Generic

Linezolid

Indications

Infections caused by Vancomycin-Resistant Enterococcus faecium, including cases with bacteremia.

Staphylococcus aureus (methicillin-susceptible and -resistant strains) or Streptococcus pneumoniae induce nosocomial pneumonia (including multi-drug resistant strains). Combination therapy may be clinically indicated if Gram-negative organisms are present in the documented or suspected infections.

Staphylococcus aureus (methicillin-susceptible and methicillin-resistant strains), Streptococcus pyogenes, or Streptococcus agalactiae cause complicated skin and skin structure infections, including diabetic foot infections (without associated osteomyelitis).

Pharmacology

Linezolid is a synthetic antibacterial drug that belongs to the oxazolidinones, a new class of antibiotics exhibiting in vitro action against Gram positive aerobic bacteria, Gram positive anaerobic bacteria, and Gram negative bacteria. It works differently than other antibacterial medicines in that it preferentially inhibits bacterial protein production. Linezolid binds to the 23S ribosomal RNA of the bacterial ribosome’s 50S subunit, preventing the creation of a functional 70S initiation complex, which is required for bacterial translation. Linezolid has been demonstrated to be bacteriostatic against enterococci and staphylococci in time-kill assays.

Dosage & Administration

Patients who commence treatment on the parenteral formulation may be switched to oral presentation when clinically indicated. In such circumstances, no dose adjustment is required as Linezolid has an oral bioavailability of approximately 100%. The injection should be administered over a period of 30 to 120 minutes. The film-coated tablets or oral suspension may be taken with or without food.

Complicated skin and skin structure infections, Community-acquired pneumonia, including concurrent bacteremia-

Pediatric Patients (Birth through 11 Years of Age): 10 mg/kg IV or oral t.i.d.

Adults and Adolescents (12 Years and Older): 600 mg IV or oral b.i.d.

Recommended Duration of Treatment (consecutive days): 10 to 14

Nosocomial pneumonia, Vancomycin-resistant Enterococcus faecium infections including concurrent bacteremia-

Pediatric Patients (Birth through 11 Years of Age): 10 mg/kg IV or oral t.i.d.

Adults and Adolescents (12 Years and Older): 600 mg IV or oral b.i.d.

Recommended Duration of Treatment (consecutive days): 14 to 28

Uncomplicated skin and skin structure infections-

Pediatric Patients (Birth through 11 Years of Age): <5 yrs: 10 mg/kg oral t.i.d. 5-11 yrs: 10 mg/kg oral b.i.d

Adults and Adolescents (12 Years and Older): Adults: 400 mg oral b.i.d. Adolescents: 600 mg oral b.i.d

Recommended Duration of Treatment (consecutive days): 10 to 14

Interaction

Monoamine Oxidase Inhibition: Linezolid inhibits monoamine oxidase in a reversible and nonselective manner. As a result, Linezolid may interact with adrenergic and serotonergic medications.

Adrenergic Drugs: Linezolid may cause a reversible increase in the pressor response to indirect-acting sympathomimetic agents, vasopressors, or dopaminergic agents in some people. To obtain the appropriate response, initial doses of adrenergic drugs such as dopamine or epinephrine should be lowered and titrated.

Serotonergic Agents: Physicians should be aware of the signs and symptoms of serotonergic syndrome in patients using Linezolid and serotonin reuptake inhibitors at the same time.

Contraindications

Patients with known hypersensitivity to Linezolid or any of the other product components should not take Linezolid formulations. Linezolid should not be used in individuals who are on or have recently taken a monoamine oxidase A or B inhibitor (e.g., phenelzine, isocarboxazid) or within two weeks of taking such a medication. Patients with uncontrolled hypertension, pheochromocytoma, thyrotoxicosis, carcinoid syndrome, and/or patients taking directly or indirectly acting sympathomimetic agents (e.g. Pseudoephedrine), vasopressive agents (e.g. Epinephrine, Norepinephrine), dopaminergic agents (e.g. Dopamine, Dobutamine), serotonin syndrome,

Side Effects

Most of the adverse events reported with Linezolid were mild to moderate in intensity. The most common adverse events in patients treated with Linezolid were diarrhea, headache and nausea. Other adverse events includes oral moniliasis, vaginal moniliasis, hypertension, dyspepsia, localized abdominal pain, pruritus, and tongue discoloration.

Pregnancy & Lactation

Pregnancy Classification C. In pregnant women, there are no sufficient and well-controlled trials. Only if the possible benefit outweighs the risk to the fetus should linezolid be administered during pregnancy. Linezolid is not known to be excreted in human milk. Due to the fact that many medications are secreted in human milk. When administering Linezolid to a breastfeeding mother, extreme caution is advised.

Precautions & Warnings

Patients who have recurring nausea or vomiting, unexplained acidosis, or low bicarbonate levels while taking Linezolid should seek medical help right once. Patients should be continuously monitored for signs and symptoms of serotonin syndrome, such as cognitive impairment, hyperpyrexia, hyperreflexia, and incoordination, when Linezolid and concomitant serotonergic medications are therapeutically suitable. If signs or symptoms appear, doctors should consider stopping one or both of the drugs. Discontinuation symptoms might occur if the concurrent serotonergic medication is stopped.

Therapeutic Class

Macrolides

Storage Conditions

Protect from light and moisture by storing in a cool, dry place below 30°C. Keep out of children’s reach.

Pharmaceutical Name

Beximco Pharmaceuticals Ltd.