Levexime

One Vial of Cefuroxime for Injection USP 750 mg: Each Vial contains: Cefuroxime (as sodium), USP 750 mg.
One Ampoule of Sterile Water for Injection BP 10 mL.
Cefuroxime is a semisynthetic, broad-spectrum, cephalosporin antibiotic for parenteral administration.
It is the sodium salt of (6R,7R)-3-carbamoyloxymethyl-7-[Z-2-methoxyimino-2-(fur-2-yl)acetamido]ceph-3-em-4-carboxylate. The empirical formula is C₁₆H₁₅N₄NaO₈S, representing a molecular weight of 446.4. A white or almost white, slightly hygroscopic powder.

Antibacterial.
Pharmacology: Cefuroxime is a bactericidal semi-synthetic cephalosporin antibiotic which is resistant to most β-lactamases and is active against a wide range of Gram-positive and Gram-negative organisms. Peak serum levels of cefuroxime are achieved within 30 to 45 minutes after intramuscular administration. The serum half-life after either intramuscular or intravenous injection is approximately 70 minutes. Concurrent administration of probenecid produces an elevated peak serum level and restricts the excretion of the antibiotic. There is almost complete recovery of unchanged cefuroxime in the urine within 24 hours of administration, the major part being eliminated in the first six hours. The tubular excretion component of renal clearance of cefuroxime is of the order of 50%.

Cefuroxime is indicated for the treatment of the following infections when caused by susceptible strains of the designated micro-organisms: Respiratory tract infections; Ear, nose and throat infections; Urinary tract infections; Soft tissue infections; Obstetrics and gynaecological infections; Gonorrhoea; Prophylaxis against infection in abdominal, gynaecological, cardiac and pulmonary surgery where there is increased risk from infection.
Bacteriology: Sensitivity tests should be carried out whenever possible. Cefuroxime has activity against: Staphylococcus aureus including penicillin-resistant strains but not the rare methicillin-resistant strains: Escherichia coli; Klebsiella spp.; Enterobacter spp.; Streptococcus pyogenes; Streptococcus viridans; Clostridium spp.; Proteus mirabilis; Proteus rettgeri; Proteus vulgaris; Proteus morganii; Neisseria spp. - including β-lactamase producing strains of N. gonorrhoeae; Haemophilus influenzae; Bacteroides fragilis; Staphylococcus epidermidis.

Dosage and Directions for Use: General Dosage Recommendations: Adults: The dosage range for cefuroxime lies between 1.5 to 6.0 g/day. Many infections will respond to 750 mg three times daily by intramuscular or intravenous injection. For more severe infections, this dose should be increased to 1.5 g three times daily intravenously. The frequency of intramuscular or intravenous injection can be increased to six hourly if necessary.
Infants and Children: Doses of 30 to 100 mg/kg/day, given as 3 or 4 divided doses. A dose of 60 mg/kg/day will be appropriate for most infections.
Other Recommendations: Gonorrhoea: 1.5 g cefuroxime should be given as a single dose. This may be given as 2 x 750 mg injections into different sites, e.g. each buttock.
Prophylaxis: The usual dose is 1.5 g intravenously with induction of anaesthesia for abdominal and gynaecological operations, but may be supplemented with two 750 mg intramuscular doses 8 and 16 hours later. In cardiac and pulmonary operations, the usual dose is 1.5 g intravenously with induction of anaesthesia continuing with 750 mg intramuscularly three times daily for a further 24 to 48 hours.
Dosage in impaired renal function: Cefuroxime is excreted by the kidneys. Therefore, 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 GFR falls below 20 ml/min. In adults with marked impairment (GFR 10 to 20 ml/min) 750 mg twice daily is recommended and with severe impairment (GFR less than 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 usually 750 mg twice daily.
Administration: Intramuscular injection: Add 1 ml sterile Water for Injections to 250 mg cefuroxime or 3 ml sterile Water for Injections to 750 mg cefuroxime. Shake gently to produce an opaque suspension. Suspensions which appear granular must be discarded.
Intravenous injection: Dissolve cefuroxime in sterile Water for Injections using at least 2 ml for 250 mg, at least 6 ml for 750 mg, or 15 ml for 1.5 g. Solutions which appear turbid must be discarded.
Intravenous infusion: For short intravenous infusion (30 to 60 minutes) 1.5 g may be dissolved in 50 ml sterile 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. Solutions which appear turbid must be discarded.
Suspensions of cefuroxime for intramuscular injection and aqueous solutions for direct intravenous injection should be used within 5 hours if kept below 25°C or within 48 hours if refrigerated. Some increase in colour may occur on storage. Solutions for short intravenous infusion (1.5 g plus 50 ml sterile Water for Injections) which show less increase in colour, should be used within 24 hours if kept below 25°C or within 72 hours if refrigerated.
Cefuroxime is compatible with the more commonly used intravenous fluids. It will retain potency for up to 24 hours at room temperature in Sodium Chloride Injection B.P. 0.9% m/v, 5% Dextrose Injection B.P., 0.18% m/v Sodium Chloride plus 4% Dextrose Injection B.P., and Compound Sodium Lactate Injection B.P. (Hartmann's solution). The pH of 2.74% m/v Sodium Bicarbonate Injection B.P. considerably affects the colour of the solution and therefore this solution is not recommended for the dilution of cefuroxime.
However, if required for patients receiving Sodium Bicarbonate Injection by infusion, the cefuroxime may be introduced into the tube of the giving set. The stability of cefuroxime in Sodium Chloride Injection B.P. 0.9% m/v and in 5% Dextrose Injection is not affected by the presence of hydrocortisone sodium phosphate.
Cefuroxime is also compatible with aqueous solutions containing up to 1% lignocaine hydrochloride.

