Sinclair, J.M.A., Birtwistle, J. and Baldwin, D.S.
The tolerability of venlafaxine
Reviews in Contemporary Pharmacotherapy, 9, (5), .
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The need to reduce unwanted effects and improve the safety profile of a drug, particularly in overdose, must be an important consideration when assessing the overall value of a new treatment. Although accurately assessing the relative burden of the adverse effects of different drugs can be difficult, the current evidence suggests that the pharmacological properties of venlafaxine may underpin its favourable safety and tolerability profile. When compared to many of the first and second generation antidepressants, it appears to be relatively well tolerated, and preliminary data indicate that it is safe in overdose. Comparison with the SSRI fluoxetine revealed no significant differences in the safety profiles of the two drugs. With its extensive frist pass metabolism to the active metabolite O-desmethylvenlafaxine, the main focus for potential drug-drug interactions with venlafaxine is the effect it may have on the cytochrome P450 system. In vitro studies suggested that, when compared to SSRIs, venlafaxine had only a modest inhibitory effect on the metabolic capacity of the P450 system, and clinical studies have shown that it has minimal drug-drug interactions. Venlafaxine is consequently well tolerated in the elderly and in those requiring concomitant medication for physical illness. New data suggest that, whilst contraindicated during pregnancy, accidental exposure to venlafaxine does not appear to be associated with an increased risk of foetal abnormalities.
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