CT Lab Farmaceutico


Full Prescribing Info
Cefuroxime sodium.
Cefuroxime (Kefox 250) IM/IV: Each vial contains 263 mg cefuroxime sodium, EP equivalent to 250 mg cefuroxime.
Cefuroxime (Kefox 750) IM/IV: Each vial contains 789 mg cefuroxime sodium, EP equivalent to 750 mg cefuroxime.
Pharmacology: Cefuroxime is the first of a new group of semi-synthetic derivatives of the cephalosporanic acid, stable to the bacterial Beta-lactamase due to the presence of metoxenous group. In particular cefuroxime is resistant to the major part of the Beta-lactamases produced by gram-negative microorganisms and to the staphylococcic penicillinase and is therefore apt to act effectively against those strains capable of inhibiting the activity of penicillin, ampicillin and cephalosporin, including Enterobacter.
The minimum inhibiting concentrations of cefuroxime practically coincide with the minimum bactericidal ones: its action is expressed through the inhibition of the cellular wall mucoprotein synthesis and consequent lysis of the bacterial cell. Cefuroxime has a broad spectrum of antibacterial activity which in vitro is exerted against many pathogenic microorganisms.
In man, following the intramuscular administration of cefuroxime, high blood levels are rapidly reached (within 15-45 mins.) corresponding to 15 and 35 mcg/mL for the doses of 250 and 750 mg respectively. The serum half-life after either IM or IV injection is approximately 70 minutes.
The level of 35 mcg/mL after the intramuscular administration of 750 mg, is widely superior to the level inhibiting most of the sensitive microorganisms, including the Beta-lactamase producers. The drug, which is present in the serum 8 hours after administration, due to reduced link with plasmatic proteins (25-50%), spreads promptly in the tissues with high concentration in the animal lung, liver, spleen and kidney. Concentrations of cefuroxime in excess of the minimum inhibitory levels for common pathogens can be achieved in bone, synovial fluid, pleural fluid, sputum and aqueous humor. Cefuroxime passes the blood-brain barrier when the meninges are inflamed. It crosses the placenta and has been detected in breast milk.
Cefuroxime in excreted unchanged, by glomerular filtration (approximately 50%) and renal tubular secretion (approximately 50%), and high concentration are achieved in the urine; 70-90% of the dose administered is found in the urine within 6-12 hours after administration.
Probenecid competes for renal tubular secretion with cefuroxime resulting in higher and more prolonged plasma concentration of cefuroxime. Small amounts of cefuroxime are excreted in bile. Plasma concentrations are reduced by dialysis.
Microbiology: Cefuroxime is usually active against the following organisms in vitro: AEROBES, Gram-Positive: Staphylococcus aureus, Staphylococcus epidermidis, Staphylococcus pneumoniae and Staphylococcus pyogenes (and other streptococci). Most strains of enterocci e.g. Enterococcus faecalis (formerly Streptococcus faecalis) are resistant to cefuroxime. Methicillin-resistant staphylococci and listeria monocitogens are resistant to cefuroxime.
AEROBES, Gram-Negative: Citrobacter spp, Enterobacter spp, Escherichia coli, Haemophilus influenzae (including ampicillin-resistant strains), Haemophilus para influenzae, Klebsiella spp (including Klebsiella penumoniae), Branhamella catarrhalis (including ampicillin and cephalotin-resistant strains), Morganella morganii (formerly Proteus morganii), Neisseria gonorrhea (including penicillinase and non-penicillinase producing strains, Neisseria meningitidis, Proteus mirabilis, Providencia rettgeri (former Proteus rettgeri), Salmonella spp, and Shigella spp. Some strains of Morganella, Enterobacter cloacae and Citrobacter spp have been shown to be resistant to cefuroxime and other cephalosporins. Pseudomonas and Campylobacter spp, Acinetobacter calcoaceticus and most strains of Serratia spp and Proteus vulgaris are resistant to most first and second generation cephalosporins.
ANAEROBES: Gram-positive and gram-negative cocci (including Peptococcus and Peptostreptococcus spp), gram-positive bacilli (including Bacteroides and Fusobacterium spp). Clostridium difficile and most strains of Bacteroides fragilis are resistant to cefuroxime.
Cefuroxime has in vitro activity against a wide range of gram-positive and gram-negative bacteria. The bactericidal action of cefuroxime results from inhibition of cell-wall synthesis.
Respiratory Tract Infections: Acute and chronic bronchitis, infected bronchiectasis, bacterial pneumonia, lung abscess and postoperative chest infections.
