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Drug Metabolism Letters


ISSN (Print): 1872-3128
ISSN (Online): 1874-0758

Pharmacokinetics and Metabolism of Diltiazem Following Multiple Doses:Comparing Normotensive Rat vs. Hypertensive Rat Models In vivo

Author(s): Pollen K.F. Yeung, Angelita Alcos, Jinglan Tang and William l. Casley

Volume 2, Issue 2, 2008

Page: [146 - 150] Pages: 5

DOI: 10.2174/187231208784040915

Price: $65


In order to identify a suitable rodent model for preclinical study of calcium antagonists, pharmacokinetics and metabolism of diltiazem (DTZ) were compared in normotensive SD and hypertensive SHR rat models following multiple doses (5 mg/kg twice daily for 5 doses). Plasma concentrations of DTZ and its major metabolites appeared to be higher in the SHR than the SD rats, although the differences did not reach statistical significance (p > 0.05). The preliminary results suggest metabolism profile of DTZ in the SHR may be closer to humans than the SD rats and may be more preferred in pre-clinical drug development studies for DTZ.

Keywords: Metabolism, pharmacokinetics, diltiazem, rats, SHR

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