CEFUROX 250 (susp)
-
Chemical Name:
Cefuroxime (Axetil) -
Therapeutic Category:
Antimicrobial -
Pharmacologic Category:
Antibiotic, Cephalosporin (Second Generation) -
Pharmaceutical Form:
Dry powder for suspension -
Composition:
Cefuroxime (Axetil) 250mg
CEFUROX
F.C.Tablets
Dry Powder for Oral Suspension
For Injection (Vial)
Cefuroxime
1. PHARMACOLOGY:
Cefuroxime is a semisynthetic, broad-spectrum, second generation cephalosporin antibiotic. Cefuroxime sodium is for parenteral administration and Cefuroxime axetil is for oral administration.
Cefuroxime is active against a wide range of gram-positive and gram-negative organisms, and it is highly stable in the presence of beta-lactamases of certain gram-negative bacteria. The bactericidal action of cefuroxime results from inhibition of bacterial cell wall synthesis.
Cefuroxime axetil is stable to many bacterial beta-lactamases, especially that are commonly found in enterobacteriaceae.
Cefuroxime is usually active against the following organisms:
Aerobes, Gram-Positive: Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes and other streptococci.
Aerobes, Gram-Negative: Citrobacter spp, Enterobacter spp, Escherichia coli, Haemophilus influenzae (including ampicillin-resistant strains), Haemophilus parainfluenzae, Klebsiella spp. (including Klebsiella pneumoniae), Moraxella catarrhalis (including ampicillin and cephalothin-resistant strains), Morganella morganii (formerly Proteus morganii), Neisseria gonorrhoeae (including penicillinase and non-penicillinase producing strains), Neisseria meningitidis, Proteus mirabilis, Providencia rettgeri (formerly Proteus rettgeri), Salmonella spp., and Shigella spp.
Anaerobes: Gram-positive and gram-negative cocci (including Peptococcus and Peptostreptococcus spp.), gram-positive bacilli (including Clostridium spp.), and gram-negative bacilli (including Bacteroides and Fusobacterium spp.).
PHARMACOKINETICS:
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. Approximately 50% of serum cefuroxime is bound to protein.
Cefuroxime is excreted unchanged in the urine; in adults, approximately 50% of the administered dose is recovered in the urine within 12 hours.
Because cefuroxime is renally excreted, the serum half-life is prolonged in patients with reduced renal function.
Food effect on pharmacokinetics: Absorption of the tablets is greater when taken after food (absolute bioavailability of cefuroxime tablets increase from 37% to 52%).
2. INDICATIONS:
CEFUROX is indicated for the treatment of patients with infections caused by susceptible strains of the designated organisms in the following diseases :
Respiratory tract infections: Pharyngitis/tonsillitis caused by Streptococcus pyogene. acute bacterial
otitis media caused by Streptococcus pneumoniae, Haemophilus influenzae (including beta-lactamase producing strains), Moraxella catarrhalis (including beta- lactamase producing strains), or Streptococcus pyogenes, acute bacterial maxillary sinusitis caused by Streptococcus pneumoniae, Haemophilus influenzae (including non-beta-lactamase producing strains), acute bacterial exacerbations of chronic bronchitis and secondary bacterial infections of acute bronchitis caused by Streptococcus pneumoniae, Haemophilus influenzae (beta-lactamase negative strains), and Haemophilus parainfluenzae (beta-lactamase negative strain), lower respiratory tract infections including pneumonia caused by Streptococcus pneumoniae, Haemophilus influenzae (including ampicillin-resistant strains), Klebsiella spp., Staphylococcus aureus (penicillinase and non–penicillinase producing strains), Streptococcus pyogenes, and Escherichia coli.
Urinary tract infections: Caused by Escherichia coli or Klebsiella.
Skin and skin structure infections: Caused by Staphylococcus aureus (penicillinase and nonpenicillinase producing strains) and Streptococcus pyogenes.
Septicemia: Caused by Streptococcus pneumoniae, Haemophilus influenzae (including ampicillin-resistant strains), Klebsiella spp., Staphylococcus aureus (penicillinase and non–penicillinase producing strains) and Escherichia coli.
Meningitis: Caused by Streptococcus pneumoniae, Haemophilus influenzae (including ampicillin-resistant strains), Neisseria meningitidis and Staphylococcus aureus (penicillinase and non penicillinase producing strains).
Gonorrhoeae: Caused by Neisseria gonorrhoeae.
Bone and joint infections: Caused by Staphylococcus aureus (penicillinase and non penicillinase producing strains).
Impetigo: Staphylococcus aureus (penicillinase and non penicillinase producing strains) and Streptococcus pyogenes.
3. CONTRAINDICATIONS:
Cefuroxime products are contraindicated in patients with known allergy to the cephalosporin group of antibiotics.
4. PRECAUTIONS:
- Cephalosporins should be given with caution to patients receiving concurrent treatment with potent diuretics as these regimens are suspected of adversely affecting renal function. The total daily dose of cefuroxime sodium should be reduced in patients with transient or persistent renal insufficiency.
