Cetirizine Dihydrochloride 10 Mg Film-Coated Tablets
SUMMARY OF PRODUCT CHARACTERISTICS
1 NAME OF THE MEDICINAL PRODUCT
Cetirizine Dihydrochloride 10mg Film-coated Tablets
2 QUALITATIVE AND QUANTITATIVE COMPOSITION
Each film-coated tablet contains 10 mg of Cetirizine Dihydrochloride
Excipients: one film-coated tablet contains 100.2 mg of lactose monohydrate (see section 4.4).
For a full list of excipients, see section 6.1.
3 PHARMACEUTICAL FORM
Film-coated tablet. The diameter of each tablet is 8mm.
White coloured, circular, biconvex film coated tablets, marked with ‘A’ on one side and a breakline score on the other.
The tablet can be divided into equal halves.
4 CLINICAL PARTICULARS
4.1 Therapeutic indications
Cetirizine is indicated for the symptomatic treatment of perennial rhinitis, seasonal allergic rhinitis and chronic idiopathic urticaria.
4.2 Posology and method of administration
Children aged from 6 to 12 years: 10mg once daily (1 tablet).
Adults and children over 12 years of age: 10 mg once daily (1 tablet).
The tablets need to be swallowed with a glass of liquid.
Elderly subjects: At present there is no data to_suggest that the dose needs to be reduced in elderly subjects provided that the renal function is normal.
Patients with renal insufficiency: the dosage should be reduced to half the usual recommended daily dose
Patients with hepatic impairment: no dose adjustment is needed in patients with solely hepatic impairment.
4.3 Contraindications
Hypersensitivity to the active substance, to any of the excipients, to hydroxyzine or to any piperazine derivatives.
Patients with severe renal impairment at less than 10 ml/min creatinine clearance.
Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose- galactose malabsorption should not take cetirizine film-coated tablet.
4.4 Special warnings and precautions for use
The use of the film-coated tablet formulation is not recommended in children aged less than 6 years since this formulation does not allow for appropriate dose adaptation.
Do not exceed the stated dose. If symptoms persist consult your doctor.
4.5 Interaction with other medicinal products and other forms of interaction
To date there have been no known interactions with other drugs. Studies with diazepam and cimetidine revealed no evidence of interactions. As with other antihistamines, it is advisable to avoid excessive alcohol consumption.
At therapeutic doses, no clinically significant interactions have been demonstrated with alcohol (for a blood alcohol level of 0.5 g/L). Nevertheless, precaution is recommended if alcohol is taken concomitantly.
The extent of absorption of cetirizine is not reduced with food, although the rate of absorption is decreased.
4.6 Fertility, pregnancy and lactation
No adverse effects have been reported from animal studies. There has been little or no clinical experience of cetirizine in pregnancy. As with other drugs the use of cetirizine in pregnancy should be avoided. Cetirizine is contraindicated in lactating women as it is excreted in breast milk.
4.7 Effects on ability to drive and use machines
Antihistamines can cause drowsiness in some patients. Although this has not been reported with cetirizine at the recommended dose, please be cautious whilst driving or operating machinery.
4.8 Undesirable effects
Clinical studies have shown that cetirizine at the recommended dosage has minor undesirable effects on the CNS, including somnolence, fatigue, dizziness and headache. In some cases, paradoxical CNS stimulation has been reported.
Although cetirizine is a selective antagonist of peripheral H1-receptors and is relatively free of anticholinergic activity, isolated cases of micturition difficulty, eye accommodation disorders and dry mouth have been reported.
Instances of abnormal hepatic function with elevated hepatic enzymes accompanied by elevated bilirubin have been reported. Mostly this resolves upon discontinuation of the treatment with cetirizine dihydrochloride.
Post-marketing experience
The following adverse drug reactions have been reported from postmarketing experience.
Very common (>1/10); common (>1/100 to <1/10); uncommon (>1/1,000 to <1/100); rare (>1/10,000 to <1,000); very rare (<1/10,000), not known, cannot be estimated from available data.
