Zinnat

Zinnat

cefuroxime

Manufacturer:

GlaxoSmithKline

Distributor:

Zuellig Pharma
Full Prescribing Info
Contents
Cefuroxime axetil.
Description
Zinnat also contains the following excipients: Tablet: Microcrystalline cellulose, croscarmellose sodium, hypromellose, sodium lauryl sulphate, hydrogenated vegetable oil, silicon dioxide, propylene glycol, methylhydroxybenzoate, propylhydroxybenzoate, titanium dioxide, sodium benzoate.
Suspension: Aspartame, xanthan gum, acesulfame potassium, povidone K30, stearic acid, sucrose, tutti frutti flavour.
Action
Cefuroxime axetil is an oral prodrug of the bactericidal cephalosporin antibiotic cefuroxime, which is resistant to most β-lactamases and is active against a wide range of gram-positive and gram-negative organisms.
Microbiology: Cefuroxime axetil owes its in vivo bactericidal activity to the parent compound cefuroxime.
Cefuroxime is a well-characterised and effective antibacterial agent which has bactericidal activity against a wide range of common pathogens, including β-lactamase-producing strains.
Cefuroxime has good stability to bacterial β-lactamase, and consequently is active against many ampicillin-resistant or amoxycillin-resistant strains.
The bactericidal action of cefuroxime results from inhibition of cell wall synthesis by binding to essential target proteins.
Microbiology: Cefuroxime is usually active against the following organisms in vitro:
Gram-Negative Aerobes: Haemophilus influenzae (including ampicillin-resistant strains); Haemophilus parainfluenzae; Moraxella (Branhamella) catarrhalis; Neisseria gonorrhoeae (including penicillinase and non-penicillinase producing strains); Escherichia coli; Klebsiella sp; Proteus mirabilis; Providencia sp; Proteus rettgeri.
Gram-Positive Aerobes: Staphylococcus aureus and Staphylococcus epidermidis (including penicillinase-producing strains but excluding methicillin-resistant strains); Streptococcus pyogenes (and other β-haemolytic streptococci); Streptococcus pneumoniae; Streptococcus Group B (Streptococcus agalactiae).
Anaerobes: Gram-positive and gram-negative cocci (including Peptococcus and Peptostreptococcus sp); gram-positive bacilli (including Clostridium sp) and gram-negative bacilli (including Bacteroides and Fusobacterium sp); Propionibacterium sp.
Other Organisms: Borrelia burgdorferi.
The following organisms are not susceptible to cefuroxime: Clostridium difficile; Pseudomonas and Campylobacter sp; Acinetobacter calcoaceticus; Listeria monocytogenes; methicillin-resistant strains of Staphylococcus aureus and Staphylococcus epidermidis; Legionella sp.
Some strains of the following genera are not susceptible to cefuroxime: Enterococcus (Streptococcus) faecalis; Morganella morganii; Proteus vulgaris; Enterobacter sp, Citrobacter sp and Serratia sp; Bacteroides fragilis.
Pharmacokinetics: After oral administration, cefuroxime 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 axetil tablets, peak serum levels (2.9 mg/L for a 125-mg dose, 4.4 mg/L for a 250-mg dose, 7.7 mg/L for a 500-mg dose and 13.6 mg/L for a 1-g dose) occur approximately 2.4 hrs after dosing when taken with food.
Peak serum levels (2-3 mg/L for a 125-mg dose, 4-6 mg/L for a 250-mg dose, 5-8 mg/L for a 500-mg dose and 9-14 mg/L for a 1-g dose) occur approximately 2-3 hrs after dosing when taken after food, unlike IV dosing which peaks immediately.
The 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).
The serum half-life is between 1 and 1.5 hrs. Protein-binding has been variously stated as 33-50% depending on the methodology used.
Cefuroxime is not metabolised and is excreted by glomerular filtration and tubular secretion. Concurrent administration of probenecid increases the area under the mean serum concentrations time curve by 50%.
Serum levels of cefuroxime are reduced by dialysis.
Toxicology: Preclinical Safety Data: Animal toxicity studies indicated that cefuroxime axetil is of low toxicity with no significant findings.
Indications/Uses
Treatment of infections caused by susceptible bacteria.
Upper Respiratory Tract Infections: Ear, nose and throat infections eg, otitis media, sinusitis, tonsillitis and pharyngitis.
Lower Respiratory Tract Infections: Pneumonia, acute bronchitis and acute exacerbations of chronic bronchitis.
Genitourinary Tract Infections: Pyelonephritis, cystitis and urethritis.
Skin and Soft Tissue Infections: 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 >12 years.
Where appropriate Zinnat tablet 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 7 days (range 5-10 days).
For optimal absorption, cefuroxime axetil should be taken with food.
Adults: Most Infections: 250 mg twice daily.
Urinary Tract Infections: 125 mg twice daily.
Mild to Moderate Lower Respiratory Tract Infections (eg, 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.
Lyme Disease: Adults and Children >12 years: 500 mg twice daily for 20 days.
Sequential Therapy: Pneumonia: 1.5 g Zinacef (cefuroxime sodium) 3 or 2 times daily (IV or IM) for 48-72 hrs, followed by 500 mg twice daily Zinnat (cefuroxime axetil) oral therapy for 7-10 days.
Acute Exacerbations of Chronic Bronchitis: 750 mg Zinacef (cefuroxime sodium) 3 or 2 times daily (IV or IM) for 48-72 hrs, followed by 500 mg twice daily Zinnat (cefuroxime axetil) oral therapy for 5-10 days.
Duration of both parenteral and oral therapy is determined by the severity of the infection and the clinical status of the patient.
Children: Most Infections: Recommended Dose: 10 mg/kg twice daily up to maximum dose of 250 mg/day. In children ≥2 years with otitis media or where appropriate, with more severe infections, the dose is 250 mg twice daily or 15 mg/kg twice daily, up to a maximum dose of 500 mg/day.
Zinnat tablets should not be crushed and are therefore unsuitable for treatment of patients eg, younger children, who cannot swallow tablets. In children, Zinnat oral suspension may be used.
There is no clinical trial data available on the use of Zinnat in children <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 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.
Tables 1 and 2, divided by age group and weight, serve as a guideline for simplified administration from measuring spoons (5 mL).
10 mg/kg Dosage for Most Infections: See Table 1.

