Effect of Itraconazole and Ticlopidine on the Pharmacokinetics and Pharmacodynamics of Oral Tramadol
Status:
Completed
Trial end date:
2010-12-01
Target enrollment:
Participant gender:
Summary
Tramadol is an opioid analgesic, which is widely used in the treatment of acute and
neuropathic pain. After oral administration, tramadol is rapidly and almost completely
absorbed. Tramadol is extensively metabolised by O- and N-demethylation, which are catalysed
by the liver CYP-450 enzymes. O-desmethyltramadol is an active metabolite and its formation
is catalysed by CYP2D6. The formation of inactive metabolites is catalysed by CYP3A4 and 2B6.
This study is aimed to investigate the possible interaction of oral tramadol with
itraconazole and ticlopidine, which are inhibitors of CYP3A4 and 2B6. Twelve healthy male or
female adult non-smoking volunteers aged 18-40 years with body weights within ±15% of the
ideal weight for height are taken into the study. Primary endpoints of the study are plasma
concentrations of tramadol and its metabolites.