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All about: Ceftin

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Generic Name: cefuroxime axetil
Dosage Form: Tablets and powder for oral suspension

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 bacteria.

Ceftin Description

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, 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:

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.

Ceftin - Clinical Pharmacology

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*

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

7.0

3.0

1.2

27.4

1,000 mg

13.6

2.5

1.3

50.0

*Mean values of 12 healthy adult volunteers.

Drug administered immediately after a meal.

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

Dose

(Cefuroxime

Equivalent)

n

Peak Plasma

Concentration

(mcg/mL)

Time of Peak

Plasma

Concentration (hr)

Mean

Elimination

Half-Life

(hr)

AUC

(mcg-hr mL)

10 mg/kg

8

3.3

3.6

1.4

12.4

15 mg/kg

12

5.1

2.7

1.9

22.5

20 mg/kg

8

7.0

3.1

1.9

32.8

*Mean age = 23 months.

Drug administered with milk or milk products.

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

Dose

(Cefuroxime

Equivalent)

Peak Plasma Concentration

(mcg/mL)

Time of Peak

Plasma

Concentration (hr)

Mean Elimination

Half-Life (hr)

AUC

(mcg-hr mL)

250 mg/5 mL

2.23

3

1.40

8.92

2 x 125 mg/5 mL

2.37

3

1.44

9.75

*Mean values of 18 healthy adult volunteers.

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.

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).

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 strains. Cefuroxime is stable to many bacterial beta-lactamases, especially plasmid-mediated enzymes that are commonly found in enterobacteriaceae.

Cefuroxime has been demonstrated to be active against most strains of the following microorganisms both in vitro and in clinical infections as described in the INDICATIONS AND USAGE section (see INDICATIONS AND USAGE section).

Aerobic Gram-Positive Microorganisms

Staphylococcus aureus (including beta­lactamase−producing strains)

Streptococcus pneumoniae

Streptococcus pyogenes

Aerobic Gram-Negative Microorganisms

Escherichia coli

Haemophilus influenzae (including beta­lactamase−producing strains)

Haemophilus parainfluenzae

Klebsiella pneumoniae

Moraxella catarrhalis (including beta­lactamase−producing strains)

Neisseria gonorrhoeae(including beta­lactamase−producing strains)

Spirochetes

Borrelia burgdorferi

Cefuroxime has been shown to be active in vitro against most strains of the following microorganisms; however, the clinical significance of these findings is unknown.

Cefuroxime exhibits in vitro minimum inhibitory concentrations (MICs) of 4.0 mcg/mL or less (systemic susceptible breakpoint) against most (≥90%) strains of the following microorganisms; however, the safety and effectiveness of cefuroxime in treating clinical infections due to these microorganisms have not been established in adequate and well-controlled trials.

Aerobic Gram-Positive Microorganisms

Staphylococcus epidermidis

Staphylococcus saprophyticus

Streptococcus agalactiae

NOTE: Certain strains of enterococci, e.g., Enterococcus faecalis (formerly Streptococcus faecalis), are resistant to cefuroxime. Methicillin­resistant staphylococci are resistant to cefuroxime.

Aerobic Gram-Negative Microorganisms

Morganella morganii

Proteus inconstans

Proteus mirabilis

Providencia rettgeri

NOTE: Pseudomonas spp., Campylobacter spp., Acinetobactercalcoaceticus, and most strains of Serratia spp. and Proteus vulgaris are resistant to most first- and second-generation cephalosporins. Some strains of Morganellamorganii, Enterobactercloacae , and Citrobacter spp. have been shown by in vitro tests to be resistant to cefuroxime and other cephalosporins.

Anaerobic Microorganisms

Peptococcusniger

NOTE: Most strains of Clostridium difficile and Bacteroides fragilis are resistant to cefuroxime.

Susceptibility Tests

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 method1 (broth, agar, or microdilution) or equivalent with cefuroxime powder. The MIC values obtained should be interpreted according to the following criteria:

MIC (mcg/mL)

Interpretation

≤4

(S) Susceptible

8­16

(I) Intermediate

≥32

(R) Resistant

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:

Microorganism

MIC (mcg/mL)

Escherichia coliATCC 25922

2­8

Staphylococcusaureus ATCC 29213

0.5­2

Diffusion Techniques

Quantitative methods that require measurement of zone diameters provide estimates of the susceptibility of bacteria to antimicrobial compounds. One such standardized procedure2 that 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:

Zone Diameter (mm)

Interpretation

≥23

(S) Susceptible

15­22

(I) Intermediate

≤14

(R) Resistant

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:

Microorganism

Zone Diameter (mm)

Escherichia coliATCC 25922

20­26

Staphylococcusaureus ATCC 25923

27­35

Indications and Usage for Ceftin

NOTE: Ceftin TABLETS AND Ceftin FOR ORAL SUSPENSION ARE NOT BIOEQUIVALENT AND ARE NOT SUBSTITUTABLE ON A MILLIGRAM-PER-MILLIGRAMBASIS (SEE CLINICAL PHARMACOLOGY).

