ZYRTEC ORAL DROPS 10 mg/ml ZYRTEC ORAL SOLUTION 1 …

ZYRTEC?

SCHEDULING STATUS: S2

PROPRIETARY NAME AND DOSAGE FORM: ZYRTEC? tablets ZYRTEC? ORAL DROPS 10 mg/ml ZYRTEC? ORAL SOLUTION 1 mg/ml

COMPOSITION: Each film-coated tablet contains 10 mg cetirizine dihydrochloride. Excipients: Tablet core: microcrystalline cellulose, colloidal anhydrous silica, lactose monohydrate and magnesium stearate. Tablet coating: Opadry Y-1-7 000 (hypromellose, titanium dioxide and polyethylene glycol.

Each 1 ml oral drops contains 10 mg cetirizine dihydrochloride. Excipients: glycerol, propylene glycol, saccharin sodium, sodium acetate, glacial acetic acid, purified water and methyl parahydroxybenzoate 0,135 % m/v and propyl parahydroxybenzoate 0,015 % m/v as preservatives.

Each 1 ml oral solution contains 1 mg cetirizine dihydrochloride. Excipients: sorbitol solution 70 %, glycerol, propylene glycol, saccharin sodium, sodium acetate, glacial acetic acid, purified water, banana flavour and methyl parahydroxybenzoate 0,135 % m/v and propyl parahydroxybenzoate 0,015 % m/v as preservatives. The oral drops and oral solution do not contain sucrose or alcohol.

PHARMACOLOGICAL CLASSIFICATION: A 5.7.1 Antihistaminics

PHARMACOLOGICAL ACTION: Cetirizine dihydrochloride, a metabolite of hydroxyzine, is an anti-allergic agent, with a histamine H1 receptor antagonism devoid of any significant anticholinergic and antiserotonin effects as demonstrated in experimental and clinical pharmacology. At the present stage of research into the mode of action of cetirizine, the anti-allergic activity seems to be exerted mainly via its effects on the release of certain mediators, such as histamine, together with a selective action on the H1 receptors. Cetirizine reduces eosinophil recruitment induced by an antigen-antibody reaction.

Pharmacokinetic properties: Peak blood levels of 300 ng/ml are reached within one hour after oral administration of cetirizine. Cetirizine does not undergo extensive first pass metabolism. The terminal half-life is approximately 10 hours in adults, 6 hours in children aged 6 to 12 years and 5 hours in children aged 2 to 6 years. These data are consistent with the urinary excretion half-life of the medicine. The cumulative urinary excretion represents about two thirds of the dose given in both adults and children. The apparent plasma clearance in children is higher than that measured in adults. Plasma levels are linearly related to the dosage given. A high proportion of cetirizine is bound to human plasma proteins. In patients with impaired renal clearance (less than 40 ml/min) and hepatic insufficiency, an increase in half-life and decrease in total clearance occurs.

INDICATIONS: Allergic processes responding to a histamine H1 receptor antagonist. ? Respiratory: Allergic rhinitis, hay fever. ? Cutaneous: Allergic skin conditions associated with pruritus e.g. urticaria.

CONTRA-INDICATIONS:

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? History of hypersensitivity to any of the constituents of the formulations, to hydroxyzine or to any piperazine derivatives.

? Patient with severe renal impairment at less than 30 ml/min creatinine clearance. ? Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or

glucose- galactose malabsorption should not take ZYRTEC tablets. ? Patients with rare hereditary problems of fructose intolerance should not take ZYRTEC oral

solution 1 mg/ml. ? ZYRTEC is contra-indicated in lactating women since the active ingredient is excreted in breast

milk. ? ZYRTEC is contra-indicated in pregnancy as the safety has not been established. ? In children under 2 years of age. ? The use of ZYRTEC tablets is not recommended in children less than 6 years since this

formulation does not allow for appropriate dose adaptation. It is recommended to use a paediatric formulation of ZYRTEC.

WARNINGS: Avoid alcohol consumption. Caution in epileptic patients and patients at risk of convulsions is recommended.

INTERACTIONS: To date there are no known interactions between cetirizine with other medicines. Studies with diazepam, glipizide, pseudoephedrine, antipyrine, ketoconazole, azithromycin, erythromycin and cimetidine have revealed no evidence of pharmacokinetic interactions. Allergy skin tests are inhibited by antihistamines such as ZYRTEC and a wash-out period of 3 days is recommended before performing them.

PREGNANCY AND LACTATION: ZYRTEC is contra-indicated in pregnancy and lactation (refer to CONTRA-INDICATIONS).

DOSAGE AND DIRECTIONS FOR USE: Tablets: Adults or children 12 years of age or older: one 10 mg tablet daily. Children 6 to 12 years old: 10 mg (one tablet) once daily or 5 mg (half a tablet) twice daily.

Oral drops: Adults or children 12 years of age or older: 10 mg (20 drops) once daily. Children 6 to 12 years old: 10 mg (20 drops) daily, either as a single dose or as divided doses of 10 drops in the morning and 10 drops in the evening. Children 2 to 6 years old: 5 mg (10 drops) daily, either as a single dose or as divided doses of 5 drops in the morning and 5 drops in the evening.

Oral solution: Adults or children 12 years of age or older: 10 mg (10 ml) once daily. Children 6 to 12 years old: 10 mg (10 ml) daily, either as a single dose or as divided doses of 5 ml in the morning and 5 ml in the evening. Children 2 to 6 years old: 5 mg (5 ml) daily, either as a single dose or as divided doses of 2,5 ml in the morning and 2,5 ml in the evening. At present there are no data to suggest that the dose needs to be reduced in elderly patients with normal renal function. In patients with renal insufficiency (creatinine clearance less than 40 ml/min), the dosage should be reduced to half the usual recommended dose. Half the recommended daily dose should be used in patients with moderate to severe hepatic impairment.

