Prescribing Details
Description
Ezolid is a preparation of Linezolid which is a synthetic antibacterial agent belonging to the oxazolidinones class, which has clinical utility in the treatment of infections caused by aerobic Gram-positive bacteria. Linezolid inhibits bacterial protein synthesis through a mechanism of action different from that of other antibacterial agents; therefore, cross resistance between Linezolid and other classes of antibiotics is unlikely. Linezolid binds to a site on the bacterial 23S ribosomal RNA of the 50S subunit and prevents the formation of a functional 70S initiation complex, which is an essential component of the bacterial translation process.
Uses
No Data
Indications
Ezolid is indicated for the treatment of:
- Nosocomial pneumonia
- Community-acquired pneumonia
- Complicated skin and skin structure infection including diabetic foot infections,without concomitant osteomyelitis
- Uncomplicated skin and skin structure infections
- Vancomycin-resistant Enterococcus faecium infections
Limitations of use
Ezolid is not indicated for the treatment of Gram-negative infections. The safety and efficacy of Ezolid given for longer than 28 days have not been evaluated in controlled clinical trials.
Dosage and administration
Route of administration: Ezolid tablets should be taken in oral route with or without food. Ezolid IV infusion should be administered by intravenous infusion over a period of 30 to 120 minutes.
The recommended daily dosage for Ezolid tablets and IV infusion is described in the following table.
| Infection | Dosage, route and frequency of administration | ||
|---|---|---|---|
| Pediatric Patients* (Birth through 11 years of age) | Adults & Adolescents (12 years and older) | Recommended duration of treatment (consecutive days) | |
| Nosocomial pneumonia |
10 mg/kg orally or intravenously every 8 hours |
600 mg orally or intravenously 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 orally or intravenously every 8 hours |
600 mg orally or intravenously every 12 hours |
14 to 28 |
| Uncomplicated skin and skin structure infections | less than 5 years: 10 mg/kg orally every 8 hours 5-11 years: 10 mg/kg orally every 12 hours |
Adults: 400 mg orally every 12 hours Adolescents: 600 mg orally every 12 hours |
10 to 14 |
| *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. Consideration may be given to the use of 10 mg/kg every 8 hours regimen in neonates with a sub-optimal clinical response. All neonatal patients should receive 10 mg/kg every 8 hours by 7 days of life. | |||
No dose adjustment is necessary when switching from intravenous to oral administration.
Intravenous administration
Ezolid IV infusion should be inspected visually against a light source for particulate matter prior to administration. Ezolid IV infusion may exhibit a yellow color that can intensify over time without adversely affecting potency. Do not use this intravenous infusion vial in series connections. Additives should not be introduced into this solution. Discard unused portion after single use.
Hepatic impairment
No dose adjustment is recommended for patients with mild-to-moderate hepatic impairment. The pharmacokinetics of Ezolid in patients with severe hepatic impairment have not been evaluated.
Use in pregnancy & lactation
Pregnancy: Available data with linezolid use in pregnant women have not identified a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes. Linezolid should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Lactation: Linezolid is present in breast milk. The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for linezolid and any potential adverse effects on the breastfed child from linezolid or from the underlying maternal condition. Advise lactating women to monitor a breastfed infant for diarrhea and vomiting.
Use in children and adolescents
The dose of linezolid for children and adolescents have been described in dose and administration section. The use of linezolid for the empiric treatment of pediatric patients with central nervous system infections is not recommended.
Geriatric use
Precautions
Complete blood counts should be monitored weekly in patients who receive linezolid, particularly in those who receive linezolid for longer than two weeks, those with pre-existing myelosuppression, those receiving concomitant drugs that produce bone marrow suppression or those with a chronic infection who have received previous or concomitant antibiotic therapy. If patients experience symptoms of visual impairment, such as changes in visual acuity, changes in color vision, blurred vision or visual field defect, prompt ophthalmic evaluation is recommended. Linezolid is not approved and should not be used for the treatment of patients with catheter-related bloodstream infections or catheter-site infections. Careful medical history is necessary since Clostridium difficile-associated Diarrhea (CDAD) has been reported to occur over two months after antibiotic administration. If CDAD is suspected or confirmed, ongoing antibiotic use not directed against C. difficile may need to be discontinued. Unless patients are monitored for potential increases in blood pressure, linezolid should not be administered to patients with uncontrolled hypertension, pheochromocytoma, thyrotoxicosis and/or patients taking sympathomimetic agents, vasopressive agents and dopaminergic agents. Patients who develop recurrent nausea or vomiting, unexplained acidosis or low bicarbonate level while receiving linezolid should receive immediate medical evaluation. If hypoglycemia occurs, a decrease in the dose of insulin or oral hypoglycemic agent or discontinuation of oral hypoglycemic agent, insulin or linezolid may be required.
Side effects
The most common side effects are diarrhea, vomiting, headache, nausea, anemia, taste alteration and eosinophilia.
Contraindications
Linezolid is contraindicated in patients with hypersensitivity to linezolid or any other component of this product. It is also contraindicated in patients taking any medicinal product which inhibits monoamine oxidases A or B (e.g., phenelzine, isocarboxazid) or within two weeks of taking any such medicinal product.
Drug interactions
Drug interaction with medication: Linezolid is a reversible, nonselective inhibitor of monoamine oxidase. Therefore, linezolid has the potential for interaction with adrenergic and serotonergic agents. Some individuals receiving linezolid may experience a reversible enhancement of the pressor response to indirect acting sympathomimetic agents, vasopressor or dopaminergic agents. Unless patients are carefully observed for signs and/or symptoms of serotonin syndrome, linezolid should not be administered to patients with carcinoid syndrome and/or patients taking serotonin re-uptake inhibitors, tricyclic antidepressants, serotonin 5-HTI receptor agonists (triptans), meperidine or buspirone.
Drug interaction with food and others: Advice patients to avoid large quantities of foods or beverages with high tyramine content while taking linezolid.
Overdose
In the event of overdosage, supportive care is advised, with maintenance of glomerular filtration. Hemodialysis may facilitate more rapid elimination of linezolid.
Preparation
No Data
Pharmaceutical precautions
Store in a cool and dry place protected from light.
Presentation
Ezolid 400 tablet: Each coated tablet contains Linezolid USP 400 mg.
Ezolid 600 tablet: Each coated tablet contains Linezolid USP 600 mg.
Ezolid 600 IV infusion: Each ml contains Linezolid USP 2 mg.
Package quantities
Storage
Store in a cool (below 30°C ) and dry place protected from the light. Keep away from the reach of children.
Packing
Ezolid 400 tablet: Carton of 10 tablets in blister pack.
Ezolid 600 tablet: Carton of 10 tablets in blister pack.
Ezolid 600 IV infusion: Each pack contains one vial of 300 ml sterile, pyrogen free and isotonic Linezolid solution, one infusion set, one alcohol pad and one first aid bandage.
Ezolid 600 IV infusion manufactured by Popular Pharmaceuticals Ltd. for Advanced Chemical Industries Limited.
