Rasalect

Rasagiline (rasagiline) Instructions
Common name: rasagiline
Trade name: Azilate
All names: rasagiline, rasagiline, rasagiline, AZILECT

Indications:
Suitable for monotherapy in patients with primary Parkinson's disease, as well as combination therapy (combined with levodopa) in patients with end-of-dose fluctuations.

Usage and dosage:
Orally administered, regardless of whether it is combined with levodopa, the dosage is 1 mg once a day.
Taking this product is not affected by eating.
Elderly: No dose adjustment required
Children: Due to lack of safety and efficacy data, this product is not recommended for use in children and adolescents.
Patients with hepatic impairment: This product is contraindicated in patients with severe hepatic impairment. Rasagiline should be avoided in patients with moderate hepatic impairment. Caution should be exercised when initiating rasagiline in patients with mild hepatic impairment. If the patient's liver function impairment progresses from mild to moderate, rasagiline should be discontinued.
Patients with renal impairment: No dosage adjustment is necessary.

Adverse reactions:
> 10%
EPS (dyskinesia/dystonia) (18%)
Headache (14%)
Nausea (10-12%)

1-10%
Orthostatic hypotension (6-9%)
Constipation (4-9%)
Weight loss ( 2-9%)
Joint pain (7%)
Indigestion (7%)
Xerostomia (2-6%)
Depression (5%)
Decrease (5%)
Influenza-like syndrome (5%)
Hallucinations (4-5%)
Conjunctivitis (3%)
Fever (3%)
Gastroenteritis (3%)
Rhinitis (3%)
Arthritis (2%)
Contusion (2%)
Malaise (2%)
Neck pain (2%)
Paresthesia (2%)
Dizziness (2%)

<1%
CVA
MI
Bundled branch block
Gastrointestinal bleeding

Contraindications:
Coadministration with pethidine, tramadol, methadone and MAOIs, including other selective MAO-B inhibitors, may increase the risk of serotonin syndrome; At least 14 days should be allowed between stopping rasagiline and starting treatment with these drugs
Coadministration with St. John's wort (Hypericum perforatum) and cyclobenzaprine
Coadministration with dextromethorphan due to risk of psychotic episodes or strange behavior

Precautions:
Recommended doses may cause hypertension (including severe hypertensive syndrome)
May exacerbate hypertension; Antihypertensive medications may require dose adjustment
May cause hypotension, especially orthostatic
May cause serotonin syndrome when used with antidepressants
Daytime sleepiness and somnolence reported during activities of daily living
May cause or worsen dyskinesias; lowering the levodopa dose may reduce or eliminate this side effect
Hallucinations and psychotic-like behavior have been reported
Impulse control/compulsive behaviors have been reported; Case reports describe patients with strong urges to gamble, increased sexual desire, strong urges to spend money, or overeating
Withdrawal has been reported with rapid dose reduction of the drug - the onset of hyperthermia and confusion, and increased central dopaminergic tone; characterized by increased temperature, muscle stiffness, altered consciousness, and autonomic instability
Patients with Parkinson's disease have a 2 to 6 times higher risk of developing melanoma than the general population; it is unclear whether this is due to the disease or other factors (such as medication); Monitor for melanoma frequently and regularly.

Storage:
Keep sealed.

Mechanism of action:
Rasagiline is an irreversible, selective MAO-B inhibitor with a similar structure to selegiline. The inhibitory effect of this drug on MAO-B is about 100 times stronger than that on MAO-A. MAO is an enzyme involved in the metabolic degradation of dopamine in the brain. When this enzyme is inhibited, the transmission signal of dopamine is enhanced, which is beneficial to Parkinson's disease and can also enhance the effect of levodopa. In vitro, the inhibitory effect of this drug and selegiline on MAO-B is similar, while the inhibitory effect in vivo is 3-15 times higher than that of selegiline.
This drug is rapidly absorbed from the gastrointestinal tract after oral administration, with a peak time of approximately 1 hour (single use), 30 to 45 minutes (combined use with levodopa), and a duration of 6 weeks. The oral bioavailability is about 36%, and the protein binding rate is 88% to 94%. It can pass through the blood-cerebrospinal fluid barrier with a distribution volume of 87L. It is extensively metabolized in the liver. The metabolites are 1-aminoindene (active), 3-hydroxy-N-propargyl-1-aminoindene and 3-hydroxy-1-aminoindene. The metabolites are mainly excreted in the urine and partially in the feces. Less than 1% of the administered dose is excreted in the urine unchanged, with a half-life of 0.6 to 2 hours.

Efficacy and safety:
Three randomized controlled clinical trials lasting 18 to 26 weeks have confirmed the safety and effectiveness of rasagiline. In a study involving 404 patients with early-stage Parkinson's disease, a rating scale showed that patients treated with rasagiline were significantly less likely to have their condition worsen compared with those in the placebo group. Two other studies compared rasagiline with placebo or levodopa in more than 1,100 patients with more advanced Parkinson's disease, with significantly shorter daily functional and activity limitations.