Kefstar Cefuroxime Axetil Tablets USP

KEFSTAR™

Cefuroxime Axetil Tablets USP

For the use only of a Registered Medical Practitioner or a Hospital or a Laboratory.

 

Composition

Each film-coated tablet contains:

Cefuroxime Axetil USP equivalent to anhydrous Cefuroxime 125mg

Each film-coated tablet contains:

Cefuroxime Axetil USP equivalent to anhydrous Cefuroxime 250mg

Each film-coated tablet contains:

Cefuroxime Axetil USP equivalent to anhydrous Cefuroxime 500mg

 

Action

KEFSTAR (Cefuroxime Axetil) is a semi-synthetic, broad-spectrum cephalosporin antibiotic for oral administration. Cefuroxime is usually bactericidal in action. Its action results from the inhibition of mucopeptide synthesis in the bacterial cell wall.

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.

After a 250mg dose of suspension administered as 2 x 125 mg/5 ml with food in adults, the mean peak serum level is reached in 3 hours and is 2.27mcg/ml. The serum half-life is approximately 1.44 hour and the AUC value is 9.75 mcg -h ml. In children administered a dose of 15 mg/kg, the peak plasma concentration is achieved at 2.7 hours and is 5.1 mcg/ml. The elimination half-life is 1.9g hours and AUC is 22.5 mcg – h ml.

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 paediatric patients has 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 peadiatric patients because Cefuroxime is renally excreted, the serum half-life is prolonged in patients with reduced renal function. Despite the lower elimination of Cefuroxime in geriatric patients, dosage adjustment based on age is not necessary.

 

Anti-microbial activity

The in vivo bactericidal activity of Cefuroxime Axetil is due to Cefuroxime’s binding to essential target proteins end 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 the following microorganisms.

Aerobic gram-positive microorganisms: Staphylococcus aureus (including beta lactamase producing strains), Staphylococcus epidermidis, Staphylococcus

saprophyticus, Staphylococcus agalactiae, Streptococcus pneumoniae and Streptococcus pyogenes.

Aerobic gram-negative microorganisms: Esherichia 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), Neisseria meningitidis, Morganella morganii, Proteus incosntans, Proteus mirabilis, Providencia rettgeri, Salmonella spp., Shigella spp.

Spirochetes: Borrelia burgdorferi.

 

Dosage and Administration

Tablets – The tablets may be given without regard to meals.

 

Adults and Adolescents (13 years and above)

– Pharyngitis / tonsillitis: 250mg bid for 10 days.

– Acute bacterial exacerbations of chronic bronchitis: 250 or 500 mg bid for 5-10 days.

– Secondary bacterial infections of acute bronchitis: 250 or 500 mg bid for 5-1 0 days.

– Uncomplicated skin and skin structure infections: 250-500 mg bid for 10 days.

– Uncomplicated urinary tract infections: 125 or 250 mg bid for 7 to 10 days.

– Uncomplicated gonorrhoea: 1000mg once as single dose.

– Early Lyme disease: 500mg bid for 20 days.

 

Pediatric Patients below 13 years (who can swallow tablets whole)

Acute bacterial otitis media: 250mg bid for 10 days.

Acute bacterial maxillary sinusitis :250mg bid for 10 days.

 

Indications

Cefuroxime axetil is a cephalosporin antibacterial drug indicated for the treatment of the following infections due to susceptible bacteria:

– Pharyngitis/tonsillitis (adults and pediatric patients).

– Acute bacterial otitis media (pediatric patients).

– Acute bacterial maxillary sinusitis (adults and pediatric patients).

– Acute bacterial exacerbations of chronic bronchitis and secondary bacterial infections of acute bronchitis (adults and pediatric patients 13 years and older).

– Uncomplicated skin and skin-structure infections (adults and pediatric patients 13 years and older).

– Uncomplicated urinary tract infections (adults and pediatric patients 13 years and older).

– Uncomplicated gonorrhea (adults and pediatric patients 13 years and older).

– Early Lyme disease (adults and pediatric patients 13 years and older).

