Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/2399
| Predicate | Object |
|---|---|
| rdf:type | |
| rdfs:label |
Cefuroxime Axetil (Tablet, Film Coated)
|
| dailymed-instance:dosage |
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)<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.
|
| dailymed-instance:descripti... |
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,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: Cefuroxime axetil tablets are film-coated and contain the equivalent of 125 mg, 250 mg or 500 mg of cefuroxime as cefuroxime axetil. Cefuroxime axetil tablets contain the inactive ingredients pregelatinized starch, croscarmellose sodium, sodium lauryl sulphate, microcrystalline cellulose, colloidal silicon dioxide, hydrogenated vegetable oil, opadry white (for 125 mg), opadry blue (for 250 mg and 500 mg). Components of Opadry White (125 mg Tablets) are Hypromellose, Titanium dioxide and Propylene glycol; Opadry Blue (250 mg Tablets) are Hypromellose, Titanium dioxide, Propylene glycol, FD&C Blue # 1 / Brilliant Blue FCF Aluminum Lake, FD&C Blue #2 / Indigo Carmine Aluminum Lake; Opadry Blue (500 mg Tablets) are Hypromellose, Titanium dioxide, Propylene glycol, FD&C Blue # 1 / Brilliant Blue FCF Aluminum Lake, D&C Red #27 / Phloxine Aluminum Lake.
|
| dailymed-instance:clinicalP... |
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 cefuroxime axetil tablets is shown in Table 1.<br/>Comparative Pharmacokinetic Properties: Cefuroxime axetil for oral suspension was not bioequivalent to cefuroxime axetil 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 cefuroxime axetil 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.<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.<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 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 .<br/>Aerobic Gram-Positive Microorganisms: Staphylococcus aureus (including beta-lactamase-producing strains) Streptococcus pneumoniae Streptococcus pyogenes<br/>Aerobic Gram-Negative Microorganisms: Escherichia coli Haemophilus influenzae (including beta-lactamase-producing strains) Haemophilus parainfluenzae Klebsiella pneumoniae Moraxella catarrhalis (including beta-lactamase-producing strains) Neisseria gonorrhoeae (including beta-lactamase-producing strains)<br/>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 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.<br/>Aerobic Gram-Positive Microorganisms: Staphylococcus epidermidis Staphylococcus saprophyticus Streptococcus agalactiae NOTE: Listeria monocytogenes and certain strains of enterococci, e.g., Enterococcus faecalis (formerly Streptococcus faecalis), are resistant to cefuroxime. Methicillin-resistant staphylococci are resistant to cefuroxime.<br/>Aerobic Gram-Negative Microorganisms: Morganella morganii Proteus inconstans Proteus mirabilis Providencia rettgeri NOTE: Pseudomonas spp., Campylobacter spp., Acinetobacter calcoaceticus, Legionella spp., and most strains of Serratia spp. and Proteus vulgaris are resistant to most first- and second-generation cephalosporins. Some strains of Morganella morganii, Enterobacter cloacae, and Citrobacter spp. have been shown by in vitro tests to be resistant to cefuroxime and other cephalosporins.<br/>Anaerobic Microorganisms: Peptococcus niger NOTE: Most strains of Clostridium difficile and Bacteroides fragilis are resistant to cefuroxime.<br/>Susceptibility Tests:<br/>DilutionTechniques: 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/>DiffusionTechniques: 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:
|
| dailymed-instance:activeIng... | |
| dailymed-instance:contraind... |
Cefuroxime axetil is contraindicated in patients with known allergy to the cephalosporin group of antibiotics.
|
| dailymed-instance:supply |
Cefuroxime axetil tablets, USP 125 mg: white to off white colored film coated, capsule shaped tablets having���125���on one side and���P124���on the other side. Tablets are supplied as follows: Bottle of 20 Tablets NDC 49884-025-07 Bottle of 60 Tablets NDC 49884-025-02 Bottle of 500 Tablets NDC 49884-025-05 Bottle of 1000 Tablets NDC 49884-025-10 10 tablets, 2 rows of 5 tablets each with NDC 49884-025-74 cross perforation and individually labeled blisters, 10 such blisters are packed in one carton.<br/>Cefuroxime axetil tablets, USP 250 mg: Light blue colored film coated, capsule shaped tablets having���526���on one side and���par���on the other side. Tablets are supplied as follows: Bottle of 20 Tablets NDC 49884-526-07 Bottle of 60 Tablets NDC 49884-526-02 Bottle of 500 Tablets NDC 49884-526-05 Bottle of 1000 Tablets NDC 49884-526-10 10 tablets, 2 rows of 5 tablets each with NDC 49884-526-74 cross perforation and individually labeled blisters, 10 such blisters are packed in one carton.<br/>Cefuroxime axetil tablets, USP 500 mg: Dark blue colored film coated, capsule shaped tablets having���527���on one side and���par���on the other side. Tablets are supplied as follows: Bottle of 20 Tablets NDC 49884-527-07 Bottle of 60 Tablets NDC 49884-527-02 Bottle of 500 Tablets NDC 49884-527-05 10 tablets, 2 rows of 5 tablets each with NDC 49884-527-74 cross perforation and individually labeled blisters, 5 such blisters are packed in one carton. Store at 20��to 25��C (68��to 77��F); [see USP Controlled Room Temperature]. Replace cap securely after each opening.
