Rasagiline (Azilect) is an irreversible, selective inhibitor of monoamine oxidase type B (MAO-B). It is used to treat the symptoms of idiopathic Parkinson's disease and can be administered as monotherapy or as an adjunct to levodopa.
Precautions for Administration of Rasagiline (Azilect)
Dosage and Administration Method
Monotherapy: The recommended dose is 1 mg, taken orally once daily.
Adjunctive Therapy: The initial dose is 0.5 mg once daily; if the therapeutic effect is insufficient, the dose can be increased to 1 mg per day.
Administration Time: It can be taken with food or on an empty stomach. However, a high-fat diet may reduce the peak plasma concentration (Cmax) of the drug.
Absolute Contraindications
Concomitant use with meperidine, tramadol, dextromethorphan, St. John's wort, mirtazapine, or cyclobenzaprine.
Patients with pheochromocytoma.
Relative Contraindications
Pregnant and lactating women (the drug may cause teratogenicity or inhibit lactation).
Patients with moderate to severe hepatic impairment (Child-Pugh Class B/C) require dosage adjustment or are prohibited from using the drug.
Drug Interactions
CYP1A2 Inhibitors: Drugs such as ciprofloxacin can double the plasma concentration of rasagiline, so the dose of rasagiline needs to be reduced to 0.5 mg per day.
Antidepressants: Concomitant use with selective serotonin reuptake inhibitors (SSRIs), serotonin-norepinephrine reuptake inhibitors (SNRIs), or tricyclic antidepressants should be avoided, and an interval of at least 14 days is required between discontinuing one drug and starting the other.
Tyramine-Containing Foods: Intake of aged cheese, pickled herring, concentrated yeast extract, etc., should be avoided to prevent hypertensive crisis.
Key Monitoring Points for Rasagiline (Azilect) Administration
Liver Function Monitoring
Frequency: Before treatment, once every 3 weeks for the first 3 months of treatment, and then once a month thereafter.
Management of Abnormalities: If alanine transaminase (ALT)/aspartate transaminase (AST) > 3 × upper limit of normal (ULN) accompanied by symptoms, or > 5 × ULN: suspend medication, and reduce the dose after liver function recovers.
If ALT/AST > 3 × ULN accompanied by bilirubin > 2 × ULN: permanently discontinue the medication.
Cardiovascular and Nervous System Monitoring
Blood Pressure Monitoring: Be alert to orthostatic hypotension (incidence rate: 3%-9%), especially in the early stage of treatment.
Psychiatric Symptoms: Hallucinations (incidence rate: 1.3%-5%) require timely evaluation and dosage adjustment.
Skin and Tumor Screening
Risk of Melanoma: Patients with Parkinson's disease themselves have a relatively high risk of melanoma, so regular skin examinations (every 6-12 months) are required.
Laboratory Indicators
Routine Items: Complete blood count, electrolytes (calcium, sodium), and urine protein.
Creatine Kinase (CPK): When muscle pain occurs or urine color darkens, test CPK to rule out rhabdomyolysis.
