Pharmacokinetics and absolute bioavailability of selegiline following treatment of healthy subjects with the selegiline transdermal system (6 mg/24 h): a comparison with oral selegiline capsules

J Clin Pharmacol. 2007 Oct;47(10):1256-67. doi: 10.1177/0091270007304779. Epub 2007 Aug 22.


The selegiline transdermal system is a monoamine oxidase inhibitor that was recently approved by the US Food and Drug Administration for the treatment of major depressive disorder. The current study was conducted during the selegiline transdermal system development program to characterize the single-dose pharmacokinetics and absolute bioavailability of selegiline administered by the 6-mg/24-h selegiline transdermal system in healthy volunteers. Selegiline transdermal system results were compared with those obtained after a single 10-mg oral dose of selegiline HCl. The selegiline pharmacokinetics differed greatly between the 2 routes of administration. Transdermal selegiline administration reduced metabolism and produced a high, sustained plasma selegiline concentration over the dosing period, with an absolute bioavailability of 73%. By contrast, oral dosing produced a sharp plasma selegiline peak that occurred within 1 hour and declined rapidly, with an absolute bioavailability of 4%. The data provide the basis for therapeutic advantages of the selegiline transdermal system in administering antidepressant doses of selegiline.

Publication types

  • Comparative Study
  • Randomized Controlled Trial

MeSH terms

  • Administration, Cutaneous
  • Administration, Oral
  • Adolescent
  • Adult
  • Antidepressive Agents / administration & dosage*
  • Antidepressive Agents / adverse effects
  • Antidepressive Agents / blood
  • Antidepressive Agents / pharmacokinetics*
  • Area Under Curve
  • Biological Availability
  • Capsules
  • Cross-Over Studies
  • Dose-Response Relationship, Drug
  • Humans
  • Male
  • Middle Aged
  • Monoamine Oxidase Inhibitors / administration & dosage*
  • Monoamine Oxidase Inhibitors / adverse effects
  • Monoamine Oxidase Inhibitors / blood
  • Monoamine Oxidase Inhibitors / pharmacokinetics*
  • Selegiline / administration & dosage*
  • Selegiline / adverse effects
  • Selegiline / blood
  • Selegiline / pharmacokinetics*


  • Antidepressive Agents
  • Capsules
  • Monoamine Oxidase Inhibitors
  • Selegiline