Rasagiline is a selective, irreversible monoamine oxidase-B (MAO-B) inhibitor used for the treatment of Parkinson's disease. It is considered a second-generation MAO-B inhibitor with improved selectivity compared to selegiline and does not produce amphetamine-like metabolites.
| Property |
Value |
| Drug Class |
MAO-B Inhibitor |
| Approval Status |
FDA Approved (2006) |
| Brand Name |
Azilect |
| Mechanism |
Selective, irreversible MAO-B inhibition |
| Route of Administration |
Oral |
| Half-life |
1-3 hours |
Rasagiline provides dopaminergic neuroprotection through multiple mechanisms:
- MAO-B Inhibition: Selectively and irreversibly inhibits MAO-B in the brain
- Metabolite Profile: Does NOT produce amphetamine metabolites (key advantage over selegiline)
- Neuroprotection: Exhibits anti-apoptotic and mitochondrial protective effects
- Synaptic Plasticity: May enhance dopaminergic neuronal survival
- Antioxidant Effects: Reduces oxidative stress in dopaminergic neurons
- Monotherapy: First-line treatment for early PD
- Adjunct to Levodopa: Reduces "off" time in advanced PD
- Motor Fluctuation Management: Improves wearing-off phenomenon
- Disease Modification: TEMPO and ADAGIO trials suggested potential disease-modifying effects
- TEMPO Trial (2002): Rasagiline monotherapy effective in early PD
- ADAGIO Trial (2009): Delayed-start study suggested disease-modifying potential
- LARGO Trial (2005): Adjunctive therapy reduced off-time
| Parameter |
Value |
| Bioavailability |
~35% |
| Protein Binding |
~60-70% |
| Metabolism |
Hepatic (CYP1A2 primarily) |
| Elimination |
Renal (~65%), Fecal (~20%) |
| Duration of Action |
24 hours (once-daily dosing) |
- Headache
- Nausea, indigestion
- Arthralgia
- Depression
- Insomnia
- Somnolence
- Dyskinesia (most common)
- Weight loss
- Orthostatic hypotension
- Hallucinations
- Hypertensive crisis (rare, with tyramine at high doses)
- Serotonin syndrome (with serotonergic drugs)
- Impulse control disorders (pathological gambling, hypersexuality)
| Interacting Drug |
Effect |
| SSRIs, SNRIs |
Serotonin syndrome risk (use with caution) |
| Tyramine-rich foods |
Hypertensive crisis (theoretical risk) |
| Ciprofloxacin |
Increased rasagiline levels |
| Tramadol, meperidine |
Serotonin syndrome risk |
| Feature |
Rasagiline |
Selegiline |
| Selectivity |
Higher MAO-B selectivity |
Lower (affects MAO-A at higher doses) |
| Metabolites |
No amphetamine-like |
Produces amphetamines |
| Dietary Restrictions |
None at therapeutic doses |
Required at higher doses |
| Dosing |
Once daily |
Often twice daily |
| Drug Interactions |
Fewer |
More common |
- Significant improvement in UPDRS scores
- Delayed need for levodopa
- Well-tolerated long-term
- Reduced off-time by ~1.5 hours/day
- Increased on-time without dyskinesia
- Allows levodopa dose reduction
- Disease Modification: Ongoing studies to confirm neuroprotective effects
- Combination Therapy: Studies with dopamine agonists
- Cognitive Benefits: Investigating effects on PD-related cognitive decline
- Biomarkers: Identifying predictors of treatment response
The study of Rasagiline Mao B Inhibitor For Parkinson'S Disease has evolved significantly over the past decades. Research in this area has revealed important insights into the underlying mechanisms of neurodegeneration and continues to drive therapeutic development.
Historical context and key discoveries in this field have shaped our current understanding and will continue to guide future research directions.
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- Olanow CW, et al. "A double-blind, delayed-start trial of rasagiline in Parkinson's disease." N Engl J Med. 2009;361(13):1268-1278. PMID:19798076
- Rascol O, et al. "Rasagiline as an adjunct to levodopa in patients with Parkinson disease and motor fluctuations: a randomized clinical trial." JAMA. 2005;293(6):737-743. PMID:15713784
- Youdim MB, Edmondson D, Tipton KF. "The therapeutic potential of monoamine oxidase inhibitors." Nat Rev Neurosci. 2006;7(4):295-309. PMID:16552415
- Jenner P, et al. "Signal transduction by monoamine oxidases: biochemical and pharmacological basis for neuroprotection." J Neural Transm. 2011;118(1):1-17. PMID:21203857
- Finberg JP. "Inhibitors of MAO-B and COMT: their role in the treatment of Parkinson's disease." Parkinsonism Relat Disord. 2014;20 Suppl 1:S147-149. PMID:24262191
- Schapira AH. "Monoamine oxidase B inhibitors for the treatment of Parkinson's disease: a review of symptomatic and potential disease-modifying effects." CNS Drugs. 2011;25(12):1061-1070. PMID:22133302
- Rabey JM, Sagi I. "Rasagiline for the treatment of Parkinson's disease." Expert Opin Pharmacother. 2010;11(14):2261-2268. PMID:20629653