Cetirizine Hydrochloride 10mg Tablets

1. Name Of The Medicinal Product

Cetirizine Hydrochloride 10mg Tablets.

2. Qualitative And Quantitative Composition

Each film-coated tablet contains 10mg of Cetirizine Hydrochloride.

Excipient: 91 mg lactose /film-coated tablet.

For a full list of excipients, see section 6.1.

3. Pharmaceutical Form

Film-coated Tablet.

White, capsule shaped, biconvex film coated tablets with score line on one side and 'C' and 'L' imprints on either side of score line, other side being plain.

4. Clinical Particulars

4.1 Therapeutic Indications

Adults and adolescents over 12 years of age:

Symptomatic treatment of allergic rhinitis (seasonal and perennial), associated allergic conjunctivitis, and chronic idiopathic urticaria.

Children 6-12 years:

Symptomatic treatment of allergic rhinitis (seasonal and perennial), and chronic idiopathic urticaria.

4.2 Posology And Method Of Administration

Adults and adolescents over 12 years of age: One tablet daily.

If drowsiness occurs, the tablet can be administered in the evening.

Children 6-12 years old, weighing 30 kg and more:

One tablet daily or 5 mg (½ tablet) taken twice daily (morning and evening).

Childern 6-12 years old, weighing less than 30 kg:

5 mg (½ tablet) taken once daily.

Children 2-5 years:

Cetirizine hydrochloride 10 mg Tablets are not recommended for use in children of 2 to 5 years of age; other oral pharmaceutical forms of cetirizine hydrochloride should be used in this age group.

In patients with moderate renal impairment the dose should be adjusted to 5 mg (1/2 a tablet a day). Caution should be exercised in patients with mild to moderate renal impairment or impaired liver function (see section 4.4).

There is no evidence that the dose needs to be modified for healthy elderly patients.

The duration of the treatment may vary depending on the symptoms. For the treatment seasonal allergic rhinitis treatment should be according to disease history and should be stopped once symptoms have resolved. For the treatment with cetirizine dihydrochloride in chronic urticaria or chronic allergic rhinitis there is up to one year's clinical experience. Clinical trials in children have not exceeded four weeks.

Method of administration

This tablet is for oral use.

4.3 Contraindications

Hypersensitivity to cetirizine hydrochloride or to any of the excipients.

Patients with severe renal impairment.

4.4 Special Warnings And Precautions For Use

In some patients, long term treatment with cetirizine hydrochloride tablets may lead to an increased risk of caries due to mouth dryness. The patients should therefore be informed about the importance of oral hygiene.

At impaired hepatic function and renal function, the elimination of cetirizine hydrochloride may be impaired. Caution should be exercised when administering cetirizine hydrochloride to these patients. (see sections 4.2 and 4.3).

Cetirizine hydrochloride may potentiate the effects of alcohol. Therefore caution is recommended at concomitant use of alcohol.

Caution is recommended with concomitant use of CNS depressants.

Cetirizine hydrochloride contains lactose. It should not be administered to patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption.

4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction

Allergy testing: Use of cetirizine hydrochloride must be discontinued three days before allergy tests.

Cetirizine hydrochloride may potentiate the effects of alcohol. Therefore caution is recommended at concomitant use of alcohol. Caution is recommended during concomitant use of CNS depressants.

4.6 Pregnancy And Lactation

Data on a limited number of exposed pregnancies indicate no adverse effects of cetirizine hydrochloride on pregnancy or on health of foetus/new born child. To date no other relevant epidemiological data are available.

Animal studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/foetal development, parturition or post natal development (see section 5.3). Caution should be exercised when prescribing to pregnant women.

Breast-feeding

Cetirizine has been reported to be excreted in human milk. Cetirizine hydrochloride should be avoided during lactation.

4.7 Effects On Ability To Drive And Use Machines

Cetirizine hydrochloride may have minor or moderate influence on the patient's ability to react.

This should be considered when extra alertness is required e.g. when driving. Cetirizine hydrochloride may potentiate the effects of alcohol and CNS depressants.

4.8 Undesirable Effects

Very common (

Blood and lymphatic system disorders

Very rare: thrombocytopenia

Immune system disorders

Rare: hypersensitivity

Very rare: anaphylactic shock

Psychiatric disorders

Uncommon: agitation

Rare: aggression, confusion, depression, hallucination, insomnia

Nervous system disorders

Common: headache, somnolence

Uncommon: dizziness, paraesthesia

Rare: convulsions

Very rare: syncope, dysgeusia

Eye disorders

Very rare: accommodation disorder, blurred vision, oculogyric crisis, especially in children

Cardiac disorders

Rare: tachycardia, palpitations

Respiratory, thoracic and mediastinal disorders

Uncommon: pharyngitis, rhinitis (in children)

