Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/699
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CEFTIN (Powder, For Suspension)
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NOTE: CEFTIN TABLETS AND CEFTIN FOR ORAL SUSPENSION
ARE NOT BIOEQUIVALENT AND ARE NOT SUBSTITUTABLE ON A MILLIGRAM-PER-MILLIGRAM
BASIS (SEE CLINICAL PHARMACOLOGY).<br/>CEFTIN for Oral Suspension: CEFTIN for Oral Suspension may be administered to
pediatric patients ranging in age from 3 months to 12 years,
according to dosages in Table 8:<br/>Patients With Renal Failure: The safety and efficacy of cefuroxime axetil in patients
with renal failure have not been established. Since cefuroxime is
renally eliminated, its half-life will be prolonged in patients with
renal failure.<br/>Directions for Mixing CEFTIN for
Oral Suspension: Prepare a suspension at the time of dispensing as
follows: NOTE: SHAKE THE ORAL
SUSPENSION WELL BEFORE EACH USE. Replace cap securely after
each opening. Store the reconstituted suspension between 2��and
8��C (36��and 46��F) (in a refrigerator). DISCARD AFTER
10 DAYS.
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CEFTIN Tablets and CEFTIN for Oral Suspension contain
cefuroxime as cefuroxime axetil. CEFTIN 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,
7-(Z)-(O-methyl-oxime), 1-acetate 3-carbamate.
Its molecular formula is CHNOS, and it has a molecular weight of 510.48. Cefuroxime axetil is in the amorphous form and has the
following structural formula: CEFTIN
Tablets are film-coated and contain the equivalent of 250 or 500 mg
of cefuroxime as cefuroxime axetil. CEFTIN Tablets contain the inactive
ingredients colloidal silicon dioxide, croscarmellose sodium, hydrogenated
vegetable oil, hypromellose, methylparaben, microcrystalline cellulose,
propylene glycol, propylparaben, sodium benzoate, sodium lauryl sulfate,
and titanium dioxide. CEFTIN for Oral Suspension,
when reconstituted with water, provides the equivalent of 125 mg
or 250 mg of cefuroxime (as cefuroxime axetil) per 5 mL
of suspension. CEFTIN for Oral Suspension contains the inactive ingredients
acesulfame potassium, aspartame, povidone K30, stearic acid, sucrose,
tutti-frutti flavoring, and xanthan gum.
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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.<br/>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.<br/>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.<br/>Food Effect on Pharmacokinetics: Absorption of the tablet is greater when taken after
food (absolute bioavailability of CEFTIN Tablets increases from 37%
to 52%). Despite this difference in absorption, the clinical and bacteriologic
responses of patients were independent of food intake at the time
of tablet administration in 2 studies where this was assessed. All pharmacokinetic and clinical effectiveness and safety
studies in pediatric patients using the suspension formulation were
conducted in the fed state. No data are available on the absorption
kinetics of the suspension formulation when administered to fasted
pediatric patients.<br/>Renal Excretion: Cefuroxime is excreted unchanged in the urine; in
adults, approximately 50% of the administered dose is recovered in
the urine within 12 hours. The pharmacokinetics of cefuroxime
in the urine of pediatric patients have not been studied at this time.
Until further data are available, the renal pharmacokinetic properties
of cefuroxime axetil established in adults should not be extrapolated
to pediatric patients. Because cefuroxime is
renally excreted, the serum half-life is prolonged in patients with
reduced renal function. In a study of 20 elderly patients (mean
age = 83.9 years) having a mean creatinine clearance
of 34.9 mL/min, the mean serum elimination half-life was 3.5 hours.
