|
KMID : 0391020070150010046
|
|
Journal of Korean Society for Clinical Pharmacology and Therapeutics
2007 Volume.15 No. 1 p.46 ~ p.56
|
|
|
Single-dose Pharmacokinetics of Desloratadine in Healthy Korean Volunteers
|
|
Yi So-Jeong
Cho Joo-Youn
Jang In-Jin
Shin Sang-Goo
Yu Kyung-Sang
Chung Jae-Yong
Kim Jung-Ryul
Lim Kyoung-Soo
Kim Jae-Woo
Kim Bo-Hyung
|
|
|
Abstract
|
|
|
Background: Desloratadine, a nonsedating histamine receptor antagonist, is an orally active major metabolite of loratadine. We investigated the pharmacokinetic (PK) characteristics of a single oral dose of desloratadine in healthy Korean male volunteers.
Methods: A parallel group, rising single dose (5, 10 and 20 mg), block (dose) randomized, double-blind, placebo-controlled study was conducted in 36 healthy male volunteers. Subjects were randomized into each dose group (placebo: active drug= 2: 10 subjects). Plasma concentrations of deslorataine and its major metabolite, 3-OH desloratadine were measured till 168 hours after drug administration. The results were compared to Caucasian data from a previous study.
Results: The mean were 37.9, 81.8, 172.2 and were 2.4, 5.0, 9.9 in 5, 10 and 20 mg dose groups, respectively. The range of mean metabolic ratio by dose groups was . and of desloratadine and 3-OH desloratadine exhibited linear properties over a dose range of 5 to 20 mg. Mean terminal elimination half-life () was 25 hours for desloratadine, and 38 hours for 3-OH desloratadine. The geometric mean ratios(90% confidence interval) for Koreans to Caucasians were 1.3 (1.06-1.60) for dose-normalized and 1.3 (1.11-1.51) for dose-normalized ; PK parameters of desloratadine in Koreans showed statistically significant differences with the PK parameters in Caucasians. However, desloratadine has a wide safety margin and flat dose-response relationship, so approximately 1.3 times higher exposure is not thought to be clinically significant.
Conclusions: The PK parameters of desloratadine in Koreans were linear according to dose increments. Comparison of the and values between Koreans and Caucasians indicates no clinically relevant difference that requires dosage adjustment for desloratadine in Koreans.
|
|
|
KEYWORD
|
|
|
Desloratadine, Pharmacokinetics, Korean
|
|
|
FullTexts / Linksout information
|
|
|
|
|
Listed journal information
|
|
 
|
|