[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [MAO-B inhibitors](https://durgical.com/en/pharmacology/classes/mao-b-inhibitors/) › Selegiline

[Pharmacology](https://durgical.com/en/pharmacology/) · [MAO-B inhibitors](https://durgical.com/en/pharmacology/classes/mao-b-inhibitors/)

# Selegiline

An irreversible MAO-B inhibitor for Parkinson disease. It forms amphetamine metabolites and has serious interactions with meperidine and antidepressants.

Updated 2026-11-01

- Class: [MAO-B inhibitors](https://durgical.com/en/pharmacology/classes/mao-b-inhibitors/)
- Enzyme: Monoamine oxidase B (MAO-B)
- ATC code: N04BD01

Also called: L-deprenyl

✂**Monoamine oxidase B (MAO-B)**Selegiline

ⓘ The figure shows deprenyl (selegiline) in human MAO-B, next to the FAD cofactor it binds covalently.

**Target in 3D:** Monoamine oxidase B (MAO-B). PDB structure 2BYB (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/2BYB) · Drag to rotate · pinch to zoom

## Mechanism of action

Selegiline is a «suicide» substrate of MAO-B: the enzyme converts it to a reactive form that binds its flavin cofactor irreversibly. Less dopamine is broken down in the striatum. Selectivity for MAO-B depends on dose and is lost at higher doses. It is metabolized to L-amphetamine and L-methamphetamine.

- MAO-B activates selegiline, which binds its FAD for good
- Striatal dopamine is broken down more slowly
- Levodopa effects last longer

## Pharmacokinetics

**Metabolism**
Extensive first-pass metabolism to desmethylselegiline, L-amphetamine and L-methamphetamine

**Onset and duration**
Enzyme inhibition lasts until new MAO-B is made, beyond the drug's presence in blood

## Indications

- Parkinson disease, as an adjunct to levodopa + carbidopa when the response is fading, or early in the disease [Parkinson disease →](https://durgical.com/en/conditions/parkinson-disease/)

## Adverse effects

### Common

- Nausea, dizziness, dry mouth
- Insomnia and anxiety (amphetamine metabolites)
- More dyskinesia and hallucinations when added to levodopa
- Orthostatic hypotension

### Serious (rare, important)

- Stupor, rigidity, agitation and fever with meperidine
- Severe CNS toxicity with tricyclic or SSRI antidepressants (serotonin syndrome)
- Hypertensive crisis with sympathomimetics or tyramine at higher doses

## Contraindications

- Meperidine (often extended to other opioids)
- Hypersensitivity to selegiline

## Key interactions

**Meperidine, tramadol, methadone**
Serotonin toxicity: agitation, rigidity, hyperthermia

**SSRIs, SNRIs, tricyclic antidepressants**
Serotonin syndrome and severe CNS toxicity

**Ephedrine and other sympathomimetics (cough and cold products)**
Hypertensive crisis

**Levodopa + carbidopa**
More dyskinesia; severe orthostatic hypotension reported

## What is monitored

- Blood pressure (high and orthostatic)
- Sleep, anxiety and hallucinations
- All new medicines, including over-the-counter cold remedies and opioids

## Administration and safety

- Doses are given with breakfast and lunch, not in the evening
- Oral tablets, capsules, orally disintegrating tablets and a skin patch are different products
- A drug-free gap is needed before starting interacting drugs

## Nursing care

- Flag the record: no meperidine; check every new opioid or antidepressant
- Teach to avoid decongestants and very tyramine-rich foods
- Check blood pressure and ask about sleep
- Watch for agitation, fever, sweating or muscle rigidity

## Pregnancy and breastfeeding

Human data are lacking; animal studies did not show malformations.

## Memory aid

«SelegiLINE draws a line: no Meperidine, no Mixing antidepressants, and it Makes amphetamine».

## Test yourself

Think of the answer, then tap the question to see it.

## Which metabolites of selegiline explain its insomnia and anxiety?

L-amphetamine and L-methamphetamine.

## Which opioid is contraindicated with selegiline?

Meperidine (stupor, rigidity, agitation, hyperthermia); the warning is often extended to other opioids.

## What happens to MAO-B selectivity at higher selegiline doses?

It is lost: MAO-A is also inhibited, so tyramine and pressor reactions become possible.

[Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/selegiline/)

## Related drugs

- [Rasagiline](https://durgical.com/en/pharmacology/rasagiline/)
- [Safinamide](https://durgical.com/en/pharmacology/safinamide/)
- [Levodopa + carbidopa](https://durgical.com/en/pharmacology/levodopa-carbidopa/)

## Related conditions

- [Parkinson disease](https://durgical.com/en/conditions/parkinson-disease/)

[← Back to the class: MAO-B inhibitors](https://durgical.com/en/pharmacology/classes/mao-b-inhibitors/)

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: [DailyMed - SELEGILINE HYDROCHLORIDE tablet](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=2aa9f8ee-6a86-6cf1-bec7-6a1ffa5e1ae2) (DailyMed (U.S. National Library of Medicine), 2026); [Selegiline: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a697046.html) (MedlinePlus (U.S. National Library of Medicine), 2022); Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed., ch. 21 (McGraw Hill, 2023).

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Representative model, for educational purposes only.

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