Despite the lower elimination of cefuroxime in geriatric patients,
dosage adjustment based on age is not necessary (see PRECAUTIONS:
Geriatric Use).<br/>Microbiology: The in vivo bactericidal activity of cefuroxime axetil is due to cefuroxime's
binding to essential target proteins and the resultant inhibition
of cell-wall synthesis. Cefuroxime has bactericidal
activity against a wide range of common pathogens, including many
beta-lactamase���producing isolates. Cefuroxime is stable to
many bacterial beta-lactamases, especially plasmid-mediated enzymes
that are commonly found in enterobacteriaceae. Cefuroxime has been shown to be active against most isolates of
the following microorganisms, both in
vitro and in clinical infections as described in the INDICATIONS AND USAGE section.<br/>Facultative Gram-Positive
Microorganisms: Staphylococcus aureus* (including beta��lactamase���producing isolates) Streptococcus pneumoniae Streptococcus
pyogenes *NOTE: Methicillin-resistant staphylococci
are resistant to cefuroxime.<br/>Facultative Gram-Negative
Microorganisms: Escherichia coli Haemophilus
influenzae (including beta��lactamase���producing
isolates) Haemophilus parainfluenzae Klebsiella pneumoniae Moraxella catarrhalis (including beta��lactamase���producing
isolates) Neisseria gonorrhoeae (including
beta��lactamase���producing isolates)<br/>Spirochetes: Borrelia burgdorferi The following in vitro data are available, but their clinical significance is unknown. At least 90 percent of the following microorganisms
exhibit an in vitro minimum
inhibitory concentration (MIC) less than or equal to the susceptible
breakpoint for cefuroxime. However, the efficacy of cefuroxime in
treating clinical infections due to these microorganisms has not been
established in adequate and well-controlled clinical trials.<br/>Facultative Gram-Positive
Microorganisms: Staphylococcus epidermidis Staphylococcus
saprophyticus Streptococcus agalactiae NOTE: Most isolates of enterococci, e.g., Enterococcus faecalis (formerly Streptococcus faecalis), are resistant
to cefuroxime. Methicillin-resistant staphylococci and Listeria monocytogenes are resistant
to cefuroxime.<br/>Facultative Gram-Negative
Microorganisms: Morganella morganii Proteus inconstans Proteus mirabilis Providencia rettgeri NOTE: Some isolates of Morganella morganii, Enterobactercloacae, and Citrobacter spp. have been shown by in vitro tests to be resistant to cefuroxime and other cephalosporins. Most
isolates of Serratia and Proteus vulgaris are resistant to cefuroxime
and most other second-generation cephalosporins, and are resistant
to first-generation cephalosporins. Pseudomonas, Campylobacter, Legionella,
and Acinetobacter are resistant to cefuroxime and most other
second-generation cephalosporins and are resistant to first-generation
cephalosporins.<br/>Anaerobic Microorganisms: Peptococcusniger NOTE: Most isolates of Clostridium difficile and Bacteroides fragilis are
resistant to cefuroxime.<br/>Susceptibility Tests:<br/>Dilution Techniques: Quantitative methods that are used to determine
MICs provide reproducible estimates of the susceptibility of bacteria
to antimicrobial compounds. One such standardized procedure uses a
standardized dilution method(broth, agar, or microdilution)
or equivalent with cefuroxime powder. The MIC values obtained should
be interpreted according to the following criteria: A report of "Susceptible" indicates that the pathogen,
if in the blood, is likely to be inhibited by usually achievable concentrations
of the antimicrobial compound in blood. A report of "Intermediate"
indicates that inhibitory concentrations of the antibiotic may be
achieved if high dosage is used or if the infection is confined to
tissues or fluids in which high antibiotic concentrations are attained.
This category also provides a buffer zone that prevents small, uncontrolled
technical factors from causing major discrepancies in interpretation.
A report of "Resistant" indicates that usually achievable concentrations
of the antimicrobial compound in the blood are unlikely to be inhibitory
and that other therapy should be selected. Standardized
susceptibility test procedures require the use of laboratory control
microorganisms. Standard cefuroxime powder should give the following
MIC values:<br/>Diffusion Techniques: Quantitative methods that require measurement of
zone diameters provide estimates of the susceptibility of bacteria
to antimicrobial compounds. One such standardized procedurethat has been recommended (for use with disks) to test the susceptibility
of microorganisms to cefuroxime uses the 30-mcg cefuroxime disk. Interpretation
involves correlation of the diameter obtained in the disk test with
the MIC for cefuroxime. Reports from the laboratory
providing results of the standard single-disk susceptibility test
with a 30-mcg cefuroxime disk should be interpreted according to the
following criteria: Interpretation should be as stated above for results
using dilution techniques. As with standard
dilution techniques, diffusion methods require the use of laboratory
control microorganisms. The 30-mcg cefuroxime disk provides the following
zone diameters in these laboratory test quality control strains:
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CEFTIN products are contraindicated in patients
with known allergy to the cephalosporin group of antibiotics.
