LEVOCETRIMARK Tablet

Symptomatic treatment of allergic rhinitis (including persistent allergic rhinitis) and chronic idiopathic urticaria.

Posology and method of administration

The tablet must be taken orally, swallowed whole with liquid and may be taken with or without food. It is recommended to take the daily dose in one single intake.

The daily recommended dose is 5mg.

Elderly: Adjustment of the dose is recommended in elderly patients with moderate to severe renal impairment.

Children aged 6-12 years: The daily recommended dose is 5mg.

For children aged 2-6 years: No adjusted dosage is possible with the tablet formulation. It is recommended to use a paediatric formulation of levocetirizine.

Hypersensitivity to levocetirizine, to other piperazine derivatives, or to any of the excipients.

Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.

See the package insert about the details below:

Adverse drug reactions were mild to moderate.

No interaction studies have been performed with levocetirizine (including with CYP3A4 inducers): studies with the racemate compound cetirizine demonstrated that there were no clinically relevant adverse interactions (with pseudoephedrine, Cimetidine, ketoconazole, erythromycin, azithromycin, glipizide and diazepam). A small decrease in the clearance of cetirizine (16%) was observed in a multiple dose study with theophylline (400mg once a day); while the disposition of theophylline was not altered by concomitant cetirizine administration.

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

In sensitive patients the simultaneous administration of cetirizine or levocetirizine and alcohol 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.

See the package insert about the details below:

Pregnancy

No clinical data on exposed pregnancies are available. Caution should be exercised when prescribing to pregnant or lactating women.

Lactation

The use of the Levocetirizine 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 levocetirizine.

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

Precaution is recommended with intake of alcohol.

Pharmacotherapeutic group: antihistamine for systemic use, piperazine derivative.

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

Binding studies revealed that levocetirizine has high affinity for human H1-receptors. Levocetirizine shows receptor occupancy of 90% at 4 hours and 57% at 24 hours.

Pharmacodynamic studies in healthy volunteers demonstrate that, at half the dose, levocetirizine has comparable activity to cetirizine, both in the skin and in the nose.

The pharmacodynamic activity of levocetirizine has been studies in randomized, controlled trials:

In a study comparing the effects of levocetirizine 5mg, desloratadine 5mg, and placebo on histamine-induced wheal and flare, levocetirizine treatment resulted in significantly decreased wheal and flare formation which was highest in the first 12 hours and lasted for 24 hours, compared with placebo and desloratadine.

The onset of action of levocetirizine 5mg in controlling pollen-induced symptoms has been observed at 1 hour post drug intake in placebo controlled trials in the method of the allergen challenge chamber.