Levocetirizine Dihydrochloride

What it is and how it works

Mechanism of Action Levocetirizine, the active enantiomer of cetirizine, is an antihistamine; its principal effects are mediated via selective inhibition of H 1 receptors. The antihistaminic activity of levocetirizine has been documented in a variety of animal and human models. In vitro binding studies revealed that levocetirizine has an affinity for the human H 1 -receptor 2-fold higher than that of cetirizine (Ki = 3 nmol/L vs . 6 nmol/L, respectively). The clinical relevance of this finding is unknown.

Indications

is a histamine H 1 -receptor antagonist indicated for: The relief of symptoms associated with perennial allergic rhinitis The treatment of the uncomplicated skin manifestations of chronic idiopathic urticaria Perennial Allergic Rhinitis XYZAL is indicated for the relief of symptoms associated with perennial allergic rhinitis in children 6 months to 2 years of age. Chronic Idiopathic Urticaria XYZAL is indicated for the treatment of the uncomplicated skin manifestations of chronic idiopathic urticaria in adults and children 6 months of age and older.

Dosage and administration (summary)

is available as 2.5 mg/5 mL (0.5 mg/mL) oral solution and as 5 mg breakable (scored) tablets, allowing for the administration of 2.5 mg, if needed. XYZAL can be taken without regard to food consumption. Perennial Allergic Rhinitis Children 6 months to 2 years of age: 1.25 mg (1/2 teaspoon oral solution) (2.5 mL) once daily in the evening Chronic Idiopathic Urticaria Adults and children 12 years of age and older: 5 mg once daily in the evening Children 6 to 11 years of age: 2.5 mg once daily in the evening Children 6 months to 5 years of age: 1.25 mg (1/2 teaspoon oral solution) (2.5 mL) once daily in the evening Renal Impairment Adjust the dose in patients 12 years of age and older with decr…

Contraindications

The use of XYZAL is contraindicated in: Patients with a known hypersensitivity to levocetirizine or any of the ingredients of XYZAL or to cetirizine Patients with end-stage renal disease at less than 10 mL/min creatinine clearance or patients undergoing hemodialysis Children 6 months to 11 years of age with renal impairment Patients with Known Hypersensitivity Patients with known hypersensitivity to levocetirizine or any of the ingredients of XYZAL, or to cetirizine.

Warnings and precautions

Somnolence: Somnolence, fatigue, and asthenia have been reported with use of XYZAL in some patients in clinical trials. Avoid engaging in hazardous occupations requiring complete mental alertness such as driving or operating machinery when taking XYZAL. Avoid concurrent use of alcohol or other central nervous system depressants with XYZAL. Urinary Retention: Urinary retention has been reported with use of XYZAL. Use with caution in patients with predisposing factors of urinary retention (e.g. spinal cord lesion, prostatic hyperplasia). Discontinue XYZAL if urinary retention occurs.

Pregnancy

Pregnancy Risk Summary Available data from published literature and postmarketing experience with levocetirizine use in pregnant women are insufficient to identify any drug-associated risks of miscarriage, birth defects, or adverse maternal or fetal outcomes.

Storage and supply

tablets are white, film-coated, oval-shaped, scored, imprinted (with the letter Y in red color on both halves of the scored tablet) and contain 5 mg levocetirizine dihydrochloride. They are supplied in unit of use HDPE bottles.

Source: Levocetirizine Dihydrochloride (Xyzal) — US FDA prescribing information, 2025-07-22, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.