Zoline

• Zoline 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

... Read more Zoline 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: Zoline is not indicated for the treatment of Gram-negative infections. The safety and efficacy of Zoline given for longer than 28 days have not been evaluated in controlled clinical trials.

Linezolid is a synthetic, antibacterial agent belonging to a new class of antibiotics, the oxazolidinones, with in vitro activity against Gram positive aerobic bacteria, some Gram positive anaerobic bacteria and certain Gram negative bacteria. It selectively inhibits bacterial protein synthesis via a mechanism of action different from that of other antibacterial agents. Linezolid binds to the 23S ribosomal RNA of the 50S subunit of the bacterial ribosome and prevents the formation of a functional 70S initiation complex which is an essential component of the bacterial translation process. The results of time-kill studies have shown Linezolid to be bacteriostatic against enterococci and staphylococci. For streptococci, Linezolid was found to be bactericidal for the majority of strains.

Linezolid tablets should be taken in oral route with or without food. Linezolid IV infusion should be administered by intravenous infusion over a period of 30 to 120 minutes. The recommended daily dosage for Linezolid 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 and adolescent (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
• Complicated skin and skin structure infections
• 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 : Linezolid IV infusion should be inspected visually against a light source for particulate matter prior to administration. Linezolid 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 Linezolid in patients with severe hepatic impairment have not been evaluated. 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

Drug interaction with medication : Zoline is a reversible, nonselective inhibitor of monoamine oxidase. Therefore, Zoline has the potential for interaction with adrenergic and serotonergic agents. Some individuals receiving Zoline 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, Zoline should not be administered to patients with carcinoid syndrome and/or patients taking serotonin re-uptake inhibitors, tricyclic antidepressants, serotonin 5-HT1 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 Zoline.

Linezolid formulations are contraindicated for using in patients who have known hypersensitivity to Linezolid or any of the other product components. Linezolid should not be used 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. Linezolid should not be administered to patients with uncontrolled hypertension, pheochromocytoma, thyrotoxicosis, carcinoid syndrome and/or patients taking directly and indirectly acting sympathomimetic agents (e.g. Pseudoephedrine), vasopressive agents (e.g. Epinephrine, Norepinephrine), dopaminergic agents (e.g. Dopamine, Dobutamine), serotonin re-uptake inhibitors, tricyclic antidepressants, serotonin 5-HT1 receptor agonists (triptans), meperidine or buspirone.

Most of the adverse events reported with Zoline were mild to moderate in intensity. The most common adverse events in patients treated with Zoline were diarrhea, headache and nausea. Other adverse events includes oral moniliasis, vaginal moniliasis, hypertension, dyspepsia, localized abdominal pain, pruritus, and tongue discoloration.

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.

Complete blood counts should be monitored weekly in patients who receive Zoline, particularly in those who receive Zoline 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. Zoline 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, Zoline 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 Zoline 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 Zoline may be required.

No cases of overdose have been reported. Symptomatic and supportive care is advised together with maintenance of glomerular filtration. Approximately 30% of a Zoline dose is removed during 3 hours of haemodialysis. No data are available for the removal of Zoline by peritoneal dialysis or haemoperfusion.

Zoline formulations should be stored at room temperature (15°C-30°C), away from light and moisture. All medicines should be kept away from children.