Zinnat

Zinnat

cefuroxime

Manufacturer:

GlaxoSmithKline

Distributor:

Zuellig Pharma
Full Prescribing Info
Contents
Cefuroxime axetil.
Description
Tablet: ZINNAT tablets containing 250 mg of cefuroxime (as cefuroxime axetil).
Oral suspension: ZINNAT Suspension contains granules of cefuroxime axetil for oral suspension.
Reconstitution of multidose bottles as directed yields a suspension containing 125mg or 250mg of cefuroxime (as cefuroxime axetil) in each 5ml.
Excipients/Inactive Ingredients: Tablet: Microcrystalline cellulose, Croscarmellose sodium, Hypromellose, Sodium lauryl sulphate, Hydrogenated vegetable oil, Silicon dioxide, Propylene glycol, Methylhydroxybenzoate (E218), Propylhydroxybenzoate (E216), Titanium dioxide (E171), Sodium benzoate (E211). Oral suspension: Aspartame, Xanthan gum, Acesulfame potassium, Povidone K30, Stearic acid, Sucrose, Tutti frutti flavour, Purified water.
Sucrose quantities: (See Table 1.)

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Action
Pharmacology: Pharmacodynamics: 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 2.)

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Pharmacokinetics: Absorption: After oral administration ZINNAT is slowly absorbed from the gastrointestinal tract and rapidly hydrolysed in the intestinal mucosa and blood to release cefuroxime into the circulation.
Following administration of ZINNAT 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.
Tablet: Optimum absorption occurs when it is administered shortly after a meal.
Oral suspension: Absorption of cefuroxime is enhanced in the presence of food.
The rate of absorption of cefuroxime from the suspension compared with the tablets is reduced, leading to later, lower peak serum levels and reduced systemic bioavailability (4-17% less).
Distribution: Protein binding has been variously stated as 33 to 50% depending on the methodology used.
Metabolism: Cefuroxime is not metabolised.
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 (See Dosage & Administration). 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.
Toxicology: Pre-clinical Safety Data: Animal toxicity studies indicated that cefuroxime is of low toxicity with no significant findings.
Indications/Uses
ZINNAT 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 ZINNAT will vary with geography and time and local susceptibility data should be consulted where available (See Pharmacology: Pharmacodynamics under Actions).
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.
Tablet: Cefuroxime is also available as the sodium salt (ZINACEF) for parenteral administration. This permits the use of sequential therapy with the same antibiotic, when a change from parenteral to oral therapy is clinically indicated.
Where appropriate ZINNAT is effective when used following initial parenteral ZINACEF (cefuroxime sodium) in the treatment of pneumonia and acute exacerbations of chronic bronchitis.
Dosage/Direction for Use
The usual course of therapy is seven days (range 5 to 10 days).
Tablet: ZINNAT should be taken after food for optimum absorption.
Oral suspension: For optimal absorption ZINNAT should be taken with food.
Adults: Tablet: Most infections: 250 mg twice daily.
Urinary tract infections: 250 mg twice daily.
Mild to moderate lower respiratory tract infections e.g. bronchitis: 250 mg twice daily.
More severe lower respiratory tract infections, or if pneumonia is suspected: 500 mg twice daily.
Pyelonephritis: 250 mg twice daily.
Uncomplicated gonorrhoea: Single dose of 1 g.
Sequential therapy: Pneumonia: 1.5 g ZINACEF twice daily (given i.v. or i.m.) for 48 to 72 hours, followed by 500 mg twice daily ZINNAT (cefuroxime axetil) oral therapy for 7 to 10 days.
Acute exacerbations of chronic bronchitis: 750 mg ZINACEF twice daily (given i.v. or i.m.) for 48 to 72 hours, followed by 500 mg twice daily ZINNAT (cefuroxime axetil) oral therapy for 5 to 10 days.
Duration of both parenteral and oral therapy is determined by the severity of the infection and the clinical status of the patient.
Oral suspension: Most infections: 250mg twice daily.
Urinary tract infections: 250mg twice daily.
Mild to moderate lower respiratory tract infections e.g. bronchitis: 250mg twice daily.
More severe lower respiratory tract infections, or if pneumonia is suspected: 500mg twice daily.
Pyelonephritis: 250mg twice daily.
Uncomplicated gonorrhoea: single dose of 1g.
Children: Tablet: See Table 3.

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ZINNAT tablets should not be crushed or split and are therefore unsuitable for treatment of patients, such as younger children, who cannot swallow whole tablets.
There is no experience of using ZINNAT in children under the age of 3 months.
Oral suspension: There are no clinical trial data available on the use of ZINNAT in children under the age of 3 months. 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 10mg/kg twice daily for most infections, to a maximum of 250mg daily. In otitis media or more severe infections the recommended dose is 15mg/kg twice daily to a maximum of 500mg daily.
The following two tables, divided by age group and weight, serve as a guideline for simplified administration from measuring spoons (5ml) for the 125mg/5ml or the 250mg/5ml multi-dose suspension, and 125 mg single dose sachets. (See Table 4 and Table 5.)

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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. (See Tables 6 and Table 7.)

