- Last edited on September 20, 2022
Selegiline (Eldepryl)
Primer
Selegiline (Tradename: Eldepryl) is a monoamine oxidase inhibitor (MAOI) used in the treatment of Parkinson's disease and depression.
Pharmacokinetics
See also article: Introduction to Pharmacology
Pharmacokinetics of Selegiline
Cytochrome P450 Metabolism
See also article: Cytochrome (CYP) P450 Metabolism
Selegiline: Cytochrome P450 Metabolism
| Substrate of (Metabolized by) | |
|---|---|
| Induces | |
| Inhibits |
Pharmacodynamics
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.
Toxicity
Indications
- Parkinson's Disease, in newly diagnosed patients, selegiline was shown to delay the need to implement levodopa therapy.
Dosing
Dosing for Selegiline
| Starting | |
|---|---|
| Titration | |
| Maximum | |
| Taper |
Formulations
- Selegiline comes in oral formulation
Monitoring
Dietary Restriction
- Selegiline can only be used safely without dietary restrictions at doses where it selectively inhibits MAO-B (e.g. - 10 mg/day).[2]
Contraindications
Absolute
- Extrapyramidal symptoms such as excessive tremor or tardive dyskinesia, or in patients with severe psychosis or severe dementia
- Do not combine with selective serotonin reuptake inhibitors and tricyclic antidepressants (risk of serotonin syndrome)
- Meperidine and opioids
- Active peptic ulcer
Relative
Drug-Drug Interactions
Side Effects
Adverse Events
Clinical Pearls
- Selegiline is thought to have no to little sexual side effects.[3]
Special Populations
Geriatric
See main article: Geriatric Pharmacology
Pediatric
See main article: Pediatric Pharmacology
Obstetric and Fetal
See main article: Obstetric and Fetal Pharmacology
Medically Ill
See main article: Psychotropic Dosing in the Medically Ill
Resources
References
1)
Health Canada. PRODUCT MONOGRAPH PrAPO-SELEGILINE Selegiline Hydrochloride Tablets USP
2)
Health Canada. PRODUCT MONOGRAPH PrAPO-SELEGILINE Selegiline Hydrochloride Tablets USP
3)
Clayton, A. H., Campbell, B. J., Favit, A., Yang, Y., Moonsammy, G., Piontek, C. M., & Amsterdam, J. D. (2007). Symptoms of sexual dysfunction in patients treated for major depressive disorder: a meta-analysis comparing selegiline transdermal system and placebo using a patient-rated scale. The Journal of clinical psychiatry, 68(12), 1860-1866.