Ceftin (Cefuroxime Axetil)


Glaxo Wellcome

Cefuroxime Axetil


Action And Clinical Pharmacology: Cefuroxime axetil is an orally active prodrug of cefuroxime. After oral administration, cefuroxime axetil is absorbed from the gastrointestinal tract and rapidly hydrolyzed by nonspecific esterases in the intestinal mucosa and blood to release cefuroxime into the blood stream. Conversion to cefuroxime, the microbiologically active form, occurs rapidly. The inherent properties of cefuroxime are unaltered after its administration as cefuroxime axetil.

Cefuroxime exerts its bactericidal effect by binding to an enzyme or enzymes referred to as penicillin-binding proteins (PBPs) involved in bacterial cell wall synthesis. This binding results in inhibition of bacterial cell wall synthesis and subsequent cell death. Specifically, cefuroxime shows high affinity for PBP 3, a primary target for cefuroxime in gram-negative organisms such as E. coli.

Indications And Clinical Uses: For the treatment of patients with mild to moderately severe infections caused by susceptible strains of the designated organisms in the following diseases:

Upper Respiratory Tract Infections: Pharyngitis and tonsillitis caused by S. pyogenes. Otitis Media caused by S. pneumoniae, S. pyogenes (group A beta-hemolytic streptococci), H. influenzae (beta-lactamase negative and beta-lactamase positive strains) or M. catarrhalis. Sinusitis caused by M. catarrhalis, S. pneumoniae or H. influenzae (including ampicillin-resistant strains).

Lower Respiratory Tract Infections: Pneumonia or bronchitis caused by S. pneumoniae, H. influenzae (including ampicillin-resistant strains), H. parainfluenzae, K. pneumoniae or M. catarrhalis.

Skin Structure Infections: Skin structure infections caused by S. aureus, S. pyogenes or S. agalactiae.

Gonorrhea: Acute uncomplicated urethritis and cervicitis caused by N. gonorrheae.

Bacteriologic studies to determine the causative organism and its susceptibility to cefuroxime should be performed. Once these results become available antibiotic treatment should be adjusted if required.

Contra-Indications: Type I hypersensitivity to cefuroxime or to any of the cephalosporin group of antibiotics.

Manufacturers’ Warnings In Clinical States: Before therapy with cefuroxime axetil is instituted, careful inquiry should be made to determine whether the patient has had previous hypersensitivity reactions to cefuroxime, cephalosporins, penicillin, or other drugs. Cefuroxime axetil should be administered with caution to any patient who has demonstrated some form of allergy, particularly to drugs. There is some clinical and laboratory evidence of partial cross allergenicity of the cephalosporins and penicillin. Special care is indicated in patients who have experienced anaphylactic reaction to penicillins. If an allergic reaction to cefuroxime axetil occurs, treatment should be discontinued and standard agents (e.g., epinephrine, antihistamines, corticosteroids) administered as necessary.

Pseudomembranous colitis has been reported to be associated with the use of cefuroxime axetil and other broad-spectrum antibiotics. Therefore, it is important to consider its diagnosis in patients administered cefuroxime axetil who develop diarrhea. Treatment with broad-spectrum antibiotics, including cefuroxime axetil, alters the normal flora of the colon and may permit overgrowth of Clostridia. Studies indicate that a toxin produced by C. difficile is one primary cause of antibiotic-associated colitis. Mild cases of colitis may respond to drug discontinuance alone. Moderate to severe cases should be managed with fluid, electrolyte, and protein supplementation as indicated. When the colitis is severe or not relieved by discontinuance of cefuroxime axetil administration, consideration should be given to the administration of oral vancomycin or other suitable therapy. Other possible causes of colitis should also be considered.

Precautions: Broad-spectrum antibiotics including cefuroxime axetil should be administered with caution to individuals with a history of gastrointestinal disease, particularly colitis.

The concomitant administration of aminoglycosides and some cephalosporins has caused nephrotoxicity. There is no evidence that cefuroxime axetil, when administered alone, is nephrotoxic, although transient elevations of BUN and serum creatinine have been observed in clinical studies. However, the effect of administering cefuroxime axetil concomitantly with aminoglycosides is not known.

Studies suggest that the concomitant use of potent diuretics, such as furosemide and ethacrynic acid, may increase the risk of renal toxicity with cephalosporins.

Prolonged treatment with cefuroxime axetil may result in the overgrowth of nonsusceptible organisms, including species originally sensitive to the drug. Repeated evaluation of the patient’s condition is essential. If superinfection occurs during therapy, appropriate measures should be taken. Should an organism become resistant during antibiotic therapy, cefuroxime axetil should be discontinued and another appropriate antibiotic should be substituted.

Pregnancy: The safety of cefuroxime axetil in pregnancy has not been established. The use of cefuroxime axetil in pregnant women requires that the likely benefit from the drug be weighed against the possible risk to the mother and fetus. Animal studies following parenteral administration have shown cefuroxime to affect bone calcification in the fetus and to cause maternal toxicity in the rabbit. Reproduction studies that have been performed in mice and rats at oral doses of up to 50 to 160 times the human dose 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.

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

Drug Interactions: Drugs which reduce gastric acidity may result in a lower bioavailability of cefuroxime axetil compared with that of the fasting state and tend to cancel the effect of post-prandial absorption.

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, Tes-Tape). 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.

Cefuroxime does not interfere with the assay of serum and urine creatinine by the alkaline picrate method.

Cephalosporins as a class tend to be absorbed onto the surface of red cell membranes and react with antibodies directed against the drug to produce a positive Coombs’ test (which can interfere with cross-matching of blood) and very rarely hemolytic anemia.

