Pharmacology · MAO-B inhibitors
Rasagiline !
An irreversible, selective MAO-B inhibitor for Parkinson disease, alone or with levodopa. No amphetamine metabolites; serious serotonergic interactions.
Updated 2026-11-01
The figure shows rasagiline in human MAO-B, attached covalently to the FAD cofactor (the crystal records the adduct form).
Mechanism of action
Rasagiline is a propargylamine that inactivates MAO-B irreversibly by bonding to its flavin. Striatal dopamine lasts longer. Unlike selegiline it is not metabolized to amphetamines. It is cleared mainly by liver CYP1A2.
- Rasagiline binds the FAD of MAO-B irreversibly
- Striatal dopamine is broken down more slowly
- Early symptoms ease; off time shortens with levodopa
Pharmacokinetics
- Metabolism
- Liver, mainly CYP1A2; levels rise with ciprofloxacin and in liver disease
- Onset and duration
- Enzyme inhibition persists until new MAO-B is synthesized
Indications
- Parkinson disease, as monotherapy in early disease or added to levodopa for wearing-off Parkinson disease →
Adverse effects
Common
- Headache, joint pain, indigestion
- Dyskinesia and orthostatic hypotension with levodopa
- Somnolence
Contraindications
- Meperidine, tramadol, methadone, propoxyphene and other MAO inhibitors (wait at least 14 days after stopping)
- Dextromethorphan, St John's wort and cyclobenzaprine
- Moderate or severe liver impairment (not used)
Key interactions
- SSRIs, SNRIs, tricyclic and other antidepressants
- Risk of serotonin syndrome; close monitoring if combined
- Ciprofloxacin and other CYP1A2 inhibitors
- Higher rasagiline levels; dose is limited
- Sympathomimetics (decongestants, some cold remedies)
- Rise in blood pressure
- Dextromethorphan
- Episodes of psychosis or bizarre behaviour; contraindicated
What is monitored
- Blood pressure
- Every new prescription and over-the-counter product for interactions
- Liver function before starting
- Dyskinesia, hallucinations and impulse-control behaviours
Administration and safety
- Given once a day by mouth
- At least two weeks must pass after stopping before starting interacting drugs
- Pharmacy should check every new opioid, antidepressant or cough medicine
Nursing care
- Teach to avoid foods with very high tyramine, such as some aged cheeses
- Teach to avoid dextromethorphan cough syrups and St John's wort
- Recognize serotonin syndrome: agitation, fever, sweating, tremor, rigidity
- Check blood pressure at visits
Pregnancy and breastfeeding
There are no adequate human data; animal studies showed reduced offspring survival.
Test yourself
Think of the answer, then tap the question to see it.
Which drugs are contraindicated with rasagiline?
Meperidine, tramadol, methadone, dextromethorphan, St John's wort, cyclobenzaprine or other MAO inhibitors.
How does rasagiline differ from selegiline in its metabolites?
Rasagiline does not produce amphetamine metabolites.
Why does ciprofloxacin matter with rasagiline?
It inhibits CYP1A2, the main enzyme that clears rasagiline, so levels rise.
Related drugs
Related conditions
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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 - RASAGILINE tablet (DailyMed (U.S. National Library of Medicine), 2026); Rasagiline: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2016); 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.