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:

  1. Pharyngitis/Tonsillitis caused by Streptococcus pyogenes.
  2. NOTE: The usual drug of choice in the treatment and prevention of streptococcal infections, including the prophylaxis of rheumatic fever, is penicillin given by the intramuscular route. Ceftin Tablets are generally effective in the eradication of streptococci from the nasopharynx; however, substantial data establishing the efficacy of cefuroxime in the subsequent prevention of rheumatic fever are not available. Please also note that in all clinical trials, all isolates had to be sensitive to both penicillin and cefuroxime. There are no data from adequate and well­controlled trials to demonstrate the effectiveness of cefuroxime in the treatment of penicillin-resistant strains of Streptococcus pyogenes.
  3. Acute Bacterial Otitis Media caused by Streptococcus pneumoniae, Haemophilus influenzae (including beta-lactamase−producing strains), Moraxella catarrhalis (including beta-lactamase−producing strains), or Streptococcus pyogenes.
  4. Acute Bacterial Maxillary Sinusitis caused by Streptococcus pneumoniae or Haemophilus influenzae (non-beta-lactamase−producing strains only). (See CLINICAL STUDIES section.)
  5. NOTE: In view of the insufficient numbers of isolates of beta-lactamase−producing strains of Haemophilus influenzae and Moraxella catarrhalis that were obtained from clinical trials with Ceftin Tablets for patients with acute bacterial maxillary sinusitis, it was not possible to adequately evaluate the effectiveness of Ceftin Tablets for sinus infections known, suspected, or considered potentially to be caused by beta-lactamase−producing Haemophilus influenzae or Moraxella catarrhalis.
  6. Acute Bacterial Exacerbations of Chronic Bronchitis and Secondary Bacterial Infections of Acute Bronchitis caused by Streptococcus pneumoniae, Haemophilus influenzae (beta-lactamase negative strains), or Haemophilus parainfluenzae (beta­lactamase negative strains). (See DOSAGE AND ADMINISTRATION section and CLINICAL STUDIES section.)
  7. Uncomplicated Skin and Skin-Structure Infections caused by Staphylococcus aureus (including beta-lactamase−producing strains) or Streptococcus pyogenes.
  8. Uncomplicated Urinary Tract Infections caused by Escherichia coli or Klebsiella pneumoniae.
  9. Uncomplicated Gonorrhea, urethral and endocervical, caused by penicillinase-producing and non­penicillinase−producing strains of Neisseria gonorrhoeae anduncomplicated gonorrhea, rectal, in females, caused by non­penicillinase−producing strains of Neisseria gonorrhoeae.
  10. Early Lyme Disease (erythema migrans) caused by Borrelia burgdorferi.

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 well­controlled trials or by pharmacokinetic data with which to determine an effective and safe dosing regimen.

  1. Pharyngitis/Tonsillitis caused by Streptococcus pyogenes.
  2. NOTE: The usual drug of choice in the treatment and prevention of streptococcal infections, including the prophylaxis of rheumatic fever, is penicillin given by the intramuscular route. Ceftin for Oral Suspension is generally effective in the eradication of streptococci from the nasopharynx; however, substantial data establishing the efficacy of cefuroxime in the subsequent prevention of rheumatic fever are not available. Please also note that in all clinical trials, all isolates had to be sensitive to both penicillin and cefuroxime. There are no data from adequate and well-controlled trials to demonstrate the effectiveness of cefuroxime in the treatment of penicillin-resistant strains of Streptococcuspyogenes.
  3. Acute Bacterial Otitis Media caused by Streptococcus pneumoniae, Haemophilus influenzae (including beta-lactamase−producing strains), Moraxella catarrhalis (including beta-lactamase−producing strains), or Streptococcus pyogenes.
  4. Impetigo caused by Staphylococcus aureus (including beta-lactamase−producing strains) or Streptococcus pyogenes.

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.

Contraindications

Ceftin products are contraindicated in patients with known allergy to the cephalosporin group of antibiotics.

Warnings

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 BETA­LACTAM 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.

