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Indications/Uses
Tablet: Cefuroxime Axetil Tablet are indicated for the treatment of patients with mild to moderate infections caused by susceptible strains of the designated microorganisms in the conditions listed as follows: Pharyngitis/Tonsillitis caused by Streptococcus pyogenes.
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 or Haemophilus influenzae (non-beta-lactamase-producing strains only).
Acute Bacterial Exacerbations of Chronic Bronchitis and Secondary Bacterial Infections of Acute Bronchitis caused by Streptococcus pneumoniae, Haemophilus influenzae (beta-lactamase negative strains), or Haemophilus parainfluenzae (beta-lactamase negative strains).
Uncomplicated Skin and Skin-Structure Infections caused by Staphylococcus aureus (including beta-lactamase-producing strains) or Streptococcus pyogenes.
Uncomplicated Urinary Tract Infections caused by Escherichia coli or Klebsiella pneumoniae.
Uncomplicated Gonorrhea, urethral and endocervical, caused by penicillinase-producing and non-penicillinase-producing strains of Neisseria gonorrhoeae and uncomplicated gonorrhea, rectal, in females, caused by non-penicillinase-producing strains of Neisseria gonorrhoeae.
Early Lyme Disease (erythema migrans) caused by Borrelia burgdorferi.
Suspension: It is a second-generation cephalosporin antibiotic used in the treatment of susceptible infections. These have included bone and joint infections, bronchitis (and other lower respiratory tract infections), gonorrhea, meningitis, otitis media, peritonitis, pharyngitis, sinusitis, skin infections (including soft tissue infections), and urinary tract infections. It is also used for surgical infection prophylaxis.
Injection: Cefuroxime sodium for injection is indicated for the treatment of infections listed as follows in adults and children, including neonates (from birth).
Community acquired pneumonia.
Acute exacerbations of chronic bronchitis.
Complicated urinary tract infections, including pyelonephritis.
Soft-tissue infections: cellulitis, erysipelas and wound infections.
Intra-abdominal infections.
Prophylaxis against infection in gastrointestinal (including oesophageal), orthopaedic, cardiovascular, and gynaecological surgery (including caesarean section).
In the treatment and prevention of infections in which it is very likely that anaerobic organisms will be encountered, cefuroxime should be administered with additional appropriate antibacterial agents. Consideration should be given to official guidance on the appropriate use of antibacterial agents.
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 or Haemophilus influenzae (non-beta-lactamase-producing strains only).
Acute Bacterial Exacerbations of Chronic Bronchitis and Secondary Bacterial Infections of Acute Bronchitis caused by Streptococcus pneumoniae, Haemophilus influenzae (beta-lactamase negative strains), or Haemophilus parainfluenzae (beta-lactamase negative strains).
Uncomplicated Skin and Skin-Structure Infections caused by Staphylococcus aureus (including beta-lactamase-producing strains) or Streptococcus pyogenes.
Uncomplicated Urinary Tract Infections caused by Escherichia coli or Klebsiella pneumoniae.
Uncomplicated Gonorrhea, urethral and endocervical, caused by penicillinase-producing and non-penicillinase-producing strains of Neisseria gonorrhoeae and uncomplicated gonorrhea, rectal, in females, caused by non-penicillinase-producing strains of Neisseria gonorrhoeae.
Early Lyme Disease (erythema migrans) caused by Borrelia burgdorferi.
Suspension: It is a second-generation cephalosporin antibiotic used in the treatment of susceptible infections. These have included bone and joint infections, bronchitis (and other lower respiratory tract infections), gonorrhea, meningitis, otitis media, peritonitis, pharyngitis, sinusitis, skin infections (including soft tissue infections), and urinary tract infections. It is also used for surgical infection prophylaxis.
Injection: Cefuroxime sodium for injection is indicated for the treatment of infections listed as follows in adults and children, including neonates (from birth).
Community acquired pneumonia.
Acute exacerbations of chronic bronchitis.
Complicated urinary tract infections, including pyelonephritis.
