Companies:

UCB and Sanofi Aventis

Antihistamine

Levocetirizine dihydrochloride 5mg; scored tabs.

Allergic rhinitis (seasonal and perennial). Chronic idiopathic urticaria.

Levocetirizine, the L-enantiomer of cetirizine, is a histamine H₁ receptor blocker. Its affinity for H₁ receptors is about two times stronger than that of cetirizine. Peak plasma levels are reached in about 1 hour after dosing, and steady-state is reached in about 2 days. Levocetirizine is eliminated primarily by the kidneys. In patients with renal insufficiency, clearance of the drug is reduced.

The efficacy of levocetirizine in relieving symptoms associated with seasonal and perennial allergic rhinitis was assessed in six randomized, placebo-controlled, double-blind studies in patients ≥12 years of age. Efficacy was evaluated using a total symptom score from patient recordings of several symptoms, including sneezing, rhinorrhea, nasal pruritus, and ocular pruritus. Symptom scores were recorded once daily in the evening reflecting the 24-hour treatment period ("reflective" score) and, in one study, they were also recorded 1 hour before the next dose was due ("instantaneous" score).

The primary endpoint was the mean total symptom score averaged over the first week and over 2 weeks for seasonal allergic rhinitis trials, and 4 weeks for perennial allergic rhinitis trials. In these studies, levocetirizine was shown to be statistically better than placebo in both the reflective and instantaneous total symptom scores.

The efficacy of levocetirizine in treating uncomplicated skin manifestations of chronic idiopathic urticaria in patients 18–85 years of age was studied in two randomized, placebo-controlled double-blind, 4-week trials. The primary endpoint was the mean reflective pruritus severity score over the first week and over the entire treatment period. Levocetirizine 5mg given once daily in the evening was shown to be statistically better than placebo in the reflective pruritus severity score. The duration of pruritus, number and size of wheals, and instantaneous pruritus severity score indicated superiority over placebo, and the instantaneous pruritus severity scale confirmed the end of dosing interval efficacy.

2.5mg–5mg once daily in the PM. Renal dysfunction: CrCl 50–80mL/min: 2.5mg once daily; CrCl 30–50mL/min: 2.5mg every other day; CrCl 10–30mL/min: 2.5mg twice per week (every 3–4 days); CrCl <10 mL/min or hemodialysis: contraindicated.

<6yrs: not recommended. 6–11yrs: max 2.5mg once daily in the PM. Renal dysfunction: contraindicated.

End-stage renal disease (CrCl <10mL/min) or hemodialysis (>12yrs of age). Impaired renal function (<12yrs of age).

Do not exceed recommended dose. Pregnancy (Cat.B). Nursing mothers: not recommended.

Avoid alcohol, other CNS depressants. May be potentiated by theophylline. Potentiated by ritonavir.

Adults: somnolence, nasopharyngitis/pharyngitis, fatigue, dry mouth. Children: pyrexia, somnolence, cough, epistaxis.

Tabs—90

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9/25/07