Zocef/Zocef Kids/Zocef Hospi

Zocef/Zocef Kids: Cefuroxime axetil.
Zocef Hospi: Cefuroxime sodium.

Zocef: Tablet: Each film-coated tablet contains: Cefuroxime Axetil USP equivalent to Anhydrous Cefuroxime 500 mg. Cefuroxime (as axetil) tablets contain cefuroxime as cefuroxime axetil. Cefuroxime axetil is a semisynthetic, broad-spectrum cephalosporin antibiotic for oral administration.
Chemically, cefuroxime axetil, the 1-(acetyloxy)ethyl ester of cefuroxime, is (RS)-1-hydroxyethyl (6R, 7R)-7-[2-(2-furyl) glyoxyl-amido]-3-(hydroxymethyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]-oct-2-ene-2-carboxylate,72 -(Z)-(O -methyl-oxime),1-acetate 3-carbamate. Its molecular formula is C₂₀H₂₂N₄O₁₀S, and it has a molecular weight of 510.48.
Cefuroxime axetil is in the amorphous form.
Cefuroxime (as axetil) tablets are film-coated and contain Cefuroxime Axetil USP equivalent to anhydrous Cefuroxime 500 mg.
Excipients/Inactive Ingredients: Cefuroxime axetil tablets contain the inactive ingredients: Pregelatinized starch, Maize Starch, Sodium Lauryl sulphate, Croscarmellose sodium, Colloidal Silicon Dioxide, Magnesium Stearate, Instacoat Universal IC-U-1308.
Suspension: Each 5 mL (1 teaspoonful) of reconstituted suspension contains: Cefuroxime Axetil USP eq. to Cefuroxime 250 mg.
Zocef Kids: Cefuroxime (as axetil) 250 mg/5 mL powder for oral suspension is an off white-colored powder. After reconstitution, it is an orange color flavored suspension.
Each 5 mL (1 teaspoonful) of reconstituted suspension contains: Cefuroxime (as axetil), USP 250 mg.
Zocef Hospi: Cefuroxime sodium (Zocef Hospi) 750 mg Powder for Injection is a white or faintly yellow powder.
Each vial contains: Cefuroxime (as sodium) 750 mg.

Pharmacology: Zocef: 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.
Zocef Hospi: 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.
Pharmacodynamics: Zocef Kids: Cefuroxime (as axetil) is an oral prodrug of the bactericidal cephalosporin antibiotic cefuroxime, which is resistant to most β (beta)-lactamases and is active against a wide range of Gram-positive and Gram-negative organisms.
It is indicated for the treatment of infections caused by susceptible bacteria.
Susceptibility to Cefuroxime (as axetil) will vary with geography and time and local susceptibility data should be consulted where available.
The prevalence of acquired resistance is geographically and time dependent and for select species may be very high. Local information on resistance is desirable, particularly when treating severe infections. (See Table 1.)

