Linezolid   (Film Coated Tablets)

Composition:
Each film coated tablet contains 600mg Linezolid.

Mechanism of Action:
Linezolid is an oxazolidinone antibacterial, is active against Gram-positive bacteria including methicillin-resistant staphylococcus aureus (MRSA), and vancomycin-resistant enterococci. It’s effective mainly against aerobic gram-positive bacteria, but in vitro it has certain activity against gram-negative bacteria and anaerobic bacteria.
Linezolid is not sufficiently active against common gram-negative organisms. Linezolid inhibits bacterial protein synthesis through a mechanism of action different from that of other antibacterial agents. Therefore, cross-resistance between Linezolid and other classes of antibiotics is unlikely. Linezolid binds to a site on the bacterial 23S ribosomal RNA of the 50S subunit and prevents the formation of a functional 70S initiation complex, which is an essential component of the bacterial translation process. Linezolid should be reserved for infections resistant to other antibacterial, or when other antibacterial are not tolerated.

Indications:         
Vancomycin- resistant enterococcus faecium infection, and including cases with concurrent bacteremia. Nosocomial pneumonia caused by staphylococcus aureus (methicillin-susceptible and resistant strains), or streptococcus pneumoniae (penicillin-susceptible strains only). Combination therapy may be clinically indicated if the documented or presumptive pathogens include gram-negative organisms. Complicated skin and skin structure infections caused by staphylococcus aureus (methicillin-susceptible and resistant strains), streptococcus pyogenes, or streptococcus agalactiae. Linezolid can be used in the treatment of diabetic foot and decubitus ulcers.

Dosage and administration:
Linezolid is indicated for adults or children over 12 years (Linezolid may be taken with or without food).


Infection

Dosage

Recommended period

  1. Vancomycin resistant enterococcus faecium infections including concurrent bacteremia
  2. Nosocomial pneumonia

600mg
every (12 hours)

14 – 28 days

  1. Complicated skin and skin structure infection
  2. Community acquired pneumonia, including concurrent bacteremia

600mg
every (12 hours)

10 – 14 days

  1. Uncomplicated skin and skin structure infections

400mg
every (12 hours)

10 – 14 days

In case of over dosage, hemodialysis facilitates rapidly the elimination of Linezolid.

Side Effects:
Diarrhea (antibiotic-associated colitis), nausea, vomiting, taste disturbances, headache, rash, insomnia.

Contraindications:
Hypersensitivity to Linezolid.

Drug Interactions:
Linezolid is a reversible, nonselective inhibitor of monoamine oxidase, it should not be given with another MAOI or within 2 weeks of stopping another MAOI. Unless close observation and blood pressure monitoring is possible, avoid in those receiving SSRIS, 5HT1 agonists (triptans), tricyclic antidepressants, sympathomimetic, dopaminergics, buspirone, pethidine and possibly other opioid analgesics.

Precautions:
Myelosuppression has been reported in patients receiving Linezolid, blood counts should be monitored weekly in patients who are at increased risk for bleeding, who have pre-existing thrombocytopenia, who receive concomitant medications that may decrease platelet count or blood count or who may require longer than 2 weeks of Linezolid therapy, or who have pre-existing myelosuppression, or who have severe renal impairment.

Use in Pregnancy or Lactation:
Category C (There are no adequate and well controlled studies in pregnant women). It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
The drug is excreted in human milk, caution should be exercised when Linezolid is administered to nursing women.

Pharmacokinetic:
Linezolid is rapidly and extensively absorbed after oral dosing. Maximum plasma concentrations are reached approximately 1 to 2 hours after dosing, and the absolute bioavailability is approximately 100%.

Information for patients:

  1. They should inform their physician if they have a history of hypertension.
  2. Linezolid is a reversible, non-selective monoamine oxidase inhibitor; patients should avoid consuming large amounts of foods or beverages with high tyramine while taking Linezolid. Tyramine-rich food such as mature cheese, yeast extracts, alcoholic beverages and fermented soya bean products meal.
  3. They should inform their physician if they are taking medications containing pseudoephedrine HCL, or serotonin re-uptake inhibitors or other antidepressants.

Presentation:
Carton pack contains 2 blisters of 10 tablets in each, with leaflet.

 

 
 
 

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