Soft-tissue infections: cellulitis, erysipelas and wound infections.
Intra-abdominal infections.
Prophylaxis against infection in gastrointestinal (including oesophageal), orthopaedic, cardiovascular, and gynaecological surgery (including caesarean section).
In the treatment and prevention of infections in which it is very likely that anaerobic organisms will be encountered, cefuroxime should be administered with additional appropriate antibacterial agents. Consideration should be given to official guidance on the appropriate use of antibacterial agents.
Dosage/Direction for Use
Tablet: Cefuroxime axetil tablets administered by oral route without regard to meal and the dosage and administration in Adults and Pediatric patients is given as follows: See Table 1.
Suspension: Cefuroxime Axetil in a form of suspension is given by mouth with or after food.
For adults: 250 mg (one 5 mL teaspoonful) twice daily for uncomplicated urinary-tract infections and 250 mg to 500 mg twice daily for respiratory-tract infections.
For children more than 3 months of age: 250 mg twice daily or 1 O mg/kg twice daily to a maximum of 250 mg daily.
For children over 2 years of age with otitis media: 250 mg twice daily or 15 mg/kg twice daily to a maximum of 500 mg daily.
Or as prescribed by the physician.
Injection: Posology: See Tables 2 and 3.
For adults: 250 mg (one 5 mL teaspoonful) twice daily for uncomplicated urinary-tract infections and 250 mg to 500 mg twice daily for respiratory-tract infections.
For children more than 3 months of age: 250 mg twice daily or 1 O mg/kg twice daily to a maximum of 250 mg daily.
For children over 2 years of age with otitis media: 250 mg twice daily or 15 mg/kg twice daily to a maximum of 500 mg daily.
Or as prescribed by the physician.
Injection: Posology: See Tables 2 and 3.
Renal impairment: Cefuroxime is primarily 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. (See Table 4.)
Hepatic impairment: Cefuroxime is primarily eliminated by the kidney. In patients with hepatic dysfunction this is not expected to effect the pharmacokinetics of cefuroxime.
Method of administration: Cefuroxime should be administered by intravenous injection over a period of 3 to 5 minutes directly into a vein or via a drip tube or infusion over 30 to 60 minutes, or by deep intramuscular injection. Intramuscular injections should be injected well within the bulk of a relatively large muscle and not more than 750 mg should be injected at one site. For doses greater than 1.5 g intravenous administration should be used.
Method of administration: Cefuroxime should be administered by intravenous injection over a period of 3 to 5 minutes directly into a vein or via a drip tube or infusion over 30 to 60 minutes, or by deep intramuscular injection. Intramuscular injections should be injected well within the bulk of a relatively large muscle and not more than 750 mg should be injected at one site. For doses greater than 1.5 g intravenous administration should be used.
Overdosage
Overdosage of cephalosporins can cause cerebral irritation leading to convulsions. Serum levels of cefuroxime can be reduced by hemodialysis and peritoneal dialysis.
Administration
FC tab: May be taken with or without food. Powd for oral susp: Should be taken with food.
Contraindications
Tablet: Cefuroxime Axetil tablet is contraindicated in patients with known allergy to the cephalosporin group of antibiotics.
Suspension and Injection: 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).
Suspension and Injection: 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).
Special Precautions
Tablet: Before therapy with cefuroxime axetil is instituted, careful inquiry should be made to determine whether the patient has had previous hypersensitivity reactions to cefuroxime axetil, other cephalosporins, penicillins, or other drugs. If this product is to be given to penicillin-sensitive patients, caution should be exercised because cross-hypersensitivity among beta-lactam antibiotics has been clearly documented and may occur in up to 10% of patients with a history of penicillin allergy. If a clinically significant allergic reaction to cefuroxime axetil occurs, discontinue the drug and institute appropriate therapy. Serious acute hypersensitivity reactions may require treatment with epinephrine and other emergency measures, including oxygen, intravenous fluids, intravenous antihistamines, corticosteroids, pressor amines, and airway management, as clinically indicated. Cephalosporins, including Cefuroxime Axetil, should be given with caution to patients receiving concurrent treatment with potent diuretics because these diuretics are suspected of adversely affecting renal function. Cefuroxime Axetil, as with other broad-spectrum antibiotics, should be prescribed with caution in individuals with a history of colitis. Cephalosporins may be associated with a fall in prothrombin activity. Those at risk include patients with renal or hepatic impairment or poor nutritional state, as well as patients receiving a protracted course of antimicrobial therapy, and patients previously stabilized on anticoagulant therapy. Diarrhea is a common problem caused by antibiotics which usually ends when the antibiotic is discontinued.
