Selegiline (Eldepryl)

Pharmacokinetics of Selegiline

Selegiline: Cytochrome P450 Metabolism

Substrate of (Metabolized by)


At the right doses, SELEgiline SELEctively inhibits MOA-B (B for Brain)
  • Selegiline is a centrally acting irreversible monoamine oxidase type B (MAO-B) inhibitor.
    • This increases dopamine availability (and hence why it is also used in Parkinson's)
  • It has greater affinity for MAO type B than MAO type A, and thus serves as a selective inhibitor of MAO-B when administered at the recommended dose.
    • At larger doses, it loses its specificity and also inhibits MAO-A.
  • Two active metabolites of selegiline are l-amphetamine and l-methamphetamine, which interfere with neuronal re-uptake and enhance the release of several neurotransmitters (e.g. - norepinephrine, dopamine, serotonin). The extent to which these neurotransmitters contribute to selegiline’s effects are unknown.[1]
  • In patients with advanced Parkinson’s Disease, selegiline increases dopamine levels reducing the breakdown of dopamine generated from levodopa. Thus, selegiline improves the therapeutic effect of levodopa.

Dosing for Selegiline

  • Selegiline comes in oral formulation
  • Selegiline can only be used safely without dietary restrictions at doses where it selectively inhibits MAO-B (e.g. - 10 mg/day).[2]
  • Selegiline is thought to have no to little sexual side effects.[3]