Cefurex, Cefurex 125, Cefurex 250

CEFUROXIME AXETIL

500 mg Film-Coated Tablet
125 mg/5 mL
250 mg/5 mL
Granules for Suspension

ANTIBACTERIAL

Category:

Description

The Cathay Drug Co., Inc.

DESCRIPTION

FORMULATION

Each 5 mL (1 teaspoonful) of reconstituted suspension contains:

Cefuroxime Axetil USP

  1. to Cefuroxime …………………………………250 mg

To reduce the development of drug-resistant bacteria and maintain the effectiveness of Cefuroxime and other antibacterial drugs, Cefuroxime should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria.

PHARMACOLOGY

PHARMACODYNAMIC PROPERTIES

Cefuroxime axetil is an oral prodrug of the bactericidal cephalosporin antibiotic cefuroxime, which is resistant to most beta-lactamases and is active against a wide range of gram-negative and gram-positive organisms.

MICROBIOLOGY

Cefuroxime axetil owes its in vivo bactericidal activity to the parent compound cefuroxime. Cefuroxime is a well-characterized and effective antibacterial agent which has broad-spectrum bactericidal activity against a wide range of common pathogens, including beta-lactamase-producing strains. Cefuroxime has good stability to bacterial beta-lactamase and consequently, is active against many ampicillin-resistant strains. The bactericidal action of cefuroxime results from the inhibition of cell-wall synthesis by binding to essential target proteins.

Cefuroxime is usually active against the following organism in vitro:

Aerobes, Gram-negative: Haemophilus influenzae (including ampicillin-resistant strains); Haemophilus parainfluenzae; Moraxella catarrhalis; Escherichia coli; Klebsiella species; Proteus mirabilis; Proteus inconstans; Providencia species; Proteus rettgeri and Neisseria gonorrheae (including penicillinase and non-penicillinase – producing strains).

Some strains of Morganella morganii, Enterobacter species and Citrobacter species have been shown by in vitro tests to be resistant to cefuroxime and other beta-lactam antibiotics.

Aerobes, Gram-positive: Staphylococcus aureus (including penicillinase-producing strains but excluding methicillin-resistant strains); Streptococcus pyogenes (and beta-hemolytic streptococci); Streptococcus pneumoniae; Streptococcus Group B (Streptococcus agalactiae) and Propionibacterium species.

Certain strains of enterococci, e.g. Streptococcus faecalis, are resistant.

Anaerobes, Gram-positive and Gram-negative cocci (including Peptococcus and Peptostreptococcus species). Most strains of Bacteroides fragilis are resistant.

Other organisms, Borrelia burgdorgeri.

Pseudomonas species, Campylobacter species, Acinetobacter calcoaceticus, Listeria monocytogenes, Legionella species and most strains of Serratia and Proteus vulgaris and Clostridium difficile are resistant to many cephalosporins including cefuroxime.

PHARMACOKINETICS

After oral administration, cefuroxime axetil is absorbed from the gastrointestinal tract and rapidly hydrolysed in the intestinal mucosa and blood to release cefuroxime into the circulation. Optimum absorption occurs when it is administered after a meal. Peak serum cefuroxime levels occur approximately two to three hours after oral dosing. The serum half-life is about 1.2 hours. Approximately 50% of serum cefuroxime is protein bound. Cefuroxime is not metabolized and is excreted by glomerular filtration and tubular secretion.

Concurrent administration of probenecid increases the area under the mean serum concentration time curve by 50%. Serum levels of cefuroxime are reduced by dialysis.

INDICATIONS

Cefuroxime axetil 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. Cefuroxime axetil is used orally for the treatment of mild to moderate respiratory tract infections (i.e. acute maxillary sinusitis, acute exacerbations of chronic bronchitis, secondary infections of acute bronchitis, community-acquired pneumonia caused by susceptible bacteria; acute bacterial otitis media; pharyngitis and tonsillitis caused by Staphylococcus pyogenes (group A beta-haemolytic streptococci); mild to moderate uncomplicated skin and skin structure infections caused by Staphylococcus aureus (including beta-lactamase-producing strains) or S. pyogenes; and uncomplicated urinary tract infections caused by Escherichia coli or Klebsiella pneumoniae. Cefuroxime axetil is also used orally for the treatment of uncomplicated gonorrhea and for the treatment of Lyme disease. The manufacturer of cefuroxime axetil oral suspension states that safety and efficacy of the suspension have been established only for the treatment of pharyngitis and tonsillitis, acute otitis media, and impetigo caused by susceptible bacteria, and for the treatment of Lyme disease.

Acute Otitis Media

Cefuroxime axetil is used orally for the treatment of acute otitis media (AOM) caused by S. pneumoniae, H. influenzae (including beta-lactamase producing strains), M. catarrhalis (including beta-lactamase producing strains) or S. pyogenes.

Pharyngitis and Tonsillitis

Cefuroxime axetil is used orally for the treatment of pharyngitis and tonsillitis caused by S. pyogenes (group A beta-hemolytic streptococci). Although cefuroxime usually is effective in eradicating S. pyogenes from the nasopharynx, efficacy of the drug in the subsequent prevention of rheumatic fever remains to be established.

Impetigo

Caused by Staphylococcus aureus (including beta-lactamase-producing stains) or Streptococcus pyogenes.

 Lyme disease

Oral cefuroxime axetil is used in adults and children for the treatment of early Lyme disease manifested as erythema migrans. When an oral regimen is indicated, oral cefuroxime axetil also is used in the treatment of early neutrologic Lyme disease in patients with cranial nerve palsy alone without evidence of meningitis, Lyme carditis, borrelial lymphocytoma and uncomplicated Lyme arthritis without clinical evidence of neurologic disease.

