Pharmacology · MAO-B inhibitors
Safinamide !
A reversible MAO-B inhibitor added to levodopa for «off» episodes. It also reduces glutamate release; same interaction cautions as other MAO-B inhibitors.
Updated 2026-11-01
The figure shows safinamide bound reversibly (not covalently) in the substrate cavity of human MAO-B.
Mechanism of action
Safinamide inhibits MAO-B reversibly, unlike selegiline and rasagiline, so striatal dopamine lasts longer. It also reduces glutamate release, an action that may add to its effect.
- Safinamide occupies the MAO-B active site reversibly
- Dopamine is broken down more slowly
- Glutamate release is also reduced
- Off episodes become shorter
Pharmacokinetics
- Metabolism
- Liver; dose limited in moderate liver impairment and avoided in severe liver disease
Indications
- Add-on to levodopa + carbidopa for off episodes in Parkinson disease Parkinson disease →
Adverse effects
Common
- Dyskinesia (worse or more frequent involuntary movements)
- Nausea
- Insomnia
Contraindications
- Severe liver impairment
- Other MAO inhibitors, including linezolid and methylene blue
- Opioids such as meperidine, dextromethorphan, St John's wort (class contraindications)
Key interactions
- MAO inhibitors, linezolid, methylene blue
- Hypertensive or serotonergic reactions
- Antidepressants (SSRIs, SNRIs, tricyclics)
- Serotonin syndrome risk
- Dextromethorphan and St John's wort
- Serotonergic toxicity
- Sympathomimetics and very tyramine-rich foods
- Rise in blood pressure
What is monitored
- Dyskinesia and hallucinations
- Blood pressure
- Liver function
- Vision changes
Administration and safety
- Always used together with levodopa
- Tapered rather than stopped abruptly
- A drug-free gap is needed before starting other MAO inhibitors
Nursing care
- Check every new medicine, cough syrup or herbal product for interactions
- Ask about sudden sleep and warn about driving
- Record changes in involuntary movements
Pregnancy and breastfeeding
Human data are limited; pregnancy during treatment is discussed with the specialist.
Test yourself
Think of the answer, then tap the question to see it.
How does safinamide differ from rasagiline at the enzyme?
Safinamide inhibits MAO-B reversibly; rasagiline and selegiline inhibit it irreversibly.
For which problem is safinamide added to levodopa?
Off episodes in Parkinson disease.
Which second action besides MAO-B inhibition does safinamide have?
It reduces glutamate release.
Related drugs
Related conditions
← Back to the class: 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: Safinamide: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2017); Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed., ch. 21 (McGraw Hill, 2023); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).
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Representative model, for educational purposes only.