Publication Cover
Xenobiotica
the fate of foreign compounds in biological systems
Volume 37, 2007 - Issue 7
282
Views
26
CrossRef citations to date
0
Altmetric
Research Article

Disposition of desloratadine in healthy volunteers

, , , , , , , , & show all
Pages 770-787 | Received 02 Apr 2007, Accepted 21 May 2007, Published online: 22 Sep 2008
 

Abstract

The absorption, metabolism and excretion of desloratadine (DL, Clarinex®) were characterized in six healthy male volunteers. Subjects received a single oral 10-mg dose of [14C]DL (∼104 µCi). Blood, urine and feces were collected over 240 h. DL was well absorbed; drug-derived radioactivity was excreted in both urine (41%) and feces (47%). With the exception of a single subject, DL was extensively metabolized; the major biotransformation pathway consisted of hydroxylation at the 3 position of the pyridine ring and subsequent glucuronidation (3-OH-DL-glucuronide or M13). In five of the six subjects, DL was slowly eliminated (mean t½ = 19.5 h) and persisted in the plasma for 48–120 h post-dose. This is in contrast to a t½ of ∼110 h and quantifiable plasma DL concentrations for the entire 240-h sampling period in one subject, who was identified phenotypically as a poor metabolizer of DL. This subject also exhibited correspondingly lower amounts of M13 in urine and 3-OH-DL (M40) in feces. Disposition of DL in this subject was characterized by slow absorption, slow metabolism and prolonged elimination. Further clinical studies confirmed the lack of safety issues associated with polymorphism of DL metabolism (Prenner et al. 2006, Expert Opinion on Drug Safety, 5: 211–223).

Acknowledgements

The authors acknowledge all LOR-related synthetic efforts of the Radiochemistry Group at SPRI under the direction of Dr Paul McNamara. We are also grateful to Dr James Hubbell (SPRI) for fruitful discussions. Finally, the authors thank PPD Pharmaco, Inc. for quantitative bioanalysis support.

Log in via your institution

Log in to Taylor & Francis Online

PDF download + Online access

  • 48 hours access to article PDF & online version
  • Article PDF can be downloaded
  • Article PDF can be printed
USD 65.00 Add to cart

Issue Purchase

  • 30 days online access to complete issue
  • Article PDFs can be downloaded
  • Article PDFs can be printed
USD 897.00 Add to cart

* Local tax will be added as applicable

Related Research

People also read lists articles that other readers of this article have read.

Recommended articles lists articles that we recommend and is powered by our AI driven recommendation engine.

Cited by lists all citing articles based on Crossref citations.
Articles with the Crossref icon will open in a new tab.