Levocetirizine

XYZAL 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

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.

XYZAL 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 decreased renal function

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

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. Risk of New Onset Pruritus After Discontinuation of XYZAL: New onset pruritus within a few days after discontinuation of XYZAL has been reported, usually after long-term use (e.g., few months to years) of XYZAL. Symptoms may improve with restarting or tapering XYZAL.

The following clinically significant adverse reactions are described elsewhere in the labeling: Somnolence Urinary Retention Risk of New Onset Pruritus After Discontinuation of XYZAL The most common adverse reactions (rate ≥2% and > placebo) were somnolence, nasopharyngitis, fatigue, dry mouth, and pharyngitis in subjects 12 years of age and older, and pyrexia, somnolence, cough, and epistaxis in children 6 to 12 years of age. In subjects 1 to 5 years of age, the most common adverse reactions (rate ≥2% and > placebo) were pyrexia, diarrhea, vomiting, and otitis media. In subjects 6 to 11 months of age, the most common adverse reactions (rate ≥3% and > placebo) were diarrhea and constipation.

In vitro data indicate that levocetirizine is unlikely to produce pharmacokinetic interactions through inhibition or induction of liver drug-metabolizing enzymes. No in vivo drug-drug interaction studies have been performed with levocetirizine. Drug interaction studies have been performed with racemic cetirizine.

Storage Store at 20ºC to 25ºC (68ºF to 77ºF), excursions permitted to 15ºC to 30ºC (59°F to 86°F).