Lyme disease is a tick-borne spirochetal disease. In the US, Lyme disease is caused by the spirochete Borrelia burgdoferi, which is transmitted by the bite of loxodes scapularis or L.pacificus ticks.

DOSAGE AND ADMINISTRATION

Cefuroxime axetil is administered orally.

Cefuroxime axetil oral suspension must be administered with food. Although cefuroxime axetil film-coated tablets may be given orally without regard to meals, administration with food maximizes bioavailability of the drug.

CEFUROXIME AXETIL FOR ORAL SUSPENSION

(Must be administered with food. Shake well each time before using)

Population/ Infection Dosage Daily Maximum Dose Duration (days)
Pediatric patients (3 months to 12 years)
Pharyngitis/Tonsillitis 20 mg/kg/day divided b.i.d 500 mg 10
Acute Otitis Media 30 mg/kg/day divided b.i.d 1000 mg 10
Acute bacterial maxillary sinusitis 30 mg/kg/day divided b.i.d 1000 mg 10
Impetigo 30 mg/kg/day divided b.i.d 1000 mg 10

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.

CONTRAINDICATIONS

Cefuroxime products are contraindicated in patients with known allergy to the cephalosporin group of antibiotics.

WARNINGS

Cefuroxime for oral suspension are not bioequivalent and are therefore not substitutable on a milligram-per-milligram bass. 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 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 and may occur in up to 10% of patients with a history of penicillin allergy. If clinically significant allergic reaction to Cefuroxime products occurs, discontinue the drug and institute appropriate therapy. Serious acute hypersensitivity reactions may require treatment with epinephrine and other emergency measures, including oxygen, intravenous fluids, intravenous antihistamines, corticosteroids, pressor amines, and airway management, as clinically indicated.

Clostridium difficile associated diarrhea (CDAD) has been reported with use of nearly all antibacterial agents, including Cefuroxime, and may range in severity from mild diarrhea to fatal colitis. Treatment with antibacterial agents alters the normal flora of the colon leading to overgrowth of C. difficile.

  1. difficile produces toxins A and B which contribute to the development of CDAD. Hypertoxin producing strains of C. difficile cause increased morbidity and mortality, as these infections can be refractory to antimicrobial therapy and may require colectomy. CDAD must be considered in all patients who present with diarrhea following antibiotic use. Careful medical history is necessary since CDAD has been reported to occur over two months after the administration of antibacterial agents.

If CDAD is suspected or confirmed, ongoing antibiotic use not directed against C. difficile may need to be discontinued. Appropriate fluid and electrolyte management, protein supplementation, antibiotic treatment of C. difficile, and surgical evaluation should be instituted as clinically indicated.

PRECAUTIONS

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 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.

ADVERSE EFFECTS

Adverse drug reactions to cefuroxime axetil are generally mild and transient in nature.

The following convention has been used for the classification of undesirable effects:

  • Very common (> 1/10)
  • Common ((> 1/100, <1/10)
  • Uncommon ((> 1/1000, <1/100)
  • Rare ((> 1/10000, <1/1000)
  • Very rare (<1/10000

Infections and Manifestations

  • Common: Candida overgrowth

Blood and lymphatic system disorders

  • Common: Eosinophilia
  • Uncommon: Positive Coomb’s test, thrombocytopenia, leukopenia (sometimes profound)
  • Very rare: Haemolyticanaemia

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 Coomb’s test (which can interfere with the cross-matching of blood) and very rarely haemolytic anaemia.

Immune system disorders

Hypersensitivity reactions including:

  • Uncommon: Skin rashes
  • Rare: Urticaria, pruritus
  • Very rare: Drug fever, serum sickness, anaphylaxis

Nervous system disorders

  • Common: Headache, dizziness

Gastrointestinal disorders

  • Common: Gastrointestinal disturbances including diarrhea, nausea, abdominal pain
  • Uncommon: Vomiting
  • Rare: Pseudomembranous colitis

Hepatobiliary disorders

  • Common: Transient increases of hepatic enzyme levels, [ALT (SGPT), AST (SGOT), LDH]
  • Very rare: Jaundice (predominantly cholestatic), hepatitis

Skin and subcutaneous tissue disorders

  • Very rare: Erythema multiforme, Steven Johnson Syndrome, toxic epidermal necrolysis (exanthematic necrolysis)

Renal and Urinary tract Infections

  • Very rare: Interstitial nephritis

DRUG INTERACTIONS

Concomitant administration of probenecid with Cefuroxime increases the area under the serum concentration vs time curve by 50% 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.

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), 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.

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/m2) have revealed no impairment of fertility.

PREGNANCY

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/m2) and in rats at doses up to 1,000 mg/kg/day (9 times the recommended maximum human dose based on mg/m2) 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.

Labor and Delivery

Cefuroxime axetil has not been studied for use during labor and delivery.

Nursing Mothers

Because cefuroxime is excreted in human milk, consideration should be given to discontinuing nursing temporarily during treatment with cefuroxime.

Pediatric Use

The safety and effectiveness of CEFUROXIME 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 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.

Geriatric Use

Of the total number of subjects who received cefuroxime axetil in 20 clinical studies of CEFUROXIME, 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.

AVAILABILITY

Cefuroxime Axetil for Oral Suspension USP 250/5mL CEFUREX 250 suspension; 50 mL in 60 mL HDPE bottle.

STORAGE

Store at temperatures not exceeding 30°C.

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