Blood and lymphatic disorders:
Very rare: thrombocytopenia
Immune system disorders:
Rare: hypersensitivity Very rare: anaphylactic shock
Psychiatric disorders:
Uncommon: agitation
Rare: aggression, confusion, depression, hallucination, insomnia Very rare: tic
Nervous system disorders:
Uncommon: paraesthesia
Rare: convulsions, movements disorders
Very rare: dysgeusia, syncope, tremor, dystonia, dyskinesia
Eye disorders:
Very rare: accommodation disorder, blurred vision, oculogyration
Cardiac disorders:
Rare: tachycardia
Gastro-intestinal disorders:
Uncommon: diarrhoea
Hepatobiliary disorders:
Rare: abnormal hepatic function (increased transaminases, alkaline phosphatase, y-GT and bilirubin)
Skin and subcutaneous tissue disorders:
Uncommon: pruritus, rash Rare: urticaria
Very rare: angioneurotic oedema, fixed drug eruption, erythema multiforme
Renal and urinary disorders:
Very rare: dysuria, enuresis, micturition difficulties
General disorders and administration site conditions:
Uncommon: asthenia, malaise
Rare: oedema Investigations:
Rare: weight increased
4.9 Overdose
Symptoms
Symptoms observed after an overdose of cetirizine are mainly associated with CNS effects or with effects that could suggest an anticholinergic effect. Adverse events reported after an intake of at least 5 times the recommended daily dose are: confusion, diarrhoea, dizziness, fatigue, headache, malaise, mydriasis, pruritus, restlessness, sedation, somnolence, stupor, tachycardia, tremor, and urinary retention.
Management
There is no known specific antidote to cetirizine.
Should overdose occur, symptomatic or supportive treatment is recommended. The patient should be kept under clinical observation for at least 4 hours after ingestion, and his blood pressure, heart rate and vital signs monitored until stable. In symptomatic cases ECG should be performed. The benefit of gastric lavage is uncertain. Oral activated charcoal (50g for an adult, 10-15g for a child) should be considered if more than 2.5mg/kg cetirizine has been ingested within 1 hour. Cetirizine is not effectively removed by dialysis.
5 PHARMACOLOGICAL PROPERTIES
5.1 Pharmacodynamic properties
Pharmacotherapeutic group: Piperazine derivatives, ATC code: R06A E07
Cetirizine is a potent antihistamine with a low potential for drowsiness at normal therapeutic doses which has additional anti-allergic properties. It is a selective H1 antagonist with negligible effects on other receptors and so is virtually free from anti-cholinergic and anti-serotonin effects. Cetirizine inhibits the histamine-mediated early phase of the allergic-reaction and also reduces the migration of certain inflammatory cells and the release of certain mediators associated with the late allergic response.
5.2 Pharmacokinetic properties
Peak blood levels of the order of 0.3micrograms/ml are reached between 30 and 60 minutes after oral administration of a 10mg dose of cetirizine. The terminal half-life is approximately ten hours in adults, approximately six hours in children aged between 6 to12 years and approximately 5 hours in children 2-6years.
This is consistent with the urinary excretion half life of the drug. The cumulative urinary excretion represents about two thirds of the administered dose for both adults and children.
The apparent plasma clearance in children is higher than that measured in adults. A high proportion of cetirizine is bound to human plasma proteins.
5.3 Preclinical safety data
Non-clinical data reveal no special hazard for humans based on conventional studies of safety pharmacology, repeated dose toxicity, genotoxicity, carcinogenic potential, toxicity to reproduction.
6.1 List of excipients
Microcrystalline Cellulose Lactose monohydrate Colloidal anhydrous silica Maize Starch Purified Talc Magnesium Stearate
Film Coating:
- Hypromellose 15cP
- Lactose monohydrate
- Titanium dioxide
- Macrogol 4000
- Sodium citrate
6.2 Incompatibilities
Not applicable.
6.3 Shelf life
3 years
6.4 Special precautions for storage
This medicinal product does not require any special temperature storage conditions. Keep the blister in the outer carton in order to protect from light.
6.5 Nature and contents of container
Aluminium/PVC clear blister strips, containing 4, 5, 7 or 14 tablets.
Not all pack sizes may be marketed.
6.6 Special precautions for disposal
No special requirements.
Any unused product or waste material should be disposed of in accordance with local requirements.
7 MARKETING AUTHORISATION HOLDER
APTIL Pharma Limited
9th Floor, CP House 97 - 107 Uxbridge Road Ealing, London W5 5TL
8 MARKETING AUTHORISATION NUMBER(S)
PL 40378/0141
9 DATE OF FIRST AUTHORISATION/RENEWAL OF THE AUTHORISATION
05/11/2012
10 DATE OF REVISION OF THE TEXT
05/11/2012