Ear, Nose and Throat Infections: Sinusitis, tonsillitis and pharyngitis.
Urinary Tract Infections: Acute and chronic pyelonephritis, cystitis and asymptomatic bacteriuria.
Soft Tissue Infections: Cellulitis, erysipelas, peritonitis and wound infections.
Bone and Joint Infections: Osteomyelitis and septic arthritis.
Obstetric and Gynecological Infections: Pelvic inflammatory diseases.
Gonorrhea particularly when penicillin is unsuitable.
Other infections including septicemia and meningitis.
Prophylaxis against infection in abdominal, pelvic, orthopaedic, cardiac pulmonary, oesophageal and vascular surgery where there is increased risk from infection.
Dosage/Direction for Use
General dosage recommendations: Adults: Many infections will respond to 750 mg 3 times a day by IM or IV injection. For more severe infections, this dose should be increased to 1.5 g 3 times a day IV. The frequency of IM or IV injections can be increased to 6-hourly if necessary, giving total daily doses of 3-6 g.
Infants and Children: Doses of 30-100 mg/kg/day, given as 3 or 4 divided doses.
A dose of 60 mg/kg/day will be appropriate for most infections.
Neonates: Doses of 30-100 mg/kg/day, given as 2 or 3 divided doses. In the first weeks of life the serum half-life of cefuroxime can be 3-5 times in adults.
Other recommendations: Gonorrhoea: 1.5 g should be given as a single dose. This may be given as 2 x 750 mg injections into different sites.
Meningitis: Cefuroxime is suitable for sole therapy of bacterial meningitis due to sensitive strains. The following dosages are recommended: Adults: 3 g IV every 8 hours.
Infants and Children: 150 - 250 mg/kg/day IV in 3 to 4 divided doses.
Neonates: The dosage should be 100 mg/kg/day IV.
Prophylaxis: The usual dose 1.5 g IV with induction of anaesthesia for abdominal, pelvic and orthopaedic operations. This may be supplemented with two 750 mg IM doses 8 and 16 hours later. In cardiac, pulmonary, oesophageal and vascular operations, the usual dose is 1.5 g IV with induction of anaesthesia continuing with 750 mg IM 3 times a day for further 24-48 hours.
In total joint replacement, 1.5 g cefuroxime powder maybe 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 cefuroxime should be reduced to compensate for its slower excretion. However, it is not necessary to reduce the dose until the creatinine clearance falls below 20 mL/min. 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 haemodialysis, 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 usually 750 mg twice daily.
For patients with renal failure on continuous arterioveneous haemodialysis or high flux-haemofiltration in intensive therapy units a suitable dosage is 750 mg twice daily.
For low-flux haemofiltration, follow the dosage recommended under impaired renal function.
Administration: IM: Add 1 mL water for injection to 250 mg Cefuroxime (Kefox) or 3 mL water for injection to 750 mg Cefuroxime (Kefox). Shake gently to produce an opaque suspension.
IV: Dissolve Cefuroxime (Kefox) in water for injection using at least 2 mL for 250 mg, at least 6 mL for 750 mg or 15 mL for 1.5 g. For short intravenous infusion (e.g. up to 30 minutes), 1.5 g may be dissolved in 50 mL water for injections. This solution may be given into the vein or introduced into the tubing of the giving set if the patient is receiving parenteral fluids.
Normal infusion rate is 1-2 mL/min.
Sodium cefuroxime is also chemically and physically compatible with Lactated Ringer's, 10% dextrose invert sugar or 0.1 M sodium lactate.
Overdosage of cephalosporins can cause cerebral irritations leading to convulsions. Serum levels of cefuroxime can be reduced by hemodialysis and peritoneal dialysis.
Ascertained hypersensitivity to cephalosporins. Acute porphyria.
Cephalosporin must be used with care in subjects with penicillin allergy. Both in the clinical and laboratory tests, partial cross allergenicity between penicillin and cephalosporin was ascertained and though very seldom, cases of patients who showed reactions to both drugs, sometimes of the anaphylactic type, particularly following the parenteral administration, were reported.
Cephalosporins of III generation like other betalactams, could induce microbic resistance and such event is greater towards opportunistic organism, especially Enterobacter and Pseudomonas, in immune-depressed subjects.
The administration of cephalosporin may interfere with some laboratory tests, causing pseudopositivity of the glycosuria according to the methods of Benedict, Fehling and "clinitest", but not according to the enzymatic methods.
During treatment with cephalosporin, positivity of Coombs test were reported (sometimes false).
During pregnancy and in the first trimester, the drug should only be administered in cases of absolute necessity and under direct medical control.