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CEFTIN Tablets: CEFTIN Tablets, 250 mg of cefuroxime (as cefuroxime
axetil), are white, capsule-shaped, film-coated tablets engraved with
"GX ES7" on one side and blank on the other side as follows: 20 Tablets/Bottle NDC 0173-0387-00 CEFTIN Tablets, 500 mg of cefuroxime (as cefuroxime axetil),
are white, capsule-shaped, film-coated tablets engraved with "GX EG2"
on one side and blank on the other side as follows: 20 Tablets/Bottle NDC 0173-0394-00 60 Tablets/Bottle
NDC 0173-0394-42 Store the tablets between
15��and 30��C (59��and 86��F). Replace cap securely
after each opening.<br/>CEFTIN for Oral Suspension: CEFTIN for Oral Suspension is provided as dry, white
to off-white, tutti-frutti���flavored powder. When reconstituted
as directed, CEFTIN for Oral Suspension provides the equivalent of
125 mg or 250 mg of cefuroxime (as cefuroxime axetil) per
5 mL of suspension. It is supplied in amber glass bottles as
follows: 125 mg/5 mL: 100��mL Suspension NDC 0173-0740-00 250 mg/5 mL: 50-mL Suspension NDC 0173-0741-10 100-mL Suspension NDC 0173-0741-00 Before
reconstitution, store dry powder between 2��and 30��C (36��and 86��F). After reconstitution, immediately
store suspension between 2��and 8��C (36��and 46��F),
in a refrigerator. DISCARD AFTER 10 DAYS.
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General: As with other broad-spectrum antibiotics, prolonged
administration of cefuroxime axetil may result in overgrowth of nonsusceptible
microorganisms. If superinfection occurs during therapy, appropriate
measures should be taken. Cephalosporins, including
cefuroxime axetil, should be given with caution to patients receiving
concurrent treatment with potent diuretics because these diuretics
are suspected of adversely affecting renal function. Cefuroxime axetil, as with other broad��spectrum antibiotics,
should be prescribed with caution in individuals with a history of
colitis. The safety and effectiveness of cefuroxime axetil have not
been established in patients with gastrointestinal malabsorption.
Patients with gastrointestinal malabsorption were excluded from participating
in clinical trials of cefuroxime axetil. Cephalosporins
may be associated with a fall in prothrombin activity. Those at risk
include patients with renal or hepatic impairment or poor nutritional
state, as well as patients receiving a protracted course of antimicrobial
therapy, and patients previously stabilized on anticoagulant therapy.
Prothrombin time should be monitored in patients at risk and exogenous
Vitamin K administered as indicated. Prescribing
CEFTIN in the absence of a proven or strongly suspected bacterial
infection or a prophylactic indication is unlikely to provide benefit
to the patient and increases the risk of the development of drug-resistant
bacteria.<br/>Information for Patients/Caregivers
(Pediatric):<br/>Phenylketonurics: CEFTIN for Oral Suspension 125 mg/5 mL
contains phenylalanine 11.8 mg per 5 mL (1 teaspoonful)
constituted suspension. CEFTIN for Oral Suspension 250 mg/5 mL
contains phenylalanine 25.2 mg per 5 mL (1 teaspoonful)
constituted suspension.<br/>Drug/Laboratory Test Interactions: A false-positive reaction for glucose in the urine
may occur with copper reduction tests (Benedict's or Fehling's solution
or with CLINITEST tablets), but not with enzyme-based
tests for glycosuria (e.g., CLINISTIX). As a false-negative
result may occur in the ferricyanide test, it is recommended that
either the glucose oxidase or hexokinase method be used to determine
blood/plasma glucose levels in patients receiving cefuroxime axetil.
