Jayasree J Nandagopal1, Melissa P DelBello. 1. University of Cincinnati, Department of Psychiatry, 260 Stetson Street, Suite 3200, Cincinnati, OH 45267-0559, USA. jayasree.nandagopal@uc.edu
Abstract
BACKGROUND: The use of monoamine oxidase inhibitors has declined owing to the risk of hypertensive crisis following the consumption of tyramine-rich foods and the consequent need for dietary tyramine restriction. However, owing to their superior efficacy in treating depression, continued efforts have been made to develop more selective and reversible monoamine oxidase inhibitors. Oral selegiline, at low doses, is a selective monoamine oxidase B (MAO-B) inhibitor, but at higher doses it loses its selectivity and can potentially interact with tyramine. Unfortunately, antidepressant effects of selegiline have been observed only at higher doses. The selegiline transdermal system was developed to deliver sustained selegiline blood concentrations sufficient to selectively inhibit MAO-A and MAO-B in the brain, producing antidepressant effects, without substantially inhibiting MAO-A in the gastrointestinal tract, thereby reducing the risk of hypertensive crisis. OBJECTIVES: This article reviews the basic pharmacology, as well as efficacy and safety data of selegiline transdermal system for the treatment of depression. CONCLUSIONS: Selegiline transdermal system is safe and effective in treating major depressive disorder at the dose range of 6 - 12 mg/24 h, without the need for dietary precautions at the 6 mg/24 h dose. No cases of hypertensive crisis were reported in clinical trials, even without dietary restrictions.
BACKGROUND: The use of monoamine oxidase inhibitors has declined owing to the risk of hypertensive crisis following the consumption of tyramine-rich foods and the consequent need for dietary tyramine restriction. However, owing to their superior efficacy in treating depression, continued efforts have been made to develop more selective and reversible monoamine oxidase inhibitors. Oral selegiline, at low doses, is a selective monoamine oxidase B (MAO-B) inhibitor, but at higher doses it loses its selectivity and can potentially interact with tyramine. Unfortunately, antidepressant effects of selegiline have been observed only at higher doses. The selegiline transdermal system was developed to deliver sustained selegiline blood concentrations sufficient to selectively inhibit MAO-A and MAO-B in the brain, producing antidepressant effects, without substantially inhibiting MAO-A in the gastrointestinal tract, thereby reducing the risk of hypertensive crisis. OBJECTIVES: This article reviews the basic pharmacology, as well as efficacy and safety data of selegiline transdermal system for the treatment of depression. CONCLUSIONS:Selegiline transdermal system is safe and effective in treating major depressive disorder at the dose range of 6 - 12 mg/24 h, without the need for dietary precautions at the 6 mg/24 h dose. No cases of hypertensive crisis were reported in clinical trials, even without dietary restrictions.
Authors: Landhing M Moran; Michael Y Aksenov; Rosemarie M Booze; Katy M Webb; Charles F Mactutus Journal: Curr HIV Res Date: 2012-07 Impact factor: 1.581