XYZAL 5 mg

11 DESCRIPTION

Levocetirizine dihydrochloride, the active component of XYZAL tablets and oral solution, is an orally active H1- receptor antagonist. The chemical name is (R)-[2-[4-[(4-chlorophenyl) phenylmethyl]-1-piperazinyl] ethoxy] acetic acid dihydrochloride. Levocetirizine dihydrochloride is the R enantiomer of cetirizine hydrochloride, a racemic compound with antihistaminic properties. The empirical formula of levocetirizine dihydrochloride is C21H25ClN2O3•2HCl.

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1 INDICATIONS AND USAGE

1.1 Allergic Rhinitis

XYZAL® is indicated for the relief of symptoms associated with allergic rhinitis (seasonal and perennial) in adults and children 6 years of age and older.

1.2 Chronic Idiopathic Urticaria

XYZAL is indicated for the treatment of the uncomplicated skin manifestations of chronic idiopathic urticaria in adults and children 6 years of age and older.

4 CONTRAINDICATIONSThe use of XYZAL is contraindicated in:

Patients with known hypersensitivity to levocetirizine or any of the ingredients of XYZAL, or to cetirizine. Observed reactions range from urticaria to anaphylaxis [see Adverse Reactions (6.2)].

6 ADVERSE REACTIONS

Use of XYZAL has been associated with somnolence, fatigue, and asthenia [see Warnings and Precautions (5.1)].

6.1 Clinical Trials Experience

The safety data described below reflect exposure to XYZAL in 2549 patients with seasonal or perennial allergic rhinitis and chronic idiopathic urticaria in 12 controlled clinical trials of 1 week to 6 months duration. The short-term (exposure up to 6 weeks) safety data for adults and adolescents are based upon eight clinical trials in which 1896 patients (825 males and 1071 females aged 12 years and older) were treated with XYZAL 2.5, 5, or 10 mg once daily in the evening. The short-term safety data from pediatric patients are based upon two clinical trials in which 243 children with seasonal or perennial allergic rhinitis (162 males and 81 females 6 to 12 years of age) were treated with XYZAL 5 mg once daily for 4 to 6 weeks. The long-term (exposure of 4 or 6 months) safety data are based upon two clinical trials in adults and adolescents in which 428 patients (190 males and 238 females) with allergic rhinitis were exposed to treatment with XYZAL 5 mg once daily. Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trial of another drug and may not reflect the rates observed in practice.

Adults and Adolescents 12 years of Age and Older

In studies up to 6 weeks in duration, the mean age of the adult and adolescent patients was 32 years, 44% of the patients were men and 56% were women, and the large majority (more than 90%) was Caucasian.

In these trials 43% and 42% of the subjects in the XYZAL 2.5 mg and 5 mg groups, respectively, had at least one adverse event compared to 43% in the placebo group.

In placebo-controlled trials of 1-6 weeks in duration, the most common adverse reactions were somnolence, nasopharyngitis, fatigue, dry mouth, and pharyngitis, and most were mild to moderate in intensity. Somnolence with XYZAL showed dose ordering between tested doses of 2.5, 5 and 10 mg and was the most common adverse reaction leading to discontinuation (0.5%).

Table 1 lists adverse reactions that were reported in greater than or equal to 2% of subjects aged 12 years and older exposed to XYZAL 2.5 mg or 5 mg in eight placebo-controlled clinical trials and that were more common with XYZAL than placebo.

Additional adverse reactions of medical significance observed at a higher incidence than in placebo in adults and adolescents aged 12 years and older exposed to XYZAL are syncope (0.2%) and weight increased (0.5%).

Pediatric Patients 6 to 12 Years of Age

A total of 243 pediatric patients 6 to 12 years of age received XYZAL 5 mg once daily in two short-term placebo controlled double-blind trials. The mean age of the patients was 9.8 years, 79 (32%) were between 6-8 years of age, and 50% were Caucasian. Table 2 lists adverse reactions that were reported in greater than or equal to 2% of subjects aged 6-12 years exposed to XYZAL 5 mg in placebo-controlled clinical trials and that were more common with XYZAL than placebo.

The safety of XYZAL in children under 6 years of age has not been established [see Use in Specific Populations (8.4)].

10 OVERDOSAGE

Overdosage has been reported with XYZAL.

Symptoms of overdose may include drowsiness in adults and initially agitation and restlessness, followed by drowsiness in children. There is no known specific antidote to XYZAL. Should overdose occur, symptomatic or supportive treatment is recommended. XYZAL is not effectively removed by dialysis, and dialysis will be ineffective unless a dialyzable agent has been concomitantly ingested.

The acute maximal non-lethal oral dose of levocetirizine was 240 mg/kg in mice (approximately 200 times the maximum recommended daily oral dose in adults and approximately 230 times the maximum recommended daily oral dose in children) on a mg/m2 basis. In rats the maximal non-lethal oral dose was 240 mg/kg (approximately 390 times the maximum recommended daily oral dose in adults and approximately 460 times the maximum recommended daily oral dose in children on a mg/m2 basis).

2 DOSAGE AND ADMINISTRATION

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.

2.1 Adults and Children 12 Years of Age and Older

The recommended dose of XYZAL is 5 mg (1 tablet or 2 teaspoons [10 mL] oral solution) once daily in the evening. Some patients may be adequately controlled by 2.5 mg (1/2 tablet or 1 teaspoon [5 mL] oral solution) once daily in the evening.

2.2 Children 6 to 11 Years of Age

The recommended dose of XYZAL is 2.5 mg (1/2 tablet or 1 teaspoon [5 mL] oral solution) once daily in the evening. The 2.5 mg dose should not be exceeded because the systemic exposure with 5 mg is approximately twice that of adults [see Clinical Pharmacology (12.3)].

XYZAL is not indicated for children under 6 years of age.

16 HOW SUPPLIED/STORAGE AND HANDLING

XYZAL 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 and unit of use blisters.

90 Tablets (NDC 0024-5800-90)

30 count box, 3 cards of 10 (NDC 0024-5800-32)

XYZAL oral solution is a clear, colorless liquid containing 0.5 mg of levocetirizine dihydrochloride per mL.

Oral solution in 5 oz glass bottles (NDC 0024-5801-20)

Storage:

Store at 20-25°C (68-77°F); excursions permitted to 15-30°C (59-86°F) [see USP Controlled Room Temperature].

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