Adult: 600 mg 12 hourly via infusion over 30-120 minutes for 14-28 days. Child: Pre-term neonates <7 days (gestational age <34 weeks) Initially, 10 mg/kg 12 hourly, may consider to increase to 10 mg/kg 8 hourly if with sub-optimal clinical response; 7 days to 11 years 10 mg/kg 8 hourly; ≥12 years Same as adult dose. All doses are given via infusion over 30-120 minutes. Treatment duration: 14-28 days. Treatment recommendations may vary among individual products and between countries (refer to specific product guidelines).
Adult: 600 mg 12 hourly via infusion over 30-120 minutes for 10-14 days. Child: Pre-term neonates <7 days (gestational age <34 weeks) Initially, 10 mg/kg 12 hourly, may consider to increase to 10 mg/kg 8 hourly if with sub-optimal clinical response; 7 days to 11 years 10 mg/kg 8 hourly; ≥12 years Same as adult dose. All doses are given via infusion over 30-120 minutes. Treatment duration: 10-14 days. Treatment recommendations may vary among individual products and between countries (refer to specific product guidelines).
Oral Vancomycin-resistant Enterococcus faecium
Adult: 600 mg 12 hourly for 14-28 days. Child: Pre-term neonates <7 days (gestational age <34 weeks) Initially, 10 mg/kg 12 hourly, may consider to increase to 10 mg/kg 8 hourly if with sub-optimal clinical response; 7 days to 11 years 10 mg/kg 8 hourly; ≥12 years Same as adult dose. Treatment duration: 14-28 days. Treatment recommendations may vary among individual products and between countries (refer to specific product guidelines).
Adult: 600 mg 12 hourly for 10-14 days. Child: Pre-term neonates <7 days (gestational age <34 weeks) Initially, 10 mg/kg 12 hourly, may consider to increase to 10 mg/kg 8 hourly if with sub-optimal clinical response; 7 days to 11 years 10 mg/kg 8 hourly; ≥12 years Same as adult dose. Treatment duration: 10-14 days. Treatment recommendations may vary among individual products and between countries (refer to specific product guidelines).
Oral Uncomplicated skin and skin structure infections
Adult: 400 mg 12 hourly for 10-14 days. Child: <5 years 10 mg/kg 8 hourly; 5-11 years 10 mg/kg 12 hourly; ≥12 years 600 mg 12 hourly. Treatment duration: 10-14 days. Treatment recommendations may vary among individual products and between countries (refer to specific product guidelines).
Administration
May be taken with or without food.
Reconstitution
Oral susp: Loosen the granules by gently tapping the bottle. Reconstitute by adding 123 mL of water in 2 equal portions to make a final concentration of 100 mg/5 mL. Vigorously shake the bottle in between each addition of water to obtain a uniform susp. Prior to administration, invert the bottle gently to mix; do not shake.
Incompatibility
Intravenous:
Physically incompatible in a simulated Y-site administration with diazepam, chlorpromazine hydrochloride, amphotericin B, pentamidine isethionate, erythromycin lactobionate, phenytoin Na, and trimethoprim-sulfamethoxazole. Chemically incompatible with ceftriaxone Na.
Contraindications
Hypersensitivity. Unless facilities are available for close observation and monitoring of blood pressure, avoid linezolid use in patients with uncontrolled hypertension, thyrotoxicosis, phaeochromocytoma, bipolar depression, acute confusional states, or schizoaffective disorder, and/or in patients taking directly and indirectly acting sympathomimetic agents (including adrenergic bronchodilators, pseudoephedrine, and phenylpropanolamine), vasopressive agents (e.g. epinephrine, norepinephrine), and dopaminergic drugs (e.g. dopamine, dobutamine). Unless patients are closely observed for signs and symptoms of serotonin syndrome, linezolid must not be given to those with carcinoid syndrome, and/or patients taking SSRIs, TCAs, serotonin 5-HT1 receptor agonists (triptans), pethidine, bupropion, or buspirone. Concomitant use or within 2 weeks of discontinuing MAOIs.
Special Precautions
Patient with a history of seizures; diabetes mellitus, liver cirrhosis. Not indicated for the treatment of Gram-negative infections and catheter-related systemic infections. If a concomitant Gram-negative pathogen is documented or suspected, specific Gram-negative treatment must be initiated immediately. Severe renal impairment (CrCl <30 mL/min), including those undergoing haemodialysis; severe hepatic impairment. Children. Pregnancy and lactation.
