What important information does the package insert for Rasagiline/Azilate contain?

Rasagiline is a monoamine oxidase B (MAO-B) inhibitor that is widely used in the treatment of Parkinson's disease (PD). By selectively inhibiting MAO-B, it reduces the degradation of dopamine in the brain, thereby increasing the level of dopamine in the synaptic cleft of neurons and improving the symptoms of Parkinson's disease. The following is important drug information about rasagiline, including indications, usage and dosage, adverse reactions, contraindications, and drug interactions.

【Indications】

Rasagiline is used to treat primary Parkinson's disease, either as a monotherapy or in combination with levodopa (Levodopa). For patients with early-stage Parkinson's disease, rasagiline can be used as a single agent to delay the progression of symptoms, and in advanced stages, it is often used as an adjunct to levodopa to reduce wear-off and motor fluctuations.

【Usage and Dosage】

Recommended doses of rasagiline vary based on treatment regimen and patient condition.

Monotherapy: The recommended dose is1 mg once daily.

Adjuvant therapy without levodopa: the recommended dose is also 1 mg once daily.

Combined use with levodopa: The recommended starting dose is0.5 mg once a day, which can be increased to 1 mg once a day if necessary to optimize efficacy and reduce levodopa-related motor fluctuations.

Combined use with CYP1A2 inhibitors (such as ciprofloxacin): The dose should be adjusted to 0.5 mg once a day to avoid excessively high plasma concentrations of rasagiline and increase the risk of adverse reactions.

Patients with mild hepatic impairment: The dose should be controlled at0.5 mg once a day. Rasagiline is contraindicated in patients with moderate to severe hepatic impairment.

Rasagiline can be taken with food or on an empty stomach. Due to its long half-life, stable blood concentrations can be maintained once a day.

【Adverse reactions】

Rasagiline is generally well tolerated, but the following adverse reactions may still occur:

Nervous system: dizziness, headache, drowsiness, insomnia, anxiety, depression, etc. Some patients may experience hallucinations and delusions, especially when used in combination with levodopa.

Digestive system: nausea, vomiting, diarrhea, constipation, loss of appetite, etc.

Cardiovascular system: hypotension, orthostatic hypotension, some patients may have palpitations, increased heart rate, etc.

Dyskinesia: When combined with levodopa treatment, dyskinesia (dyskinesia) or dystonia may be aggravated.

Others: rash, joint pain, myalgia, weight changes, etc.

【Contraindications】

It is contraindicated in patients allergic to rasagiline or its excipients.

It is contraindicated for those taking non-selective monoamine oxidase inhibitors (MAOIs) to avoid severe hypertensive crisis.

Rasagiline is contraindicated in patients taking pethidine (Pethidine, an analgesic) to prevent severe central nervous system depression or serotonin syndrome.

Rasagiline is contraindicated in patients with moderate to severe hepatic impairment because its reduced metabolism may lead to drug accumulation and increase the risk of adverse reactions.

【Drug use for special groups】

Elderly people: Parkinson's disease is more common in the elderly. This group tolerates rasagiline better, but they still need to monitor for hypotension, cognitive impairment, and changes in motor function.

Patients with hepatic impairment: Patients with mild hepatic impairment should reduce the dose (0.5 mg once daily), and patients with moderate to severe hepatic impairment should not take this drug.

Pregnant and lactating women: There is currently insufficient clinical data to support the safety of rasagiline in pregnant or lactating women. It is recommended to use it with caution or adjust the treatment plan as directed by your doctor.

Reference materials:https://www.azilect.com/