Rasagiline

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Antiparkinsonian Drug

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.