SIDE EFFECTS AND SPECIAL PRECAUTIONS: Side effects: ZYRTEC has potential adverse effects on the CNS, including somnolence, fatigue, dizziness and headache. In some cases, paradoxical CNS stimulation has been reported.

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ZYRTEC is a selective antagonist of peripheral H1-receptors and is relatively free of anticholinergic activity. Nevertheless, 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.

Clinical trial data: Double blind controlled clinical trials at the recommended dosage (10 mg daily for ZYRTEC), of which quantified safety data are available, included more than 3 200 subjects exposed to ZYRTEC. Frequencies are defined as follows: Very common ( 1/10); common ( 1/100 to < 1/10); uncommon ( 1/1 000 to < 1/100); rare ( 1/10 000 to < 1/1 000); very rare (< 1/10 000), not known (cannot be estimated from the available data). The following adverse reactions were reported: Psychiatric disorders: Common: somnolence Nervous system disorders: Common: dizziness, headache Respiratory, thoracic and mediastinal disorders: Common: pharyngitis Gastrointestinal disorders: Common: dry mouth, nausea Uncommon: abdominal pain General disorders and administration site conditions: Common: fatigue.

Children 6 months to 12 years of age: Adverse reactions at rates of 1 % or greater in controlled clinical trials are: Psychiatric disorders: Common: somnolence Respiratory, thoracic and mediastinal disorders: Common: rhinitis Gastrointestinal disorders: Common: diarrhoea General disorders and administration site conditions: Common: fatigue.

Post-marketing data: In addition to the adverse reactions reported during clinical studies and listed above, the following undesirable effects have been reported in post-marketing experience. Blood and lymphatic disorders: thrombocytopenia Immune system disorders: hypersensitivity, anaphylactic shock Psychiatric disorders: agitation, aggression, confusion, depression, hallucination, insomnia, tic Nervous system disorders: paraesthesia, convulsions, dysgeusia, dyskinesia, dystonia, syncope, tremor, amnesia, memory impairment Eye disorders: accommodation disorder, blurred vision, oculogyration Cardiac disorders: tachycardia Gastrointestinal disorders: diarrhoea Hepatobiliary disorders: hepatic function abnormal (increased transaminases, alkaline phosphatase, -GT and bilirubin) Skin and subcutaneous tissue disorders: pruritus, rash, urticaria, angioneurotic oedema, fixed drug eruption Renal and urinary disorders: dysuria, enuresis General disorders and administration site conditions: asthenia, malaise, oedema Investigations: weight increased.

Special Precautions: Methyl parahydroxybenzoate and propyl parahydroxybenzoate included in ZYRTEC oral drops and ZYRTEC oral solution may cause allergic reactions (possibly delayed).

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Effects on ability to drive and use machines: Patients should be warned that some individuals may experience sedation. It is therefore advisable to determine individual response before driving or performing complicated tasks. This effect may be compounded by the simultaneous intake of alcohol or other central nervous system depressants.

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT: Symptoms: Symptoms observed after an overdose of ZYRTEC are mainly associated with CNS effects or with effects that 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 ZYRTEC. Should overdose occur, symptomatic or supportive treatment is recommended. Gastric lavage should be considered following ingestion of a short occurrence. Cetirizine is not effectively removed by dialysis.

IDENTIFICATION: ZYRTEC tablets: White oblong, film-coated tablet scored on one side and marked Y/Y. ZYRTEC ORAL DROPS 10 mg/ml: Clear and colourless solution, free from particulate matter, with a slightly sweet taste and a bitter flavour. ZYRTEC ORAL SOLUTION 1 mg/ml: Clear and colourless solution, free from particulate matter, with a slightly sweet taste and a banana flavour.

PRESENTATION: ZYRTEC tablets are available in aluminium foil blister packs of 10 and 30 tablets. ZYRTEC ORAL DROPS 10 mg/ml is available in 15 ml and 20 ml amber glass bottles fitted with a white plastic dropper and white plastic cap. ZYRTEC ORAL SOLUTION 1 mg/ml is available in 50 ml and 150 ml amber glass bottles fitted with a white plastic cap.

STORAGE INSTRUCTIONS: Store at or below 25 ?C. Keep tablets in a dry place. Keep out of reach of children.

REGISTRATION NUMBERS: ZYRTEC: W/5.7.1/148 ZYRTEC ORAL DROPS 10 mg/ml: 28/5.7.1/0477 ZYRTEC ORAL SOLUTION 1 mg/ml: 28/5.7.1/0478

NAME AND BUSINESS ADDRESS OF THE HOLDER OF THE CERTIFICATE OF REGISTRATION: GlaxoSmithKline South Africa (Pty) Ltd 39 Hawkins Avenue Epping Industria 1, 7460

DATE OF PUBLICATION OF THE PACKAGE INSERT: Registration date: ZYRTEC: 16 November 1990 ZYRTEC ORAL DROPS 10 mg/ml: 14 November 1994 ZYRTEC ORAL SOLUTION 1 mg/ml: 09 January 1996 Revision approval date: 26 October 2012

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Botswana: Zyrtec: Reg No BOT0600861 S2 Zyrtec oral drops: Reg No BOT0600863 S2 Zyterc oral solution: Reg No BOT0600862 S2

Namibia: Zyrtec: Reg No 04/5.7.1/0823 S1 Zyrtec oral drops: Reg No 04/5.7.1/0822 S1 Zyterc oral solution: Reg No 04/5.7.1/0821 S1

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