Special Precautions
In case of pronounced renal insufficiency, the dosage of cephalosporin has to be appropriately reduced according to the renal function tests.
The concomitant administration of other nephrotoxic drug increases the renal toxicity and therefore the renal function has to be assiduously checked.
The long term administration of antibiotics may favour the development of nonsusceptible microorganisms. In such case, appropriate therapeutic measures are to be adopted.
Cefuroxime at high dosage should be given with caution to patients receiving concurrent treatment with diuretics such as furosemide and aminoglycosides.
Clinical experience with cefuroxime has shown that this is not likely to have problem at the recommended dose levels.
Probenecid administration reduces the excretion of cephalosporins resulting in increased plasma concentrations.
No other incompatibility with other drugs (like heparin) have been reported.
Side Effects
As in the case of other cephalosporins, undesirable reactions are mainly limited to gastrointestinal disorders and occasionally to phenomena of hypersensitivity.
The possibility of appearance of the latter is greater in individuals who have previously showed hypersensitivity reactions and in those who have a previous case history of allergy, asthma, hay fever and urticaria.
The following side effects were reported: glossitis, nausea, vomiting, diarrhea, gastric pyrosis, abdominal pain in some patients, very seldom urticaria or cutaneous rash, pruritus, arthralgia. There have been rare reports of pseudomembranous colitis, erythema multiforme, Stevens-Johnson syndrome, anaphylaxis and toxic epidermal necrolysis following administration of cephalosporins.
Occasionally, transitory changes in some laboratory parameters, like eosinophilia, leucopenia, neutropenia, decreased hemoglobin concentration and very rarely thrombocytopenia, haemolytic anemia, agranulocytosis and aplastic anemia were reported. Increase of serum transaminase, total bilirubin and azotemia were noticed. Other reactions observed were: vertigo, sensation of thoracic constriction, candida vaginitis also in relation to the development of non-susceptible microorganisms, fever, headache, reversible interstitial nephritis, nervousness, sleep disturbances, confusion, hypertonia, serum sickness-like reactions, transient hepatitis and cholestatic jaundice. Rarely, such side effects were sufficiently intense as to require the discontinuation of therapy. Cases of hemolytic anemia have been reported after the treatment of cephalosporin. There may be pain at the injection site following intramuscular administration and occasionally thrombophlebitis has occurred following intravenous injection.
Drug Interactions
Some reported events of cross allergy of penicillin. In vitro, the activities of cefuroxime and aminoglycoside antibiotics in combination have been shown to be at least additive with occasional evidence of synergy.
Caution For Usage
Injections: Cefuroxime (Kefox) should not be mixed in the syringe with aminoglycoside antibiotics. Suspensions of Cefuroxime (Kefox) for IM injections and aqueous solutions for direct IV injection retain with potency for 5 hours if kept below 25°C and for 48 hours if refrigerated. More dilute solution, i.e. 1.5 g 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 the prepared solutions and suspension may occur on storage.
1.5 g Cefuroxime (Kefox) constituted with 15 mL water for injection may be added to metronidazole injection (500 mg/100 mL) and both retain their activity for up to 24 hours at 25°C.
1.5 g Cefuroxime (Kefox) 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.
Cefuroxime (Kefox) (5 mg/mL) in 5% w/v xylitol injection may be stored for up to 24 hours at 25°C.
Cefuroxime (Kefox) is compatible with the more commonly used IV infusion fluids. It will retain potency for up to 24 hours at room temperature in 0.9% w/v Sodium chloride Injection BP, 5% Dextrose Injection BP, 0.18% w/v Sodium chloride plus 4% Dextrose Injection BP and Compound Sodium lactate Injection BP (Hartmann's solution). The pH of 2.74% w/v Sodium bicarbonate Injection BP considerably affects the color of the solution and therefore, this solution is not recommended for dilution. However, if required, for patients receiving Sodium bicarbonate Injection by infusion it may be introduced into the tube of the giving set. The stability in 0.9% w/v Sodium chloride Injection BP in 5% Dextrose Injection is not affected by the presence of hydrocortisone sodium phosphate. Cefuroxime (Kefox) is also compatible with aqueous solutions containing up to 1% Lignocaine hydrochloride.
Store below 25°C.
MIMS Class
ATC Classification
J01DC02 - cefuroxime ; Belongs to the class of second-generation cephalosporins. Used in the systemic treatment of infections.
Kefox powd for inj 250 mg
1's (P220/vial)
Kefox powd for inj 750 mg
1's (P520/vial)
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