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Pharmacokinetics: Zocef: Tablet: Cefuroxime axetil is absorbed from the gastrointestinal tract and is rapidly hydrolysed in the intestinal mucosa and blood to cefuroxime; absorption is enhanced in the presence of food. Peak plasma concentrations are reported about 2 to 3 hours after an oral dose. Up to 50% of cefuroxime in the circulation is bound to plasma proteins. The plasma half-life is about 70 minutes and is prolonged in patients with renal impairment and in neonates. 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. Cefuroxime is excreted unchanged, by glomerular filtration and renal tubular secretion and high concentrations are achieved in the urine. 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.
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.
Zocef Kids: Absorption: After oral administration Cefuroxime (as axetil) is slowly absorbed from the gastrointestinal tract and rapidly hydrolysed in the intestinal mucosa and blood to release cefuroxime into the circulation.
Optimum absorption occurs when it is administered shortly after a meal.
Following administration of Cefuroxime (as axetil) tablets peak serum levels (2.1 mg/l for a 125 mg dose, 4.1 mg/l for a 250 mg dose, 7.0 mg/l for a 500 mg dose and 13.6 mg/l for a 1 g dose) occur approximately 2 to 3 hours after dosing when taken with food.
Distribution: Protein binding has been variously stated as 33 to 50% depending on the methodology used.
Metabolism: Cefuroxime is not metabolized.
Elimination: The serum half life is between 1 and 1.5 hours.
Cefuroxime is excreted by glomerular filtration and tubular secretion. Concurrent administration of probenecid increases the area under the mean serum concentrations time curve by 50%.
Renal Impairment: Cefuroxime pharmacokinetics have been investigated in patients with various degrees of renal impairment. Cefuroxime elimination half life increases with decrease in renal function which serves as the basis for dosage adjustment recommendations in this group of patients. In patients undergoing haemodialysis, at least 60% of the total amount of cefuroxime present in the body at the start of dialysis will be removed during a 4-hour dialysis period. Therefore, an additional single dose of cefuroxime should be administered following the completion of haemodialysis.
Zocef Hospi: 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 C_max 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).
Microbiology: Zocef: Tablet: The in vivo bactericidal activity of cefuroxime axetil is due to cefuroxime's binding to essential target proteins and the resultant inhibition of cell-wall synthesis. Cefuroxime has bactericidal activity against a wide range of common pathogens, including many beta-lactamase-producing strains. Cefuroxime is stable to many bacterial beta-lactamases, especially plasmid-mediated enzymes that are commonly found in enterobacteriaceae. Cefuroxime has been demonstrated to be active against most strains of the following microorganisms both in vitro and in clinical infections.
Aerobic Gram-Positive Microorganisms: Staphylococcus aureus (including beta-lactamase producing strains), Streptococcus pneumonia, Streptococcus pyogenes, Staphylococcus epidermidis, Staphylococcus saprophyticus, Streptococcus agalactiae.
Aerobic Gram-Negative Microorganisms: Escherichia coli, Haemophilus influenzae (including beta-lactamase-producing strains), Haemophilus parainfluenzae, Klebsiella pneumonia, Moraxella catarrhalis (including beta-lactamase-producing strains), Neisseria gonorrhoeae (including beta-lactamase-producing strains), Spirochetes, Borrelia burgdorferi.

Zocef: Cefuroxime is a second generation cephalosporin antibacterial used in the treatment of susceptible infections. These have included bone and joint infections, bronchitis (and other lower respiratory tract infections), gonorrhea, meningitis (although treatment failures have been reported in H. influenzae meningitis), otitis media, peritonitis, pharyngitis, sinusitis, skin infections (including soft-tissue infections) and urinary tract infections. It is also used for surgical infection prophylaxis.
Zocef Kids: Indications include: Upper respiratory tract infections for example, ear, nose and throat infections, such as otitis media, sinusitis, tonsillitis and pharyngitis.
Lower respiratory tract infections for example, pneumonia, acute bronchitis, and acute exacerbations of chronic bronchitis.
Genito-urinary tract infections for example, pyelonephritis, cystitis and urethritis.
Skin and soft tissue infections for example, furunculosis, pyoderma and impetigo.
Gonorrhoea, acute uncomplicated gonococcal urethritis, and cervicitis.
Treatment of early Lyme disease and subsequent prevention of late Lyme disease in adults and children over 12 years old.
Zocef Hospi: 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.

Zocef: Tablet: Usual oral doses for adults are 125 mg twice daily for uncomplicated urinary tract infections and 250 mg to 500 mg twice daily for respiratory tract infections. A dose for children more than 3 months of age is 125 mg twice daily or 10 mg/kg twice daily to a maximum of 250 mg daily. Children over 2 years of age with otitis media may be given 250 mg twice daily or 15 mg/kg twice daily to a maximum of 500 mg daily.
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 10 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.
Zocef Kids: The usual course of therapy is seven days (range 5 to 10 days).
Cefuroxime (as axetil) should be taken after food for optimum absorption.
Adults: See Table 2.

