IntravenousCommunity-acquired pneumonia, Complicated skin and skin structure infections, Nosocomial pneumoniaAdult: 600 mg 12 hrly for 10-14 days.
Child: <7 days 10 mg/kg 12 hrly, may increase to 10 mg/kg 8 hrly depending on clinical response; 7 days to 11 yr 10 mg/kg 8 hrly; ≥12 yr 600 mg 12 hrly. All doses to be taken for 10-14 days.
Elderly: No dosage adjustment needed.
IntravenousMethicillin-resistant Staphylococcus aureus infectionsAdult: 600 mg bid for 7-21 days.
Elderly: No dosage adjustment needed.
IntravenousVancomycin-resistant Enterococcus faeciumAdult: 600 mg 12 hrly for 14-28 days.
Child: <7 days 10 mg/kg 12 hrly, may increase to 10 mg/kg 8 hrly depending on clinical response; 7 days to 11 yr 10 mg/kg 8 hrly; ≥12 yr 600 mg 12 hrly. All doses to be taken for 14-28 days.
Elderly: No dosage adjustment needed.
OralUncomplicated skin and skin structure infectionsAdult: 400 mg 12 hrly for 10-14 days.
Child: <5 yr 10 mg/kg 8 hrly; 5-11 yr 10 mg/kg 12 hrly; ≥12 yr 600 mg 12 hrly. All doses to be taken for 10-14 days.
Elderly: No dosage adjustment needed.
OralCommunity-acquired pneumonia, Complicated skin and skin structure infections, Nosocomial pneumoniaAdult: 600 mg 12 hrly for 10-14 days.
Child: <7 days 10 mg/kg 12 hrly, may increase to 10 mg/kg 8 hrly depending on clinical response; 7 days to 11 yr 10 mg/kg 8 hrly; ≥12 yr 600 mg 12 hrly. All doses to be taken for 10-14 days.
Elderly: No dosage adjustment needed.
OralVancomycin-resistant Enterococcus faeciumAdult: 600 mg 12 hrly for 14-28 days.
Child: <7 days 10 mg/kg 12 hrly, may increase to 10 mg/kg 8 hrly depending on clinical response; 7 days to 11 yr 10 mg/kg 8 hrly; ≥12 yr 600 mg 12 hrly. All doses to be taken for 14-28 days.
Elderly: No dosage adjustment needed.
OralMethicillin-resistant Staphylococcus aureus infectionsAdult: 600 mg bid for 7-21 days.
Elderly: No dosage adjustment needed.
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No dosage adjustment needed.
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Mild to moderate: No dosage adjustment needed.
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May be taken with or without food.
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Granules for oral susp: Add 123 mL of water in 2 equal aliquots and shake well after each addition to make 150 mL susp. Gently invert the bottle a few times before use. Do not shake after reconstitution.
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Y-site incompatibility: Diazepam, amphotericin B, phenytoin, chlorpromazine, pentamidine.
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Unless facilities for close observation and BP monitoring, avoid use in patients w/ uncontrolled HTN, pheochromocytoma, thyrotoxicosis, carcinoid syndrome, bipolar depression, schizoaffective disorder, acute confusional states. Patients w/ gm-ve bacterial infections. Concomitant use w/ MAOI or w/in 2 wk of discontinuing MAOI; SSRIs, TCAs, selective serotonin- and norepinephrine-reuptake inhibitors (SNRIs), or other serotonergic drugs (e.g. bupropion, vilazodone, mirtazapine, amoxapine, buspirone, maprotiline, meperidine, trazodone, nefazodone), dopamine, dobutamine, epinephrine, norepinephrine, pseudoephedrine.
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Patients w/ pre-existing myelosuppression, history of seizure, DM, phenylketonuria, mixed (gm+ve and gm-ve) infections. Severe renal impairment. Pregnancy and lactation.
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Reversible myelosuppression (e.g. leucopenia, thrombocytopenia, anaemia, pancytopenia); headache, fever, convulsions and seizures, rashes, dizziness, nausea and vomiting, metallic taste, insomnia, constipation, diarrhoea, abdominal pain, skin disorder, cough, pharyngitis, upper resp tract infection, visual impairment (e.g. changes in visual acuity or color vision, visual field defect or blurred vision), peripheral and optic neuropathy which progress to loss of vision, lactic acidosis, oral and vaginal candidiasis, superficial teeth and tongue discoloration and abnormal LFT.
Potentially Fatal: Serotonin syndrome; transient ischaemic attacks, Stevens-Johnson syndrome.
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Monitor CBC wkly. Monitor visual function in patients on extended therapy (≥3 mth) or in patients w/ new visual symptoms.
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May reduce serum levels w/ rifampicin and phenytoin. May cause hypoglycaemia w/ insulin or oral antidiabetics. May increase risk of seizures w/ tramadol.
Potentially Fatal: Increased risk of serotonin syndrome w/ MAOIs, SSRIs, TCAs, SNRIs or other serotonergic drugs (e.g. bupropion, vilazodone, mirtazapine, amoxapine, buspirone, maprotiline, meperidine, trazodone, nefazodone). Significant increase in BP w/ vasopressive agents (e.g. epinephrine, norepinephrine), sympathomimetic agents (e.g. pseudoephedrine) and dopaminergic agents (e.g. dopamine, dobutamine).
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May increase the risk of hypertensive crisis w/ beverages and foods rich in tyramine content. Supplements w/ high tryptophan, caffeine, phenylalanine and tyrosine content may increase the risk of hypertensive crisis and serotonin syndrome. May increase CNS depressant effect w/ alcohol.
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Description: Linezolid is a bacteriostatic oxazolidinone which acts by inhibiting ribosomal protein synthesis. It is active against gm+ve bacteria including vancomycin-resistant enterococci and MRSA. It has limited in vitro activity against gm-ve bacteria.
Pharmacokinetics:
Absorption: Rapidly and extensively absorbed after oral admin. Absolute bioavailability: Approx 100%. Time to peak plasma concentration: 1-2 hr but reduced when administered w/ high-fat meal.
Distribution: Readily distributed into well-perfused tissues; lungs, fats, bone, skin blister fluids, muscle and into the CSF. Volume of distribution: 40-50 L. Plasma protein binding: Approx 31%.
Metabolism: Undergoes hepatic metabolism via oxidation to its 2 inactive metabolites (hydroxyethyl glycine and the aminoethoxyacetic acid metabolite).
Excretion: Via urine (approx 30% as parent drug and approx 50% as metabolites); faeces (approx 9% as metabolites). Elimination half-life: Approx 5-7 hr.
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Store at 25°C. Reconstituted oral susp should be used w/in 21 days. Protect from light.
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Anon. Linezolid. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 30/10/2013. Buckingham R (ed). Linezolid. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 30/10/2013. Joint Formulary Committee. Linezolid. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 30/10/2013. McEvoy GK, Snow EK, Miller J et al (eds). Linezolid. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 30/10/2013. Zyvox (Pharmacia and Upjohn Company). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 30/06/2014. Zyvox 2 mg/mL Solution for Infusion (Pharmacia Ltd.). U.S. FDA. https://www.fda.gov/. Accessed 16/10/2013.
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