Suspension: It should not be given to patients who are hypersensitive to it or to other cephalosporins. About 10% of penicillin-sensitive patients may also be allergic to cephalosporins although the true incidence is uncertain. Great care should be taken if it is to be given to such patients. Care is also necessary in patients with a history of allergy. It should be given with caution to patients with renal impairment; a dosage reduction may be necessary. Renal and hematological status should be monitored especially drug-prolonged and high-dose therapy.
Injection: 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 750 mg 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.
Suspension: It should not be given to patients who are hypersensitive to it or to other cephalosporins. About 10% of penicillin-sensitive patients may also be allergic to cephalosporins although the true incidence is uncertain. Great care should be taken if it is to be given to such patients. Care is also necessary in patients with a history of allergy. It should be given with caution to patients with renal impairment; a dosage reduction may be necessary. Renal and hematological status should be monitored especially drug-prolonged and high-dose therapy.
Injection: 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 750 mg 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.
Use In Pregnancy & Lactation
Tablet and suspension: There is no experimental evidence of embryopathic or teratogenic effects attributable to cefuroxime axetil but, as with all 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.
Injection: 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 breast-feeding 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.
Cefuroxime is excreted in human milk, and consequently caution should be exercised when cefuroxime axetil is administered to a nursing mother.
Injection: 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 breast-feeding 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.
Adverse Reactions
Tablet: The following hypersensitivity reactions have been reported: anaphylaxis, angioedema, pruritus, rash, serum sickness-like reaction, urticaria.
Gastrointestinal: Pseudomembranous colitis.
Hematologic: Hemolytic anemia, leukopenia, pancytopenia, thrombocytopenia, and increased prothrombin time.
Hepatic: Hepatic impairment including hepatitis and cholestasis, jaundice.
Neurologic: Seizure.
Skin: Erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis.
Urologic: Renal dysfunction.
The following adverse events were thought by the investigators to be possibly, probably, or almost certainly related to Cefuroxime Axetil tablets in multiple-dose clinical trials: Diarrhea/loose stools, nausea/vomiting, transient elevation in AST, transient elevation in ALT, eosinophilia, transient elevation in LDH, abdominal pain, abdominal cramps, flatulence, indigestion, headache, vaginitis, vulvar itch, chills, rash, hives, itch, dysuria, chest pain.
Suspension: Gastrointestinal Disorders: diarrhea, nausea, vomiting.
Skin and subcutaneous tissue disorders: erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis.
Injection: The most common adverse reactions are neutropenia, eosinophilia, transient rise in liver enzymes or bilirubin, particularly in patients with pre-existing liver disease, but there is no evidence of harm to the liver and injection site reactions.
The frequency categories assigned to the adverse reactions as follows are estimates, as for most reactions suitable data for calculating incidence are not available. In addition the incidence of adverse reactions associated with cefuroxime sodium may vary according to the indication.
Data from clinical trials were used to determine the frequency of very common to rare adverse reactions. The frequencies assigned to all other adverse reactions (i.e. those occurring at <1/10,000) were mainly determined using post-marketing data, and refer to a reporting rate rather than a true frequency.
Treatment related adverse reactions, all grades, are listed as follows by MedDRA body system organ class, frequency and grade of severity. The following convention has been utilised for the classification of frequency: very common ≥ 1/10; common ≥ 1/100 to < 1/10, uncommon ≥ 1/1,000 to < 1/100; rare ≥ 1/10,000 to < 1/1,000; very rare < 1/10,000 and not known (cannot be estimated from the available data). (See Table 5.)
