NOVO-CEFUROXIME TABLET

Country: Canada

Language: English

Source: Health Canada

Active ingredient:

CEFUROXIME (CEFUROXIME AXETIL)

Available from:

NOVOPHARM LIMITED

ATC code:

J01DC02

INN (International Name):

CEFUROXIME

Dosage:

250MG

Pharmaceutical form:

TABLET

Composition:

CEFUROXIME (CEFUROXIME AXETIL) 250MG

Administration route:

ORAL

Units in package:

100

Prescription type:

Prescription

Therapeutic area:

SECOND GENERATION CEPHALOSPORINS

Product summary:

Active ingredient group (AIG) number: 0122448001; AHFS:

Authorization status:

CANCELLED PRE MARKET

Authorization date:

2015-11-25

Summary of Product characteristics

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