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Product
Anti-infective Products (Gatiquin)
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Linospan
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Linospan
COMPOSITION
Each film coated tablet contains 600 mg of Linezolid
Presentation
Strip pack of 4 tablets
Description
Synthetic antibacterial agent of a new class of antibiotics,the oxazolidinones for the infection caused by aerobic gram-positive bacteria.( multi-resistant bacteria )
» It inhibit bacterial protein synthesis by interfering with ribosomal function.
» Bacteriostatic against enterococci & staphylococci
» Bactericidal against streptococci
Chemical data
Formula C16 H20 FN3 O4
Pharmacokinetic data
Bioavailability ˜ 100%(oral)
Proteinbinding › › › › › › › › › › 31%
Metabolism › › › › › › › › Hepatic 50–70%
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Half life › › › › › › › ›4.2 − 5.4 hours
Excretion › › › › › › › ›Renal 80−85%
Mechanism of Action
• Linezolid works on the initiation of protein synthesis.
• It does this by stopping the 30S and 50S subunit from binding together.
• It binds on the 50S subunit close to the peptidyl transferase » » The enzymatic centre in the ribosome responsible for peptide bond formation
Ribosome » »
a small, dense organelle in cells that assembles proteins.
• This then stops the interaction with the 30S subunit.
Absorption
• Rapidly & extensively absorbed after oral dosing
• Maximum plasma concentration – 1-2 hrs after dosing
• Absolute bioavailability – nearly 100 %
• No need to the timing of meals
Pharmacokinetics
• Linezolid is highly absorbed when administered orally, with a bioavailability of approximately 100 percent.
• It is metabolized via hepatic oxidation .
• Elimination occurs through renal and fecal routes.
• The half-life is approximately 5 hours.
• Presently, no dosage adjustment is recommended for patients with renal insufficiency; however, linezolid is removed by hemodialysis .
Indication
Indicated in the treatment of following infections caused by susceptible microorganisms
• Vancomycin resistant Enterococcus faecium infections
• Nosocomial pneumonia
• Complicated skin & skin structure infections including diabetic foot infection
• Uncomplicated skin & skin structure infections
• Community-acquired pneumonia
Dosage & Administration
◊ Vancomycin resistant Enterococcus faecium infections
600 mg b.d for 14-28 days
◊ Nosocomial pneumonia
600 mg b.d for 14-28 days
◊ Complicated skin & skin structure infections
◊ Community-acquired pneumonia
600 mg b.d for 10-14 days
◊ Uncomplicated skin & skin structure infections
400 mg b.d for 10-14 days
ø ø ø ø In paediatric < 7 days – 10 mg /kg 12 hrly
upto 11 yrs - 10 mg /kg 8 hrly
Precautions
• Platelet counts should be monitored in patients who
are at increased risk of bleeding. ( Thrombocytopenia)
• It may be taken with or without food.
• Should inform to doctor if patients have a h/o of H/T.
• Large quantities of foods with high tyramine content
should be avoided while taking it.
» Tyramine – an amine (organic compound of N2 ) which causes B.P & H.R
» All protein rich foods contain more tyramine
Pregnancy & Lactation
No adequate and well controlled studies .
Renal & Hepatic impairment
No dose adjustments is required for patients with renal & mild to moderate hepatic insuffciency.
Side Effects
• Diarrhoea
• Headache > the most common
• Nausea
• Hypertension
• Dyspepsia
• Localized abdominal pain
• Pruritus
• Thrombocytopenia d/o duration of therapy
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