Gastrointestinal disorders

Common: dry mouth

Uncommon: abdominal complaints such as abdominal pains, nausea, diarrhoea, digestive disorders

Hepatobiliary disorders

Rare: abnormal hepatic function (increased transaminases, alkaline, phosphatase, gamma-GT and bilirubin)

Very rare: hepatitis

Skin and subcutaneous tissue disorders

Uncommon: rash, pruritus

Rare: urticaria

Very rare: angioneurotic oedema, erythema multiforme

Renal and urinary disorders

Very rare: dysuria, enuresis, micturition difficulties

General disorders and administration site conditions

Common: fatigue

Uncommon: asthenia, malaise

Rare: oedema

Investigations

Rare: weight increase

4.9 Overdose

Toxicity: Limited experience of overdosing. 20 mg to a 2 year old, 30 mg to a 3 year old and 40 mg to an 11 year old did not give any symptoms. 60 mg to a 4 year old gave mild intoxication, 400 mg to a 14 year old gave mild symptoms while 400-500 mg to an adult gave no symptoms at all.

Symptoms of overdosage reported with antihistamine substances: Somnolence, unconsciousness and/or excitation (principally in children). Ataxia, tremor, headache, hallucinations, seizures, dry mouth, flush, hyperthermia, mydriasis, urine retention tachycardia and in the case of massive doses, possible fall in blood pressure and arrhythmias. Nausea and vomiting. Also extrapyramidal symptoms are possible. Cetirizine hydrochloride has a low sedative and anticholinergic effect. Sedation can be a symptom of overdose, it can occur after a single dose of less than 50 mg.

Treatment: At the present time there is no specific antidote. Experience of overdosing is limited and no severe intoxication has been reported to date. Primary treatment should be gastric lavage, if justified and charcoal. Symptomatic treatment should be instituted in the case of acute intoxication, such as diazepam for seizures or acute dystonias.

5. Pharmacological Properties

5.1 Pharmacodynamic Properties

Pharmacotherapeutic group: Antihistamines for systemic use. Piperazine derivatives.

ATC code: R06AE07

Cetirizine hydrochloride is a racemate and an anti-allergic with specific histamine H1-receptor blocking characteristics.

Cetirizine hydrochloride inhibits cutaneous reactions in allergic individuals by VIP (Vasoactive Intestinal Polypeptide) and the P substance, neuropeptides that are considered involved in the allergic reaction. Effect is reached within 2 hours with a maximum effect after 4 hours, and remains for at least 24 hours. In allergic individuals, cetirizine hydrochloride inhibits the recruitment of eosinophils after stimulation with allergens and unselective histamine liberators, by a mechanism that is not primarily explained by the H1-receptor blocking characteristics of the pharmaceutical.

5.2 Pharmacokinetic Properties

Cetirizine hydrochloride is absorbed with small inter-individual variations. Cetirizine hydrochloride has not been given intravenously, therefore the bioavailability, clearance and distribution volume (Vd) are unknown. Maximum plasma concentration is achieved within 1 hour and the terminal half-life is about 10 hours in adults and 6 hours in children between the age of 6-12 years. The grade of protein binding in plasma is about 93%. Cetirizine is metabolised to a small extent with a known inactive main metabolite. Cetirizine is eliminated to 60% in unchanged form via the kidneys within 96 hours. At repeated administration there is no accumulation at hand, nor is the absorption or elimination affected. At impaired kidney function, the elimination is slower and the half-life is prolonged. Elimination will also be decreased in cases of hepatic impairment.

There is no evidence that the pharmacokinetics of cetirizine hydrochloride is altered in elderly patients unless renal or hepatic function is reduced.

5.3 Preclinical Safety Data

Preclinical data reveal no special hazard for humans based on conventional studies of safety pharmacology, repeated dose toxicity, toxicity to reproduction, genotoxicity or carcinogenicity.

6. Pharmaceutical Particulars

6.1 List Of Excipients

Tablet core:

Lactose monohydrate

Maize starch

Povidone K30

Magnesium stearate

Film-coat:

Hypromellose

Titanium Dioxide (E171)

Macrogol 400

6.2 Incompatibilities

Not applicable.

6.3 Shelf Life

2 years.

6.4 Special Precautions For Storage

Do not store above 25ºC. Store in the original package.

6.5 Nature And Contents Of Container

PVC/Aluminium blister

Pack size 7, 10, 14, 20, 30, 40, 50, 60, 80, 100 and 100x1 (unit dose).

Not all pack sizes may be marketed.

6.6 Special Precautions For Disposal And Other Handling

No special requirements.

7. Marketing Authorisation Holder

Sandoz Limited

Woolmer Way

Bordon

Hampshire, GU35 9QE

8. Marketing Authorisation Number(S)

PL 04416/0381

9. Date Of First Authorisation/Renewal Of The Authorisation

30 April 2002

28 April 2008

10. Date Of Revision Of The Text

13 February 2009