title: Effect of race and sex on single and multiple dose pharmacokinetics of desloratadine.
abstract: OBJECTIVE
  This study was designed to characterise the single and multiple dose pharmacokinetic profile of desloratadine, a new antihistamine, and its main metabolite, 3-hydroxy (3-OH) desloratadine, in healthy volunteers differing in sex and race.
  
  
  METHODS
  An open-label, parallel-group, single- and multiple-dose pharmacokinetic trial.
  
  
  METHODS
  A single 7.5mg oral tablet of desloratadine on day 1, followed by 7.5mg daily doses on days 4 to 17.
  
  
  METHODS
  48 healthy, nonsmoking volunteers (12 White men, 12 Black men, 12 White women, 12 Black women).
  
  
  METHODS
  AUC(24h) and C(max) determined from serial blood samples of desloratadine and 3-OH desloratadine.
  
  
  RESULTS
  There were no clinically relevant differences between men and women or Black participants and White participants for desloratadine and 3-OH desloratadine maximum plasma concentrations (C(max)) and area under the plasma concentration-time curve (AUC). Following multiple doses, the geometric mean C(max) was 5.17 microg/L in men, 5.68 microg/L in women, 5.87 microg/L in Black participants and 5.00 microg/L in White participants; the corresponding AUC from 0 to 24 hours (AUC(24h)) values were 77.9, 80.0, 90.6 and 68.8 micro g/L x h. Corresponding 3-OH desloratadine geometric mean C(max) values were 1.93, 2.79, 2.20 and 2.45 microg/L, and the AUC(24h) values were 32.1, 47.5, 37.1 and 41.1 microg/L. h.
  
  
  CONCLUSIONS
  Oral administration of multiple doses of desloratadine 7.5mg, a dose 50% higher than the recommended 5mg clinical dose, was well tolerated by healthy adults differing in sex and race. Comparison of the C(max) and AUC values following 14 days of treatment with desloratadine indicates that no dosage adjustment is needed on the basis of sex or race.
authors.affiliation: Schering-Plough Research Institute, Kenilworth, New Jersey 07033-0539, USA.
authors.forename: Melton
authors.initials: M
authors.lastname: Affrime
authors.forename: Christopher
authors.initials: C
authors.lastname: Banfield
authors.forename: Samir
authors.initials: S
authors.lastname: Gupta
authors.forename: Albert
authors.initials: A
authors.lastname: Cohen
authors.forename: Tanya
authors.initials: T
authors.lastname: Boutros
authors.forename: Mohan
authors.initials: M
authors.lastname: Thonoor
authors.forename: Mitchell
authors.initials: M
authors.lastname: Cayen
mesh_terms: D000284:Administration, Oral; D000328:Adult; D019540:Area Under Curve; D044383:Black People; D004334:Drug Administration Schedule; D005260:Female; D006634:Histamine H1 Antagonists / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D006801:Humans; D017336:Loratadine / Q000008:administration & dosage / Q000031:analogs & derivatives / Q000097:blood / Q000493:pharmacokinetics*; D008297:Male; D008875:Middle Aged; D012737:Sex Factors; D044465:White People
chemical_list: D006634:Histamine H1 Antagonists; D017336:Loratadine; C121345:desloratadine