Axacef Cefuroxime Suspension and Tablets

Axacef®
cefuroxime

 

Presentations

Tablets: 125 mg, 250 mg, 500 mg

Oral Suspension: 125 mg/5 ml, 250 mg/5 ml

 

Qualitative and Quantitative Composition

Suspension: Each 5 ml after reconstitution contains: Cefuroxime Axetil equivalent to cefuroxime 125 mg or 250mg.

Tablet: Each Film-coated tablet contains: Cefuroxime Axetil equivalent to cefuroxime 125 mg, 250 mg or 500 mg.

 

Excipients

Suspension : Stearic acid, Xanthan gum, Povidone (k30), Acesulphame Potassium Sunset, Aspartame, Tutti Frutti 51880 Sucrose.

Tablets: Colloidal Anhydrous Silica; Microcrystalline cellulose, Sodium Lauryl sulphate, Croscarmellose sodium, Magnesium Stearate, Hypromellose (E-15), Hypromellose (E-5) Opaspray white.

 

Pharmaceutical Forms

Film coated tablet for oral administration.

Granules for oral suspension.

 

Clinical Particulars

Therapeutic Indications

Cefuroxime is a bactericidal cepholosporin antibiotic which is resistant to most β-lactamases and is active against a wide range of Gram-positive and Gram-negative organisms. Indications include:

Respiratory tract infections: acute and chronic bronchitis, infected bronchiectasis, bacterial pneumonia, lung abscess and post-operative chest infections.

Ear, nose and throat infections: sinusitis, tonsillitis, pharyngitis and otitis media.
Urinary tract infections: acute and chronic pyelonephritis, cystitis and asymptomatic bacteriuria.

Soft-tissue infections: cellulitis, erysipelas and wound infections.

Bone and joint infections: osteomyelitis and septic arthritis.

Obstetric and gynaecological infections pelvic inflammatory diseases.

Gonorchoea particularly when penicillin is unsuitable.

Other infections including septicaemia, meningitis and peritonitis.

Prophylaxis against infection in abdominal, pelvic, orthopaedic, cardiac, pulmonary, oesophageal and vascular surgery where there is increased risk from infection.

Usually Axacef will be effective alone, but when appropriate it may be used in combination with an aminoglycoside antibiotic, or in conjunction with metronidazole (orally or by suppository or injection), especially for prophylaxis in colonic or gynaecological surgery.

Cefuroxime is also available as the cefuroxime axetil with brand name Axacef for oral administration. This permits the use of oral follow through therapy with the same antibiotic, when a change from parenteral to oral therapy is clinically indicated.

Adults with pneumonia and acute exacerbations of chronic bronchitis may respond to sequential therapy with parenteral Axacef followed by oral administration.

Cefuroxime is also available as the sodium salt as brand Roxicef for parenteral administration. This permits oral follow through with the same antibiotic, when a change from parenteral to oral therapy is clinically indicated, with the added benefits of a reduction in cost and greater convenience. Where appropriate Axacef has been shown to be effective when used following initial parenteral Roxicef in the treatment of pneumonia and acute exacerbations of chronic bronchitis.

 

Dosage and Method of Administration

Adults

Most infections will respond to 250 mg b.d. in mild to moderate lower respiratory tract infections e.g. bronchitis 250 mg b.d. should be given. For more severe lower respiratory tract infections, or if pneumonia is suspected then 500 mg b.d. should be given. For urinary tract infections a dose of 125 mg b.d. is usually adequate; in pyelonephritis the recommended dose is 250 mg b.d. A single dose of one gram is recommended for the treatment of uncomplicated gonorrhoea.

Lyme disease in adults and children over the age of 12 years: the recommended dose is 500 mg b.d. for 20 days.

Injectable with oral follow through therapy:

Pneumonia: 1.5 g cefuroxime (as cefuroxime sodium) b.d. (iv or im) for 48-72 hours, followed by 500 mg b.d. cefuroxime (as cefuroxime axetil) oral therapy for 7 days.

