Ceftin Information
Ceftin ()
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 ()-1-hydroxyethyl (6,7)-7-[2-(2-furyl)glyoxyl-amido]-3-(hydroxymethyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]-oct-2-ene-2-carboxylate, 7-()-(-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.
Ceftin () Clinical Pharmacology
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.
a
b
a
b
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). 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.
a
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.
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).
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 (see INDICATIONS AND USAGE).
Ceftin () Indications And Usage
NOTE: Ceftin () TABLETS AND Ceftin () FOR ORAL SUSPENSION ARE NOT BIOEQUIVALENT AND ARE NOT SUBSTITUTABLE ON A MILLIGRAM-PER-MILLIGRAM BASIS (SEE CLINICAL PHARMACOLOGY).
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.
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.
Ceftin () Contraindications
Ceftin () products are contraindicated in patients with known allergy to the cephalosporin group of antibiotics.
Ceftin () Warnings
If CDAD is suspected or confirmed, ongoing antibiotic use not directed against may need to be discontinued. Appropriate fluid and electrolyte management, protein supplementation, antibiotic treatment of , and surgical evaluation should be instituted as clinically indicated.
Ceftin () Precautions
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.
Diarrhea is a common problem caused by antibiotics which usually ends when the antibiotic is discontinued. Sometimes after starting treatment with antibiotics, patients can develop watery and bloody stools (with or without stomach cramps and fever) even as late as 2 or more months after having taken the last dose of the antibiotic. If this occurs, patients should contact their physician as soon as possible.
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.
Ceftin () Adverse Reactions
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.
Table 5. Adverse Reactions--Ceftin () Tablets
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).
Table 6. Adverse Reactions—Ceftin () for Oral Suspension
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.
Ceftin () Overdosage
Overdosage of cephalosporins can cause cerebral irritation leading to convulsions. Serum levels of cefuroxime can be reduced by hemodialysis and peritoneal dialysis.
Ceftin () How Supplied
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
Store the tablets between 15° and 30°C (59° and 86°F). Replace cap securely after each opening.
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:
100mL 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.
Ceftin () References
Ceftin () and AUGMENTIN are registered trademarks of GlaxoSmithKline.
CLINITEST and CLINISTIX are registered trademarks of Ames Division, Miles Laboratories, Inc.
GlaxoSmithKline
Research Triangle Park, NC 27709
©2010, GlaxoSmithKline
All rights reserved.
January 2010
CFT:1PI
Ceftin () Principal Display Panel
See package insert for Dosage and Administration.
Store between 15 and 30C (59 and 86F).
Replace cap securely after each opening.
GlaxoSmithKline
Research Triangle Park, NC 27709
Made in England
4142817
Rev. 2/02
Ceftin () Principal Display Panel
Each tablet contains cefuroxime axetil equivalent to 500 mg of cefuroxime.
See package insert for Dosage and Administration.
Store between 15 and 30C (59 and 86F). Replace cap securely after each opening.
GlaxoSmithKline
Research Triangle Park, NC 27709
Made in England
4141667 Rev. 12/01
Ceftin () Principal Display Panel
Contains 3.0 g cefuroxime axetil equivalent to 2.5 g of cefuroxime.
Phenylketonurics: Contains Phenylalanine 11.8 mg per 5 mL (1 teaspoonful) constituted suspension.
See package insert for Dosage and Administration.
Before reconstitution, store dry powder between 2 and 30C (36 and 86F).
After reconstitution, store suspension between 2 and 8C (36 and 46F), in a refrigerator. . Replace cap securely after each opening. Discard after 10 days.
GlaxoSmithKline
Research Triangle Park, NC 27709
Made in England
10000000022540 Rev. 12/05
Ceftin () Principal Display Panel
Contains 3.6 g cefuroxime axetil equivalent to 3 g of cefuroxime.
Phenylketonurics: Contains Phenylalanine 25.2 mg per 5 mL (1 teaspoonful) constituted suspension.
See package insert for Dosage and Administration.
Before reconstitution, store dry powder between 2 and 30C (36 and 86F).
After reconstitution, store suspension between 2 and 8C (36 and 46F), in a refrigerator. Replace cap securely after each opening. Discard after 10 days.
GlaxoSmithKline
Research Triangle Park, NC 27709
Made in England
10000000022489 Rev. 12/05
