País: Canadá
Língua: inglês
Origem: Health Canada
CEFUROXIME (CEFUROXIME AXETIL)
NOVOPHARM LIMITED
J01DC02
CEFUROXIME
125MG
TABLET
CEFUROXIME (CEFUROXIME AXETIL) 125MG
ORAL
100
Prescription
SECOND GENERATION CEPHALOSPORINS
Active ingredient group (AIG) number: 0122448006; AHFS:
CANCELLED PRE MARKET
2015-10-16
PRODUCT MONOGRAPH PR NOVO–CEFUROXIME (Cefuroxime Axetil Tablets, USP) 125 mg, 250 mg and 500 mg cefuroxime/tablet Antibiotic Control Number: 031000 Novopharm Limited Date of Preparation: Toronto, Canada April 03, 2008 PR NOVO–CEFUROXIME (Cefuroxime Axetil Tablets, USP) 125 mg, 250 mg and 500 mg cefuroxime/tablet Antibiotic ACTIONS AND CLINICAL PHARMACOLOGY Cefuroxime axetil is an orally active prodrug of cefuroxime. After oral administration, NOVO- CEFUROXIME (cefuroxime axetil) is absorbed from the gastrointestinal tract and rapidly hydrolyzed by nonspecific esterases in the intestinal mucosa and blood to release cefuroxime into the blood stream. Conversion to cefuroxime, the microbiologically active form, occurs rapidly. The inherent properties of cefuroxime are unaltered after its administration as cefuroxime axetil. Cefuroxime exerts its bactericidal effect by binding to an enzyme or enzymes referred to as penicillin-binding proteins (PBPs) involved in bacterial cell wall synthesis. This binding results in inhibition of bacterial cell wall synthesis and subsequent cell death. Specifically, cefuroxime shows high affinity for PBP 3, a primary target for cefuroxime in gram-negative organisms such as _E. coli._ A comparative, two-way, single-dose, fasting bioavailability study was performed on two 250 mg cefuroxime axetil products, NOVO-CEFUROXIME 250 mg tablets and Ceftin ® 250 mg tablets. The pharmacokinetic data calculated for cefuroxime axetil in the NOVO- CEFUROXIME and Ceftin ® tablet formulations is tabulated in Table 1. Table 1 Geometric Mean Arithmetic Mean (C.V.) Novo-Cefuroxime (2 x 250 mg) Ceftin ®** (2 x 250 mg) Percentage of Ceftin ® AUC T (ng•hr/mL) 15.65 16.33 (28) 16.44 17.48 (36) 95 AUC I (ng•hr/mL) 16.36 16.97 (27) 17.12 18.16 (35) 96 C max (ng/mL) 5.39 5.63 (28) 5.50 5.76 (32) 98 T max * (hr) 1.33 (0.25) 1.74 (0.97) --- T 1/2 * (hr) 1.26 (0.20) 1.32 (0.19) --- *For the T max and T 1/2 parameters these are the arithmetic means (standard deviation). **Ceftin® manufactured by Glaxo C Leia o documento completo