Acute exacerbations of chronic bronchitis

750 mg Roxicef (cefuroxime sodium) b. d. (iv or im) for 48-72 hours, followed by Axacef (cefuroxime axetil) oral therapy for 5-7 days.

Duration of both parenteral and oral therapy is determined by the severity of the infection and the clinical status of the patient.

Children

The usual dose is 125 mg b.d. (1 x 125 mg tablet or 5 ml of suspension), or 10 mg/kg b.d. to a maximum of 250 mg daily. For otitis media in children less than 2 years of age the usual dosage is 125 mg b.d. (1 x 125 mg tablet or 5 ml of suspension), or 10 mg/kg b.d. to a maximum of 250 mg daily and in children over 2 years of age, 250 mg b.d. (1 x 250 mg tablet or 10 ml of suspension), or 15 mg/kg b.d. to a maximum of 500 mg daily. There is no experience of the use of Axacef in children under 3 months of age. Axacef tablets should not be crushed; therefore in younger children the suspension is more appropriate.

Elderly and Patients with Renal Impairment

No special precautions are necessary in patients with renal impairment or on renal dialysis or in the elderly at dosages up to the normal maximum of 1 g per day.
The usual course of therapy is seven days and so Axacef tablets and suspension are available in 5 or 7 day treatment pack sizes.

Axacef should be taken after food for optimum absorption.

 

Contra-Indications

Hypersensitivity to cephalosporins.

 

Special Warnings and Precautions for Use

Special care is indicated in patients who have experienced an allergic reaction to penicillins or other β-lactams. As with other antibiotics, prolonged use of cefuroxime axetil may result in the overgrowth of non-susceptible organisms (e.g. Candida, Enterococci, Clostridium difficile), which may require interruption of treatment.

Pseudomembranous colitis has been reported with the use of broad-spectrum antibiotics; therefore, it is important to consider its diagnosis in patients who develop serious diarrhoea during or after antibiotic use. The Jarisch-Herxheimer reaction has been seen following cefuroxime axetil treatment of Lyme disease. It results from the bactericidal activity of cefuroxime axetil on the causative organism of Lyme disease, the spirochaete Borrelia burgdorferi. Patients should be reassured that this is a common and usually self-limited consequence of antibiotic treatment of Lyme disease. With a sequential therapy regime the timing of change to oral follow through therapy is determined by severity of the infection, clinical status of the patient and susceptibility of the pathogens involved. The change to oral therapy should only be made once there is a clear clinical improvement.

If there has been no clinical improvement after 72 hours of parenteral treatment, then the patient’s treatment should be reviewed and if possible the results of microbiological culture should be reviewed. Please refer to the relevant prescribing information for Roxicef (cefuroxime sodium) before initiating sequential therapy.

 

Pregnancy and Lactation

There is no experimental evidence of embryopathic or teratogenic effects attributable to cefuroxime axetil but, as with oil drugs, it should be administered with caution during early months of pregnancy.

Cefuroxime is excreted in human milk, and consequently caution should be exercised when cefuroxime axetil is administered to a nursing mother.

 

Effects on Ability to Drive and Use Machines

Not applicable.

 

Undesirable Effects

Adverse reactions to cefuroxime have occurred relatively infrequently and have been generally mild and transient in nature. There have been rare reports of hypersensitivity reactions including skin rashes, urticaria, pruritus, interstitial nephritis, drug fever and very rarely anaphylaxis. As with other cephalosporins, there have been rare reports of erythema multiforme, Stevens-Johnson syndrome and toxic epidermal necrolysis (exanthematic necrolysis), headache and dizziness. As with other antibiotics, prolonged use may result in the overgrowth of non-susceptible organisms, e.g. Candida.

Gastro-intestinal disturbance, including, very rarely, symptoms of pseudomembranous colitis may occur during or after treatment. The principal changes in haematological parameters seen in some patients have been decreased haemogloblin concentration, eosinophilia, leukopenia, neutropenia and thrombocytopenia. Although there are sometimes transient rises in serum liver enzymes or serum bilirubin, particularly in patients with pre-existing liver disease, there is no evidence of harm to the liver.

