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Pharmacology: Pharmacodynamics: Cefotaxime is classified as a third generation cephalosporin. It has a bactericidal effect by inhibiting bacterial cell wall synthesis.
Cefotaxime has a broad spectrum of bactericidal activity and Pseudomonas aeruginosa.
Cefotaxime is active in vitro against the following bacteria: Gram-positive aerobic bacteria: Streptococcus pneumoniae, S. pyogenes (group A beta-hemolytic streptococci), Staphylococcus aureus (penicillinase-producing and nonpenicillinase-producing strains), S. epidermidis and viridans streptococci (some strains).
Gram-negative aerobic bacteria: Escherichia coli, Klebsiella (including K. pneumoniae), Haemophilus influenzae (including ampicillin-resistant strains), H. parainfluenzae, Proteus mirabilis, Serratia marcescens, Citrobacter, Enterobacter, Providencia stuartii, P. rettgeri, Morganella morganii, Neisseria gonorrhoeae, N. meningitidis, Pseudomonas aeruginosa (some strains).
Anaerobic bacteria: Bacteroides (including B. fragilis), Clostridium (including C. perfringens), Fusobacterium (including F. nucleatum), Peptococcus, Peptostreptococcus, Propionibacterium.
Resistance strains of some organisms, especially Enterobacter, Pseudomonas aeruginosa, Serratia, have developed during therapy with Cefotaxime.
Pharmacokinetics: Cefotaxime is not appreciably absorbed from the GI tract which must be given parenterally. Following IM administration, peak serum concentration of the drug are attained within 30 minutes. The antibiotic activity is considered from Cefotaxime and its major metabolite (desacetylcefotaxime). After entering the systemic circulation it is distributed to the body tissues and fluids including aqueous humor, bronchial secretion, sputum, bone, bile, ascitic, pleural and prostatic fluid; penetrates CSF best when meninges are inflamed.
Cefotaxime crosses the placenta and is distributed into milk. It is 13-38% bound to serum proteins and partially metabolized in the liver to desacetylcefotaxime. Cefotaxime is excreted principally in urine as unchanged drug and metabolite. Elimination half-life of Cefotaxime have 2 phases are initial phase and terminal phase; the serum half-life of the drug in the initial phase (t1/2α) average 0.2-0.4 hours and the serum half-life of the drug in the terminal phase (t1/2β) average 0.9-1.7 hours. The t1/2β of desacetylcefotaxime is 1.4-1.9 hours. The t1/2β of both Cefotaxime and desacetylcefotaxime may be prolonged in patients with impaired hepatic and renal function.
Both Cefotaxime and desacetylcefotaxime are removed by hemodialysis. Only minimal amounts of Cefotaxime are removed by peritoneal dialysis.
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