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Children: In infants and children, it may be preferable to adjust dosage according to weight or age. The dose in infants and children 3 months to 12 years is 10 mg/kg twice daily for most infections, to a maximum of 250 mg daily. In otitis media or more severe infections the recommended dose is 15 mg/kg twice daily to a maximum of 500 mg daily. In Lyme disease, the recommended dose is 15 mg/kg twice daily to a maximum of 500 mg daily for 14 days (range of 10 to 21 days).
The following two tables, divided by age group and weight, serve as a guideline for simplified administration from measuring spoons (5 ml) for the 125 mg/5 ml or the 250 mg/5 ml multi-dose suspension. (See Tables 3 and 4.)

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To enhance compliance and improve the dosing accuracy in very young children, a dosing syringe can be supplied with a multidose bottle containing 50 ml of suspension. However, dosing in spoonfuls should be considered a more favourable option if the child is able to take the medication from the spoon.
If required, the dosing syringe may also be used in older children (refer to the dosing tables as follows).
The recommended doses for the paediatric dosing syringe are expressed in ml or mg and according to bodyweight in the following tables. (Countries must select the relevant columns as required). (See Tables 5 and 6.)

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Cefuroxime is also available as the sodium salt for parenteral administration. This permits parenteral therapy with cefuroxime to be followed by oral therapy in situations where a change from parenteral to oral treatment is clinically indicated.
Renal impairment: Cefuroxime is primarily excreted by the kidneys. In patients with markedly impaired renal function it is recommended that the dosage of cefuroxime be reduced to compensate for its slower excretion (see the table as follows). (See Table 7.)

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Zocef Hospi: Posology: See Tables 8 and 9.

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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 10.)

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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.

Signs and symptoms: Overdosage of cephalosporins can cause cerebral irritation leading to convulsions.
Treatment: Serum levels of cefuroxime can be reduced by haemodialysis and peritoneal dialysis.

Zocef: Tablet: Cefuroxime (as axetil) is contraindicated in patients with known allergy to the cephalosporin group of antibiotics and any of its components.
Zocef Suspension/Zocef Hospi: 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).
Zocef Kids: Patients with known hypersensitivity to cephalosporin antibiotics.