Elevations in serum creatinine and/or blood urea nitrogen and a decreased creatinine clearance have been observed. Transient pain may be experienced at the site of intramuscular injection. This is more likely to occur with higher doses. However it is unlikely to be a cause for discontinuation or treatment. Occasionally, thrombophlebitis may follow intravenous injection.

 

Overdose

Overdosage of cephalosporins can cause cerebral irritancy leading to convulsions.

Serum levels of cefuroxime can be reduced by haemodialysis or peritoneal dialysis.

 

Pharmacological Properties

Pharmacodynamic Properties

Axacef is an oral prodrug of the bactericidal cephalosporin antibiotic cefuroxime, which is resistant to most β-lactamose and is active against a wide range of gram-positive and gram-negative 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 β-lactamase-producing strains. Cefuroxime has good stability to bacterial β-lactamase and consequently, is active against many ampicillin-resistant and amoxycillin-resistant strains. The bactericidal action of cefuroxime results from inhibition of cell-wall synthesis by binding to essential target proteins. Cefuroxime is usually active against the following organisms in vitro:

Escherichia coli.

Klebsiella spp.

Proteus mirabilis.

Providencia spp.

Proteus rettgeri.

Haemophilus influenzae (including ampicillin-resistant strains).

Haemophilus parainfluenzae (including ampicillin-resistont strains).

Moraxella (Bronhamella) catarrhalis.

Neisseria gonorrhoeae (including penicillinase and non-penicillinase producing strains).

Neisseria meningitidis.

Salmonellae spp.

Aerobes Gram-positive

Staphylococcus aureus and Staphylococcus epidermidis (including penicillinase producing strains but excluding methicillin resistant strains).

Streptococcus pyogenes (and other β-haemolytic streptococci).

Streptococcus pneumoniae.

Streptococcus Group B (Streptococcus agalactiae).

Streptococcus mitis (viridans group).

Bordetella pertussis.

Anaerobes

Gram-positive and Gram-negative cocci (including Peptococcus and Peptostreptococcus species).

Gram-positive bacilli (including most Clostridium species) and Gram-negative bacilli (including Bacteroides and Fusobacterium species).

Propionibacterium spp.

Other organisms

Borrelia burgdorferi.

 

Pharmacokinetic Properties

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 just over 1 hour. Approximately 50% of serum cefuroxime is protein bound. Cefuroxime is not metabolized and is excreted by glomerular filtration and tubular secretion.

 

Pharmaceutical Particulars

Shelf Life and Precautions for Storage

The shelf life of Axacef dry powder for suspension is 24 months when stored below 25°C. The reconstituted suspension can be kept for up to 10 days when stored below 25°C, however if is preferable to store at 2-8°C in a refrigerator. Tablets of Axacef packed in blisters have a shelf-life of 36 months when stored below 25°C. Tablets should be stored in a dry place below 25oC and protected from light.

 

Nature and Contents of Container

Axacef granules for oral suspension, 125 mg/5 ml and 250 mg/5 ml, are supplied in bottles of 70 ml. A 50 ml bottle is available in some markets.

Axacef tablets of 125 mg, 250 mg and 500 mg are supplied in blisters of 7 or 10 tablets, normally in packs of 1 x 10s, 2 x 7’s and 2 x 10’s respectively. Hospital packs of 10 x 7 tablets are available in some markets.

 

Instructions for Use/Handling

Directions for reconstituting the suspension: Tap the bottle gently to loosen the dry powder. Add half the required amount of water and shake vigourously. Slowly add water up to the mark on the bottle. Invert bottle and shake granules down into water using a rocking action. Continue to shake the bottle, until the suspension is well dispersed. Shake well immediately prior to use.

Further information is available upon request.

Not all presentations are available in every country.

 

KEEP OUT OF THE SIGHT AND REACH OF CHILDREN

Revision date: January 2015

 

Manufacturer

MEDREICH LIMITED

Plot No. 45 A&B, Anrich Industrial Estate, I.D.A.

Bollaram, Medak District. – 502 325 (A.P), INDIA

For: SANOFI

ZeNTIVA

A SANOFI COMPANY

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