Adverse Reactions: The following adverse reactions have been reported: Gastrointestinal (approximately 8% of patients): diarrhea (5.6%), nausea (2.4%), vomiting (2%), loose stools (1.3%). Reports of pseudomembranous colitis (see Warnings) have occurred.

Hepatic (3% of patients): transient elevations of AST (2%), ALT (1.6%) and LDH (1%). Jaundice has been reported very rarely.

CNS (2.2% of patients): headache and dizziness.

Hypersensitivity (1.3% of patients): rashes (0.6%), pruritus (0.3%), urticaria (0.2%), shortness of breath and rare reports of bronchospasm. Hypersensitivity reactions to cefuroxime axetil may occur in patients who report delayed hypersensitivity to penicillins (see Warnings). As with other cephalosporins, there have been rare reports of erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, serum sickness, drug fever and very rarely anaphylaxis.

Hematologic: thrombocytopenia and leukopenia (sometimes profound), increased erythrocyte sedimentation rate, eosinophilia, decreased hemoglobin and very rarely hemolytic anemia.

Miscellaneous: The following adverse reactions have been observed to occur, although infrequently, in association with parenteral cefuroxime sodium and may be potential adverse effects of oral cefuroxime axetil: drowsiness, vaginitis, positive direct Coombs’ test, and transient increases in serum bilirubin, creatinine, alkaline phosphatase and urea nitrogen (BUN). In addition, the incidence of diaper rash (1.4%) has been associated with cefuroxime axetil suspension in children.

Symptoms And Treatment Of Overdose: Symptoms and Treatment: Other than general supportive treatment, no specific antidote is known. Excessive serum levels of cefuroxime can be reduced by dialysis. For treatment of hypersensitive reactions, see Warnings.

Dosage And Administration: Cefuroxime axetil may be given orally without regard to meals. Absorption is enhanced when cefuroxime axetil is administered with food. In comparative bioavailability studies in healthy adults, the suspension was not bioequivalent to the tablets. The area under the curve for the suspension averaged 91% of that for the tablet, while the Cmax for the suspension averaged 71% of the Cmax of the tablets.

Tablets: Adults and Children (12 Years of Age and Older): The usual recommended dosage is 250 mg twice a day. However, dosage may be modified according to the type of infection present as indicated in.

The usual duration of treatment for tablets and oral suspension is 7 to 10 days. For B-hemolytic streptococcal infections, therapy should be continued for at least 10 days.

Directions for Constituting Suspension in Bottles: Prepare a suspension at time of dispensing as follows: 1. Shake the bottle to loosen the granules and remove the cap. 2. Add the total amount of water for reconstitution all at once and replace cap. 3 Invert the bottle and rock the bottle vigorously until the sound of the granules against the container disappears. 4. Turn the bottle into an upright position and shake vigorously. Each 5 mL provides 125 mg cefuroxime.

Note: Shake the bottle vigorously until the suspension can be heard moving in the bottle before each use. Replace cap securely after each opening. If desired, the dose of the reconstituted suspension may be added to one of the following cold beverages immediately prior to administration: milk (i.e. skim, 2% or homogenized), fruit juice (i.e. apple, orange, or grape) or lemonade.

Directions for Constituting Suspension From Sachets: 1. Empty granules from sachet into a glass. 2. Add at least 10 mL of one of the following cold beverages: water, milk (i.e. skim, 2% or homogenized), juice (apple, orange, or grape) or lemonade. 3. Stir well and drink it all immediately.

Note: Ceftin granules should not be reconstituted in hot beverages.

Availability And Storage: Suspension: Dry, white to pale yellow, tutti-frutti-flavored granules. After reconstitution each 5 mL contains: cefuroxime axetil equivalent to cefuroxime (base) 125 mg. The reconstituted suspension from the sachets contains: cefuroxime axetil equivalent to cefuroxime (base) 250 mg. Nonmedicinal ingredients: polyvinyl pyrrolidone, stearic acid, sucrose and tutti-frutti flavoring. Bottles of 70 and 100 mL. Sachets of 250 mg, boxes of 10 and 14. Store granules between 2 and 30°C. The reconstituted suspension should be stored between 2 and 25°C, preferably in a refrigerator, and discarded after 10 days. The reconstituted suspension from sachets should be taken immediately.

Tablets: 250 mg: Each white, capsule-shaped tablet, engraved with “250” on one side and “Glaxo” on the other, contains: cefuroxime axetil equivalent to 250 mg of cefuroxime (base). Nonmedicinal ingredients: colloidal silicon dioxide, croscarmellose sodium, hydrogenated vegetable oil, hydroxypropyl methylcellulose, methylparaben, microcrystalline cellulose, propylene glycol, propylparaben, sodium benzoate, sodium lauryl sulfate and titanium dioxide. Bottles of 60. Store between 15 and 30°C.

500 mg: Each white, capsule-shaped tablet, engraved with “500” on one side and “Glaxo” on the other, contains: cefuroxime axetil equivalent to 500 mg of cefuroxime (base). Nonmedicinal ingredients: colloidal silicon dioxide, croscarmellose sodium, hydrogenated vegetable oil, hydroxypropyl methylcellulose, methylparaben, microcrystalline cellulose, propylene glycol, propylparaben, sodium benzoate, sodium lauryl sulfate and titanium dioxide. Bottles of 60. Store between 15 and 30°C. (Shown in Product Recognition Section)

CEFTIN® Glaxo Wellcome Cefuroxime Axetil Antibiotic

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