Pharmacy & Therapeutics - April 2008 - (Page 237) Pharmaceutical Approval Update scores compared with patients treated with placebo. These improvements were sustained over time with continued rilonacept treatment. The most commonly reported adverse reactions were injection-site reactions and upper respiratory tract infections. The approval of rilonacept represents a major advance in the treatment of CAPS. Source: www.regeneron.com were based on two trials in adults and adolescents in which 428 patients (190 males and 238 females) with allergic rhinitis received the oral solution at a dose of 5 mg once daily. Adults and adolescents 12 years of age and older: In studies up to six 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 most (more than 90%) were Caucasian. In these trials, 43% and 42% of the subjects in the 2.5-mg and 5-mg groups, respectively, had at least one adverse event, compared with 43% of placebo subjects. In placebocontrolled trials of one to six weeks in duration, the most common adverse reactions were somnolence, nasopharyngitis, fatigue, dry mouth, and pharyngitis. Most of these were mild to moderate in intensity. Somnolence was the most common adverse reaction, leading to discontinuation of therapy in 0.5% of patients. Dosage and Administration: Levocetirizine is available as an oral solution of 2.5 mg/5 mL (0.5 mg/mL), allowing for the administration of 2.5 mg if needed. That is, the 2.5-mg dose can be given, or a dose of 5 mg can be given by just doubling the volume (i.e., two teasoons instead of one teaspoon). The oral solution can be taken without regard to food consumption. Children 6 to 11 years of age: The recommended dose is 2.5 mg (one teaspoon, or 5 mL) once daily in the evening. Adults and children 12 years of age and older: The recommended dose is 5 mg (two teaspoons, or 10 mL) once daily in the evening. Some patients may achieve adequate control of symptoms with 2.5 mg, or one teaspoon (5 mL) of the oral solution once daily in the evening. The 2.5-mg dose should not be exceeded; a systemic exposure of 5 mg is approximately twice the exposure recommended for adults. Commentar y: Unlike the oral tablets of levocetirizine, the oral solution provides a welcome alternative for patients who have difficulty swallowing or who prefer liquid medication. This is especially helpful for younger patients. The oral solution offers potent and long-lasting allergy relief when taken once daily. In studies of allergic rhinitis patients, levocetirizine significantly reduced the symptoms of sneezing, itchy nose, runny nose, and itchy eyes. Studies of patients with chronic idiopathic urticaria showed that levocetirizine significantly reduced the severity of itching and the number and size of wheals. Sources: www.xyzal.com; www.rxlist.com I Levocetirizine (Xyzal Oral Solution) Manufacturer: Sanofi-Aventis, Bridgewater, N.J., and UCB, Brussels, Belgium Indication: Levocetirizine dihydrochloride oral solution is indicated for the relief of symptoms associated with seasonal and perennial allergic rhinitis in adults and children six years of age and older as well as for uncomplicated skin manifestations of chronic idiopathic urticaria in adults and children six years of age and older. Drug Class: Levocetirizine is an orally active and selective histamine H1-receptor antagonist. The drug’s chemical name is (R)-[2-[4-[(4-chlorophenyl) phenylmethyl]-1-piperazinyl] ethoxy] acetic acid dihydrochloride. It is the R enantiomer of cetirizine HCl, a racemic compound with antihistaminic properties. Uniqueness of Drug: Levocetirizine is an antihistamine whose principal effects are mediated via inhibition of H1 receptors. The drug’s antihistaminic activity has been documented in animal and human models. In vitro binding studies have shown that levocetirizine has an af finity for the human H1-receptor two-fold higher than that of cetirizine. The clinical relevance of this finding is unknown. Warnings and Precautions: Activities requiring mental alertness. In clinical trials, somnolence, fatigue, and asthenia have been reported in some patients receiving the oral solution. 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. The concurrent use of levocetirizine solution with alcohol or other CNS depressants should be avoided, because of possible additional reductions in alertness and additional impairment of CNS performance. Adverse Drug Reactions: The safety data reflect 2,549 patients with seasonal or perennial allergic rhinitis and chronic idiopathic urticaria in 12 controlled clinical trials lasting from one week to six months. Because trials were conducted under varying conditions, the rates of adverse reactions from the clinical trials of a drug cannot be directly compared with rates in a clinical trial of another drug and might not reflect the rates observed in practice. Short-term data: The short-term data (up to six weeks) for adults and adolescents were based on eight trials in which 1,896 patients (825 males and 1,071 females aged 12 years and older) received the oral solution at a dose of 2.5, 5, or 10 mg once daily in the evening. The short-term data from pediatric patients were based upon two clinical trials in which 243 children with seasonal or perennial allergic rhinitis (162 boys and 81 girls six to 12 years of age) received the oral solution at a dose of 5 mg once daily for four to six weeks. Long-term data: The long-term data (four to six months) Too busy to write an article? Send us your ideas anyway! Contact Sonja Sherritze at ssherritze@medimedia.com or at 267-685-2779. Vol. 33 No. 4 • April 2008 • P&T® 237 http://www.regeneron.com http://www.xyzal.com http://www.rxlist.com
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