Cefisal-200 Mechanism of Action

Pharmacotherapeutic group: third generation cephalosporin.
Pharmacology: Pharmacodynamics: Cefixime is an oral third generation cephalosporin which has marked in vitro bactericidal activity against a wide variety of Gram-positive and Gram-negative organisms. Clinical efficacy has been demonstrated in infections caused by commonly occurring pathogens including Streptococcus pneumoniae, Streptococcus pyogenes, Escherichia coli, Proteus mirabilis, Klebsiella species, Haemophilus influenzae (beta-lactamase positive and negative strains), Branhamella catarrhalis (beta-lactamase positive and negative) and Enterobacter species. It is highly stable in the presence of beta-lactamase enzymes. Most strains of enterococci (Streptococcus faecalis, group D Streptococci) and Staphylococci (including coagulase positive and negative strains and methicillin-resistant strains) are resistant to Cefixime. In addition, most strains of Pseudomonas, Bacteroides fragilis, Listeria monocytogenes and Clostridia are resistant to Cefixime.
Pharmacokinetics: The absolute oral bioavailability of Cefixime is in the range of 22-54%. Absorption is not significantly modified by the presence of food. Cefixime may therefore be given without regard to meals. From in vitro studies, serum or urine concentrations of 1 mcg/mL or greater were considered to be adequate for most common pathogens against which Cefixime is active. Typically, the peak serum levels following the recommended adult or pediatric doses are between 1.5 and 3 mcg/mL. Little or no accumulation of Cefixime occurs following multiple dosing.
The pharmacokinetics of Cefixime in healthy elderly (age > 64 years) and young volunteers (11-35). Compared the administration of 400 mg doses once daily for 5 days. Mean Cmax and AUC values were slightly greater in the elderly. Elderly patients may be given the same dose as the general population. Cefixime is predominantly eliminated as unchanged drug in the urine. Glomerular filtration is considered the predominant mechanism. Metabolites of Cefixime have not been isolated from human serum or urine. Serum protein binding is well characterised for human and animal sera; Cefixime is almost exclusively bound to the albumin fraction, the mean free fraction being approximately 30%. Protein binding of Cefixime is only concentration dependent in human serum at very high concentrations which are not seen following clinical dosing.
Transfer of ¹⁴C-labelled Cefixime from lactating rats to their nursing offspring through breast milk was quantitatively small (approximately 1.5% of the mothers' body content of Cefixime in the pup). No data are available on secretion of Cefixime in human breast milk. Placental transfer of Cefixime was small in pregnant rats dosed with labelled Cefixime.