Linezolid

Indications
Oral
Uncomplicated skin and skin structure infections
Adult: 400 mg every 12 hr for 10-14 days.
Child: Preterm neonates (<34 wk gestational age): 10 mg/kg every 12 hr; may increase to 10 mg/kg every 8 hr if response is suboptimal. By day 7 of life, all neonates should receive 10 mg/kg every 8 hr. Infant (excluding preterm neonates <1 wk) and children <5 yr: 10 mg/kg every 8 hr for 10-14 days. Children 5-11 yr: 10 mg/kg every 12 hr for 10-14 days; 12-18 yr: 600 mg every 12 hr for 10-14 days.
Intravenous
Complicated skin and skin structure infections
Adult: 600 mg 12 hrly for 10-14 days, as an infusion over 30-120 minutes. Similar doses can also be given via oral route.
Child: Preterm neonates (<34 wk gestational age): 10 mg/kg every 12 hr; may increase to 10 mg/kg every 8 hr if response is suboptimal. By day 7 of life, all neonates should receive 10 mg/kg every 8 hr. Infant (excluding preterm neonates <1 wk) and children ≤11 yr: 10 mg/kg every 8 hr for 10-14 days.
CrCl (ml/min)Dosage Recommendation
<30Use with caution.

Intravenous
Community-acquired pneumonia
Adult: 600 mg 12 hrly for 10-14 days, as an infusion over 30-120 minutes. Similar doses can also be given via oral route.
Child: Preterm neonates (<34 wk gestational age): 10 mg/kg every 12 hr; may increase to 10 mg/kg every 8 hr if response is suboptimal. By day 7 of life, all neonates should receive 10 mg/kg every 8 hr. Infant (excluding preterm neonates <1 wk) and children ≤11 yr: 10 mg/kg every 8 hr for 10-14 days.
CrCl (ml/min)Dosage Recommendation
<30Use with caution.

Intravenous
Nosocomial pneumonia
Adult: 600 mg 12 hrly for 10-14 days, as an infusion over 30-120 minutes. Similar doses can also be given via oral route.
Child: Preterm neonates (<34 wk gestational age): 10 mg/kg every 12 hr; may increase to 10 mg/kg every 8 hr if response is suboptimal. By day 7 of life, all neonates should receive 10 mg/kg every 8 hr. Infant (excluding preterm neonates <1 wk) and children ≤11 yr: 10 mg/kg every 8 hr for 10-14 days.
CrCl (ml/min)Dosage Recommendation
<30Use with caution.

Intravenous
Vancomycin-resistant enterococci infections
Adult: 600 mg every 12 hr. Treatment duration for vancomycin-resistant enterococci: 14-28 day. Similar doses can also be given via oral route.
Child: For VRE infections: Preterm neonates (<34 wk gestational age): 10 mg/kg every 12 hr; may increase to 10 mg/kg every 8 hr if response is suboptimal. By day 7 of life, all neonates should receive 10 mg/kg every 8 hr. Infant (excluding preterm neonates <1 wk) and children ≤11 yr: 10 mg/kg every 8 hr for 14-28 days.
Intravenous
Methicillin-resistant Staphylococcus aureus infections
Adult: 600 mg every 12 hr. Treatment duration for vancomycin-resistant enterococci: 14-28 day. Similar doses can also be given via oral route.
Child: For VRE infections: Preterm neonates (<34 wk gestational age): 10 mg/kg every 12 hr; may increase to 10 mg/kg every 8 hr if response is suboptimal. By day 7 of life, all neonates should receive 10 mg/kg every 8 hr. Infant (excluding preterm neonates <1 wk) and children ≤11 yr: 10 mg/kg every 8 hr for 14-28 days.

Reconstitution: To reconstitute granules for oral suspension, add 123 ml in 2 equal aliquots and shake well to make 150 ml suspension.
Contraindications
Hypersensitivity.
Warnings / Precautions
Preexisting myelosuppression, renal impairment (CrCl < 30ml/min), uncontrolled hypertension, phaeochromocytoma, carcinoid syndrome, untreated hyperthyroidism, chronic infection, history of seizures, bipolar depression, schizophrenia or acute confusional states. Pregnancy and lactation. Monitor complete blood counts weekly. Give after haemodialysis. Not known if linezolid or metabolites removed during peritoneal dialysis.
Adverse Reactions
Diarrhoea (antibiotic associated colitis reported), headache, nausea, vomiting, constipation, abnormal liver function tests, fever, vaginal and oral candidiasis, skin rash, pruritus, dizziness, insomnia, anaemia, tongue discoloration, taste disturbance, lactic acidosis, optic and peripheral neuropathy (particularly if used ≥ 28 days).
Potentially Fatal: Reversible myelosuppression including anaemia, leukopenia, pancytopenia and thrombocytopenia (particularly if using > 10-14 days), transient ischaemic attacks, renal failure, Stevens-Johnson syndrome.
Drug Interactions
Use with caution with serotonergic, vasopressor or dopaminergic agents to reduce the incidence of serotonin syndrome. Adrenergic drugs Eg. dopamine, epinephrine, phenylpropanolamine and pseudoephedrine may cause hypertension. Concurrent use with tramadol may increase risk of seizures.
Potentially Fatal: MAOI; avoid concurrent use or use within 2 wk of stopping another MAOI to reduce risk of hypertensive crisis.
See Below for More linezolid Drug Interactions
Lab Interactions
May alter blood counts.
Food Interactions
Beverages and foods high in tyramine content may cause hypertensive crisis. Avoid dietary tyramine ≥100 mg per meal.
Mechanism of Actions
Linezolid is an bacteriostatic oxazolidinone, inhibiting ribosomal protein synthesis. It is active against gram-positive bacteria including vancomycin-resistant enterococci and MRSA. It has limited in-vitro activity against gram-negative bacteria.
Absorption: Oral bioavaiability: Approx 100%. Rapidly absorbed after oral admin. Peak plasma concentrations after 1-2 hrs, although delayed if administered with high fat meal.
Distribution: Plasma protein binking: Approx 31%. Readily distributed into well perfused tissues; bone, fat, lungs, muscle, skin blister fluids and CSF. Animal studies have shown Linezolid in milk but not known if distributed into human milk. Therapeutic concentrations not achieved or maintained in CNS fluid. Volume of distribution at steady state: 40-50 L.
Metabolism: Oxidised to 2 main inactive metabolites.
Excretion: Approx 65% of dose eliminated via non renal route. Renal clearance low. Elimination half life: 4.6-7hr (oral).
Administration
May be taken with or without food.
Storage Conditions
Intravenous: Infusion: Store at 25°C. Protect from light. Oral: Store at 25°C. Reconstituted oral suspension should be used within 21 days of constitution. Protect from light.
ATC Classification
J01XX08 - linezolid ; Belongs to the class of other antibacterials. Used in the systemic treatment of infections.
Storage
Intravenous: Infusion: Store at 25°C. Protect from light. Oral: Store at 25°C. Reconstituted oral suspension should be used within 21 days of constitution. Protect from light.
Available As
  • Linezolid 100 mg
  • Linezolid 2 mg
  • Linezolid 200 mg
  • Linezolid 60 mg
  • Linezolid 600 mg
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