Instructions for Rasagiline

1. Common name: rasagiline

Product name:AZILECT

All names: Rasagiline, Rasagiline, Azilect,

2. Indications:

Rasagiline(Rasagiline) is indicated for the treatment of Parkinson's disease (PD).

3. Usage and dosage:

1. Recommended dosage:

When rasagiline is used as monotherapy or as adjunctive therapy in patients not taking levodopa, patients may begin taking rasagiline at the recommended dose of 1 mg taken orally once daily. In patients taking levodopa, with or without other PD medications (e.g., dopamine agonists, amantadine, anticholinergics), the recommended initial dose of rasagiline is 0.5 mg once daily. If the patient tolerates a daily dose of 0.5 mg but does not achieve an adequate clinical response, the dose may be increased to 1 mg once daily. When rasagiline is used concomitantly with levodopa, a dose reduction of levodopa may be considered based on individual response.

2. Combination medication: The once-daily dose of rasagiline for patients who are concurrently taking ciprofloxacin or other CYP1A2 inhibitors should not exceed 0.5mg.

3. Patients with hepatic impairment: The daily dose of rasagiline for patients with mild hepatic impairment should not exceed 0.5 mg. Patients with moderate or severe hepatic impairment should not use rasagiline.

4. Adverse reactions:

Side effects in patients treated with rasagiline alone include flu-like symptoms, joint pain, depression, stomach upset, headache, dizziness, and insomnia; when taken with levodopa, side effects include increased movement problems, accidental injuries, sudden drops in blood pressure, joint pain and swelling, dry mouth, rash, abnormal dreams, and digestive problems; and when taken with Parkinson's medications other than levodopa, side effects include peripheral edema, falls, joint pain, cough, and insomnia.

5. Storage:

Rasagiline is normally stored at 25°C (77°F), with an allowed excursion to 15-30°C (59-86°F).

6. Taboo:

Due to the risk of serotonin syndrome, rasagiline is contraindicated with pethidine, tramadol, methadone, propoxyphene, and MAO inhibitors (MAOIs), including other selective MAO-B inhibitors, and an interval of at least 14 days should elapse between discontinuing rasagiline and starting treatment with these drugs. Rasagiline is contraindicated for use with dextromethorphan due to the risk of psychotic episodes or bizarre behavior.

7. Mechanism of action:

雷沙吉兰是一种选择性、不可逆的MAO-B抑制剂，用于治疗特发性帕金森病。 Results from a clinical trial suggest that when healthy subjects ingest large amounts of tyramine concurrently with recommended doses of rasagiline, functional selectivity may be incomplete and selectivity for inhibiting MAO-B is reduced in a dose-related manner. MAO-B is the predominant form in the human brain, and this activity leads to increased extracellular levels of dopamine in the striatum. Elevated dopamine levels and subsequent increases in dopaminergic activity may mediate the beneficial effects of rasagiline observed in models of dopaminergic motor dysfunction.