Adverse Reactions
Significant: Myelosuppression, including anaemia, thrombocytopenia, pancytopenia, and leucopenia; peripheral neuropathy and optic neuropathy and neuritis, particularly in patients treated for >28 days; convulsions, lactic acidosis, hyponatraemia, syndrome of inappropriate antidiuretic hormone secretion (SIADH); symptomatic hypoglycaemia, particularly in patients with diabetes mellitus receiving insulin or oral hypoglycaemic agents; fungal or bacterial superinfection (prolonged use). Blood and lymphatic system disorders: Eosinophilia, sideroblastic anaemia. Cardiac disorders: Tachycardia. Ear and labyrinth disorders: Tinnitus. Eye disorders: Blurred vision, changes in visual acuity or colour vision, loss of vision. Gastrointestinal disorders: Diarrhoea, nausea, vomiting, abdominal pain, constipation, dyspepsia, abdominal distention, stomatitis, gastritis, pancreatitis, dry mouth, glossitis, tongue discolouration, taste perversion (metallic taste). Rarely, superficial tooth discolouration. General disorders and administration site conditions: Fever, localised pain, chills, fatigue, increased thirst, inj site pain. Immune system disorders: Anaphylaxis. Infections and infestations: Candidiasis, fungal infections. Investigations: Increased ALT, AST, alkaline phosphatase, total bilirubin, BUN, serum creatinine, lactate dehydrogenase, creatine kinase, serum lipase, amylase, and non-fasting glucose; decreased total protein, albumin, and Ca levels; increased or decreased K or bicarbonate levels. Nervous system disorders: Headache, dizziness, hypoaesthesia, paraesthesia. Psychiatric disorders: Insomnia. Renal and urinary disorders: Renal failure, polyuria. Reproductive system and breast disorders: Vaginitis, vulvovaginal disorder. Skin and subcutaneous tissue disorders: Rash, pruritus, dermatitis, diaphoresis, urticaria, bullous disorders (e.g. Stevens-Johnson syndrome, toxic epidermal necrolysis), angioedema, alopecia. Potentially Fatal:Clostridioides difficile-associated diarrhoea (CDAD), pseudomembranous colitis; serotonin syndrome.
This drug may cause dizziness or visual impairment, if affected, do not drive or operate machinery.
Monitoring Parameters
Perform culture and sensitivity tests; consult local institutional recommendations before treatment initiation due to antibiotic resistance risks. Obtain CBC weekly; closely monitor blood counts in patients at risk of bleeding, with pre-existing myelosuppression or renal impairment, those receiving >2 weeks of therapy or concomitant agents that cause bone marrow suppression. Monitor blood pressure; serum Na levels regularly in patients taking diuretics, at risk of hyponatraemia and/or SIADH, and in the elderly. Perform visual function tests in patients on prolonged therapy or with vision changes. Closely monitor for signs and symptoms of serotonin syndrome and neuropathic adverse effects (e.g. peripheral neuropathy, optic neuritis); signs of bone marrow suppression in patients with renal impairment.
Drug Interactions
May enhance the hypoglycaemic effect of antidiabetic agents. Plasma concentration may be decreased by rifampicin. Potentially Fatal: Increased risk of serotonin syndrome with MAOIs and other serotonergic agents such as SSRIs (e.g. citalopram, fluoxetine, fluvoxamine, paroxetine), serotonin norepinephrine reuptake inhibitors (SNRIs), TCAs, serotonin 5-HT1 receptor agonists (triptans), pethidine, buspirone, and bupropion. May enhance the elevated blood pressure caused by pseudoephedrine, phenylpropanolamine, epinephrine, norepinephrine, dopamine, and dobutamine.
Food Interaction
Avoid consuming large amounts of tyramine-rich foods or beverages (e.g. aged or matured cheese, air-dried or cured meats, fava or broad bean pods, yeast extracts, sauerkraut, soy sauce, red wine, tap or draft beers), and foods rich in dopamine, tyrosine, tryptophan, phenylalanine, or caffeine as these may cause sudden and severe high blood pressure (hypertensive crisis or serotonin syndrome). May increase the risk of serotonin syndrome with St. John's wort.
Action
Description: Linezolid is an oxazolidinone antibacterial agent that selectively inhibits the bacterial protein synthesis by binding to the 23S ribosomal ribonucleic acid (RNA) of the 50S subunit of the bacteria, thereby preventing the formation of a functional 70S initiation complex essential for the bacterial translation process. It is active against Gram-positive bacteria only and has no clinical activity against Gram-negative bacteria. Pharmacokinetics: Absorption: Rapidly and extensively absorbed. Bioavailability: Approx 100% (oral). Time to peak plasma concentration: 1-2 hours (oral). Distribution: Readily distributes into well-perfused tissues, and into CSF. Enters breast milk. Volume of distribution: 0.65 L/kg. Plasma protein binding: 31%. Metabolism: Metabolised in the liver mainly via oxidation of the morpholine ring into 2 inactive metabolites, aminoethoxyacetic acid and hydroxyethyl glycine. Excretion: Via urine (approx 30% as linezolid; approx 50% as metabolites); faeces (approx 9% as metabolites). Elimination half-life: Approx 5-7 hours.
Chemical Structure
Linezolid Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 441401, Linezolid. https://pubchem.ncbi.nlm.nih.gov/compound/441401. Accessed July 26, 2022.
Storage
Tab: Store below 30°C. Protect from light. Oral susp: Store at 25°C. Protect from light and moisture. After reconstitution, store at room temperature and use within 21 days. Solution for infusion: Store at 25°C. Do not freeze. Keep infusion bags in the overwrap until ready to use to protect from light.
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