Click on icon to see table/diagram/image

15 mg/kg Dosage for Otitis Media and More Serious Infections: See Table 2.

Click on icon to see table/diagram/image

Cefuroxime 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.
Administration: Suspension: 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, Zinnat suspension can be further diluted from multidose bottles in cold fruit juices or milk drinks and should be taken immediately.
The reconstituted suspension or granules should not be mixed with hot liquids.
Directions for Reconstituting Suspension in Multidose Bottles: Shake the bottle to loosen the granules. Remove the cap and the heat seal membrane. If the latter is damaged or not present, the product should be returned to the pharmacist.
Add the total amount of water to the bottle as stated on its label. Replace the cap.
Invert the bottle and rock vigorously (for at least 15 sec).
Turn the bottle into an upright position and shake vigorously.
If using a dosing syringe, allow the reconstituted suspension to stand for at least 1 hr before taking the first dose.
Overdosage
Overdosage of cephalosporins can cause cerebral irritation leading to convulsions. 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 penicillin or other β-lactams.
As with other antibiotics, use of Zinnat may result in the overgrowth of Candida. Prolonged use may also result in the overgrowth of nonsusceptible organisms (eg, Enterococci, Clostridium difficile), which may require interruption of treatment.
Pseudomembranous colitis has been reported with the use of broad-spectrum antibiotics, therefore, it is important to consider its diagnosis in patients who develop serious diarrhoea during or after antibiotic use.
The Jarisch-Herxheimer reaction has been seen following Zinnat treatment of Lyme disease. It results directly from the bactericidal activity of Zinnat 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.
The sucrose content of Zinnat suspension and granules 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.
With a sequential therapy regimen, 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 hrs, then the parenteral course of treatment must be continued.
Refer to the relevant prescribing information for cefuroxime sodium before initiating sequential therapy.
Effects on the Ability to Drive or Operate Machinery: As Zinnat 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 reactions to cefuroxime axetil are generally mild and transient in nature.
The frequency categories assigned to the following adverse reactions are estimates, as for most reactions suitable data (eg, from placebo-controlled studies) for calculating incidence were not available. In addition, the incidence of adverse reactions associated with cefuroxime axetil 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 (ie, those occurring at <1/10,000) 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 and <1/10; uncommon ≥1/1000 and <1/100; rare ≥1/10,000 and <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.
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.
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 absorption after food.
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.
Storage
Tablet: Store at temperatures not exceeding 30°C.
Suspension: Store below 30°C. The reconstituted suspension must be refrigerated immediately between 2°C and 8°C which 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
Tab 250 mg (white to off-white, film-coated, capsule-shaped, engraved with 'GX ES7' on one side and plain on the other) x 10's. 500 mg (white to off-white, film-coated, capsule-shaped, engraved with 'GX EG2' on one side and plain on the other) x 10's. Susp (white to off-white) 125 mg/5 mL x 50 mL. 250 mg/5 mL x 50 mL.
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