- Pregnancy: Category B. The drug should be used during pregnancy only if clearly needed.
- Nursing Mothers: Since cefuroxime is excreted in human milk, caution should be exercised when cefuroxime is administered to a nursing woman.
5. SIDE EFFECTS:
Cefuroxime sodium is generally well tolerated. The most common adverse effects have been local reactions following IV administration.
Other adverse reactions have been encountered only rarely as: gastrointestinal effects, diarrhea and nausea. Onset of pseudomembranous colitis symptoms may occur during or after treatment.
Hypersensitivity Reactions: Pruritus, urticaria, vaginitis (including vaginal candidiasis).
6. DRUG INTERACTIONS:
Cefuroxime Sodium:
Solutions of cefuroxime sodium, like those of most beta-lactam antibiotics, should not be added to solutions of aminoglycoside antibiotics because of potential interaction. However, if concurrent therapy with cefuroxime sodium and an aminoglycoside is indicated, each of these antibiotics can be administered separately to the same patient.
Cefuroxime Axetil:
Concomitant administration of probenecid with cefuroxime axetil tablets increases the area under the curve of the serum concentration versus time by 50%.
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.
7. DOSAGE & ADMINISTRATION:
CEFUROX - F.C.Tablets and Dry Powder for Oral Suspension:
| Adolescents and Adults (13 years and older) | ||
| Infection | Dosage/day | Duration (days) |
| Pharyngitis/tonsillitis | 500 mg | 10 |
| Sinusitis | 500 mg | 10 |
| Bronchitis | 250 or 500 mg b.i.d. | 10 |
| Skin and skin-structure infections | 250 or 500 mg b.i.d. | 10 |
| Urinary tract infections | 125 or 250 mg b.i.d. | 7 - 10 |
| Gonorrhea | 1,000 mg once | Single dose |
| Infants and children (3 months to 12 years) | |||
| Infection | Dosage | Daily Maximum Dose | Duration (days) |
| Pharyngitis/tonsillitis | 20 mg/kg/day divided b.i.d. | 500 mg | 10 |
| Acute otitis media | 30 mg/kg/day divided b.i.d. | 1,000 mg | 10 |
| Impetigo | 30 mg/kg/day divided b.i.d. | 1,000 mg | 10 |
CEFUROX – For Injection:
General dosage recommendations:
Adults: Many infections respond to 750 mg three times daily by i.m. or i.v. injection. For more severe infections the dose should be increased to 1.5 g three times daily given i.v.. The frequency of i.m. or i.v. injections may be increased to 6-hourly if necessary, giving total daily doses of 3 to 6 g.
Infants and Children: 30 to 100 mg/kg/day given as 3 or 4 divided doses. A dose of 60 mg/kg/day is appropriate for most infections.
Neonates: 30 to 100 mg/kg/day given as 2 or 3 divided doses. In the first weeks of life, the serum half life of Cefuroxime can be three to five times that in adults.
Other recommendations:
GONORRHOEA:
Adults: 1.5 g as a single dose (this may given as 2 x 750 mg injections given i.m. into different sites, e.g. each buttock).
MENINGITIS:
CEFUROX is suitable for sole therapy of bacterial meningitis due to sensitive strains. The following dosages are recommended:
Adults: 3 g given i.v. every eight hours.
Infants and Children: 200 to 240 mg/kg/day given i.v. in 3 or 4 divided doses. This dosage may be reduced to 100 mg/kg/day i.v. after 3 days or when clinical improvement occurs.
Neonates: The initial dosage should be 100 mg/kg/day given i.v. A reduction to 50 mg/kg/day i.v. may be made when clinically indicated.
Data are not yet sufficient to recommend a dose for intrathecal administration.
PROPHYLAXIS:
The usual dose is 1.5 g given i.v. with induction of anaesthesia for abdominal, pelvic and orthopaedic operations. This may be supplemented with two 750 mg i.m. doses eight and sixteen hours later.
In cardiac, pulmonary, oesophageal and vascular operations, the usual dose is 1.5 g given i.v. with induction of anaesthesia, continuing with 750 mg given i.m. three times daily for a further 24 to 48 hours.
In total joint replacement, 1.5 g CEFUROX powder may be mixed dry with each pack of methyl methacrylate cement polymer before adding the liquid monomer.
DOSAGE IN IMPAIRED RENAL FUNCTION:
Cefuroxime is excreted by the kidneys. Therefore, as with all such antibiotics, in patients with markedly impaired renal function it is recommended that the dosage of CEFUROX should be reduced to compensate for its slower excretion.
However, it is not necessary to reduce the dose until the creatinine clearance falls to 20 ml/min or below. In adults with marked impairment (creatinine clearance 10 - 20 ml/min) 750 mg twice daily is recommended and with severe impairment (creatinine clearance <10 ml/min) 750 mg once daily is adequate.
For patients on dialysis a further 750 mg dose should be given at the end of each dialysis. When continuous peritoneal dialysis is being used, a suitable dosage is 750 mg twice daily.
