CEFUROXIME AXETIL tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

CEFUROXIME AXETIL (UNII: Z49QDT0J8Z) (CEFUROXIME - UNII:O1R9FJ93ED)

Available from:

DIRECT RX

INN (International Name):

CEFUROXIME AXETIL

Composition:

CEFUROXIME 250 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

To reduce the development of drug-resistant bacteria and maintain the effectiveness of cefuroxime axetil and other antibacterial drugs, cefuroxime axetil should be used only to treat or prevent infections that are proven or strongly suspected to be caused by susceptible bacteria. When culture and susceptibility information are available, they should be considered in selecting or modifying antibacterial therapy. In the absence of such data, local epidemiology and susceptibility patterns may contribute to the empiric selection of therapy. NOTE: CEFUROXIME AXETIL TABLETS AND CEFUROXIME AXETIL FOR ORAL SUSPENSION ARE NOT BIO­EQUIVALENT AND ARE NOT SUBSTITUTABLE ON A MILLIGRAM-PER-MILLIGRAM BASIS (SEE CLINICAL PHARMACOLOGY). Cefuroxime Axetil Tablets Cefuroxime axetil tablets are indicated for the treatment of patients with mild to moderate infections caused by susceptible strains of the designated microorganisms in the conditions listed below:   - Pharyngitis/Tonsillitis caused by Streptococcus pyoge

Product summary:

Cefuroxime Axetil Tablets USP, 125 mg of cefuroxime (as cefuroxime axetil), are  white to off-white, uncoated, capsule shaped tablets with “A32” debossed on one side and plain on the other side.          20 Tablets/Bottle                                 NDC 65862-033-20          60 Tablets/Bottle                                 NDC 65862-033-60 Cefuroxime Axetil Tablets, USP 250 mg of cefuroxime (as cefuroxime axetil), are  white to off-white, uncoated, capsule-shaped tablets with “A33” debossed on one side and plain on the other side.         20 Tablets/Bottle                                 NDC 65862-034-20          60 Tablets/Bottle                                 NDC 65862-034-60 Cefuroxime Axetil Tablets, USP 500 mg of cefuroxime (as cefuroxime axetil), are  white to off-white, uncoated, capsule-shaped tablets with “A34” debossed on one side and plain on the other side.         20 Tablets/Bottle                                 NDC 65862-035-20          60 Tablets/Bottle                                 NDC 65862-035-60 Store at 20° to 25°C (68° to 77°F); excursions permitted to 15° to 30°C (59° to 86°F) [see USP Controlled Room Temperature]. Replace cap securely after each opening.

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

CEFUROXIME AXETIL- CEFUROXIME AXETIL TABLET
DIRECT RX
----------
CEFUROXIME AXETIL
DESCRIPTION SECTION
Cefuroxime axetil tablets contain cefuroxime as cefuroxime axetil.
Cefuroxime axetil is a
semisynthetic, broad-spectrum cephalosporin antibiotic for oral
administration.
Chemically, cefuroxime axetil, the 1-(acetyloxy) ethyl ester of
cefuroxime, is (RS )-1-hydroxyethyl
(6R,7R)-7-[2-(2-furyl)glyoxyl-amido]-3-(hydroxymethyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]-oct-2-ene-
2-carboxylate, 72-(Z)-(O-methyl-oxime), 1-acetate 3-carbamate. Its
molecular formula is
C20H22N4O10S, and it has a molecular weight of 510.48.
Cefuroxime axetil is in the amorphous form and has the following
structural formula:
Cefuroxime axetil tablets are uncoated and contain the equivalent of
125, 250 or 500 mg of cefuroxime
as cefuroxime axetil. Cefuroxime axetil tablets contain the inactive
ingredients colloidal silicon
dioxide, croscarmellose sodium, hydrogenated vegetable oil,
microcrystalline cellulose, and sodium
lauryl sulfate.
CLINICAL PHARMACOLOGY SECTION
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
cefuroxime axetil tablets are shown in Table 1.
TABLE 1. POSTPRANDIAL PHARMACOKINETICS OF CEFUROXIME ADMINISTERED AS
CEFUROXIME AXETIL TABLETS TO ADULTS*
*Mean values of 12 healthy adult
volunteers.
† Drug administered immediately
after a meal.
Dose†
(Cefuroxime
Equivalent)
Peak Plasma
Concentration
(mcg/mL)
Time of Peak
Plasma
Concentration
(hr)
Mean
Elimination
Half-Life
(hr)
AUC
(mcg-hr
mL)
125 mg
2.1
2.2
1.2
6.7
250 mg
4.1
2.5
1.2
12.9
500 mg
7
3
1.2
27.4
1,000 mg
13.6
2.5
1.3
50
Comparative Pharmacokinetic Properties: C