The presence of cefuroxime does not interfere with the assay of serum
and urine creatinine by the alkaline picrate method.<br/>Drug/Drug Interactions: Concomitant administration of probenecid with cefuroxime
axetil tablets increases the area under the serum concentration versus
time curve by 50%. The peak serum cefuroxime concentration after a
1.5-g single dose is greater when taken with 1 g of probenecid
(mean = 14.8 mcg/mL) than without probenecid (mean = 12.2 mcg/mL). Drugs that reduce gastric acidity may result in a lower
bioavailability of CEFTIN compared with that of fasting state and
tend to cancel the effect of postprandial absorption. In common with other antibiotics, cefuroxime axetil may affect the
gut flora, leading to lower estrogen reabsorption and reduced efficacy
of combined oral estrogen/progesterone contraceptives.<br/>Carcinogenesis, Mutagenesis, Impairment
of Fertility: Although lifetime studies in animals have not been
performed to evaluate carcinogenic potential, no mutagenic activity
was found for cefuroxime axetil in a battery of bacterial mutation
tests. Positive results were obtained in an in vitro chromosome aberration
assay; however, negative results were found in an in vivo micronucleus
test at doses up to 1.5 g/kg. Reproduction studies in rats at
doses up to 1,000 mg/kg/day (9 times the recommended maximum
human dose basedon mg/m) have revealed no impairment
of fertility.<br/>Pregnancy:<br/>Teratogenic Effects: Pregnancy Category B. Reproduction studies have
been performed in mice at doses up to 3,200 mg/kg/day (14 times
the recommended maximum human dose based on mg/m) and
in rats at doses up to 1,000 mg/kg/day (9 times the recommended
maximum human dose based on mg/m) and have revealed no
evidence of impaired fertility or harm to the fetus due to cefuroxime
axetil. There are, however, no adequate and well-controlled studies
in pregnant women. Because animal reproduction studies are not always
predictive of human response, this drug should be used during pregnancy
only if clearly needed.<br/>Labor and Delivery: Cefuroxime axetil has not been studied for use during
labor and delivery.<br/>Nursing Mothers: Because cefuroxime is excreted in human milk, consideration
should be given to discontinuing nursing temporarily during treatment
with cefuroxime axetil.<br/>Pediatric Use: The safety and effectiveness of CEFTIN have been
established for pediatric patients aged 3 months to 12 years
for acute bacterial maxillary sinusitis based upon its approval in
adults. Use of CEFTIN in pediatric patients is supported by pharmacokinetic
and safety data in adults and pediatric patients, and by clinical
and microbiological data from adequate and well-controlled studies
of the treatment of acute bacterial maxillary sinusitis in adults
and of acute otitis media with effusion in pediatric patients. It
is also supported by postmarketing adverse events surveillance (see
CLINICAL PHARMACOLOGY, INDICATIONS AND USAGE, ADVERSE REACTIONS, DOSAGE
AND ADMINISTRATION, and CLINICAL STUDIES).<br/>Geriatric Use: Of the total number of subjects who received cefuroxime
axetil in 20 clinical studies of CEFTIN, 375 were 65 and over
while 151 were 75 and over. No overall differences in safety or effectiveness
were observed between these subjects and younger adult subjects. The geriatric patients reported somewhat fewer gastrointestinal
events and less frequent vaginal candidiasis compared with patients
aged 12 to 64 years old; however, no clinically significant differences
were reported between the elderly and younger adult patients. Other
reported clinical experience has not identified differences in responses
between the elderly and younger adult patients.
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Overdosage of cephalosporins can cause cerebral
irritation leading to convulsions. Serum levels of cefuroxime can
be reduced by hemodialysis and peritoneal dialysis.
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cefuroxime axetil
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CEFTIN (Powder, For Suspension)
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CEFTIN TABLETS IN CLINICAL TRIALS: 7 to 10 Days
Dosing Multiple-Dose
Dosing Regimens Using multiple doses
of cefuroxime axetil tablets, 912 patients were treated with cefuroxime
axetil (125 to 500 mg twice daily). There were no deaths or permanent
disabilities thought related to drug toxicity. Twenty (2.2%) patients
discontinued medication due to adverse events thought by the investigators
to be possibly, probably, or almost certainly related to drug toxicity.
Seventeen (85%) of the 20 patients who discontinued therapy did sobecause of gastrointestinal disturbances, including diarrhea, nausea,
vomiting, and abdominal pain. The percentage of cefuroxime axetil
tablet-treated patients who discontinued study drug because of adverse
events was very similar at daily doses of 1,000, 500, and 250 mg
(2.3%, 2.1%, and 2.2%, respectively). However, the incidence of gastrointestinal
adverse events increased with the higher recommended doses. The following adverse events were thought by the investigators
to be possibly, probably, or almost certainly related to cefuroximeaxetil tablets in multiple-dose clinical trials (n = 912
cefuroxime axetil-treated patients).<br/>5-Day Experience (see CLINICAL
STUDIES section): In clinical trials using CEFTIN in a dose of 250 mg
twice daily in the treatment of secondary bacterial infections of
acute bronchitis, 399 patients were treated for 5 days and
402 patients were treated for 10 days. No difference in
the occurrence of adverse events was found between the 2 regimens.<br/>In Clinical Trials for Early
Lyme Disease With 20 Days Dosing: Two multicenter trials assessed cefuroxime axetil
tablets 500 mg twice a day for 20 days. The most common
drug-related adverse experiences were diarrhea (10.6% of patients),
Jarisch-Herxheimer reaction (5.6%), and vaginitis (5.4%). Other adverse
experiences occurred with frequencies comparable to those reported
with 7 to 10 days dosing.<br/>Single-Dose Regimen for Uncomplicated
Gonorrhea: In clinical trials using a single dose of cefuroxime
axetil tablets, 1,061 patients were treated with the recommended
dosage of cefuroxime axetil (1,000 mg) for the treatment of uncomplicated
gonorrhea. There were no deaths or permanent disabilities thought
related to drug toxicity in these studies. The
following adverse events were thought by the investigators to be possibly,
probably, or almost certainly related to cefuroxime axetil in 1,000-mg
single-dose clinical trials of cefuroxime axetil tablets in the treatment
of uncomplicated gonorrhea conducted in the United States.
