Rasagiline
Drug class: Monoamine Oxidase B Inhibitor, MAO-B Inhibitor
Rasagiline (AZILECT)(中文:雷沙吉蘭)
Common Strengths of Rasagiline[edit]
Rasagiline is available in the following strength: 1 mg
Drug Trade Names[edit]
Azilect
Drug Usage[edit]
Rasagiline is used to treat symptoms of Parkinson's disease, including:
- Stiffness
- Tremors
- Spasms
- Poor muscle contorl
Mechanism of Action[edit]
Rasagiline act as an irreversible inhibitor of monoamine oxidase B (MAO-B), leading to increased levels of dopamine in the brain. This mechanism helps improve dopaminergic activity, which is beneficial for managing motor dysfunction in Parkinson's disease.
Route of Administration[edit]
Oral
Dosage[edit]
- Monotherapy: 1 mg once daily.
- Adjunct therapy with levodopa: Initial dose of 0.5 mg once daily, can be increased to 1 mg as tolerated.
Side Effects[edit]
| Frequency | Adverse reactions |
|---|---|
| Common Side Effects | Insomnia |
| Weight loss | |
| Nausea | |
| Dizziness | |
| Serious Side Effects | Serotonin syndrome (symptoms include agitation and hallucinations) |
| Severe headache or blurred vision | |
| Exterme drowsiness or sudden sleep spisodes | |
| Uncontrolled muscle movements or worsening Parkinson's sympotms |
Pharmacokinetics[edit]
Rasagiline has an absolute bioavailability of approximately 36%.
The onset time for therapeutic effects typically ranges from two to three weeks, with lasting throughout the day when taken once daily.
Drug Precautions[edit]
Pregnancy
Rasagiline is categorized as Pregnancy Category C, indicating that risk cannot be ruled out; it should only be used if clearly needed.
Breastfeeding
Caution is advised as it may inhibit milk secretion; the safety during breastfeeding has not been established.
Drug Monitoring Items
- Impulse contorl disorders: Some patients may experience increased urges related to gambling or sexuality.
- Monitoring blood pressure: hypertensive crises, particularly when combined with tyramine-rich food or certain medications.
- Assessing for signs of serotonin syndrome including agitation and hallucination, rapid heart rate and muscle twitching.
Drug Interactions
Rasagiline can interact with several medications, including:
- Other MAO inhibitor (e.g. selegiline): Coadministration with other MAO inhibitors can lead to severe hypertensive episodes. It is advised to avoid such combinations for at least 14 days.
- Certain antidepressant (e.g. St. John's wort) and over-the-counter products like dextromethorphan should be avoided unless under strict medical supervision
- Opioids (e.g. meperidine)
- Food interactions: Patients are advised to avoid high-tyramine foods (e.g. aged cheeses) to prevent hypertensive crises.
FAQ[edit]
How Should I Take the Tablet?
Take rasagiline orally once daily, with or without food.
What Should I Avoid While Taking?
Avoid consuming tyramine-rich food (e.g. aged cheese) and other MAO inhibitors, as they can cause hypertensive crisis.
What Happens if I Miss a Dose?
If you miss a dose, take it as soon as you remember on the same day; do not double up on doses if it's close to your next scheduled dose.