Zocef: Tablet: Clostridium difficile associated diarrhea (CDAD) has been reported with use of nearly all antibacterial agents, including cefuroxime axetil, and may range in severity from mild diarrhea to fatal colitis. Treatment with antibacterial agents alters the normal flora of the colon leading to overgrowth of C. difficile. C. difficile produces toxins A and B which contribute to the development of CDAD. Hypertoxin producing strains of C. difficile cause increased morbidity and mortality, as these infections can be refractory to antimicrobial therapy and may require colectomy. CDAD must be considered in all patients who present with diarrhea following antibiotic use. Careful medical history is necessary since CDAD has been reported to occur over two months after the administration of antibacterial agents. If CDAD is suspected or confirmed, ongoing antibiotic use not directed against C. difficile may need to be discontinued. Appropriate fluid and electrolyte management, protein supplementation, antibiotic treatment of C. difficile and surgical evaluation should be instituted as clinically indicated.
General: As with other broad-spectrum antibiotics, prolonged administration of cefuroxime axetil may result in overgrowth of nonsusceptible microorganisms. If superinfection occurs during therapy, appropriate measures should be taken. 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. Prothrombin time should be monitored in patients at risk and exogenous Vitamin K administered as indicated.
Drug Interactions: Concomitant administration of probenecid with cefuroxime axetil tablets increases the area under the serum concentration versus time curve by 50%. The peak serum cefuroxime concentration after a 1.5 g single dose is greater when taken with 1 g of probenecid (mean=14.8 mcg/mL) than without probenecid (mean=12.2 mcg/mL). Drugs that reduce gastric acidity may result in a lower bioavailability of cefuroxime axetil tablets compared with that of fasting state and tend to cancel the effect of postprandial absorption. In common with other antibiotics, cefuroxime axetil may affect the gut flora, leading to lower estrogen reabsorption and reduced efficacy of combined oral estrogen/progesterone contraceptives.
Carcinogenesis, Mutagenesis, Impairment of Fertility: Although lifetime studies in animals have not been performed to evaluate carcinogenic potential, no mutagenic activity was found for cefuroxime axetil in a battery of bacterial mutation tests. Positive results were obtained in an in vitro chromosome aberration assay; however, negative results were found in an in vivo micronucleus test at doses up to 1.5 g/kg. Reproduction studies in rats at doses up to 1,000 mg/kg/day (9 times the recommended maximum human dose based on mg/m2) have revealed no impairment of fertility.
Patients with Renal Failure: The safety and efficacy of cefuroxime axetil in patients with renal failure have not been established. Since cefuroxime is renally eliminated, its half-life will be prolonged in patients with renal failure.
Use in Pregnancy: See Use in Pregnancy & Lactation section for further information.
Use in Lactation: See Use in Pregnancy & Lactation section for further information.
Use in the Elderly: Tablet: No clinically significant differences in safety or effectiveness were observed between geriatric patients and younger adult subjects in many clinical trials.
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.
Zocef Kids: Special care is indicated in patients who have experienced an allergic reaction to penicillins or other beta-lactams.
As with other antibiotics, use of Cefuroxime (as axetil) may result in the overgrowth of Candida. Prolonged use may also result in the overgrowth of other non-susceptible organisms (e.g. enterococci and Clostridium difficile), which may require interruption of treatment.
Pseudomembranous colitis has been reported with the use of antibiotics, and may range in severity from mild to life-threatening.
Therefore, it is important to consider its diagnosis in patients who develop diarrhoea during or after antibiotic use. If prolonged or significant diarrhoea occurs or the patient experiences abdominal cramps, treatment should be discontinued immediately and the patient investigated further.
The Jarisch-Herxheimer reaction has been seen following Cefuroxime (as axetil) treatment of Lyme disease. It results directly from the bactericidal activity of Cefuroxime (as axetil) on the causative organism of Lyme disease, the spirochaete Borrelia burgdorferi. Patients should be reassured that this is a common and usually self-limiting consequence of antibiotic treatment of Lyme disease.
With a sequential therapy regime the timing of change to oral therapy is determined by severity of the infection, clinical status of the patient and susceptibility of the pathogens involved. If there is no clinical improvement within 72 hours, then the parenteral course of treatment must be continued.
Refer to the relevant prescribing information for cefuroxime sodium before initiating sequential therapy.
Ability to perform tasks that require judgement, motor or cognitive skills: As this medicine may cause dizziness, patients should be warned to be cautious when driving or operating machinery.
Zocef Hospi: 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.

Zocef: Tablet: Pregnancy, Teratogenic Effects: Reproduction studies have been performed in mice at doses up to 3,200 mg/kg/day (14 times the recommended maximum human dose based on mg/m2) and in rats at doses up to 1,000 mg/kg/day (9 times the recommended maximum human dose based on mg/m2) and have revealed no evidence of impaired fertility or harm to the fetus due to cefuroxime axetil. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.
Nursing Mothers: Because cefuroxime is excreted in human milk, consideration should be given to discontinuing nursing temporarily during treatment with cefuroxime axetil.
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.
Zocef Kids: 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 the 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.
Zocef Hospi: 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.