– Impetigo (pediatric patients)

 

Contraindications

Cefuroxime is contraindicated in patients with a known hypersensitivity (e.g., anaphylaxis) to Cefuroxime or to other β-lactam antibacterial drugs (e.g., penicillins and cephalosporins).

 

Warnings and Precautions

Before therapy with Cefuroxime is instituted, careful inquiry should be made to determine whether the patient has had previous hypersensitivity reactions to 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.

Pseudomembranous colitis has been reported with nearly all anti-bacterial agents, including Cefuroxime and may range from mild to life threatening. Therefore, it is important to consider this diagnosis in patients who present with diarrhoea subsequent to the administration of antibacterial agents.

 

Drug laboratory test Interactions

A false positive reaction for glucose in the urine may occur with copper reduction tests but not with enzyme based tests for glycosuria. 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

Oral Contraceptives

Cefuroxime axetil may affect the gut flora, leading to lower estrogen reabsorption and reduced efficacy of combined oral estrogen/progesterone contraceptives. Counsel patients to consider alternate supplementary (non-hormonal) contraceptive measures during treatment.

 

Drugs that Reduce Gastric Acidity

Drugs that reduce gastric acidity may result in a lower bioavailability of Cefuroxime compared with administration in the fasting state. Administer Cefuroxime at least 1 hour before or 2 hours after administration of short-acting antacids. Histamine-2 (H2) antagonists and proton pump inhibitors should be avoided.

 

Probenecid

Concomitant administration of probenecid with Cefuroxime axetil suspension increases serum concentrations of Cefuroxime. Co-administration of probenecid with Cefuroxime axetil is not recommended.

 

Drug/Laboratory Test Interactions

A false-positive reaction for glucose in the urine may occur with copper reduction tests (e.g., Benedict’s or Fehling’s solution), but not with enzyme-based tests for glycosuria.

 

Carcinogenesis, Mutagenesis, Impairment of fertility

Although lifetime studies in animals have not been performed to evaluate carcinogenic potential, no mutagenic potential was found for Cefuroxime Axetil.

Reproduction studies in rats at doses up to 1000 mg/kg per day have revealed no evidence of impaired fertility.

 

Pregnancy and lactation

Pregnancy Category B. There are no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, Cefuroxime should be used during pregnancy only if clearly needed.
B

ecause Cefuroxime is excreted in human milk, caution should be exercised when Cefuroxime is administered to a nursing woman.

 

Adverse reactions

Cefuroxime is usually well tolerated. The adverse reactions seen are diarrhoea, nausea, and vomiting, transient elevation of SGOT, SGPT and LDH. In <1% of patients, abdominal pain and cramps, flatulence, dyspepsia, headache, vulvar itch, vaginitis, dysuria, chills, swollen tongue, sleepiness, thirst, positive Coomb’s test, muscle stiffness, tightness in chest.

Rarely, haemolytic anemia, Ieukopenia, thrombocytopaenia, jaundice, pseudomembranous colitis, hypersensitivity reactions like anaphylasis angioedema, pruritis, rash and urticaria, seizure, encephalopathy, hepatic impairment including hepatitis and cholestasis, pancytopenia, joint swelling, arthralgia, cough, fever, renal dysfunction, skin reactions like erythema multiforme, Steven Johnsons syndrome and toxic epidermal necrolysis.

 

Overdosage

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

 

Storage

Store in a cool dry place, protected from light.

 

Presentation

125mg, 250mg and 500 mg: Blister of 4 tablets. Blister of 10 tablets.

Kefstar 250mg: NAFDAC Reg. No. 04-8147

Kefstar 500mg: NAFDAC Reg. No. 04-8148

 

Manufactured by

Sance Laboratories Pvt. Ltd.

VI/51B, P.B. No.2, Kozhuvanal,

Pala, Kottayam – 686573,

Kerala, India.

 

Manufactured for

WOCKHARDT LIMITED

Wockhardt Towers, Bandra Kurla Complex,

Mumbai 400051, India