Linzowel

Each film-coated tablet contains: Linezolid 600 mg.

Pharmacology: Pharmacokinetics: Linezolid is rapidly and extensively absorbed after oral doses and maximum plasma concentrations are achieved after 1 to 2 hours. It is about 31% bound to plasma proteins. Linezolid is reported to be distributed into bone, fat, lungs, muscle, skin blister fluids, and into CSF. It is metabolised mainly by oxidation to 2 main inactive metabolites, the hydroxyethyl glycine metabolite (PNU-142586) and the aminoethoxyacetic acid metabolite (PNU-1423000) other minor inactive metabolites have also been identified. About 40% of a dose is excreted in the urine as PNU-142586, 30% as Linezolid, and 10% as PNU-142300. Small amounts of metabolite are excreted in the feces. The elimination half-life of Linezolid is about 5 to 7 hours.

Linezolid is an oxazolidinone antibacterial used for the treatment of Gram-positive infections of the skin and respiratory tract, including those due to vancomycin-resistant enterococci and methicillin-resistant Staphylococcus aureus.

It is given by mouth in usual adult dose of 600 mg every 12 hours for 10 to 14 days treatment for up to 28 days may be necessary if there is vancomycin resistance. In uncomplicated skin and skin structure infections a dose of 400 mg by mouth every 12 hours for 10 to 14 days is usually sufficient. Children have more rapid clearance of Linezolid than adults.
Duration of treatment is the same as that for adults but with a basic regimen for those aged 7 days to 12 years of 10 mg/kg every 8 hours by mouth or intravenously neonates up to 7 days old should be given 10 mg/kg every 12 hours, although 8-hourly dosing may be considered if the clinical response is sub-optimal. For uncomplicated skin and skin structure oral doses every 12 hours are sufficient in those aged 5 to 11 years. Or as prescribed by the physician.

Linezolid should be used with caution in patients with renal impairment (creatinine clearance less than 30 mL/minute).
Although no dosage adjustment is required licensed product information states that the peak plasma concentrations of Linezolid's two major metabolites were about ten fold higher in such patients after several days of treatment. As about 30% of a dose is removed during 3 hours of hemodialysis it is recommended that Linezolid should be given after dialysis.

The adverse effects most frequently reported in patients receiving Linezolid include diarrhea, nausea and vomiting, metallic taste, headache, insomnia, constipation, rashes, dizziness, fever, oral and vaginal candidiasis, and abnormal liver function tests. Lactic acidosis has been reported. There have been rare reports of bullous skin eruptions including Stevens-Johnson syndrome. Peripheral and optic neuropathy, sometimes progressing to loss of vision, have occurred rarely, mainly in patients receiving Linezolid for more than 28 days. Visual blurring has been reported in some patients who received less than 28 days of treatment. Reversible myelosuppresson including anemia, leukopenia, pancytopenia and, in particular, thrombocytopenia has been reported and blood counts should be monitored weekly in patients receiving Linezolid. Patients particularly at risk are those who have received Linezolid for more than 10 to 14 days, who are receiving other bone marrow suppressant drugs, or who have pre-existing myelosuppression or severe renal impairment.
Effects on blood: Reversible myelosuppression with red cell hypoplasia occurred in 3 patients treated with Linezolid.
Features of the myelosuppression were considered by some to be similar to those associated with chloramphenicol, although this was disputed by the manufacturers. There have been reports of thrombocytopenia occurring at a higher incidence than that reported by the manufacturers in one study, 6 of 19 patients who had been treated with Linezolid developed thrombocytopenia while another found that it occurred in 23 of 48 patients who had received the drug for more than 45 days.
Effects on the nervous system: Linezolid treated patient with new visual symptoms should be evaluated promptly and referred to an ophthalmologist if necessary regular monitoring is advised in all patients who may require treatment for more than 28 days.

Linezolid is reversible, nonselective Monoamine Oxidase Inhibitor (MAOI's) and therefore has the potential to interact with adrenergic and serotonergic drugs. Enhanced pressor activity has reported in patients receiving Linezolid with phenylpropanolamine or pseudoephedrine and initial doses of dopamine or adrenaline should be reduced. There have also been cases of serotonin syndrome when Linezolid was taken with serotonin reuptake inhibitors, and similar symptoms when it was taken with dextromethorpan. The interactions of conventional Monoamine Oxidase Inhibitor (MAOI's) both with other drugs and with foods.

Store at temperatures not exceeding 30°C. Protect from light.

Other Antibiotics

J01XX08 - linezolid ; Belongs to the class of other antibacterials. Used in the systemic treatment of infections.

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