Levocetirizine: uses, appearance and warnings

Levocetirizine dihydrochloride tablets are a histamine H 1 -receptor antagonist indicated for: • The relief of symptoms associated with perennial allergic rhinitis ( 1.1 ) • The treatment of the uncomplicated skin manifestations of chronic idiopathic urticaria ( 1.2 ) 1.1 Perennial Allergic Rhinitis Levocetirizine dihydrochloride tablets are indicated for the relief of symptoms associated with perennial allergic rhinitis in children 6 months to 2 years of age. 1.2 Chronic Idiopathic Urticaria Levocetirizine dihydrochloride tablets are indicated for the treatment of the uncomplicated skin manifestations of chronic idiopathic urticaria in adults and children 6 months of age and older.

Levocetirizine Dihydrochloride Tablets, USP are white, oval, film-coated, biconvex tablets, one side embossed with 'G' break line ‘G’ and the other side plain and contain 5 mg levocetirizine dihydrochloride, USP. • Immediate release breakable (scored) tablets, 5 mg (3)

Levocetirizine Dihydrochloride Tablets, USP are white, oval, film-coated biconvex tablets, one side embossed with ‘G’ break line ‘G’ and the other side plain and contain 5 mg levocetirizine dihydrochloride, USP. They are available as follows: HDPE bottles of 30 tablets with child-resistant closures (NDC 68462-346-30) HDPE bottles of 90 tablets with child-resistant closures (NDC 68462-346-90) HDPE bottles of 180 tablets with child-resistant closures (NDC 68462-346-18) HDPE bottles of 500 tablets with continuous thread closures (NDC 68462-346-05) HDPE bottles of 1,000 tablets with continuous thread closures (NDC 68462-346-10) Cartons of 50 tablets (NDC 68462-346-11) containing 5 x 10 Unit-Dose Blisters (NDC 68462-346-40) Storage Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature].

The use of levocetirizine dihydrochloride tablets are contraindicated in: • Patients with a known hypersensitivity to levocetirizine or any of the ingredients of levocetirizine dihydrochloride tablets or to cetirizine ( 4.1 ) • Patients with end-stage renal disease at less than 10 mL/min creatinine clearance or patients undergoing hemodialysis ( 4.2 ) • Children 6 months to 11 years of age with renal impairment ( 4.3 ) 4.1 Patients with Known Hypersensitivity Patients with known hypersensitivity to levocetirizine or any of the ingredients of levocetirizine dihydrochloride tablets, or to cetirizine. Observed reactions range from urticaria to anaphylaxis [ see Adverse Reactions ( 6.2 ) ]. 4.2 Patients with End-Stage Renal Disease Patients with end-stage renal disease (CL CR < 10 mL/min) and patients undergoing hemodialysis 4.3 Pediatric Patients with Impaired Renal Function Children 6 months to 11 years of age with impaired renal function

• Avoid engaging in hazardous occupations requiring complete mental alertness such as driving or operating machinery when taking levocetirizine dihydrochloride ( 5.1 ). • Avoid concurrent use of alcohol or other central nervous system depressants with levocetirizine dihydrochloride ( 5.1 ). • Use with caution in patients with predisposing factors of urinary retention (e.g. spinal cord lesion, prostatic hyperplasia). Discontinue levocetirizine dihydrochloride if urinary retention occurs ( 5.2 ). • Risk of New Onset Pruritus After Discontinuation of levocetirizine dihydrochloride : New onset pruritus within a few days after discontinuation of levocetirizine dihydrochloride has been reported, usually after long-term use (e.g., few months to years) of levocetirizine dihydrochloride Symptoms may improve with restarting or tapering levocetirizine dihydrochloride ( 5.3 ). 5.1 Somnolence In clinical trials the occurrence of somnolence, fatigue, and asthenia has been reported in some patients under therapy with levocetirizine dihydrochloride. Patients should be cautioned against engaging in hazardous occupations requiring complete mental alertness, and motor coordination such as operating machinery or driving a motor vehicle after ingestion of levocetirizine dihydrochloride. Concurrent use of levocetirizine dihydrochloride with alcohol or other central nervous system depressants should be avoided because additional reductions in alertness and additional impairment of central nervous system performance may occur. 5.2 Urinary Retention Urinary retention has been reported postmarketing with levocetirizine dihydrochloride. Levocetirizine dihydrochloride should be used with caution in patients with predisposing factors of urinary retention (e.g. spinal cord lesion, prostatic hyperplasia) as levocetirizine dihydrochloride may increase the risk of urinary retention. Discontinue levocetirizine dihydrochloride if urinary retention occurs. 5.3 Risk of New Onset Pruritus After Discontinuation of Levocetirizine Dihydrochloride Tablets Cases of pruritus after discontinuation of levocetirizine dihydrochloride tablets have been reported in the postmarketing setting in patients where pruritus was not present before initiation of Levocetirizine dihydrochloride tablets. Pruritus occurred within a few days of discontinuing levocetirizine dihydrochloride tablets among patients who used levocetirizine dihydrochloride tablets long-term (e.g., few months to years). Reported cases of pruritus were infrequent, but some were serious with patients experiencing widespread severe pruritus [see Adverse Reactions ( 6.2 )] . If pruritus occurs after discontinuation of levocetirizine dihydrochloride tablets, symptoms may improve with restarting or tapering levocetirizine dihydrochloride tablets.

The following clinically significant adverse reactions are described elsewhere in the labeling: • Somnolence [see Warnings and Precautions ( 5.1 )] • Urinary Retention [see Warnings and Precautions ( 5.2 )] • Risk of New Onset Pruritus After Discontinuation of Levocetirizine Dihydrochloride [see Warnings and Precautions ( 5.3 )] 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. ( 6.1 ). …

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. 7.1 Antipyrine, Azithromycin, Cimetidine, Erythromycin, Ketoconazole, Theophylline, and Pseudoephedrine Pharmacokinetic interaction studies performed with racemic cetirizine demonstrated that cetirizine did not interact with antipyrine, pseudoephedrine, erythromycin, azithromycin, ketoconazole, and cimetidine. There was a small decrease (~16%) in the clearance of cetirizine caused by a 400 mg dose of theophylline. It is possible that higher theophylline doses could have a greater effect. …