XYZAL Oral drops

・hypersensitivity to levocetirizine, to any piperazine derivatives or any of the excitients

・severe renal impairment at less from 10 ml/min creatinine clearance

Clinical Trial Data

In therapeutic studies in women and man aged 12 to 71 years, 15.1% of the patients in the levocetirizine 5mg group had at least on adverse drug reaction compared to 11.3% in the placebo group. 91.6% of these adverse drug reactions were mild to moderate.

In therapeutic included 935 subjects exposed to the drug at the recommended dose of 5mg daily.

Adverse reactions are ranked under headings of frequency using the following convention:

Very common ≥ 1/10

Common　　 ≥ 1/100 to < 1/10

Uncommon　 ≥ 1/1000 to < 1/100

Rare　　　　 ≥ 1/10000 to < 1/1000

Very rare　　 < 1/10000

Not known (cannot be estimated from the available data).

Nervous system disorders

Common: headache, somnolence

Gastrointestinal disorders

Common: dry mouth

Uncommon: abdominal pain

General disorders and administration site conditions

Common: fatigue

Uncommon: asthenia

The incidence of sedating adverse drug reactions such as somnolence, fatigue and asthenia was altogether more common (8.1%) under levocetirizine 5mg than under placebo (3.1%).

Oral drops, Oral solution

Paediatric Patients

In two placebo-controlled studies aged 6-11 months and aged 1 year to less than 6 years, 159 subjects were exposed to levocetirizine at the dose of 1.25mg daily for 2 weeks and 1.25mg twice daily respectively. The following incidence of adverse drug reactions was reported under levocetirizine.

Psychiatric disorders

Common: sleep disorders

Nervous system disorders:

Common: somnolence

Gastrointestinal disorders

Common: diarrhea, constipation

Uncommon: vomiting

In children aged 6-12 years double blind placebo controlled studies were performed where 243 children were exposed to 5mg levocetirizine daily for variable periods ranging from less than 1 week to 13 weeks. The following incidence of adverse drug reactions was reported.

Nervous system disorders

Common: somnolence

Uncommon: headache

Please not that even if clinical data presented in this section are available in children aged 6 months to 12 years, we do not have sufficient data to support the administration of the product to infants and toddlers less than 2 years.

Post Marketing Data

In addition to the adverse reactions reported during clinical studies and listed above, very rare cases of the following adverse drug reactions have been reported in post-marketing experience.

Immune system disorders

Not known: hypersensitivity including anaphylaxis

Metabolism and nutrition disorders

Not known: increased weight, increased appetite

Psychiatric disorders

Not known: aggression, agitation, hallucination, depression, insomnia, suicidal ideation

Nervous system disorders

Not known: convulsions, paraesthesia, dizziness, syncope, tremor, dysgeusia

Eye disorders

Not known: Visual disturbances, blurred vision

Ear and labyrinth disorders

Not known: vertigo

Cardiac disorders

Not known: palpitations, tachycardia

Respiratory, thoracic and mediastinal disorders

Not known: dyspnea

Gastrointestinal disorders

Not known: nausea, vomiting

Hepatobiliary disorders

Not known: hepatitis, abnormal liver function test

Skin and subcutaneous tissue disorders

Not known: angioneurotic oedema, fixed drug eruption, pruritus, rash, urticaria

Musculoskeletal and connective tissue disorders

Not known: myalgia

Renal and urinary disorders

Not known: dysuria, urinary retention

General disorders and administration site conditions

Not known: oedema

No interaction studies have been performed with levocertirizine (including no studies with CYP34 inducers); studies with the racemate compound certirizine demonstrated that there were no clinically relevant adverse interactions(with pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, glipizide and diazepam).

Theophyline

A small decrease in the clearance of cetirizine (16%) was observed in a multiple dose study with theophyline (400mg once a day); while the disposition of theophyline was not altered by concomitant cetirizine administration.

Ritonavir

In a multiple dose study of ritonavir (600mg twice a day) and cetirizine (10mg daily), the extent to cetirizine was increased by about 40% while the disposition of ritonavir was slightly altered (-11%) further to concomitant cetirizine administration.

Food

The extent of absorption of levocetirizine is not reduced with food, although the rate of absorption is decreased.

Alcohol

In sensitive patients the simultanous administration of cetirizine of levocetirizine and aldohol or other CNS depressants may have effects on the central nervous system, although it has been shown that the racemate cetirizine does not potentiate the effect of alcohol.

Fertility

There are no relevant data available.

Pregnancy

Caution should be exercised when prescribing to pregnant women.

For levocetirizine no clinical data on exposed pregnancies are avalable.

Animal studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/foetal development, parturitaion or postnatal development.

Lactation

Caution should be exercised when prescribing to lactating women. Cetirizine is excreted inn human milk.

Alcohol

Precaution is recommended with intake of alcohol (see Section Interactions).

Risk of urinary retention

Caution should be taken in patients with predisposing factors of urinary retention (e.g. spinal cord lesion, prostatic hyperplasia) as levocetirizine may increase the risk of urinary retention.

Infants and children under 2 years

Even if some clinical data are available in children aged 6 months to 12 years, these data are not sufficient to support the administration of levocetirizine to infants and toddlers aged less than 2 years.

Therefore the administration of levocetirizine to infants and toddlers aged less than 2 years is not recommended.

Oral drops

Methyl parahydroxybenzoate, propyl parahydroxybenzoate

The presence of methyl parahydroxybenzoate and propyl parahydroxybenzoate may cause allergic reactions (possibly delayed).

Antihistamine for systemic use, piperazine derivative.

levocetirizine, the (R) enantiomer of cetirizine, is a potent and selective antagonist of peripheral H1-receptors.