Hypersensitivity to cephalosporin antibiotics.

Special care is indicated in patients who have experienced an allergic reaction to penicillins or other beta-lactams.
Safety in pregnancy and lactation has not been established.
Cefuroxime does not interfere in enzyme-based tests for glucosuria. Slight interference with copper reduction methods (Benedict's, Fehling's, Clinitest) may be observed. However, this should not lead to false-positive results. Cefuroxime may cause false-negative reactions in the ferricyanide test. Some cephalosporins can cause a falsely high reading in the alkaline picrate assay for creatinine, although the degree of elevation is unlikely to be of clinical importance. It is possible that cefuroxime may also interfere with this determination.
Prolonged use may result in the overgrowth of non-susceptible organisms. Patients developing frequent loose stools should be carefully monitored for the possible development of an antibiotic colitis.
Concomitant use of cefuroxime and furosemide should be avoided when possible. If they are used together renal function should be monitored closely as furosemide may enhance the nephrotoxic potential of the cephalosporins.
The combined use of cephalosporins and aminoglycosides seems to increase the risk of nephrotoxicity and should be undertaken with caution and with close monitoring of renal function. Cefuroxime must not be administered simultaneously with other medicines.

Effects reported include rashes, thrombophlebitis after intravenous injection, gastrointestinal disturbance and Candida intertrigo. The principal changes in haematological parameters seen in some patients have been of unexplained decreased haemoglobin concentration and of eosinophilia. Patients developing eosinophilia should have renal function closely monitored since hypersensitivity with acute renal failure has previously been documented. Patients developing decreased haemoglobin concentration should have bone marrow response monitored. Leukopenia and neutropenia have also been noted.
A positive Coombs' test has been found in patients treated with cefuroxime, this phenomenon can interfere with the cross-matching of blood. There are sometimes rises in serum liver enzymes or serum bilirubin particularly in patients with pre-existing liver disease. There may also be some variation in the results of biochemical tests of renal function but these do not appear to be of clinical importance.
As a precaution, renal function should be monitored if this is already impaired. Hypersensitivity reactions including skin rashes (maculopapular and urticarial), drug fever and anaphylaxis have been reported.
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 of treatment.

Store at temperature not exceeding 30°C. Protect from light.

Cephalosporins

J01DC02 - cefuroxime ; Belongs to the class of second-generation cephalosporins. Used in the systemic treatment of infections.

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