Zinacare

Zinacare

cefuroxime

Manufacturer:

NCPC Hebei Huamin Pharma

Distributor:

AGlobal Care
Full Prescribing Info
Contents
Cefuroxime sodium.
Description
Each vial contains: Cefuroxime (as sodium) 750 mg.
Action
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. 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: 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 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. Cefurox1me 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. Clcr <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).
Indications/Uses
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
Posology: See Table 1.

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See Table 2.

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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 3.)

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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.
Directions for Reconstitution: Instructions for constitution: See Table 4.

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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 dear 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, ii may be yellowish.
For single use. Any unused medicinal product or waste material should be disposed of in accordance with local requirements
Overdosage
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.
Contraindications
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
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 du ring 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
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 cefuroxime therapy taking into account the benefit of breast feeding for the child and the benefit of therapy for the woman.
Adverse Reactions
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 below 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 below 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.)

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Paediatric population: The safety profile for cefuroxime sodium in children is consistent with the profile in adults.
Drug Interactions
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).
Storage
Store at temperatures not exceeding 30°C. Protect from light.
MIMS Class
ATC Classification
J01DC02 - cefuroxime ; Belongs to the class of second-generation cephalosporins. Used in the systemic treatment of infections.
Presentation/Packing
Powd for inj (vial + sterile water for inj) 750 mg (white or faintly yellow) x 1's.
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