1. Name Of The Medicinal Product
ZADITEN® ELIXIR 1mg/5ml
2. Qualitative And Quantitative Composition
Ketotifen hydrogen fumarate 1.38mg/5ml
3. Pharmaceutical Form
Clear, colourless, strawberry flavoured elixir.
4. Clinical Particulars
4.1 Therapeutic Indications
Prophylactic treatment of bronchial asthma.
Symptomatic treatment of allergic conditions including rhinitis and conjunctivitis.
4.2 Posology And Method Of Administration
Adults
1mg twice daily with food. If necessary the dose may be increased to 2mg twice daily.
Children
(From 2 years of age): 1mg twice daily with food.
Use in the elderly
No evidence exists that elderly patients require different dosages or show different side-effects from younger patients.
Patients known to be easily sedated should be given 0.5-1mg at night for the first few days.
4.3 Contraindications
Hypersensitivity to ketotifen or any of the excipients. A reversible fall in the thrombocyte count in patients receiving ZADITEN concomitantly with oral anti-diabetic agents has been observed in a few cases. This combination of drugs should therefore be avoided until this phenomenon has been satisfactorily explained.
4.4 Special Warnings And Precautions For Use
Post-marketing surveillance has shown exacerbation of asthma in approximately 2 per 1000 patients. Since some of these asthmatic attacks might have been related to stopping existing treatment it is important to continue such treatment for a minimum of 2 weeks after starting ZADITEN. This applies especially to systemic corticosteroids and ACTH because of the possible existence of adrenocortical insufficiency in steroid dependent patients: in such cases recovery of a normal pituitary-adrenal response to stress may take up to one year. If it is necessary to withdraw ZADITEN this should be done progressively over a period of 2 to 4 weeks. Symptoms of asthma may recur. If intercurrent infection occurs, ZADITEN treatment must be supplemented by specific antimicrobial therapy.
4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction
ZADITEN may potentiate the effects of sedatives, hypnotics, antihistamines and alcohol. Patients should be warned not to take charge of vehicles or machinery until the effect of ZADITEN treatment on the individual is known.
4.6 Pregnancy And Lactation
Although there is no evidence of any teratogenic effect, recommendation for ZADITEN in pregnancy cannot be given. Ketotifen is excreted in breast milk, therefore mothers receiving ZADITEN should not breast feed.
4.7 Effects On Ability To Drive And Use Machines
During the first few days of treatment with ZADITEN reactions may be impaired. Patients should be warned not to take charge of vehicles or machinery until the effect of ZADITEN treatment on the individual is known. Patients should be advised to avoid alcoholic drinks.
4.8 Undesirable Effects
Drowsiness and, in isolated cases, dry mouth and slight dizziness may occur at the beginning of treatment, but usually disappear spontaneously after a few days. Occasionally symptoms of CNS stimulation have been observed. Weight gain has been reported.
Cystitis has been rarely described in association with ZADITEN. Isolated cases of severe skin reactions (erythema multiforme, Stevens-Johnson syndrome) have been reported.
4.9 Overdose
The reported features of overdose include confusion, drowsiness, nystagmus, headache, disorientation, tachycardia, hypotension, reversible coma; especially in children, hyperexcitability or convulsions. Bradycardia and respiratory depression should be watched for. Elimination of the drug with gastric lavage or emesis is recommended. Otherwise, general supportive treatment is all that is required.
5. Pharmacological Properties
5.1 Pharmacodynamic Properties
ZADITEN is a non-bronchodilator anti-asthmatic drug which inhibits the effect of certain endogenous substances known to be inflammatory mediators, and thereby exerts anti-allergic activity.
Laboratory experiments indicate that this anti-asthmatic activity may be due to the inhibition of release of allergic mediators such as histamine and leukotrienes and the inhibition of the development of airway hyperactivity associated with activation of platelets by PAF (platelet activating factor) or caused by neural activation following the use of sympathomimetic drugs or the exposure to allergen. In addition, ZADITEN exerts a non-competitive blocking effect on histamine (H1) receptors.
Experimental investigations in asthmatic subjects have shown that ZADITEN is as effective orally as a selective mast cell stabiliser administered by inhalation: antihistamines are ineffective in these tests. The effectiveness of ZADITEN in the prevention of bronchial asthma has been studied in long-term clinical trials. Asthma attacks were reduced in number, severity and duration and in some cases the patients were completely freed from attacks. Progressive reduction of corticosteroids and/or bronchodilators was also possible.
The prophylactic activity of ZADITEN may take several weeks to become fully established.
ZADITEN will not abort established attacks of asthma.
5.2 Pharmacokinetic Properties
After oral administration the absorption of ZADITEN is nearly complete. Bioavailability amounts to approximately 50% due to a first pass effect of about 50% in the liver. Maximal plasma concentrations are reached within 2-4 hours. Protein binding is 75%. Ketotifen is eliminated biphasically with a short half-life of 3-5 hours and a longer one of 21 hours. In urine about 1% of the substance is excreted unchanged within 48 hours and 60-70% as metabolites. The main metabolite in the urine is the practically inactive ketotifen-N-glucuronide.
5.3 Preclinical Safety Data
Not stated.
6. Pharmaceutical Particulars
6.1 List Of Excipients
Strawberry flavour, propyl hydroxybenzoate, methyl hydroxybenzoate, citric acid anhydrous, disodium phosphate anhydrous, ethyl alcohol 96% w/w, maltitol liquid (grade 80/55) and purified water.
6.2 Incompatibilities
Not applicable.
6.3 Shelf Life
36 months
6.4 Special Precautions For Storage
Store below 25oC
6.5 Nature And Contents Of Container
Amber glass bottle with a child resistant, tamper evident closure, composed of a polypropylene or polyethylene outer, a polypropylene or polyethylene inner, with a wad faced with PP, PVDC or PET lining. Bottle size 300ml.
6.6 Special Precautions For Disposal And Other Handling
None
7. Marketing Authorisation Holder
NOVARTIS PHARMACEUTICALS UK LIMITED
Trading as Sandoz Pharmaceuticals
Frimley Business Park
Frimley
Camberley
Surrey
GU16 7SR
8. Marketing Authorisation Number(S)
PL 0101/0137
9. Date Of First Authorisation/Renewal Of The Authorisation
Date Present Licence Granted: 18 April 1997
Date of Expiry: 18 April 2002
10. Date Of Revision Of The Text
August 2000
Legal Category : POM
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