DESCRIPTION:
Nirzolid I.V. Injection contains linezolid, which is a synthetic antibacterial agent of the oxazolidinone class. The chemical name for linezolid is (S)-N-[[3-[3-Fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl] methyl]-acetamide.

The empirical formula is C16H20FN3O4. Its molecular weight is 337.35, Nirzolid I.V. Injection is supplied as a ready-to-use sterile isotonic solution for intravenous infusion.

Each mL contains 2 mg of linezolid. Inactive ingredients are Sodium Citrate, Citric Acid, and Glucose in an aqueous vehicle for intravenous administration. The sodium (Na+) content is 0.422 mg/ml.

COMPOSITION:

Each 100ml contains:
Linezolid 200 mg
Dextrose (As Anhydrous) 5% w/v
Water for Injections q. s.

AVAILABILITY:

Linezolid I.V. 200 mg/100 ml
Domestic Export Yes Domestic Product insert
Linezolid I.V. 600 mg/300 ml
Domestic Yes Export Yes Domestic Product insert

INDICATIONS AND USAGE:

Nirzolid Injection is indicated in the treatment of the following infections caused by susceptible strains of the designated microorganisms.

Vancomycin-Resistant Enterococcus faecium infections, including cases with concurrent bacteremia.
Nosocomial pneumonia caused by Staphylococcus aureus (methicillin-susceptible and -resistant strains), or Streptococcus pneumoniae (including multi-drug resistant strains [MDRSP]).

Complicated skin and skin structure infections, including diabetic foot infections, without concomitant osteomyelitis, caused by Staphylococcus aureus (methicillin-susceptible and resistant strains), treptococcus pyogenes, or Streptococcus agalactiae. Linezolid has not been studied in the treatment of decubitus ulcers.

Uncomplicated skin and skin structure infections caused by Staphylococcus aureus (methicillin- usceptible only) or Streptococcus pyogenes.

Community-acquired pneumonia caused by Streptococcus pneumoniae, including cases with concurrent bacteremia, or Staphylococcus aureus

WARNING:

Myelosuppression (including anemia, leukopenia, pancytopenia, and thrombocytopenia) has been reported in patients receiving linezolid. In cases where the outcome is known, when linezolid was discontinued, the a_ected hematologic parameters have risen toward pretreatment levels.

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. Discontinuation of therapy with linezolid should be considered in patients who develop or have worsening myelosuppression.

PRECAUTIONS:

Lactic Acidosis – Lactic acidosis has been reported with the use of Linezolid. In reported cases, patients experienced repeated episodes of nausea and vomiting. Patients who develop recurrent nausea or vomiting, unexplained acidosis, or low bicarbonate level while receiving Linezolid should receive immediate medical evaluation.

Serotonin Syndrome – Spontaneous reports of serotonin syndrome associated with the co-administration of Linezolid and serotonergic agents, including antidepressants such as selective serotonin reuptake inhibitors (SSRIs), have been reported.

Where administration of Linezolid and concomitant serotonergic agents is clinically appropriate, patients should be closely observed for signs and symptoms of serotonin syndrome such as cognitive dysfunction, hyperpyrexia, hyperpyrexia and incoordination. If signs or symptoms occur physicians should consider discontinuation of either one or both agents. If the concomitant serotonergic agent is withdrawn, discontinuation symptoms can be observed.

Peripheral and Optic Neuropathy – Peripheral and optic neuropathy have been reported in patients treated with Linezolid, primarily those patients treated for longer than the maximum recommended duration of 28 days. In cases of optic neuropathy that progressed to loss of vision, patients were treated for extended periods beyond the maximum recommended duration. Visual blurring has been reported in some patients treated with Linezolid for less than 28 days.

DOSAGE AND ADMINISTRATION:

Infection

Dosage and Route of Administration

Recommended Duration

of Treatment (consecutive days)

Pediatric Patients

(Birth through 11 Years of Age)

Adults and Adolescents

(12 Years and Older)

Complicated skin and

skin structure infections

Community-acquired pneumonia,

including concurrent bacteremia

Nosocomial pneumonia

10 mg/kg IV or oral‡ q8h 600 mg IV or oral‡ q12h 10 to 14
Vancomycin-resistant

Enterococcus faecium infections, including concurrent bacteremia

10 mg/kg IV or oral‡ q8h 600 mg IV or oral‡ q12h 14 to 28
Uncomplicated skin and

skin structure infections

<5 yrs: 10 mg/kg oral‡ q8h

5-11 yrs: 10 mg/kg oral‡ q12h

Adults: 400 mg oral‡ q12h

Adolescents: 600 mg oral‡ q12h

10 to 14

Adult patients with infection due to MRSA should be treated with Linezolid 600 mg q12h.

However, pediatric patients exhibit wider variability in linezolid clearance and systemic exposure (AUC) compared with adults. In pediatric patients with a sub-optimal clinical response, particularly those with pathogens with MIC of 4 μg/mL, lower systemic exposure, site and severity of infection, and the underlying medical condition should be considered when assessing clinical response

Total treatment duration was determined by the treating physician based on site and severity of the infection, and on the patient’s clinical response.

PRESENTATION:

100 ml Bottle (200 mg Linezolid)
300 ml Bottle (600 mg Linezolid)