|
| dailymed-instance:activeMoi... | |
| dailymed-instance:inactiveI... |
dailymed-ingredient:colloidal_silicon_dioxide,
dailymed-ingredient:croscarmellose_sodium,
dailymed-ingredient:hydrogenated_vegetable_oil,
dailymed-ingredient:microcrystalline_cellulose,
dailymed-ingredient:opadry_white,
dailymed-ingredient:pregelatinized_starch,
dailymed-ingredient:sodium_lauryl_sulphate
|
| dailymed-instance:precautio... |
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 cefuroxime axetil tablets 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.<br/>Information for Patients / Caregivers (Pediatric): 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. Patients should be counseled that antibacterial drugs, including cefuroxime axetil tablets, should only be used to treat bacterial infections. They do not treat viral infections (e.g., the common cold). When cefuroxime axetil tablet 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 cefuroxime axetil tablets or other antibacterial drugs in the future.<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 cefuroxime axetil tablets 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 based on 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 cefuroxime axetil 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 cefuroxime axetil 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 .<br/>Geriatric Use: Of the total number of subjects who received cefuroxime axetil in 20 clinical studies of cefuroxime axetil, 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.
|
| dailymed-instance:genericMe... |
cefuroxime Axetil
|
| dailymed-instance:fullName |
Cefuroxime Axetil (Tablet, Film Coated)
|
| dailymed-instance:adverseRe... |
CEFUROXIME AXETIL TABLETS IN CLINICAL TRIALS:<br/>Multiple-Dose Dosing Regimens:<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.<br/>POSTMARKETING EXPERIENCE WITH CEFUROXIME AXETIL TABLETS: In addition to adverse events reported during clinical trials, the following events have been identified during clinical practice in patients treated with cefuroxime axetil tablets were reported spontaneously. Data are generally insufficient to allow an estimate of incidence or to establish causation.<br/>General: The following hypersensitivity reactions have been reported: anaphylaxis, angioedema, pruritus, rash, serum sickness-like reaction, urticaria.<br/>Gastrointestinal: Pseudomembranous colitis .<br/>Hematologic: Hemolytic anemia, leukopenia, pancytopenia, thrombocytopenia, and increased prothrombin time.<br/>Hepatic: Hepatic impairment including hepatitis and cholestasis, jaundice.<br/>Neurologic: Seizure.<br/>Skin: Erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis.<br/>Urologic: Renal dysfunction.<br/>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 . If seizures associated with drug therapy occur, the drug should be discontinued. Anticonvulsant therapy can be given if clinically indicated.
|
| dailymed-instance:indicatio... |
To reduce the development of drug-resistant bacteria and maintain the effectiveness of cefuroxime axetil tablets and other antibacterial drugs, cefuroxime axetil tablets 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)<br/>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: 1. Pharyngitis/Tonsillitis caused by Streptococcus pyogenes. 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. Cefuroxime axetil 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 well-controlled trials to demonstrate the effectiveness of cefuroxime in the treatment of penicillin-resistant strains of Streptococcus pyogenes. 2. 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. 3. Acute Bacterial Maxillary Sinusitis caused by Streptococcus pneumoniae or Haemophilus influenzae (non-beta-lactamase-producing strains only). 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 cefuroxime axetil tablets for patients with acute bacterial maxillary sinusitis, it was not possible to adequately evaluate the effectiveness of cefuroxime axetil tablets for sinus infections known, suspected, or considered potentially to be caused by beta-lactamase-producing Haemophilus influenzae or Moraxella catarrhalis. 4. 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 (beta-lactamase negative strains). 5. Uncomplicated Skin and Skin-Structure Infections caused by Staphylococcus aureus (including beta-lactamase-producing strains) or Streptococcus pyogenes. 6. Uncomplicated Urinary Tract Infections caused by Escherichia coli or Klebsiella pneumoniae. 7. Uncomplicated Gonorrhea, urethral and endocervical, caused by penicillinase-producing and non-penicillinase-producing strains of Neisseria gonorrhoeae and uncomplicated gonorrhea, rectal, in females, caused by non-penicillinase-producing strains of Neisseria gonorrhoeae. 8. Early Lyme Disease (erythema migrans) caused by Borrelia burgdorferi.
|
| dailymed-instance:represent... | |
| dailymed-instance:routeOfAd... | |
| dailymed-instance:name |
Cefuroxime Axetil
|