Selegiline (Eldepryl)

Selegiline (Tradename: Eldepryl) is a monoamine oxidase inhibitor (MAOI) used in the treatment of Parkinson's disease and depression.

Pharmacokinetics of Selegiline

Selegiline: Cytochrome P450 Metabolism

Substrate of (Metabolized by)
Induces
Inhibits

Mnemonic

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

Starting
Titration
Maximum
Taper
  • 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]