Overview
11 DESCRIPTION Linezolid for Oral Suspension contains linezolid, which is a synthetic antibacterial agent of the oxazolidinone class. The chemical name for linezolid is N-[[(S)-3-(3-Fluoro-4-morpholinophenyl)-2-oxo-5-ox- azolidinyl]methyl] acetamide. The molecular formula is C 16 H 20 FN 3 O 4 . Its molecular weight is 337.
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action Linezolid is an antibacterial drug [see Microbiology ( 12.4 )] . 12.2 Pharmacodynamics In a randomized, positive- and placebo-controlled crossover thorough QT study, 40 healthy subjects were administered a single linezolid 600 mg dose via a 1 hour IV infusion, a single linezolid 1,200 mg dose via a 1 hour IV infusion, placebo, and a single oral dose of positive control. At both the 600 mg and 1,200 mg linezolid doses, no significant effect on QTc interval was detected at peak plasma concentration or at any other time. 12.3 Pharmacokinetics The mean pharmacokinetic parameters of linezolid in adults after single and multiple oral and intravenous doses are summarized in Table 8.
Indications
- 1 INDICATIONS AND USAGE 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. 3); Uncomplicated skin and skin structure infections ( 1. 4); Vancomycin-resistant Enterococcus faecium infections. ( 1. 5) Limitations of Use ( 1.
Common Doses
- 10 mg
- 600 mg
- 400 mg
- 123 mL
Dosage
2 DOSAGE AND ADMINISTRATION 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...
Contraindications
- 4 CONTRAINDICATIONS • 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 ) 4.1 Hypersensitivity Linezolid formulations are contraindicated for use in patients who have known hypersensitivity to linezolid or any of the other product components . 4.2 Monoamine Oxidase Inhibitors Linezolid should not be used in patients taking any medicinal product which inhibits monoamine oxidases A or B (e.g.
Side Effects
- 6 ADVERSE REACTIONS 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 ()]...
Interactions
- 7 DRUG INTERACTIONS Monoamine oxidase inhibitors and potential for interaction with adrenergic and serotonergic agents. ( 4.2 , 5.3 , 5.6 , 7 , 12.3 ) 7.1 Monoamine Oxidase Inhibitors Linezolid is a reversible, nonselective inhibitor of monoamine oxidase [see Contraindications ( 4.2 ) and Clinical Pharmacology ( 12.3 )]. 7.2 Adrenergic and Serotonergic Agents Linezolid has the potential for interaction with adrenergic and serotonergic agents [see Warnings and Precautions ( 5.3 , 5.6 ) and Clinical Pharmacology ( 12.3 )] .