Precautions

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 broad­spectrum 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.

Information for Patients/Caregivers (Pediatric)

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.

  1. During clinical trials, the tablet was tolerated by pediatric patients old enough to swallow the cefuroxime axetil tablet whole. The crushed tablet has a strong, persistent, bitter taste and should not be administered to pediatric patients in this manner. Pediatric patients who cannot swallow the tablet whole should receive the oral suspension.
  2. Discontinuation of therapy due to taste and/or problems of administering this drug occurred in 1.4% of pediatric patients given the oral suspension. Complaints about taste (which may impair compliance) occurred in 5% of pediatric patients.
  3. Patients should be counseled that antibacterial drugs, including Ceftin, should only be used to treat bacterial infections. They do not treat viral infections (e.g., the common cold). When Ceftin is prescribed to treat a bacterial infection, patients should be told that although it is common to feel better early in the course of therapy, the medication should be taken exactly as directed. Skipping doses or not completing the full course of therapy may: (1) decrease the effectiveness of the immediate treatment, and (2) increase the likelihood that bacteria will develop resistance and will not be treatable by Ceftin or other antibacterial drugs in the future.

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.

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.

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 based on mg/m2) have revealed no impairment of fertility.

Pregnancy

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/m2) and in rats at doses up to 1,000 mg/kg/day (9 times the recommended maximum human dose based on mg/m2) 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.

Labor and Delivery

Cefuroxime axetil has not been studied for use during labor and delivery.

Nursing Mothers

Because cefuroxime is excreted in human milk, consideration should be given to discontinuing nursing temporarily during treatment with cefuroxime axetil.

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).

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.

Adverse Reactions

Ceftin TABLETS IN CLINICAL TRIALS

Multiple-Dose Dosing Regimens

7 to 10 Days Dosing

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 so because 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 cefuroxime axetil tablets in multiple-dose clinical trials (n = 912 cefuroxime axetil-treated patients).

Multiple-Dose Dosing Regimens—Clinical Trials

Table 4. Adverse Reactions—Ceftin Tablets

Incidence ≥1%

Diarrhea/loose stools 3.7%

Nausea/vomiting 3.0%

Transient elevation in AST 2.0%

Transient elevation in ALT 1.6%

Eosinophilia 1.1%

Transient elevation in LDH 1.0%

Incidence

<1% but >0.1%

Abdominal pain

Abdominal cramps

Flatulence

Indigestion

Headache

Vaginitis

Vulvar itch

Rash

Hives

Itch

Dysuria

Chills

Chest pain

Shortness of breath

Mouth ulcers

Swollen tongue

Sleepiness

Thirst

Anorexia

Positive Coombs test

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.

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.

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.

1-g Single­Dose Regimen for Uncomplicated Gonorrhea—Clinical Trials

Table 5. Adverse Reactions—Ceftin Tablets

Incidence ≥1%

Nausea/vomiting 6.8%

Diarrhea 4.2%

Incidence

<1% but >0.1%

Abdominal pain

Dyspepsia

Erythema

Rash

Pruritus

Vaginal candidiasis

Vaginal itch

Vaginal discharge

Headache

Dizziness

Somnolence

Muscle cramps

Muscle stiffness

Muscle spasm of neck

Tightness/pain in chest

Bleeding/pain in urethra

Kidney pain

Tachycardia

Lockjaw­type reaction

Ceftin FOR ORAL SUSPENSION IN CLINICAL TRIALS

In clinical trials using multiple doses of cefuroxime axetil powder for oral suspension, pediatric patients (96.7% of whom were younger than 12 years of age) were treated with the recommended dosages of cefuroxime axetil (20 to 30 mg/kg/day divided twice a day up to a maximum dose of 500 or 1,000 mg/day, respectively). There were no deaths or permanent disabilities in any of the patients in these studies. Eleven US patients (1.2%) discontinued medication due to adverse events thought by the investigators to be possibly, probably, or almost certainly related to drug toxicity. The discontinuations were primarily for gastrointestinal disturbances, usually diarrhea or vomiting. During clinical trials, discontinuation of therapy due to the taste and/or problems with administering this drug occurred in 13 (1.4%) pediatric patients enrolled at centers in the United States.

The following adverse events were thought by the investigators to be possibly, probably, or almost certainly related to cefuroxime axetil for oral suspension in multiple-dose clinical trials (n = 931 cefuroxime axetil-treated US patients).