ADMINISTRATION:
CEFUROX - F.C.Tablets and Dry Powder for Oral Suspension:
CEFUROX should be taken after meals.
Preparation of CEFUROX – Dry Powder for Oral Suspension:
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CEFUROX – For Injection:
- Intramuscular: Add 1.5 ml water for injections to 250 mg CEFUROX or 3 ml Water for Injections to 750 mg CEFUROX. Shake gently to produce an opaque suspension.
- Intravenous (Slowly over a period of 3 – 5 minutes): Dissolve CEFUROX in water for injections using at least 2.5 ml for 250 mg, at least 8 ml for 750 mg, or 16 ml for 1.5 g.
- For short intravenous infusion (e.g. up to 30 minutes): Dissolve 1.5 g of CEFUROX in 50 ml of water for injections.
These solutions may be given directly into the vein or introduced into the tubing of the giving set if the patient is receiving parenteral fluids.
- Preparation of solution for continuous IV infusion: A solution of cefuroxime sodium may be added to an IV infusion pack containing one of the following fluids: 0.9% sodium chloride injection; 5% dextrose injection; 10% dextrose injection; 5% dextrose and 0.9% sodium chloride injection; 5% dextrose and 0.45% sodium chloride injection; or 1/6 M sodium lactate injection.
Solutions of cefuroxime sodium, like those of most beta-lactam antibiotics, should not be added to solutions of aminoglycoside antibiotics because of potential interaction. However, if concurrent therapy with cefuroxime sodium and an aminoglycoside is indicated, each of these antibiotics can be administered separately to the same patient. As with other cephalosporins, cefuroxime sodium powder as well as solutions and suspensions tend to darken, depending on storage conditions, without adversely affecting product potency.
8. COMPATIBILITY & STABILITY:
- CEFUROX should not be mixed in the syringe with aminoglycoside antibiotics.
- Reconstituted suspensions of CEFUROX for i.m. injection and aqueous solutions for direct i.v. injection retain their potency for five hours if kept below 25°C and for 48 hours if refrigerated. More dilute solutions, i.e. 1500 mg plus 50 ml water for injections, retain satisfactory potency for 24 hours if kept below 25°C and for 72 hours if refrigerated.
- Some increase in the color of prepared solutions and suspensions of Cefuroxime may occur on storage.
- 1.5 g CEFUROX constituted with 16 ml water for injections may be added to metronidazole injection (500 mg/100 ml) and both retain their activity for up to 24 hours below 25°C.
- 1.5 g CEFUROX is compatible with azlocillin 1 g (in 15 ml) or 5 g (in 50 ml) for up to 24 hours at 4°C or 6 hours below 25°C.
- CEFUROX (5 mg/ml) in 5% or 10% xylitol injection may be stored for up to 24 hours at 25°C.
- CEFUROX is compatible with the more commonly used i.v. infusion fluids. It will retain potency for up to 24 hours at room temperature in: 0.9% Sodium Chloride Injection, 5% Dextrose Injection, 0.18% Sodium Chloride plus 4% Dextrose Injection and compound Sodium Lactate Injection (Hartmann’s Solution).
- The pH of 2.74% w/v Sodium Bicarbonate Injection considerably affects the colour of the solution and therefore this solution is not recommended for the dilution of CEFUROX. However, if required, for patients receiving Sodium Bicarbonate Injection by infusion CEFUROX may be introduced into the tube of the giving set.
- The stability of CEFUROX in Sodium Chloride Injection 0.9% and 5% Dextrose Injection is not affected by the presence of hydrocortisone sodium phosphate.
- CEFUROX is compatible with aqueous solutions containing up to 1% lignocaine hydrochloride.
9. PACKAGING & COMPOSITION:
- CEFUROX 250 - F.C.Tablets: A pack of 10 f.c.tablets. Each f.c.tablet contains Cefuroxime Axetil equivalent to Cefuroxime 250mg.
- CEFUROX 500 - F.C.Tablets: A pack of 10 f.c.tablets. Each f.c.tablet contains Cefuroxime Axetil equivalent to Cefuroxime 250mg.
- CEFUROX 125 - Dry Powder for Oral Suspension: A Glass bottle of 60 ml. After reconstitution, each 5 ml contains Cefuroxime Axetil equivalent to Cefuroxime 125 mg.
- CEFUROX 250 - Dry Powder for Oral Suspension: A Glass bottle of 60 ml. After reconstitution, each 5 ml contains Cefuroxime Axetil equivalent to Cefuroxime 250 mg.
- CEFUROX 250 - For Injection: A pack of 1 vial. Each vial contains Cefuroxime Sodium equivalent to Cefuroxime 250 mg .
- CEFUROX 750 - For Injection: A pack of 1 vial. Each vial contains Cefuroxime Sodium equivalent to Cefuroxime 750 mg .
- CEFUROX 1500 - For Injection: A pack of 1 vial. Each vial contains Cefuroxime Sodium equivalent to Cefuroxime 1500 mg
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