Rasagiline
A selective, irreversible MAO-B inhibitor for Parkinson's disease, used alone early on or added to levodopa.
Drug card
- Class
- MAO-B inhibitor
- How it works
- Blocking MAO-B, the brain enzyme that breaks down dopamine
- Used for
- Early Parkinson's disease, on its own
- Add-on to levodopa for end-of-dose wearing off
- Known for
- Serotonin syndrome with antidepressants or opioids
- Its name
- -giline means an MAO-B inhibitor
Study it as a flashcard, and it comes back before you forget it.
Mechanism of action
How does rasagiline work?
A potent, irreversible and selective MAO-B inhibitor that raises extracellular dopamine in the striatum. The liver breaks it down, mainly through CYP1A2, to aminoindan metabolites; the main one, 1-aminoindan, does not inhibit MAO-B. Unlike selegiline it forms no amphetamine metabolites.
Like other MAO-B inhibitors: MAO-B inhibitors irreversibly block monoamine oxidase type B, the main form of the enzyme in the human brain, where it breaks down dopamine. With less breakdown, more dopamine stays in the striatum, easing Parkinson's symptoms and cutting 'off' time on levodopa. At licensed doses they spare MAO-A, which clears dietary tyramine in the gut, but this selectivity fades as the dose rises.
Uses
What is rasagiline used for?
- Early Parkinson's disease, on its own
- Add-on to levodopa for end-of-dose wearing off
Side effects
Side effects of rasagiline
- Serotonin syndrome with antidepressants or opioidsKnown forSerious
- Headache
- Joint and muscle pain
- Flu-like symptoms
- Low mood (depression)
- Dyskinesia and falls when added to levodopa
- Low blood pressure on standing
- Raised blood pressure
- Hypertensive crisis with very tyramine-rich foodSerious
- HallucinationsSerious
- Daytime sleepiness and sudden sleepSerious
- Compulsive gambling or spendingSerious
Known for marks what an exam expects you to know it for.
Watch for
Cautions and what sets it apart
- Contraindicated with other MAO inhibitors, pethidine, tramadol, methadone, St John's wort and dextromethorphan.
- Fluoxetine and fluvoxamine are avoided; at least 5 weeks must pass after fluoxetine before starting it.
- Ciprofloxacin and other CYP1A2 inhibitors raise its levels; it is avoided in moderate or severe liver disease.
- A possible link to melanoma means new or changing skin lesions are checked.
Good to know: At its licensed dose it is selective enough that tyramine limits are not usually needed, though foods with very large amounts are avoided.
Remember it
A way to remember it
B for brain, A for abdomen.
MAO-B is the main form in the brain, where blocking it spares dopamine; MAO-A dominates in the gut, where it breaks down tyramine from food, so sparing it keeps the cheese reaction rare at licensed doses.
Written for biofideX
Its name
-giline means MAO-B inhibitor
Selegiline and rasagiline block MAO-B, the main form of the enzyme in the brain, slowing dopamine breakdown in Parkinson's disease. Phenelzine, an MAO inhibitor for depression, lacks it.
- Every drug name stem
Its class
MAO-B inhibitors
Other MAO-B inhibitors with a card:
Easily mixed up with monoamine oxidase inhibitors and dopamine agonists.
Sources
Checked against
Written for biofideX in plain words, after checking these references:
For learning pharmacology, not for treatment decisions: no doses are given, and a prescriber, pharmacist or the product's own label is the word on any one patient. Spotted a mistake? Tell us and we'll correct it.
Parkinson's, dementia and migraine
Rasagiline is one of 9 drugs practiced together here: their classes, how they work, what they treat and what they're known for.
Start Practicing