Zocef: Tablet: The following adverse effects have been reported in the use of cefuroxime.
Gastrointestinal: Diarrhea, loose stools, abdominal pain, dyspepsia, flatulence, nausea and vomiting.
Hypersensitivity Reactions: Anaphylactic/anaphylactoid reactions, skin rashes, urticaria, drug fever, pruritus, angioedema and facial edema. There have been rare reports of erythema multiform, Stevens-Johnson syndrome and toxic epidermal necrolysis.
Hepatic: Transient elevations in SGPT, SGOT, LDH.
Renal: Transient elevations in BUN or creatinine, acute renal failure.
Central Nervous System: Headache, Dizziness, Somnolence.
Other: Genital pruritus, vaginitis, candidiasis, muscle cramps, muscle stiffness, muscle spasm of neck, dysuria, chest pain, chills, shortness of breath, mouth ulcers, swollen tongue. Mild to moderate hearing loss has been reported in some children given cefuroxime for the treatment of meningitis.
Suspension: Gastrointestinal Disorders: diarrhea, nausea, vomiting.
Skin and subcutaneous tissue disorders: erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis.
Zocef Kids: Adverse drug reactions to Cefuroxime (as axetil) are generally mild and transient in nature.
Cefuroxime (as axetil) may vary according to the indication.
The following convention has been used for the classification of frequency: very common ≥1/10; common ≥1/100 to <1/10; uncommon ≥1/1000 to <1/100; rare ≥1/10,000 to <1/1000; very rare <1/10,000.
Infections and infestations: Common: Overgrowth of Candida.
Blood and lymphatic system disorders: Common: *Eosinophilia.
Uncommon: *Positive Coombs' test, *thrombocytopenia, *leukopenia (sometimes profound).
Very rare: *Haemolytic anaemia.
Cephalosporins as a class tend to be absorbed onto the surface of red cells membranes and react with antibodies directed against the drug to produce a positive Coombs' test (which can interfere with cross-matching of blood) and very rarely haemolytic anaemia.
Immune system disorders: *Hypersensitivity reactions including: Uncommon: *Skin rashes.
Rare: *Urticaria, *pruritus.
Very rare: *Drug fever, *serum sickness, *anaphylaxis.
Nervous system disorders: Common: *Headache, dizziness.
Gastrointestinal disorders: Common: *Gastrointestinal disturbances including *diarrhoea, *nausea, abdominal pain.
Uncommon: *Vomiting.
Rare: *Pseudomembranous colitis (see Precautions).
Hepatobiliary disorders: Common: *Transient increases of hepatic enzyme levels, [ALT (SGPT), AST (SGOT), LDH].
Very rare: *Jaundice (predominantly cholestatic), *hepatitis.
Skin and subcutaneous tissue disorders: Very rare: *Erythema multiforme, *Stevens-Johnson syndrome, *toxic epidermal necrolysis (exanthematic necrolysis).
Zocef Hospi: 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 11.)

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Paediatric population: The safety profile for cefuroxime sodium in children is consistent with the profile in adults.

Zocef: Suspension: Probenecid reduces the renal clearance of cefuroxime.
Zocef Kids: Drugs which reduce gastric acidity may result in a lower bioavailability of Cefuroxime (as axetil) compared with that of the fasting state and tend to cancel the effect of enhanced post-prandial absorption.
In common with other antibiotics, Cefuroxime (as 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 (as axetil). This antibiotic does not interfere in the alkaline picrate assay for creatinine.
Zocef Hospi: 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).

Direction for Reconstitution: Zocef: 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.
Zocef Kids: Cefuroxime axetil suspension is supplied in a bottle packed in a carton box with either a measuring cup, dosing spoon or syringe and package leaflet.
Always shake the bottle vigorously before taking the medication.
The reconstituted suspension when refrigerated between 2 and 8°C can be kept for up to 10 days.
If desired Cefuroxime axetil suspension can be further diluted from multidose bottles in cold fruit juices, or milk drinks and should be taken immediately.
1. Shake the bottle to loosen the content. All the granules should be free-flowing in the bottle. Remove the cap and the heat-seal membrane. If the latter is damaged or not present, return the product to the pharmacist.
2. Add an amount of cold water up to the volume line on the cup provided. If the water was previously boiled it must be allowed to cool to room temperature before adding. Do not mix Cefuroxime axetil oral suspension with hot or warm liquids. Cold water must be used to prevent the suspension becoming too thick.
3. Pour the total amount of cold water into the bottle. Replace the cap. Allow the bottle to stand to allow the water to fully soak through the granules; this should take about one-minute.
4. Invert the bottle and shake well (for at least 15 seconds) until all the granules have mixed with the water.
5. Turn the bottle into an upright position and shake well for at least one-minute until all the granules have blended with the water.
Zocef Hospi: Instructions for constitution: See Table 12.

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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 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.

Store at temperatures not exceeding 30°C.
Zocef Hospi: 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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