Gastrointestinal: Pseudomembranous colitis.
Hematologic: Hemolytic anemia, leukopenia, pancytopenia, thrombocytopenia, and increased prothrombin time.
Hepatic: Hepatic impairment including hepatitis and cholestasis, jaundice.
Neurologic: Seizure.
Skin: Erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis.
Urologic: Renal dysfunction.
The following adverse events were thought by the investigators to be possibly, probably, or almost certainly related to Cefuroxime Axetil tablets in multiple-dose clinical trials: Diarrhea/loose stools, nausea/vomiting, transient elevation in AST, transient elevation in ALT, eosinophilia, transient elevation in LDH, abdominal pain, abdominal cramps, flatulence, indigestion, headache, vaginitis, vulvar itch, chills, rash, hives, itch, dysuria, chest pain.
Suspension: Gastrointestinal Disorders: diarrhea, nausea, vomiting.
Skin and subcutaneous tissue disorders: erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis.
Injection: The most common adverse reactions are neutropenia, eosinophilia, transient rise in liver enzymes or bilirubin, particularly in patients with pre-existing liver disease, but there is no evidence of harm to the liver and injection site reactions.
The frequency categories assigned to the adverse reactions as follows are estimates, as for most reactions suitable data for calculating incidence are not available. In addition the incidence of adverse reactions associated with cefuroxime sodium may vary according to the indication.
Data from clinical trials were used to determine the frequency of very common to rare adverse reactions. The frequencies assigned to all other adverse reactions (i.e. those occurring at <1/10,000) were mainly determined using post-marketing data, and refer to a reporting rate rather than a true frequency.
Treatment related adverse reactions, all grades, are listed as follows by MedDRA body system organ class, frequency and grade of severity. The following convention has been utilised for the classification of frequency: very common ≥ 1/10; common ≥ 1/100 to < 1/10, uncommon ≥ 1/1,000 to < 1/100; rare ≥ 1/10,000 to < 1/1,000; very rare < 1/10,000 and not known (cannot be estimated from the available data). (See Table 5.)
Paediatric population: The safety profile for cefuroxime sodium in children is consistent with the profile in adults.
Drug Interactions
Tablet: In common with other antibiotics, Cefuroxime axetil may affect the gut flora, leading to lower oestrogen reabsorption and reduced efficacy of combined oral contraceptives. 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 axetil. This antibiotic does not interfere in the alkaline picrate assay for creatinine.
Concurrent administration of probenecid increases the area under the mean serum concentration time curve by 50%. Serum levels of cefuroxime are reduced by dialysis. A positive Coomb's test has been reported during treatment with cephalosporins. This phenomenon can interfere with cross matching of blood.
Suspension: Probenecid reduces the renal clearance of cefuroxime.
Injection: 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: Determination of blood/plasma glucose levels.
Concomitant use with oral anticoagulants may give rise to increased international normalised ratio (INR).
Concurrent administration of probenecid increases the area under the mean serum concentration time curve by 50%. Serum levels of cefuroxime are reduced by dialysis. A positive Coomb's test has been reported during treatment with cephalosporins. This phenomenon can interfere with cross matching of blood.
Suspension: Probenecid reduces the renal clearance of cefuroxime.
Injection: 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: Determination of blood/plasma glucose levels.
Concomitant use with oral anticoagulants may give rise to increased international normalised ratio (INR).
Caution For Usage
Direction for Reconstitution: Suspension: Tap the bottle to loosen the powder. Slowly add boiled and cooled water up to the mark on the bottle and shake well. Add water if necessary to adjust the volume to the mark. The reconstituted suspension should be stored in a refrigerator and should be used within 7 days after reconstitution.
DO NOT FREEZE.
SHAKE WELL BEFORE USE.
Injection: Instructions for constitution: See Table 6.
DO NOT FREEZE.
SHAKE WELL BEFORE USE.
