Generic
Rasagiline
8 brands available in the market
At a glance
Rasagiline is an irreversible, selective MAO-B inhibitor used as monotherapy or adjunct therapy for Parkinson's disease. It increases extracellular dopamine levels in the striatum, reducing motor deficits.
Description
Rasagiline is an irreversible MAO-B inhibitor that increases extracellular dopamine levels in the striatum. It is used as monotherapy in early Parkinson's disease or as adjunct therapy in more advanced cases. Elevated dopamine levels and subsequent increased dopaminergic activity mediate rasagiline's beneficial effects.
Indications
- Parkinson's disease (monotherapy)
- Parkinson's disease (adjunct therapy with levodopa)
Therapeutic class
Antiparkinson drugs
Pharmacological class
MAO-B Inhibitor (Selective, Irreversible)
Pharmacology
Rasagiline is an irreversible MAO-B inhibitor that increases extracellular dopamine levels in the striatum. It reduces dopamine breakdown and enhances dopaminergic tone, improving motor symptoms in Parkinson's disease.
Mechanism of action
Reduces dopamine breakdown by irreversibly inhibiting MAO-B.
Dosage
Adult Dose (Oral):
- Monotherapy (without levodopa): 1 mg once daily
- Adjunct with levodopa: 0.5 mg once daily initially; may increase to 1 mg/day if needed and tolerated; consider reducing levodopa dose
- Mild hepatic impairment: Not to exceed 0.5 mg/day
- Moderate-severe hepatic impairment: Do not use
Administration
- May be taken with or without food; take at a fixed time
- Swallow tablet whole; do not chew, crush, or break
Missed dose
If you miss a dose, take it as soon as you remember; skip if it's almost time for next dose; do not double the dose.
Side effects
Common Side Effects:
- Joint pain
- Insomnia
- Dyspepsia
- Flu-like symptoms
- Depression
- