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Bestrix IM-IV (Ceftriaxone Sodium)

Information for medical Professionals

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Each vial of 250mg, 500mg & 1000mg contains:
Ceftriaxone (as ceftriaxone sodium) 250mg, 500mg & 1000mg respectively.

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Ceftriaxone is a  long acting, 3rd generation cephalosporin antibiotic for parenteral use.  

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Ceftriaxone Inhibits bacterial cell wall synthesis by blocking transpeptidation of peptidoglycan.
Ceftriaxone activate autolytic enzymes in the cell wall, which results in lesions that cause bacterial death.

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Ceftriaxone is reversibly bound to albumin. Half-life ranged from 5.8 to 8.7 hours. Bioavailability after intramuscular injection is 100%. It has shown excellent tissue and body fluid penetration. Concentrations, well above the MICs of most pathogens are detectable for more than 24 hours in over 60 tissues or body fluids including lung, heart, biliary tract/liver, tonsils, middle ear and nasal mucosa, bone; and cerebrospinal, pleural, prostatic and synovial fluids. It penetrates the inflamed as well as non inflamed meninges. Ceftriaxone crosses the placental barrier and is secreted in the breast milk at low concentrations.

ELIMINATION:
Ceftriaxone is not metabolized systemically; only the intestinal flora transforms the agent into inactive metabolites. 50-60% of ceftriaxone is excreted unchanged in the urine, while 40-50% is excreted unchanged in the bile.

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In the first week of life, 80% of the dose is excreted in the urine; over the first month, this falls to levels similar to those in the adult. In elderly persons aged over 75 years, the average elimination half-life is usually 2 to 3 times longer than in the young adult group. Evidence gathered to date with ceftriaxone, however, suggests that no modification of the dosage regimen is needed.

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In patients with renal or hepatic dysfunction, the pharmacokinetics of ceftriaxone are only minimally altered and the elimination half-life is only slightly increased. If kidney function alone is impaired, biliary elimination of ceftriaxone is increased; if liver function alone is impaired, renal elimination is increased.

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