Injection: Instructions for constitution: See Table 6.
As for all parenteral medicinal products, inspect the reconstituted solution or suspension visually for particulate matter and discoloration prior to administration.
Intramuscular injection: After addition of the specified amount of diluent for intramuscular injection, a suspension is formed.
Intravenous bolus injection or intravenous infusion: After addition of the specified amount of diluent for intravenous bolus or infusion, a clear solution is formed. The solution should only be used if the solution is clear and practically free from particles.
Solutions and suspensions range in colour from clear to yellow coloured depending on concentration, diluent and storage conditions used. When made up for intramuscular use, it becomes off-white and opaque. When made up for intravenous administration, it may be yellowish.
For single use. Any unused medicinal product or waste material should be disposed of in accordance with local requirements.
Intramuscular injection: After addition of the specified amount of diluent for intramuscular injection, a suspension is formed.
Intravenous bolus injection or intravenous infusion: After addition of the specified amount of diluent for intravenous bolus or infusion, a clear solution is formed. The solution should only be used if the solution is clear and practically free from particles.
Solutions and suspensions range in colour from clear to yellow coloured depending on concentration, diluent and storage conditions used. When made up for intramuscular use, it becomes off-white and opaque. When made up for intravenous administration, it may be yellowish.
For single use. Any unused medicinal product or waste material should be disposed of in accordance with local requirements.
Storage
Store at temperatures not exceeding 30°C.
Tablet and injection: Protect from light.
Tablet and injection: Protect from light.
Action
Pharmacology: Tablet: Mode of Action: Pharmacological effects/mode of action Cefuroxime, like the penicillins, is a beta-lactam antibiotic. By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, it inhibits the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins; it is possible that cefuroxime interferes with an autolysin inhibitor. Cefuroxime axetil is an oral prodrug of the bactericidal cephalosporin antibiotic cefuroxime, which is resistant to most beta-lactamases and is active against a wide range of gram-positive and gram-negative organisms.
Suspension: Mechanism of Action: Like other beta-lactam drugs, cefuroxime exerts antibacterial activity by binding to and inhibiting the action of certain bacterial cell wall synthetic enzymes namely the penicillin-binding proteins. This results in the interruption of cell wall (peptidoglycan) biosynthesis which leads to bacterial cell lysis and death.
Mechanisms of resistance: Bacterial resistance to cefuroxime may be due to one or more of the following mechanisms: Hydrolysis by beta-lactamases; cefuroxime may be efficiently hydrolysed by certain extended-spectrum beta-lactamases (ESBLs) and by the chromosomally encoded (AmpC) enzyme that may be induced or stably depressed 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 organisms; Drug efflux pumps.
Breakpoints: The following clinical MIC breakpoints for bacteria have been defined for cefuroxime according to EUCAST: Enterobacteriaceae: :≤8 mg/L for susceptible, >8 mg/L for resistant; S. pneumoniae: ≤0.5 mg/L for susceptible, >1 mg/L for resistant; Streptococcus spp.: ≤0.5 mg/L for susceptible, >0.5 mg/L for resistant; H. influenzae and M. catarrhalis: ≤1 mg/L for susceptible, >2 mg/L for resistant; Non-species related breakpoints: ≤4 mg/L for susceptible, >8 mg/L for resistant.
Susceptibility: The prevalence of acquired resistance may vary geographically and with time for selected species and local information on resistance is desirable, particularly when treating severe infections. As necessary, expert advice should be sought when the local prevalence is such that the utility of the agent in at least some types of infections are questionable.
Injection: 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: Suspension: 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.
Injection: Absorption: After intramuscular (IM) injection of cefuroxime to normal volunteers, the mean peak serum concentrations ranged from 27 to 35 μg/mL for a 750 mg dose and from 33 to 40 μg/mL for a 1000 mg dose, and were achieved within 30 to 60 minutes after administration. Following intravenous (IV) doses of 750 and 1500 mg, serum concentrations were approximately 50 and 100 μg/mL, respectively, at 15 minutes.
