Source: Health Sciences Authority (SG) Revision Year: 2018 Publisher: Manufacturer for tablets: UCB FARCHIM SA, BULLE SWITZERLAND Manufacturer for oral solution and drops: AESICA PHARMCEUTICALS S.R.L., PIANEZZA (TO) – ITALY
ZYRTEC is contraindicated during lactation.
Hypersensitivity to any of the constituents of the formulation, 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.
Patients with rare hereditary problems of fructose intolerance should not take cetirizine 1 mg/ml oral solution.
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 (see Section Interactions).
Caution should be taken in patients with predisposition factors of urinary retention (e.g. spinal cord lesion, prostatic hyperplasia) as cetirizine may increase the risk of urinary retention. (see Section Adverse Reactions)
Caution in epileptic patients and patients at risk of convulsions is recommended.
Pruritus and/or urticaria may occur when cetirizine is stopped, even if those symptoms were not present before treatment initiation (see Section Adverse Reactions). In some cases, the symptoms may be intense and may require treatment to be restarted. The symptoms should resolve when the treatment is restarted.
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. It is recommended to use a paediatric formulation of cetirizine.
Allergy skin tests are inhibited by antihistamines and a wash-out period of 3 days is recommended before performing them.
The extent of absorption of cetirizine is not reduced with food, although the rate of absorption is decreased by 1 hour.
Objective measurements of driving ability, sleep latency and assembly line performance have not demonstrated any clinically relevant effects at the recommended dose of 10 mg. However, patients who experience somnolence should refrain from driving, engaging in potentially hazardous activities or operating machinery.
Patients intending to drive, engaging in potentially hazardous activities or operating machinery should not exceed the recommended dose and should take their response to the medicinal product into account.
Activities requiring mental alertness. In clinical trials, the occurrence of somnolence has been reported in some patients taking ZYRTEC. Due caution should therefore be exercised when driving a car or operating potentially dangerous machinery.
Due to the pharmacokinetic, pharmacodynamic and tolerance profile of cetirizine, no interactions are expected with this antihistamine. Neither pharmacodynamic nor significant pharmacokinetic interaction was reported in drug-drug interaction studies performed, notably with pseudoephedrine or theophylline (400 mg/day).
In sensitive patients, the concurrent use of alcohol or other CNS depressants may cause additional reductions in alertness and impairment of performance, although cetirizine does not potentiate the effect of alcohol (0.5 g/L blood levels) (see Section Warnings and Precautions).
Limited data is available on human fertility but no safety concern has been identified. Animal data show no safety concern for human reproduction.
For cetirizine prospectively collected data on pregnancy outcomes do not suggest potential for maternal or foetal/embryonic toxicity above background rates. Animal studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/foetal development, parturition or postnatal development.
Caution should be exercised when prescribing to pregnant women. ZYRTEC should not be administered to pregnant women during the first three months of pregnancy.
Cetirizine is excreted in human milk at concentrations representing 25% to 90% of those measured in plasma, depending on sampling time after administration. Therefore, ZYRTEC is contraindicated in lactating women since the active ingredient, cetirizine is excreted in breast milk.
Clinical studies have shown that cetirizine at the recommended dosage has minor adverse 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.
Double blind controlled clinical trials comparing cetirizine to placebo or other antihistamines at the recommended dosage (10 mg daily for cetirizine), of which quantified safety data are available, included more than 3200 subjects exposed to cetirizine.
From this pooling, the following adverse reactions were reported for cetirizine 10 mg in the placebo-controlled trials at rates of 1.0% or greater:
| Adverse reactions (WHO-ART) | Cetirizine 10 mg (n=3260) | Placebo (n=3061) |
|---|---|---|
| General disorders and administration site conditions | ||
| Fatigue | 1.63% | 0.95% |
| Nervous system disorders | ||
| Dizziness | 1.10% | 0.98% |
| Headache | 7.42% | 8.07% |
| Gastro-intestinal system disorders | ||
| Abdominal pain | 0.98% | 1.08% |
| Dry mouth | 2.09% | 0.82% |
| Nausea | 1.07% | 1.14% |
| Psychiatric disorders | ||
| Somnolence | 9.63% | 5.00% |
| Respiratory thoracic and mediastinal disorders | ||
| Pharyngitis | 1.29% | 1.34% |
Although statistically more common than under placebo, somnolence was mild to moderate in the majority of cases. Objective tests as demonstrated by other studies have demonstrated that usual daily activities are unaffected at the recommended daily dose in healthy young volunteers.
Adverse reactions at rates of 1% or greater in children aged from 6 months to 12 years, included in placebo-controlled clinical trials are:
| Adverse reactions (WHO-ART) | Cetirizine (n=1656) | Placebo (n=1294) |
|---|---|---|
| Gastro-intestinal system disorders | ||
| Diarrhoea | 1.0% | 0.6% |
| Psychiatric disorders | ||
| Somnolence | 1.8% | 1.4% |
| Respiratory thoracic and mediastinal disorders | ||
| Rhinitis | 1.4% | 1.1% |
| General disorders and administration site conditions | ||
| Fatigue | 1.0% | 0.3% |
Adverse drug reactions (ADRs) are listed below by MedDRA system organ class and by frequency.
Frequencies are defined as: 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).
Very rare: thrombocytopenia
Rare: hypersensitivity
Very rare: anaphylactic shock
Not known: increased appetite
Uncommon: agitation
Rare: aggression, confusion, depression, hallucination, insomnia
Very rare: tics
Not known: suicidal ideation, nightmare
Uncommon: paraesthesia
Rare: convulsions
Very rare: dysgeusia, dyskinesia, dystonia, syncope, tremor
Not known:amnesia, memory impairment
Very rare: accommodation disorder, blurred vision, oculogyration
Not known:vertigo
Rare: tachycardia
Uncommon: diarrhoea
Rare: hepatic function abnormal (increased transaminases, alkaline phosphatase, gamma-glutamyl transferase and bilirubin)
Not known: hepatitis
Uncommon: pruritus, rash
Rare: urticaria
Very rare: angioedema, fixed drug eruption
Not known: acute generalized exanthematous pustulosis (AGEP)
Not known: arthralgia
Very rare: dysuria, enuresis
Not known: urinary retention (see Section Warnings and Precautions)
Uncommon: asthenia, malaise
Rare: oedema
Rare: weight increased
After discontinuation of cetirizine, pruritus (intense itching) and/or urticarial have been reported (see Section Warnings and Precautions).
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