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ZINNAT is also available as the sodium salt (ZINACEF) for parenteral administration. This permits parenteral therapy with ZINNAT 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 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 8).

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Overdosage
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.
Contraindications
Patients with known hypersensitivity to cephalosporin antibiotics.
Special Precautions
Special care is indicated in patients who have experienced an allergic reaction to penicillins or other beta-lactams.
As with other antibiotics, use of ZINNAT 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.
Tablet: 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.
Please refer to the relevant prescribing information for cefuroxime sodium before initiating sequential therapy.
Oral suspension: The sucrose content of ZINNAT suspension and granules (see Excipients/Inactive Ingredients under Description) should be taken into account when treating diabetic patients, and appropriate advice provided.
ZINNAT suspension contains aspartame, which is a source of phenylalanine and so should be used with caution in patients with phenylketonuria.
Effects on Ability to Drive and Use Machines: As this medicine may cause dizziness, patients should be warned to be cautious when driving or operating machinery.
Use In Pregnancy & Lactation
There is no experimental evidence of embryopathic or teratogenic effects attributable to ZINNAT 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 ZINNAT is administered to a nursing mother.
Adverse Reactions
Adverse drug reactions to ZINNAT are generally mild and transient in nature.
The frequency categories assigned to the adverse reactions as follows are estimates, as for most reactions suitable data (for example from placebo-controlled studies) for calculating incidence were not available. In addition the incidence of adverse reactions associated with ZINNAT may vary according to the indication.
Data from large clinical studies were used to determine the frequency of very common to rare undesirable effects. The frequencies assigned to all other undesirable effects (i.e. those occurring at <1/1000) were mainly determined using post-marketing data and refer to a reporting rate rather than true frequency. Placebo-controlled trial data were not available. Where incidences have been calculated from clinical trial data, these were based on drug-related (investigator assessed) data.
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).
See also Immune system disorders as previously mentioned.
Drug Interactions
Drugs which reduce gastric acidity may result in a lower bioavailability of ZINNAT compared with that of the fasting state and tend to cancel the effect of enhanced post-prandial absorption.
In common with other antibiotics, Zinnat 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 ZINNAT. This antibiotic does not interfere in the alkaline picrate assay for creatinine.
Caution For Usage
Instructions for Use and Handling: Tablet: None.
Oral suspension: Constitution/Administration Instructions: 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.
Directions for reconstituting suspension in multidose bottles: 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 damage or not present, return the product to the pharmacist.
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 Zinnat oral suspension with hot or warm liquids. Cold water must be used to prevent the suspension becoming too thick.
Pour the total amount of cold water into the bottle. Replace the cap. Allow the bottle to stand to allow the water to full soak through the granules; this should take about one-minute.
Invert the bottle and shake well (for at least 15 seconds) until all the granules have mixed with the water.
Turn the bottle into an upright position and shake well for at least one-minute until all the granules have blended with the water.
Store the cefuroxime axetil suspension immediately at between 2 and 8°C (do not freeze) and let it rest for at least one hour before taking the first dose. The reconstituted suspension when refrigerated between 2 and 8°C can be kept for up to 10 days.
Always shake the bottle well before taking the medication. A dosing syringe or spoon is provided for the administration of each dose.
If desired, cefuroxime axetil suspension from multidose bottles can be further diluted in cold fruit juices, or cold milk drinks and should be taken immediately after mixing.
Directions for using the dosing syringe:
Remove the bottle cap and insert the syringe-collar assembly into the neck of the bottle. Press it down completely until the collar fits in the neck firmly. Invert the bottle and syringe.
Pull the plunger up the barrel until the barrels rim is aligned with the mark on the plunger corresponding to the required dose.
Turn the bottle and syringe into an upright position. While holding onto the syringe and the plunger to ensure that the plunger does not move, remove the syringe from the bottle, leaving the plastic collar in the bottle neck.
With the patient seated in an upright position, place the tip of the syringe just inside the patients mouth, pointing towards the inside of the cheek.
Press the plunger of the syringe in slowly to expel the medicine without causing choking.
After giving the dose, replace the bottle cap without removing the plastic collar. Dismantle the syringe and wash it thoroughly in water. Allow the plunger and the barrel to dry naturally.
Incompatibilities: None reported.
Storage
Tablet: ZINNAT tablets should be stored at temperatures not exceeding 30°C.
Oral suspension: The reconstituted suspension must be refrigerated immediately at between 2 and 8°C.
Shelf-Life:
The unreconstituted suspension should be stored below 30°C.
The reconstituted suspension when refrigerated between 2 and 8°C can be kept for up to 10 days.
MIMS Class
ATC Classification
J01DC02 - cefuroxime ; Belongs to the class of second-generation cephalosporins. Used in the systemic treatment of infections.
Presentation/Packing
FC tab 250 mg (white, capsule-shaped engraved "GXES7" on one side and plain on the other) x 10's, 50's. Oral susp (dry, white to off-white, tutti-frutti flavoured granules) 125 mg/5 mL x 50 mL. 250 mg/5 mL x 50 mL, 100 mL.
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