Multiple­Dose Dosing Regimens—Clinical Trials

Table 6. Adverse Reactions—Ceftin for Oral Suspension

Incidence ≥1%

Diarrhea/loose stools 8.6%

Dislike of taste 5.0%

Diaper rash 3.4%

Nausea/vomiting 2.6%

Incidence

<1% but >0.1%

Abdominal pain

Flatulence

Gastrointestinal infection

Candidiasis

Vaginal irritation

Rash

Hyperactivity

Irritable behavior

Eosinophilia

Positive direct Coombs test

Elevated liver enzymes

Viral illness

Upper respiratory infection

Sinusitis

Cough

Urinary tract infection

Joint swelling

Arthralgia

Fever

Ptyalism

CEPHALOSPORIN-CLASS ADVERSE REACTIONS

In addition to the adverse reactions listed above that have been observed in patients treated with cefuroxime axetil, the following adverse reactions and altered laboratory tests have been reported for cephalosporin-class antibiotics: toxic nephropathy, aplastic anemia, hemorrhage, increased BUN, increased creatinine, false-positive test for urinary glucose, increased alkaline phosphatase, neutropenia, elevated bilirubin, and agranulocytosis.

Several cephalosporins have been implicated in triggering seizures, particularly in patients with renal impairment when the dosage was not reduced (see DOSAGE AND ADMINISTRATION and OVERDOSAGE). If seizures associated with drug therapy occur, the drug should be discontinued. Anticonvulsant therapy can be given if clinically indicated.

Overdosage

Overdosage of cephalosporins can cause cerebral irritation leading to convulsions. Serum levels of cefuroxime can be reduced by hemodialysis and peritoneal dialysis.

Ceftin Dosage and Administration

NOTE: Ceftin TABLETS AND Ceftin FOR ORAL SUSPENSION ARE NOT BIOEQUIVALENT AND ARE NOT SUBSTITUTABLE ON A MILLIGRAM-PER-MILLIGRAM BASIS (SEE CLINICAL PHARMACOLOGY).

(May be administered without regard to meals.)

Table 7. Ceftin Tablets

Population/Infection

Dosage

Duration (days)

Adolescents and Adults (13 years and older)

Pharyngitis/tonsillitis

250 mg b.i.d.

10

Acute bacterial maxillary sinusitis

250 mg b.i.d.

10

Acute bacterial exacerbations of chronic bronchitis

250 or 500 mg b.i.d.

10*

Secondary bacterial infections of acute bronchitis

250 or 500 mg b.i.d.

5-10

Uncomplicated skin and skin-structure infections

250 or 500 mg b.i.d.

10

Uncomplicated urinary tract infections

250 mg b.i.d.

7-10

Uncomplicated gonorrhea

1,000 mg once

single dose

Early Lyme disease

500 mg b.i.d.

20

Pediatric Patients (who can swallow tablets whole)

Acute otitis media

250 mg b.i.d.

10

Acute bacterial maxillary sinusitis

250 mg b.i.d.

10

* The safety and effectiveness of Ceftin administered for less than 10 days in patients with acute exacerbations of chronic bronchitis have not been established.

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:

(Must be administered with food. Shake well each time before using.)

Table 8. Ceftin for Oral Suspension

Population/Infection

Dosage

Daily Maximum Dose

Duration (days)

Pediatric Patients (3 months to 12 years)

Pharyngitis/tonsillitis

20 mg/kg/day divided b.i.d.

500 mg

10

Acute otitis media

30 mg/kg/day divided b.i.d.

1,000 mg

10

Acute bacterial maxillary sinusitis

30 mg/kg/day divided b.i.d.

1,000 mg

10

Impetigo

30 mg/kg/day divided b.i.d.

1,000 mg

10

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.

Directions for Mixing Ceftin for Oral Suspension

Prepare a suspension at the time of dispensing as follows:

  1. Shake the bottle to loosen the powder.
  2. Remove the cap.
  3. Add the total amount of water for reconstitution (see Table 9) and replace the cap.
  4. Invert the bottle and vigorously rock the bottle from side to side so that water rises through the powder.
  5. Once the sound of the powder against the bottle disappears, turn the bottle upright and vigorously shake it in a diagonal direction.
    Table 9. Amount of Water Required for Reconstitution of Labeled Volumes of Ceftin for Oral Suspension

    Ceftin for Oral Suspension

    Labeled Volume After Reconstitution

    Amount of Water Required

    for Reconstitution

    125 mg/5 mL

    100 mL

    37 mL

    250 mg/5 mL

    50 mL

    19 mL

    100 mL

    35 mL

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.

How is Ceftin Supplied

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

60 Tablets/Bottle NDC 0173-0387-42

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.

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 c

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