Linezolid


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intravenous
Community-acquired pneumonia, Complicated skin and skin structure infections, Nosocomial pneumonia
Adult: 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.

Intravenous
Methicillin-resistant Staphylococcus aureus infections
Adult: 600 mg bid for 7-21 days.
Elderly: No dosage adjustment needed.

Intravenous
Vancomycin-resistant Enterococcus faecium
Adult: 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.

Oral
Uncomplicated skin and skin structure infections
Adult: 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.

Oral
Community-acquired pneumonia, Complicated skin and skin structure infections, Nosocomial pneumonia
Adult: 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.

Oral
Vancomycin-resistant Enterococcus faecium
Adult: 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.

Oral
Methicillin-resistant Staphylococcus aureus infections
Adult: 600 mg bid for 7-21 days.
Elderly: No dosage adjustment needed.
Renal Impairment
No dosage adjustment needed.
Hepatic Impairment
Mild to moderate: No dosage adjustment needed.
Cách dùng
May be taken with or without food.
Hướng dẫn pha thuốc
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.
Tương kỵ
Y-site incompatibility: Diazepam, amphotericin B, phenytoin, chlorpromazine, pentamidine.
Chống chỉ định
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.
Thận trọng
Patients w/ pre-existing myelosuppression, history of seizure, DM, phenylketonuria, mixed (gm+ve and gm-ve) infections. Severe renal impairment. Pregnancy and lactation.
Phản ứng phụ
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.
IV/Parenteral/PO: C
MonitoringParameters
Monitor CBC wkly. Monitor visual function in patients on extended therapy (≥3 mth) or in patients w/ new visual symptoms.
Tương tác
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).
Food Interaction
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.
Tác dụng
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.
Bảo quản
Store at 25°C. Reconstituted oral susp should be used w/in 21 days. Protect from light.
Phân loại MIMS
References
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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  • Linid
  • Lizolid
  • Macdin
  • Zyvox
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