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

Biochemical Pharmacology

Volumn 66, Issue 7, 2003, Pages 1123-1126

  Tillement, Jean Paul ^a   Testa, Bernard ^b   Brée, Françoise ^a  

^a FACULTÉ DE MÉDECINE   (France)

^b UNIVERSITY OF LAUSANNE   (Switzerland)

Author keywords

Cetirizine; Chiral switch; Distomer; Drug drug interactions; Eutomer; Levocetirizine; Racemate; Racemization; Volume of distribution

Indexed keywords

CETIRIZINE; DEXTROCETIRIZINE; HISTAMINE H1 RECEPTOR ANTAGONIST; LEVOCETIRIZINE; UNCLASSIFIED DRUG;

COMPARATIVE STUDY; DRUG ABSORPTION; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG METABOLISM; ENANTIOMER; ENANTIOSELECTIVITY; HUMAN; INTESTINE ABSORPTION; KIDNEY CLEARANCE; LIVER CLEARANCE; PRIORITY JOURNAL; RACEMIC MIXTURE; REVIEW; STATISTICAL SIGNIFICANCE;

EID: 0141628931     PISSN: 00062952     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0006-2952(03)00558-6     Document Type: Note

References (19)

1. Walsh G.M., Annunziato L., Frossard N., Knol K., Levander S., Nicolas J.M., Taglialatela M., Tharp M.D., Tillement J.P., Timmerman H. New insights into second generation antihistamines. Drugs. 61:2001;207-236.
2. Nicolas J.M., Whomsley R., Collart P., Roba J. In vitro inhibition of human liver drug metabolizing enzymes by second generation antihistamines. Chem. Biol. Interact. 123:1999;63-79.
3. Eichelbaum M, Testa B, Somogyi A, editors. Stereochemical aspects of drug action and disposition. Handbook of clinical pharmacology, vol. 153. Heidelberg: Springer-Verlag; 2003.
4. Testa B., Trager W.F. Racemates versus enantiomers in drug development. Dogmatism or pragmatism? Chirality. 2:1990;129-133.
5. Testa B, Carrupt P-A, Christiansen L, Christoffersen P, Reist M. Chirality in drug research: stereomania, stereophobia, or stereophilia? In: Claassen V, editor. Trends in receptor research. Amsterdam: Elsevier; 1993. p. 1-8.
6. 194. Mol. Pharmacol. 61:2002;1-9.
7. Devalia J.L., De Vos C., Hanotte F., Baltes E. A randomised, double-blind, crossover comparison among cetirizine, levocetirizine, and UCB 28557 on histamine-induced cutaneous responses in healthy adult volunteers. Allergy. 56:2001;50-57.
8. Wang D.Y., Hanotte F., De Vos C., Clement P. Effect of cetirizine, levocetirizine, and dextrocetirizine on histamine induced nasal response in healthy adult volunteers. Allergy. 56:2001;339-343.
9. Baltes E., Coupez R., Giezek H., Voss G., Meyerhoff C., Strolin Benedetti M. Absorption and disposition of levocetirizine, the eutomer of cetirizine administered alone or as cetirizine to healthy volunteers. Fundam. Clin. Pharmacol. 15:2001;269-277.
10. 14C ]levocetirizine, the R enantiomer of cetirizine, in healthy volunteers Eur. J. Clin. Pharmacol. 57:2001;571-582.
11. Reist M. Racemization of clinical drugs: methods, mechanisms and applications. Ph.D. thesis, University of Lausanne; 1996.
12. Slater J.W., Zechnich A.D., Haxby D.G. Second-generation antihistamines. A comparative review. Drugs. 57:1999;31-47.
13. Campoli-Richards D.M., Buckley M.M., Fitton A. Cetirizine: a review of its pharmacological properties and clinical potential in allergic rhinitis, pollen-induced asthma, and chronic urticaria. Drugs. 40:1990;762-781.
14. Renwick A.G. The metabolism of antihistamines and drug interactions: the role of cytochrome P450 enzymes. Clin. Exp. Allergy. 29:1999;116-124.
15. 1-receptor antagonist. J. Med. Chem. 41:1998;853-863.
16. 1) antagonists. Allergy. 50:1995;12-16.
17. 1 receptor antagonist in humans. Fundam. Clin. Pharmacol. 16:2002;471-478.
18. Sienra-Monge J.J., Gazca-Aguilar A., Del Rio-Navarro B. Double-blind comparison of cetirizine and loratadine in children ages 2 to 6 with perennial allergic rhinitis. Am. J. Ther. 6:1999;149-155.
19. 14C ]-cetirizine in humans Ann. Allergy. 59:1987;31-34.