AUC and Cmax appear to increase linearly with increase in dose over the single dose range of 250 to 1000 max mg following IM and IV administration. There was no evidence of accumulation of cefuroxime in the serum from normal volunteers following repeat intravenous administration of 1500 mg doses every 8 hours.
Distribution: Protein binding has been stated as 33 to 50%, depending on the methodology used. The average volume of distribution ranges from 9.3 to 15.8 L/1.73 m2 following IM or IV administration over the dosage range of 250 to 1000 mg. Concentrations of cefuroxime in excess of the minimum inhibitory levels for common pathogens can be achieved in the tonsilla, sinus tissues, bronchial mucosa, bone, pleural fluid, joint fluid, synovial fluid, interstitial fluid, bile, sputum and aqueous humour. Cefuroxime passes the blood-brain barrier when the meninges are inflamed.
Biotransformation: Cefuroxime is not metabolised.
Elimination: Cefuroxime is excreted by glomerular filtration and tubular secretion. The serum half-life after either intramuscular or intravenous administration is approximately 70 minutes. There is an almost complete recovery (85 to 90%) of unchanged cefuroxime in urine within 24 hours of administration. The majority of the cefuroxime is excreted within the first 6 hours. The average renal clearance ranges from 114 to 170 mL/min/1.73 m2 following IM or IV administration over the dosage range of 250 to 1000 mg.
Special patient populations: Gender: No differences in the pharmacokinetics of cefuroxime were observed between males and females following a single IV bolus injection of 1000 mg of cefuroxime as the sodium salt.
Elderly: Following IM or IV administration, the absorption, distribution and excretion of cefuroxime in elderly patients are similar to younger patients with equivalent renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in cefuroxime dose selection, and it may be useful to monitor renal function.
Paediatrics: The serum half-life of cefuroxime has been shown to be substantially prolonged in neonates according to gestational age. However, in older infants (aged >3 weeks) and in children, the serum half-life of 60 to 90 minutes is similar to that observed in adults.
Renal impairment: Cefuroxime is primarily excreted by the kidneys. As with all such antibiotics, in patients with markedly impaired renal function (i.e. C1cr <20 mL/minute) it is recommended that the dosage of cefuroxime should be reduced to compensate for its slower excretion. Cefuroxime is effectively removed by haemodialysis and peritoneal dialysis.
Hepatic impairment: Since cefuroxime is primarily eliminated by the kidney, hepatic dysfunction is not expected to have an effect on the pharmacokinetics of cefuroxime.
PK/PD relationship: For cephalosporins, the most important pharmacokinetic-pharmacodynamic index correlating with in vivo efficacy has been shown to be the percentage of the dosing interval (%T) that the unbound concentration remains above the minimum inhibitory concentration (MIC) of cefuroxime for individual target species (i.e. %T>MIC).
Suspension: Mechanism of Action: Like other beta-lactam drugs, cefuroxime exerts antibacterial activity by binding to and inhibiting the action of certain bacterial cell wall synthetic enzymes namely the penicillin-binding proteins. This results in the interruption of cell wall (peptidoglycan) biosynthesis which leads to bacterial cell lysis and death.
Mechanisms of resistance: Bacterial resistance to cefuroxime may be due to one or more of the following mechanisms: Hydrolysis by beta-lactamases; cefuroxime may be efficiently hydrolysed by certain extended-spectrum beta-lactamases (ESBLs) and by the chromosomally encoded (AmpC) enzyme that may be induced or stably depressed 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 organisms; Drug efflux pumps.
Breakpoints: The following clinical MIC breakpoints for bacteria have been defined for cefuroxime according to EUCAST: Enterobacteriaceae: :≤8 mg/L for susceptible, >8 mg/L for resistant; S. pneumoniae: ≤0.5 mg/L for susceptible, >1 mg/L for resistant; Streptococcus spp.: ≤0.5 mg/L for susceptible, >0.5 mg/L for resistant; H. influenzae and M. catarrhalis: ≤1 mg/L for susceptible, >2 mg/L for resistant; Non-species related breakpoints: ≤4 mg/L for susceptible, >8 mg/L for resistant.
