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Titolo:
Absorption and disposition of levocetirizine, the eutomer of cetirizine, administered alone or as cetirizine to healthy volunteers
Autore:
Baltes, E; Coupez, R; Giezek, H; Voss, G; Meyerhoff, C; Benedetti, MS;
Indirizzi:
UCB Pharma, F-92003 Nanterre, France UCB Pharma Nanterre France F-92003UCB Pharma, F-92003 Nanterre, France UCB Pharma, B-1420 Braine Lalleud, Belgium UCB Pharma Braine Lalleud Belgium B-1420 B-1420 Braine Lalleud, Belgium UCB GMBH, D-50170 Kerpen Sindorf, Germany UCB GMBH Kerpen Sindorf Germany D-50170 D-50170 Kerpen Sindorf, Germany AAI Deutschland GMBH & Co KG, D-89231 Neu Ulm, Germany AAI Deutschland GMBH & Co KG Neu Ulm Germany D-89231 31 Neu Ulm, Germany
Titolo Testata:
FUNDAMENTAL & CLINICAL PHARMACOLOGY
fascicolo: 4, volume: 15, anno: 2001,
pagine: 269 - 277
SICI:
0767-3981(200108)15:4<269:AADOLT>2.0.ZU;2-4
Fonte:
ISI
Lingua:
ENG
Soggetto:
CHIRAL INVERSION; SPARTEINE; OXIDATION; DEBRISOQUINE; ENANTIOMERS; DRUGS;
Keywords:
absorption; cetirizine; configurational stability; disposition; distomer; enantiomers; eutomer; levocetirizine;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
20
Recensione:
Indirizzi per estratti:
Indirizzo: Benedetti, MS UCB Pharma, 21 Rue de Neuilly, F-92003 Nanterre, France UCB Pharma 21 Rue de Neuilly Nanterre France F-92003 France
Citazione:
E. Baltes et al., "Absorption and disposition of levocetirizine, the eutomer of cetirizine, administered alone or as cetirizine to healthy volunteers", FUN CL PHAR, 15(4), 2001, pp. 269-277

Abstract

The primary objective of the present study was to compare the absorption and disposition of levocetirizine, the eutomer of cetirizine. when administered alone (10 mg) or in presence of the distomer. An additional objective was also to investigate the configurational stability of levocetirizine in vivo in humans. The study was performed in a randomized, two-way cross-over,single-dose design with a wash-out phase of 7 days between the two periods. A total of 12 healthy male and 12 healthy female volunteers were includedin the study. Bioequivalence can be concluded from the analysis of the pharmacokinetic parameters of levocetirizine when administered alone or as theracemate cetirizine. No chiral inversion occurs in humans when levocetirizine is administered, i.e. there is no formation of the distomer. When comparing the pharmacokinetic characteristics of levocetirizine and the distomer, the apparent volume of distribution of the eutomer is significantly smaller than that of the distomer (0.41 and 0.60 L/kg, respectively). For an H-1-antagonist a small distribution volume can be considered as a positive aspect, both in terms of efficacy and safety. Moreover the non-renal clearanceof levocetirizine is also significantly lower than that of the distomer (9.70 and 28.70 mL/min, respectively), which constitutes an additional positive aspect particularly as far as metabolism-based drug interactions are concerned. The information collected in the present study on the pharmacokinetics of levocetirizine and the distomer provide additional reasons for eliminating the distomer and developing levocetirizine as an improvement on cetirizine.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 18/01/20 alle ore 07:58:08