DrugInfoSys

Linezolid

Drug #1725

Linezolid is a synthetic antibacterial, belongs to oxazolidinone class. Linezolid is active against gram +ve bacteria including staphylococci. streptococci, enterococci, gram +ve anaerobic cocci, and gram +ve rods. It has poor activity against gram -ve aerobic and anaerobic organisms. Linezolid is bacteriostatic against enterococci and staphylococci and bactericidal against streptococci. It produces its action by inhibiting protein synthesis within the bacterial cell. Linezolid is used in the treatment of infections caused by vancomycin-resistant E. faecium; nosocomial pneumonia caused by methicillin-susceptible and resistant strains of S. aureus, and complicated skin and soft tissue infections caused by gram +ve bacteria.

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Primary Characteristics

It is of Synthetic origin and belongs to Oxazolidine.

Molecular Weight: 337.5 · pKa: 0.47 · Solubility in Water: soluble · Solubility in Alcohol: Insoluble · Non-proprietary name: Linezolid.

Molecular structure of Linezolid

Pharmacokinetics

Distribution: Linezolid has a volume of distribution is 0.6 to 0.7 L/kg. plasma protein binding is Drug donot bind to plasma protein 31%.

Elimination: it is metabolised via Non enzymatic oxidation, plasma half-life is 5-7 hr, renal excretion is drug is excreted by urine.

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Indications

Linezolid is primarily indicated in conditions like Pneumonia, Respiratory tract infections, Severe or recurrent duodenal and gastric ulcertion, Skin infections.

Contraindications

Linezolid is contraindicated in conditions like Breast feeding.

Dosage

Linezolid's dosage details are as follows:

DoseSingle DoseFrequencyRouteInstructions
Adult Dosage
500 mg500 mgEvery 12hOralFor 10-14 days
Paediatric Dosage (20kg)
10 mg/kg10 mg/kgEvery 8hOrally
Neonatal Dosage (3kg)
No data.

Drug Interactions

6 interactions

Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Side Effects

Linezolid in overdosage may give rise to further complications which include Convulsions , Stevens johnson syndrome , Stevens johnson syndrome , Leucopenia, Pancytopenia , Abnormal liver function , Anaemia , Lactic acidosis.

The signs and symptoms that are produced after acute overdosage of Linezolid are Weakness .

Linezolid is known to cause more or less tolerable side effects which are usually transient. These include Constipation , Diarrhea, Dizziness, Dry mouth, Fatigue, Fever, Headache, Hypotension , Insomnia, Nausea and vomiting, Neuropathy, Pruritus , Rashes , Tinnitus, Tongue discoloration, Urticaria.

Warnings / Precautions

Linezolid should be used with caution in patients with hepatic impairment; renal impairment; pregnancy (use only if potential benefit outweighs risk); monitor full blood count (including platelet count) weekly uless close observation and blood-pressure monitoring possible, avoid in uncontrolled hypertension, phaeocytochroma, carcinoid tumour, thyrotoxicosis, bipolar depression, schizophrenia, or acute confusional states. Monoamine Oxidase Inhibition: Linezolid is a reversible, non-selective monoamine oxidase inhibitor (MAOI). Patients should avoid consuming large amounts of tyramine-rich foods (such as mature cheese, yeast extracts, undistilled alcoholic beverages and fermented soya bean products). In addition, Linezolid should not be given with another MAOI or within two weeks of stopping another MAOI.Unless close observation and blood-pressure monitoringis possible, avoid in those receiving SSRIs, 5HT1 agonists (triptans), tricyclic antidepressants, sympathomimitics, dopaminergics, buspirone, pethidine and possibly other opiod analgesics.

Available Brands

Click on a strength to view available brands.

Single Ingredient

Inf
2 mg2 mg/ml200 mg200 mg/100ml400 mg400 mg/200ml600 mg600 mg/300ml
Inj
2 mg
Oral Soln
100 mg
Susp
100 mg100 mg/5ml
Tabs
400 mg600 mg

Storage Conditions

Linezolid should be stored .

Drug Classification

  1. 1.6.2.2.12 — oxazolidinones

Manufacturers