Absorption and Metabolism

After oral administration, cefuroxime axetil is absorbed from the gastrointestinal tract and rapidly hydrolyzed by nonspecific esterases in the intestinal mucosa and blood to cefuroxime. Cefuroxime is subsequently distributed throughout the extracellular fluids. The axetil moiety is metabolized to acetaldehyde and acetic acid.

Pharmacokinetics

Approximately 50% of serum cefuroxime is bound to protein. Serum pharmacokinetic parameters for CEFTIN Tablets and CEFTIN for Oral Suspension are shown in Tables 1 and 2.

Table 1. Postprandial Pharmacokinetics of Cefuroxime Administered as CEFTIN Tablets to Adults*

Table 2. Postprandial Pharmacokinetics of Cefuroxime Administered as CEFTIN for Oral Suspension to Pediatric Patients*

Comparative Pharmacokinetic Properties

A 250 mg/5 mL-dose of CEFTIN Suspension is bioequivalent to 2 times 125 mg/5 mL-dose of CEFTIN Suspension when administered with food (see Table 3). CEFTIN for Oral Suspension was not bioequivalent to CEFTIN Tablets when tested in healthy adults. The tablet and powder for oral suspension formulations are NOT substitutable on a milligram-per-milligram basis. The area under the curve for the suspension averaged 91% of that for the tablet, and the peak plasma concentration for the suspension averaged 71% of the peak plasma concentration of the tablets. Therefore, the safety and effectiveness of both the tablet and oral suspension formulations had to be established in separate clinical trials.

Table 3. Pharmacokinetics of Cefuroxime Administered as 250 mg/5 mL or 2 x 125 mg/5 mL CEFTIN for Oral Suspension to Adults* With Food

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