Route, and Frequency of Administration Infection Pediatric Patients (Birth through 11 years of age) Adults and Adolescents (12 years and older) Duration (Days) Nosocomial pneumonia Community-acquired pneumonia, including concurrent bacteremia 10 mg/kg intravenous or oral every 8 hours 600 mg intravenous or oral every 12 hours 10 to 14 Complicated skin and skin structure infections Vancomycin-resistant Enterococcus faecium infections, including concurrent bacteremia 10 mg/kg intravenous or oral every 8 hours 600 mg intravenous or oral every 12 hours 14 to 28 Uncomplicated skin and skin structure infections less than 5 yrs: 10 mg/kg oral every 8 hours 5 to 11 yrs: 10 mg/kg oral every 12 hours Adults: 400 mg oral every 12 hours Adolescents: 600 mg oral every 12 hours 10 to 14 2.1 General Dosage and Administration The recommended dosage for linezolid formulations for the treatment of infections is described in Table 1. Table 1. Dosage Guidelines for Linezolid Infection Due to the designated pathogens [see Indications and Usage ( 1 )]. Dosage, Route, and Frequency of Administration Recommended Duration of Treatment (Consecutive Days) Pediatric Patients Neonates less than 7 days: Most pre-term neonates less than 7 days of age (gestational age less than 34 weeks) have lower systemic linezolid clearance values and larger AUC values than many full-term neonates and older infants. These neonates should be initiated with a dosing regimen of 10 mg/kg every 12 hours.

Warnings & precautions

Sourced from openFDA

• Myelosuppression: Monitor complete blood counts weekly. Thrombocytopenia has been reported more often in patients with severe renal and in patients with moderate to severe hepatic impairment. Consider discontinuation in patients who develop or have worsening myelosuppression. ( 5.1 ) • Peripheral and Optic Neuropathy: Reported primarily in patients treated for longer than 28 days. If patients experience symptoms of visual impairment, prompt ophthalmic evaluation is recommended. ( 5.2 ) • Serotonin Syndrome: Monitor patients taking serotonergic agents, including antidepressants and opioids, for signs of serotonin syndrome. Patients taking serotonergic antidepressants should receive linezolid only if no other therapies are available. Discontinue serotonergic antidepressants and monitor patients for signs and symptoms of both serotonin syndrome and antidepressant discontinuation. ( 5.3 ) • A mortality imbalance was seen in an investigational study in linezolid‑treated patients with catheter-related bloodstream infections. ( 5.4 ) • Clostridioides difficile- Associated Diarrhea: Evaluate if diarrhea occurs. ( 5.5 ) • Potential interactions producing elevation of blood pressure: monitor blood pressure. ( 5.6 ) • Rhabdomyolysis: If signs or symptoms of rhabdomyolysis are observed, discontinue linezolid and initiate appropriate therapy. ( 5.9 ) • Hypoglycemia: Postmarketing cases of symptomatic hypoglycemia have been reported in patients with diabetes mellitus receiving insulin or oral hypoglycemic agents.

Adverse reactions

Sourced from openFDA

Most common adverse reactions (>5% of adult and/or pediatric patients treated with linezolid) include: diarrhea, vomiting, headache, nausea, and anemia. ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact Hikma Pharmaceuticals USA Inc. at 1-800-962-8364 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. The following clinically significant adverse reactions are described elsewhere in the labeling: Myelosuppression [see Warnings and Precautions ()] Peripheral and Optic Neuropathy [see Warnings and Precautions ()] Serotonin Syndrome [see Warnings and Precautions ()] Clostridioides difficile -Associated Diarrhea [see Warnings and Precautions ()] Lactic Acidosis [see Warnings and Precautions ()] Convulsions [see Warnings and Precautions ()] Rhabdomyolysis [see Warnings and Precautions ()] Hypoglycemia [see Warnings and Precautions ()] Hyponatremia and/or Syndrome of Inappropriate Antidiuretic Hormone Secretion (SIADH) [see Warnings and Precautions ()] 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Adults : The safety of linezolid formulations was evaluated in 2,046 adult patients enrolled in seven Phase 3 comparator-controlled clinical trials, who were treated for up to 28 days.

