Description
The Cathay Drug Co., Inc.
FORMULATION
Each film-coated tablet contains:
Cefuroxime (as axetil) ……………… 500 mg
PHARMACOLOGY
Mechanism of Action
Cefuroxime axetil (CEFUREX) acts by binding to penicillin binding proteins. 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.
ANTIMICROBIAL ACTION
Cefuroxime is bactericidal and has a similar spectrum of antimicrobial action and pattern of resistance to those of cefamandole. It is more resistant to hydrolysis by beta-lactamases than cefamandole, and therefore may be more active against beta-lactamase producing strains, Haemophilus influenzae and Neisseria gonorrhea. However, treatment failures have occurred in patients with H. influenzae menigitis given cefuroxime and might be associated with a relatively high minimum bactericidal concentration when compared with the minimum inhibitory concentration or with a significant inoculum effect. Reduced affinity of penicillin-binding proteins for cefuroxime has also been reported to be responsible for resistance in a beta-lactamase-negative strain of H. influenzae.
PHARMACOKINETICS
Absorption and Distribution
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. Cefuroxime is approximately 50% bound to serum protein.
Metabolism/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 has not been studied at this time. Until further data are available, the renal pharmacokinetic properties of cefuroxime established in adults should not be extrapolated to pediatric patients.
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.
INDICATIONS
Cefuroxime axetil (CEFUREX) is indicated for the treatment of patients with infections caused by susceptible strains of the designated organisms in the following diseases:
- Lower Respiratory Tract Infections (including pneumonia) caused by Streptococcus pneumoniae, Haemophilus influenzae (including ampicillin-resistant strains), Klebsiella, Staphylococcus aureus (penicillinase- and non-penicillinase-producing strains), Streptococcus pyogenes, and Escherichia coli.
- Pharyngitis/Tonsillitis caused by Streptococcus pyogenes.
- Urinary Tract Infections caused by Escherichia coli and Klebsiella
- Skin and Skin-Structure Infections caused by Staphylococcus aureus (penicillinase- and non-penicillinase-producing strains), Streptococcus pyogenes, Escherichia coli, Klebsiella, and Enterobacter spp.
- Septicemia caused by Staphylococcus aureus (penicillinase- and non-penicillmase-producing strains), Streptococcus pneumoniae, Escherichia coli, Haemophilus influenzae (including ampicillin-resistant strains), and Klebsiella
- Meningitis caused by Streptococcus pneumoniae, Haemophilus influenzae (including ampicillin-resistant strains), Neisseria meningitidis, and Staphylococcus aureus (penicillinase- and non-penicillinase-producing strains).
- Uncomplicated and disseminated gonococcal infections due to Neisseria gonorrhoeae (penicillinase- and non-penicillinase-producing strains) in both males and females.
- Bone and Joint Infections caused by Staphylococcus aureus (penicillinase- and non-penicillinase-producing strains).
DOSAGE AND ADMINISTRATION
Cefuroxime axetil (CEFUREX) may be given orally without regard to meals. Absorption is enhanced when administered with food.
Adolescents and Adults (13 years and older)
Pharyngitis/tonsillitis: 250 mg PO q12hr for 10 days
Acute Bacterial Maxillary Sinusitis: 250 mg PO q12hr for 10 days
Acute Bacterial Exacerbation of Chronic Bronchitis: 250-500 mg PO q12hr for 10 days or 500-750 mg q8hr
Uncomplicated Skin and Skin Structure Infections: 250-500 mg PO q12hr for 10 days
Uncomplicated Urinary Tract Infections: 250 mg PO q12hr for 7-10 days
Uncomplicated Gonorrhea: 1000 mg PO Once
Pediatric Patients (those who can swallow the tablet whole)
Acute Otitis Media: 250 mg q12hr for 10 days
Acute bacterial maxillary sinusitis: 250 mg q12hr for 10 days
CONTRAINDICATIONS
Cefuroxime axetil (CEFUREX) tablets are contraindicated in patients with known hypersensitivity to cephalosphorins.
WARNINGS
Before therapy with Cefuroxime products is instituted, careful inquiry should be made to DETERMINE WHETHER THE PATIENT HAS HAD PREVIOUS HYPERSENSITIVITY REACTIONS TO CEFUROXIME PRODUCTS, OTHER CEPHALOSPORINS, PENICILLINS, OR OTHER DRUGS. If the product is to be given to PENICILLIN-SENSITIVE PATIENTS, caution should be exercised because cross-hypersensitivity among beta-lactam antibiotics have been clearly documented and may occur in up to 10% of patients with prior allergy to penicillin products. If a clinically significant allergic reaction to cefuroxime product occurs, DISCONTINUE THE DRUG AND INSTITUTE APPROPRIATE THERAPY.
Treatment with epinephrine and other emergency measures (including oxygen, IV fluids, IV antihistamines, corticosteroids, pressor amines and/or airway management) may be required for serious acute hypersensitivity to Cefuroxime products.
PRECAUTIONS
As with other broad-spectrum antibiotics, prolonged administration of cefuroxime may result in overgrowth of nonsusceptible microorganisms. If superinfection occurs during therapy, appropriate measures should be taken. Cefuroxime axetil (CEFUREX) should be administered with caution to individuals with a history of gastrointestinal disease (colitis).
Cefuroxime axetil (CEFUREX) should be given with caution to patients receiving concurrent treatment with potent diuretics because these diuretics are suspected of adversely affecting renal function.
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.
ADVERSE EFFECTS
| >10%
|
Diarrhea (4-11%), duration-dependent |
| 1-10%
|
Decreased Hgb/Hct (10%); Eosinophilia (7%) ; Nausea/vomiting (3-7%); Vaginitis (<5%); Transient rise in hepatic transaminases (2-4%); Thrombophlebitis (2%) |
| <1%
|
Transient neutropenia & leukopenia; increase in BUN & creatinine; rash; dysuria; indigestion; headache; chills; flatulence; abdominal pain and cramps; shortness of breath; mouth ulcers; swollen tongue; sleepiness; thirst; anorexia |
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.
DRUG INTERACTION
Probenecid
Concomitant administration of probenecid with cefuroxime 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 compared with that of fasting state and tend to cancel the effect of postprandial absorption.
In common with other antibiotics, cefuroxime may affect the gut flora, leading to lower estrogen reabsorption and reduced efficacy of combined oral estrogen/progesterone contraceptives.
PREGNANCY AND LACTATION
Cefuroxime has been assigned to pregnancy category B by the FDA. Its safety in pregnancy has not been established. The use of Cefuroxime axetil (CEFUREX) in pregnant women requires that the likely benefit from the drug be weighed against the possible risk to the mother and fetus.
AVAILABILITY
500 mg film-coated tablet
STORAGE
Store at temperatures not exceeding 30oC.
Manufactured by:
Lloyd Laboratories Inc.
#10 Lloyd Ave, First Bulacan Industrial City, City of Malolos, Bulacan
Manufactured for:
The Cathay Drug Co., Inc.
2/F Vernida I Condominium 120 Amorsolo St. Legaspi Village, Makati City
Date of revision: July 2019
REFERENCES
http://reference.medscape.com/drug/ceftin-zinacef-cefuroxime-342500#10
http://druginformation.com/RxDrugs/C/Cefuroxime%20Axetil%20Tablet%20and%20Oral%20Suspension.htm#MOA
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