Reference

Compared pharmacological characteristics in humans of racemic cetirizine and levocetirizine, two histamine H1-receptor antagonists

Compared pharmacological characteristics in humans of racemic cetirizine and levocetirizine, two histamine H1-receptor antagonists. Tillement, Jean-Paul; Testa, Bernard; Bree, Francoise (Laboratoire de Pharmacologie, Faculte de Medecine de Paris XII, Creteil F-94010, Fr.). Biochemical Pharmacology, 66(7), 1123-1126 (English) 2003 Elsevier Science B.V. CODEN: BCPCA6. ISSN: 0006-2952. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The potent histamine H1-receptor antagonist cetirizine (Zyrtec) is a racemic mixt. of levocetirizine (now available under the trademark Xyzal) and dextrocetirizine. In this Commentary, we examine some biol. properties of cetirizine and levocetirizine, namely enantioselectivity in pharmacol. activity and pharmacokinetic properties, with emphasis on the possibility of racemization, the compared behavior of the two enantiomers, and the potential for interactions with other drugs. Recent data demonstrate that the antihistaminergic activity of the racemate is primarily due to levocetirizine. Levocetirizine is rapidly and extensively absorbed, poorly metabolized, and not subject to racemization. Its pharmacokinetic characteristics are comparable after administration alone or in the racemate. Its apparent vol. of distribution is smaller than that of dextrocetirizine (0.41 L kg-1 vs. 0.60 L kg-1). Moreover, the non-renal (mostly hepatic) clearance of levocetirizine is also significantly lower than that of dextrocetirizine (11.8 mL min-1 vs. 29.2 mL min-1). Our conclusion is that levocetirizine is indeed the eutomer of cetirizine. The evidence reviewed here confirms preclin. findings and offers a rationale for the chiral switch from the racemate to levocetirizine.Except for chemicals metioned above, 130018-77-8 and 130018-76-7 are also used. .

Levocetirizine improves quality of life and reduces costs in long-term management of persistent allergic rhinitis

Levocetirizine improves quality of life and reduces costs in long-term management of persistent allergic rhinitis. Bachert, Claus; Bousquet, Jean; Canonica, G. Walter; Durham, Stephen R.; Klimek, Ludger; Mullol, Joaquim; Van Cauwenberge, Paul B.; Van Hammee, Genevieve (XPERT Study Group; Department of Oto-Rhino-Laryngology, University Hospital, Germany). Journal of Allergy and Clinical Immunology, 114(4), 838-844 (English) 2004 Elsevier Inc. CODEN: JACIBY. ISSN: 0091-6749. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Background: Allergic Rhinitis and its Impact on Asthma in collaboration with the World Health Organization initiative reclassified allergic rhinitis, like asthma, by duration and severity.There are some reagents like 130018-77-8 is used in this study. The Xyzal in Persistent Rhinitis Trial is the first large, long-term clin. trial studying patients with persistent rhinitis as defined by Allergic Rhinitis and its Impact on Asthma. Objective: Two primary objectives were defined: comparison of the Rhinoconjunctivitis Quality of Life Questionnaire overall score and Total 5 Symptoms Score (rhinorrhea, sneezing, nasal congestion, and nasal and ocular pruritus) over a period of 4 wk between levocetirizine 5 mg and placebo. Secondary endpoints included similar evaluations at 1 wk and 3, 4.5, and 6 mo, summary scores for a general health status questionnaire (Medical Outcomes Survey Short Form 36), a pharmacoeconomic assessment, comorbidities, and a safety evaluation. Methods: The Xyzal in Persistent Rhinitis Trial was a 6-mo double-blind, placebo-controlled, multicenter, multinational trial in 551 patients. Adults with persistent rhinitis sensitized to both grass pollen and house dust mite were randomized to receive levocetirizine 5 mg/d or placebo. Results: A total of 421 patients completed the full study. Levocetirizine significantly improved both the Rhinoconjunctivitis Quality of Life Questionnaire overall score and the Total 5 Symptoms Score from week 1 to 6 mo (all P values <.001). Medical Outcomes Survey Short Form 36 summary scores were also improved in the levocetirizine group compared with the placebo group. Treatment cessation because of lack of effect, comorbidities, and overall costs of disease, and comorbidities per working patient per mo (euro 160.27 vs euro 108.18) were lower in the levocetirizine group. Conclusion: Levocetirizine was shown to improve quality of life and symptoms and to decrease the overall costs of the disease over the 6-mo treatment period. .