Use in specific populations

Sourced from openFDA

8.1 Pregnancy Risk Summary Available data from published and postmarketing case reports with linezolid use in pregnant women have not identified a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. When administered during organogenesis, linezolid did not cause malformations in mice, rats, or rabbits at maternal exposure levels approximately 6.5 times (mice), equivalent to (rats), or 0.06 times (rabbits) the clinical therapeutic exposure, based on AUCs. However, embryo-fetal lethality was observed in mice at 6.5 times the estimated human exposure. When female rats were dosed during organogenesis through lactation, postnatal survival of pups was decreased at doses approximately equivalent to the estimated human exposure based on AUCs ( see Data ) . The background risk of major birth defects and miscarriage for the indicated populations is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively. Data Animal Data : In mice, embryo-fetal toxicities were observed only at doses that caused maternal toxicity (clinical signs and reduced body weight gain).

Pharmacokinetics

Sourced from openFDA
Metabolism
The mean pharmacokinetic parameters of linezolid in adults after single and multiple oral and intravenous doses are summarized in Table 8. Plasma concentrations of linezolid at steady-state after oral doses of 600 mg given every 12 hours are shown in Figure 1.

Overdosage

Sourced from openFDA

In the event of overdosage, supportive care is advised, with maintenance of glomerular filtration. Hemodialysis may facilitate more rapid elimination of linezolid. In a Phase 1 clinical trial, approximately 30% of a dose of linezolid was removed during a 3-hour hemodialysis session beginning 3 hours after the dose of linezolid was administered. Data are not available for removal of linezolid with peritoneal dialysis or hemoperfusion. Clinical signs of acute toxicity in animals were decreased activity and ataxia in rats and vomiting and tremors in dogs treated with 3,000 mg/kg/day and 2,000 mg/kg/day, respectively.

Approval history

Sourced from openFDA
  • Apr 18, 2000NDANDA021131Pfizer
  • Apr 18, 2000NDANDA021130Pfizer
  • Apr 18, 2000NDANDA021132Pfizer
  • Jun 3, 2015ANDAANDA200068Hikma
  • Jun 18, 2015NDANDA206473Hospira
  • Jul 16, 2015ANDAANDA200904Sandoz
  • Dec 21, 2015ANDAANDA204239Hetero Labs Ltd V
  • Dec 21, 2015ANDAANDA205517Alkem Labs Ltd

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
28,882 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Off Label Use2,5198.7%
  2. 2Thrombocytopenia2,1277.4%
  3. 3Drug Ineffective2,0447.1%
  4. 4Anaemia1,6745.8%
  5. 5Drug Interaction1,4204.9%
  6. 6Nausea1,3494.7%
  7. 7Vomiting1,0913.8%
  8. 8Platelet Count Decreased1,0313.6%
  9. 9Diarrhoea1,0253.5%
  10. 10Pyrexia1,0083.5%
  11. 11Lactic Acidosis9863.4%
  12. 12Neuropathy Peripheral9613.3%
  13. 13Acute Kidney Injury9073.1%
  14. 14Serotonin Syndrome9043.1%
  15. 15Pancytopenia8893.1%

Literature

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Recent PubMed references pinned to Linezolid as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 222 ClinicalTrials.gov registrations naming Linezolid as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Structural analogs

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Ranked by 2D fingerprint (Tanimoto) similarity over PubChem structures. Structural proximity only — not a claim of therapeutic equivalence.

Frequently asked questions

How does Linezolid work?
Linezolid is an antibacterial drug [see Microbiology ( 12.4 )] .
What is Linezolid used for?
According to FDA labeling, Linezolid carries indications including: Linezolid for Oral Suspension is an oxazolidinone-class antibacterial indicated in adults and children for the treatment of the following infections caused by susceptible Gram-positive bacteria: Nosocomial pneumonia ( 1.1 ); Community-acquired pneumonia ( 1. 2); Complicated skin and skin structure infections, including diabetic foot infections, without concomitant osteomyelitis ( 1.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Linezolid?
Linezolid is classified as Other antibacterials, Oxazolidinone Antibacterial, Monoamine Oxidase Inhibitors, Protein Synthesis Inhibitors, Decreased Protein Synthesis.
What are the brand names for Linezolid?
Linezolid is marketed under brand names including Zyvox.
What are the contraindications for Linezolid?
Linezolid labeling lists contraindications including: • Known hypersensitivity to linezolid or any of the other product components. ( 4.1 ) • Patients taking any monoamine oxidase inhibitors (MAOI) or within two weeks of taking an MAOI.. Always consult the full prescribing information and a clinician.
Note. Data for linezolid is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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