Susceptibility: The prevalence of acquired resistance may vary geographically and with time for selected species and local information on resistance is desirable, particularly when treating severe infections. As necessary, expert advice should be sought when the local prevalence is such that the utility of the agent in at least some types of infections are questionable.
Injection: 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: Suspension: 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.
Injection: Absorption: After intramuscular (IM) injection of cefuroxime to normal volunteers, the mean peak serum concentrations ranged from 27 to 35 μg/mL for a 750 mg dose and from 33 to 40 μg/mL for a 1000 mg dose, and were achieved within 30 to 60 minutes after administration. Following intravenous (IV) doses of 750 and 1500 mg, serum concentrations were approximately 50 and 100 μg/mL, respectively, at 15 minutes.
AUC and Cmax appear to increase linearly with increase in dose over the single dose range of 250 to 1000 max mg following IM and IV administration. There was no evidence of accumulation of cefuroxime in the serum from normal volunteers following repeat intravenous administration of 1500 mg doses every 8 hours.
Distribution: Protein binding has been stated as 33 to 50%, depending on the methodology used. The average volume of distribution ranges from 9.3 to 15.8 L/1.73 m2 following IM or IV administration over the dosage range of 250 to 1000 mg. Concentrations of cefuroxime in excess of the minimum inhibitory levels for common pathogens can be achieved in the tonsilla, sinus tissues, bronchial mucosa, bone, pleural fluid, joint fluid, synovial fluid, interstitial fluid, bile, sputum and aqueous humour. Cefuroxime passes the blood-brain barrier when the meninges are inflamed.
Biotransformation: Cefuroxime is not metabolised.
Elimination: Cefuroxime is excreted by glomerular filtration and tubular secretion. The serum half-life after either intramuscular or intravenous administration is approximately 70 minutes. There is an almost complete recovery (85 to 90%) of unchanged cefuroxime in urine within 24 hours of administration. The majority of the cefuroxime is excreted within the first 6 hours. The average renal clearance ranges from 114 to 170 mL/min/1.73 m2 following IM or IV administration over the dosage range of 250 to 1000 mg.
Special patient populations: Gender: No differences in the pharmacokinetics of cefuroxime were observed between males and females following a single IV bolus injection of 1000 mg of cefuroxime as the sodium salt.
Elderly: Following IM or IV administration, the absorption, distribution and excretion of cefuroxime in elderly patients are similar to younger patients with equivalent renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in cefuroxime dose selection, and it may be useful to monitor renal function.
Paediatrics: The serum half-life of cefuroxime has been shown to be substantially prolonged in neonates according to gestational age. However, in older infants (aged >3 weeks) and in children, the serum half-life of 60 to 90 minutes is similar to that observed in adults.
Renal impairment: Cefuroxime is primarily excreted by the kidneys. As with all such antibiotics, in patients with markedly impaired renal function (i.e. C1cr <20 mL/minute) it is recommended that the dosage of cefuroxime should be reduced to compensate for its slower excretion. Cefuroxime is effectively removed by haemodialysis and peritoneal dialysis.
Hepatic impairment: Since cefuroxime is primarily eliminated by the kidney, hepatic dysfunction is not expected to have an effect on the pharmacokinetics of cefuroxime.
PK/PD relationship: For cephalosporins, the most important pharmacokinetic-pharmacodynamic index correlating with in vivo efficacy has been shown to be the percentage of the dosing interval (%T) that the unbound concentration remains above the minimum inhibitory concentration (MIC) of cefuroxime for individual target species (i.e. %T>MIC).
MedsGo Class
Cephalosporins
Features
Brand
Zocef
Full Details
Dosage Strength
750mg
Drug Ingredients
- Cefuroxime
Drug Packaging
Powder for Injection 1's
Generic Name
Cefuroxime Sodium
Dosage Form
Powder For Injection
Registration Number
DRP-5748
Drug Classification
Prescription Drug (RX)