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CEFTIN TABLETS AND CEFTIN FOR ORAL SUSPENSION ARE
NOT BIOEQUIVALENT AND ARE THEREFORE NOT SUBSTITUTABLE ON A MILLIGRAM-PER-MILLIGRAM
BASIS (SEE CLINICAL PHARMACOLOGY). BEFORE THERAPY
WITH CEFTIN PRODUCTS IS INSTITUTED, CAREFUL INQUIRY SHOULD BE MADE
TO DETERMINE WHETHER THE PATIENT HAS HAD PREVIOUS HYPERSENSITIVITY
REACTIONS TO CEFTIN PRODUCTS, OTHER CEPHALOSPORINS, PENICILLINS, OR
OTHER DRUGS. IF THIS PRODUCT IS TO BE GIVEN TO PENICILLIN-SENSITIVE
PATIENTS, CAUTION SHOULD BE EXERCISED BECAUSE CROSS-HYPERSENSITIVITY
AMONG BETA��LACTAM ANTIBIOTICS HAS BEEN CLEARLY DOCUMENTED AND
MAY OCCUR IN UP TO 10% OF PATIENTS WITH A HISTORY OF PENICILLIN ALLERGY.
IF A CLINICALLY SIGNIFICANT ALLERGIC REACTION TO CEFTIN PRODUCTS OCCURS,
DISCONTINUE THE DRUG AND INSTITUTE APPROPRIATE THERAPY. SERIOUS ACUTE
HYPERSENSITIVITY REACTIONS MAY REQUIRE TREATMENT WITH EPINEPHRINE
AND OTHER EMERGENCY MEASURES, INCLUDING OXYGEN, INTRAVENOUS FLUIDS,
INTRAVENOUS ANTIHISTAMINES, CORTICOSTEROIDS, PRESSOR AMINES, AND AIRWAY
MANAGEMENT, AS CLINICALLY INDICATED. Pseudomembranous
colitis has been reported with nearly all antibacterial agents, including
cefuroxime, and may range from mild to life threatening. Therefore,
it is important to consider this diagnosis in patients who present
with diarrhea subsequent to the administration of antibacterial agents. Treatment with antibacterial agents alters normal flora
of the colon and may permit overgrowth of clostridia. Studies indicate
that a toxin produced by Clostridium
difficile is one primary cause of antibiotic-associated
colitis. After the diagnosis of pseudomembranous
colitis has been established, appropriate therapeutic measures should
be initiated. Mild cases of pseudomembranous colitis usually respond
to drug discontinuation alone. In moderate to severe cases, consideration
should be given to management with fluids and electrolytes, protein
supplementation, and treatment with an antibacterial drug effective
against Clostridium difficile.
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NOTE: CEFTIN TABLETS AND CEFTIN FOR ORAL SUSPENSION
ARE NOT BIOEQUIVALENT AND ARE NOT SUBSTITUTABLE ON A MILLIGRAM-PER-MILLIGRAM
BASIS (SEE CLINICAL PHARMACOLOGY).<br/>CEFTIN Tablets: CEFTIN 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:<br/>CEFTIN for Oral Suspension: CEFTIN for Oral Suspension is indicated for the
treatment of pediatric patients 3 months to 12 years of
age with mild to moderate infections caused by susceptible strains
of the designated microorganisms in the conditions listed below. The
safety and effectiveness of CEFTIN for Oral Suspension in the treatment
of infections other than those specifically listed below have not
been established either by adequate and well��controlled trials
or by pharmacokinetic data with which to determine an effective and
safe dosing regimen. To reduce the development of drug-resistant bacteria
and maintain the effectiveness of CEFTIN and other antibacterial drugs,
CEFTIN 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.
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CEFTIN
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