Zefur IV

White to faintly yellow powder filled in 10 mL colorless glass vials, closed with grey butyl rubber stopper and sealed with aluminum seal with white flip off seal.
Each vial contains: Sterile Cefuroxime USP (as Sodium) 750 mg.

Pharmacotherapeutic group: Antibacterials for systemic use, Second-generation cephalosporins.
Pharmacology: Pharmacodynamics: Mechanism of action: Cefuroxime inhibits bacterial cell wall synthesis following attachment to penicillin binding proteins (PBPs). This results in the interruption of cell wall (peptidoglycan) biosynthesis, which leads to bacterial cell lysis and death.
Mechanism of resistance: Bacterial resistance to Cefuroxime may be due to one or more of the following mechanisms: hydrolysis by beta-lactamases including (but not limited to) extended-spectrum beta-lactamases (ESBLs), and Amp-C enzymes, that may be induced or stably derepressed in certain aerobic Gram-negative bacterial species; reduced affinity of penicillin-binding proteins for Cefuroxime; outer membrane impermeability, which restricts access of Cefuroxime to penicillin binding proteins in Gram-negative bacteria; bacterial efflux pumps.
Organisms that have acquired resistance to other injectable cephalosporins are expected to be resistant to Cefuroxime. Depending on the mechanism of resistance, organisms with acquired resistance to penicillins may demonstrate reduced susceptibility or resistance to Cefuroxime.
Pharmacokinetics: Cefuroxime is widely distributed in the body including pleural fluid, sputum, bone, synovial fluid, and aqueous humour, but only achieves therapeutic concentrations in the CSF when the meninges are inflamed. It crosses the placenta and has been detected in breast milk. It is excreted unchanged, by glomerular filtration and renal tubular secretion, and high concentrations are achieved in the urine. Following injection most of a dose of Cefuroxime is excreted within 24 hours, the majority within 6 hours. Probenecid competes for renal tubular secretion with Cefuroxime resulting in higher and more prolonged plasma concentrations of Cefuroxime. Small amounts of Cefuroxime are excreted in bile. Plasma concentrations are reduced by dialysis.

For the treatment of susceptible infections, such as bone and joint infections, lower respiratory tract infections, skin infections and urinary tract infections.

Cefuroxime Sodium may be given by deep intramuscular injection, by slow intravenous injection over 3 to 5 minutes, or by intravenous infusion.
For Adult: 750 mg every 8 hours. Severe infection 1.5 g IV every 6 to 8 hours for 5 to 10 days.
Infant and children: 30-60 mg/kg/day, dose may be increased to 100 mg/kg/day in 3-4 divided doses.
Neonates: Same total daily dose as children but in 2-3 divided doses. Or as prescribed by the physician.

Overdose can lead to neurological sequelae including encephalopathy, convulsions and coma. Symptoms of overdose can occur if the dose is not reduced appropriately in patients with renal impairment.
Serum levels of Cefuroxime can be reduced by haemodialysis or peritoneal dialysis.

Hypersensitivity to Cefuroxime or to any of the excipients; Patients with known hypersensitivity to cephalosporin antibiotics; History of severe hypersensitivity (e.g. anaphylactic reaction) to any other type of beta-lactam antibacterial agent (penicillins, monobactams and carbapenems).

