The influence of a single and chronic administration of venlafaxine on tramadol pharmacokinetics in a rabbit model
The combined use of tramadol with selective serotonin and norepinephrine reuptake inhibitors e.g. venlafaxine may be associated with serotonin syndrome. No previous studies exist examining the influence of a weak CYP2D6 inhibitor venlafaxine on the pharmacokinetics of tramadol. Therefore, the aim of...
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Published in | Pharmacological reports Vol. 69; no. 3; p. 555 |
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Main Authors | , , , , , , , |
Format | Journal Article |
Language | English |
Published |
Switzerland
01.05.2017
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Subjects | |
Online Access | Get full text |
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Summary: | The combined use of tramadol with selective serotonin and norepinephrine reuptake inhibitors e.g. venlafaxine may be associated with serotonin syndrome. No previous studies exist examining the influence of a weak CYP2D6 inhibitor venlafaxine on the pharmacokinetics of tramadol. Therefore, the aim of this study was to determine the effect of a single and chronic administration of venlafaxine on the pharmacokinetics of tramadol using a rabbit model.
Adult New Zealand white rabbits of both sexes (n = 21) were used. Animals received 100 mg of tramadol per os (one slow release tablet) and 75 mg of venlafaxine (one prolonged release capsule), and were divided into four groups: control group - a single dose of tramadol alone, 1 day group - a single dose of tramadol and venlafaxine, 7 and 14 days groups - seven and fourteen days administration of venlafaxine once daily plus a single dose of tramadol on the last day of the study.
Venlafaxine administration over a period of 7 and 14 days resulted in faster elimination of tramadol compared to the control group: significantly higher values of k
, and lower values of t
and MRT for the 7 and 14 days group were observed. Although no differences in bioavailability of tramadol were obtained.
Using a rabbit model, there is no evidence that the combined administration of tramadol and venlafaxine may increase the plasma exposure of tramadol and therefore increase the risk of serotonin syndrome. |
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ISSN: | 1734-1140 |