Linezolid - Linezolid tablet, Film Coated
(Linezolid)Linezolid - Linezolid tablet, Film Coated Prescribing Information
Linezolid tablets are indicated for the treatment of infections caused by susceptible strains of the designated microorganisms in the specific conditions listed below. Linezolid tablets are not indicated for the treatment of Gram-negative infections. It is critical that specific Gram-negative therapy be initiated immediately if a concomitant Gram-negative pathogen is documented or suspected [
| Dosage, Route, and Frequency of Administration | |||
| Infection | Pediatric Patients | Adults and Adolescents | Duration (days) |
| Nosocomial pneumonia | 10 mg/kg oral every 8 hours | 600 mg oral every 12 hours | 10 to 14 |
| Community-acquired pneumonia, including concurrent bacteremia | |||
| Complicated skin and skin structure infections | |||
| Vancomycin-resistant Enterococcus faecium infections, including concurrent bacteremia | 10 mg/kg oral every 8 hours | 600 mg 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 |
Linezolid tablets 600 mg are available as “White to off white, oval shaped, film-coated tablets debossed with “L340” on one side and plain on the other side.
Linezolid was not teratogenic in mice, rats, or rabbits at exposure levels 6.5-fold (in mice), equivalent to (in rats), or 0.06-fold (in rabbits) the expected human exposure level, based on AUCs. However, embryo and fetal toxicities were seen (
In mice, embryo and fetal toxicities were seen only at doses that caused maternal toxicity (clinical signs and reduced body weight gain). A dose of 450 mg/kg/day (6.5-fold the estimated human exposure level based on AUCs) correlated with increased postimplantational embryo death, including total litter loss, decreased fetal body weights, and an increased incidence of costal cartilage fusion.
In rats, mild fetal toxicity was observed at 15 and 50 mg/kg/day (exposure levels 0.22-fold to approximately equivalent to the estimated human exposure, respectively, based on AUCs). The effects consisted of decreased fetal body weights and reduced ossification of sternebrae, a finding often seen in association with decreased fetal body weights. Slight maternal toxicity, in the form of reduced body weight gain, was seen at 50 mg/kg/day.
In rabbits, reduced fetal body weight occurred only in the presence of maternal toxicity (clinical signs, reduced body weight gain and food consumption) when administered at a dose of 15 mg/kg/day (0.06-fold the estimated human exposure based on AUCs).
When female rats were treated with 50 mg/kg/day (approximately equivalent to the estimated human exposure based on AUCs) of linezolid during pregnancy and lactation, survival of pups was decreased on postnatal days 1 to 4. Male and female pups permitted to mature to reproductive age, when mated, showed an increase in preimplantation loss.
· 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. (4.2)
· Myelosuppression: Monitor complete blood counts weekly. 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: 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)
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· Potential interactions producing elevation of blood pressure: monitor blood pressure. (5.6)
· Hypoglycemia: Postmarketing cases of symptomatic hypoglycemia have been reported in patients with diabetes mellitus receiving insulin or oral hypoglycemic agents. (5.9)