Hypersensitivity reactions: As with all beta-lactam antibacterial agents, serious and occasionally fatal hypersensitivity reactions have been reported. In case of severe hypersensitivity reactions, treatment with Cefuroxime must be discontinued immediately and adequate emergency measures must be initiated.
Before beginning treatment, it should be established whether the patient has a history of severe hypersensitivity reactions to Cefuroxime, to other cephalosporins or to any other type of beta-lactam agent. Caution should be used if Cefuroxime is given to patients with a history of non-severe hypersensitivity to other beta-lactam agents.
Cephalosporin antibiotics may, in general, be given safely to patients who are hypersensitive to penicillins, although cross reactions have been reported. Special care is indicated in patients who have experienced an anaphylactic reaction to penicillin.
Concurrent treatment with potent diuretics or aminoglycosides: Cephalosporin antibiotics at high dosage should be given with caution to patients receiving concurrent treatment with potent diuretics such as furosemide or aminoglycosides. Renal impairment has been reported during use of these combinations. Renal function should be monitored in the elderly and those with known pre-existing renal impairment.
Overgrowth of non-susceptible microorganisms: Use of Cefuroxime may result in the overgrowth of Candida. Prolonged use may also result in the overgrowth of other non-susceptible microorganisms (e.g. enterococci and Clostridium difficile), which may require interruption of treatment.
Antibacterial agent-associated pseudomembranous colitis has been reported with use of Cefuroxime and may range in severity from mild to life threatening. This diagnosis should be considered in patients with diarrhoea during or subsequent to the administration of Cefuroxime. Discontinuation of therapy with Cefuroxime and the administration of specific treatment for Clostridium difficile should be considered. Medicinal products that inhibit peristalsis should not be given.
Intra-abdominal infections: Due to its spectrum of activity, Cefuroxime is not suitable for the treatment of infections caused by Gram-negative non-fermenting bacteria.
Interference with diagnostic tests: The development of a positive Coombs Test associated with the use of Cefuroxime may interfere with cross matching of blood.
Slight interference with copper reduction methods (Benedict's, Fehling's, Clinitest) may be observed. However, this should not lead to false-positive results, as may be experienced with some other cephalosporins.
As a false negative result may occur in the ferricyanide test, it is recommended that either the glucose oxidase or hexokinase methods are used to determine blood/plasma glucose levels in patients receiving Cefuroxime sodium.
Intracameral use and eye disorders: Cefuroxime is not formulated for intracameral use. Individual cases and clusters of serious ocular adverse reactions have been reported following unapproved intracameral use of Cefuroxime sodium compounded from vials approved for intravenous/intramuscular administration. These reactions included macular oedema, retinal oedema, retinal detachment, retinal toxicity, visual impairment, visual acuity reduced, vision blurred, corneal opacity and corneal oedema.
Important information about excipients: Cefuroxime powder for solution for injection and infusion contains 40.6 mg sodium per 750mg vial, equivalent to 2% of the WHO recommended maximum daily intake of 2 g sodium for an adult. This should be considered for patients who are on a controlled sodium diet.

Pregnancy: There are limited amounts of data from the use of Cefuroxime in pregnant women. Studies in animals have shown no reproductive toxicity. Cefuroxime should be prescribed to pregnant women only if the benefit outweighs the risk.
Cefuroxime has been shown to cross the placenta and attain therapeutic levels in amniotic fluid and cord blood after intramuscular or intravenous dose to the mother.
Lactation: Cefuroxime is excreted in human milk in small quantities. Adverse reactions at therapeutic doses are not expected, although a risk of diarrhoea and fungus infection of the mucous membranes cannot be excluded. A decision must be made whether to discontinue breastfeeding or to discontinue/abstain from Cefuroxime therapy taking into account the benefit of breast feeding for the child and the benefit of therapy for the woman.

Gastrointestinal disturbances, including diarrhoea, nausea, and vomiting have occured in some patients receiving Cefuroxime sodium. There have been rare reports of erythema multiforme, Stevens-Johnson syndrome, and toxic epidermal necrolysis.

Cefuroxime may affect the gut flora, leading to lower oestrogen reabsorption and reduced efficacy of combined oral contraceptives.
Cefuroxime is excreted by glomerular filtration and tubular secretion. Concomitant use of probenecid is not recommended. Concurrent administration of probenecid prolongs the excretion of Cefuroxime and produces an elevated peak serum level.
Potential nephrotoxic drugs and loop diuretics: High-dosage treatments with cephalosporins should be carried out with caution on patients who are taking strong-acting diuretics (such as furosemide) or potential nephrotoxic preparations (such as aminoglycoside antibiotics), since impairment of renal function through such combinations cannot be ruled out.
Other Interactions: Concomitant use with oral anticoagulants may give rise to increased international normalised ratio (INR).

Direction for Reconstitution: Dissolve the content in 6 mL of Sterilised Water For Injections for IV use and 3 mL of Sterilised Water For Injections for IM use.
Use immediately after reconstitution. Discard any unused portion of the solution.
The prepared solution should be used only, if it is clear.

Store at temperatures not exceeding 30°C.

Cephalosporins

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

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