Formulary
Linezolid: Indications, Dosing, Side Effects and Interactions
Linezolid, an oxazolidinone antibacterial, is active against Gram-positive bacteria including meticillin-resistant Staphylococcus aureus (MRSA), and...
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Linezolid: Indications, Dosing, Side Effects and Interactions
Linezolid, an oxazolidinone antibacterial, is active against Gram-positive bacteria including meticillin-resistant Staphylococcus aureus (MRSA), and...
Drug action
Linezolid, an oxazolidinone antibacterial, is active against Gram-positive bacteria including meticillin-resistant Staphylococcus aureus (MRSA), and glycopeptide-resistant enterococci. Resistance to linezolid can develop with prolonged treatment or if the dose is less than that recommended. Linezolid is not active against common Gram-negative organisms; it must be given in combination with other antibacterials for mixed infections that also involve Gram-negative organisms.
Indications and dose
**Pneumonia (when other antibacterials e.g. a glycopetide, such as vancomycin, cannot be used) (initiated under specialist supervision),Complicated skin and soft-tissue infections caused by Gram-positive bacteria, when other antibacterials cannot be used (initiated under specialist supervision)**
- **Adult** (By Mouth): 600 mg every 12 hours usually for 10-14 days (maximum duration of treatment 28 days).
- **Adult** (By Intravenous Infusion): 600 mg every 12 hours.
**Cellulitis (specialist use only),Erysipelas (specialist use only)**
- **Adult** (By Mouth, Or By Intravenous Infusion): 600 mg every 12 hours.
**Moderate diabetic foot infection (specialist use only),Severe diabetic foot infection (specialist use only),Leg ulcer infection (specialist use only)**
- **Adult** (By Mouth, Or By Intravenous Infusion): 600 mg every 12 hours.
**Pneumonia (when other antibacterials e.g. a glycopetide, such as vancomycin, cannot be used) (initiated under specialist supervision), Complicated skin and soft-tissue infections caused by Gram-positive bacteria, when other antibacterials cannot be used (initiated under specialist supervision) for linezolid**
- **Neonate up to 7 days** (By mouth, or by intravenous infusion): 10 mg/kg every 12 hours, increased if necessary to 10 mg/kg every 8 hours, increased dose can be used if poor response.
- **Neonate 7 days to 28 days** (By mouth, or by intravenous infusion): 10 mg/kg every 8 hours.
- **Child 1 month-11 years** (By mouth, or by intravenous infusion): 10 mg/kg every 8 hours (max. per dose 600 mg).
- **Child 12-17 years** (By mouth, or by intravenous infusion): 600 mg every 12 hours.
**Cellulitis (specialist use only), Erysipelas (specialist use only) for linezolid**
- **Child 1 month-11 years** (By mouth, or by intravenous infusion): 10 mg/kg every 8 hours (max. per dose 600 mg).
- **Child 12-17 years** (By mouth, or by intravenous infusion): 600 mg every 12 hours.
Cautions
Acute confusional states; bipolar depression; carcinoid tumour; elderly (increased risk of blood disorders); history of seizures; phaeochromocytoma; schizophrenia; thyrotoxicosis; uncontrolled hypertension Cautions, further information Close observation Unless close observation and blood pressure monitoring possible, linezolid should be avoided in uncontrolled hypertension, phaeochromocytoma, carcinoid tumour, thyrotoxicosis, bipolar depression, schizophrenia, or acute confusional states.
Side effects
Common or very common Anaemia; constipation; diarrhoea; dizziness; gastrointestinal discomfort; headache; hypertension; increased risk of infection; insomnia; localised pain; nausea; skin reactions; taste altered; thrombocytopenia; vomiting Uncommon Angioedema; antibiotic associated colitis; arrhythmias; bone marrow disorders; chills; dry mouth; eosinophilia; fatigue; gastritis; hyperhidrosis; hyponatraemia; leucopenia; nerve disorders; neutropenia; oral disorders; pancreatitis; polyuria; pseudomembranous enterocolitis; renal failure; seizure; sensation abnormal; thirst; thrombophlebitis; tinnitus; tongue discolouration; transient ischaemic attack; vision disorders; vulvovaginal disorder Rare or very rare Hypersensitivity vasculitis; lactic acidosis; rhabdomyolysis; severe cutaneous adverse reactions (SCARs); tooth discolouration Frequency not known Alopecia; Clostridioides difficile colitis; serotonin syndrome; SIADH
Interactions
**Severe interactions:**
- Use with tyramine-rich foods No significant pressor response was observed in subjects receiving both linezolid and less than 100 mg tyramine.
- Drugs metabolised by cytochrome P450 Linezolid is not detectably metabolised by the cytochrome P450 (CYP) enzyme system and it does not inhibit any of the clinically significant human CYP isoforms...
**Other interactions (17):**
- Monoamine oxidase inhibitors Linezolid is a reversible, non-selective inhibitor of monoamine oxidase (MAOI).
- There are limited data from drug interaction studies and on the safety of linezolid when administered to patients on concomitant medications that might put them at risk from MAO inhibition.
- Therefore, linezolid is not recommended for use in these circumstances unless close observation and monitoring of the recipient is possible (see section 4.3 and 4.4).
- Potential interactions producing elevation of blood pressure In normotensive healthy volunteers, linezolid enhanced the increases in blood pressure caused by pseudoephedrine and phenylpropanolamine...
- Co-administration of linezolid with either pseudoephedrine or phenylpropanolamine resulted in mean increases in systolic blood pressure of the order of 30-40 mmHg, compared with 11-15 mmHg increases...
- It is recommended that doses of drugs with a vasopressive action, including dopaminergic agents, should be carefully titrated to achieve the desired response when co-administered with linezolid.
Pregnancy
Manufacturer advises use only if potential benefit outweighs risk-no information available.
Breast feeding
Manufacturer advises avoid-present in milk in animal studies.
Hepatic impairment
Manufacturer advises caution in severe impairment (no information available).
Renal impairment
Use with caution if creatinine clearance less than 30 mL/minute (metabolites may accumulate), M see Prescribing in renal impairment .
Medicinal forms
Tablet,Suspension
Clinical governance
**Author:** MedNext Clinical Team. **Clinical reviewer:** Dr Shameer Deen, MBBS, MS, MRCS. **Sources:** BNF, Indian Pharmacopoeia, CIMS India. **Correction:** Report errors at support@mednext.academy.
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