Trade names are Eldepryl, Zelapar and Selgene.
Routes of administrative are oral, transdermal, and buccal.
Has a bioavailability of 4.4% oral fasting, 20% after food and 18% by patch.
Has protein binding of 90% and hepatic metabolism.
Half-life of 10 hours orally and 18-25 hours transdermally.
A drug for the treatment of early-stage Parkinson’s disease, depression and dementia.
It is a selective irreversible MAO-B inhibitor, however, in larger doses it also inhibits MAO-A.
Dietary restrictions for lower doses is unnecessary.
In the treatment of Parkinson’s disease it can be used alone or in a combination with another agent, most often L-DOPA.
For the newly diagnosed Parkinson’s patients, it may slow the progression of the disease, although this is controversial.
Felt to delay the time when the L-DOPA (levodopa) treatment for Parkinson’s disease becomes necessary from 10-12 to 18 months.
Adding selegiline to levodopa decreases the dose of levodopa by about 40% and reduces its the motor complications.
Selegiline + levodopa also extends the time until the levodopa dose had to be increased from 2.6 to 4.9 years.
Approved to treat major depression using a transdermal patch (Emsam Patch).
Minor side effects: dizziness, dry mouth, difficulty falling or staying asleep, muscle pain, rash, nausea and constipation.
More serious side effects: headache, tachycardia, arrhythmia, hallucinations, chorea, or difficulty breathing.
A selective inhibitor of MAO-B.
MAO-B metabolizes dopamine and phenylethylamine.
Has little therapeutic benefit when used alone in PD, but enhances and prolongs the anti-Parkinson effects of levodopa.
Has a low oral bioavailability, which increases when ingested together with a high-fat meal.
Oral bioavailability is significantly increased in females taking oral contraceptives by10- to 20-fold.
Selegiline is partly metabolized to L-methamphetamine, and may also cause persons taking selegiline to test positive for amphetamine and or methamphetamine on drug screening tests.
Selegiline in combination with the older non-selective MAOIs requires a low tyramine diet.
The risk of a true serotonin syndrome with SSRIs and selegiline is quite low.
A combination of selegiline with fluoxetine can lead to severe reactions.
Is available as a transdermal patch for use in treating major depression (EMSAM).
Available as a transmucosal preparation with lowered GI effects compared to oral selegiline (Zelapar).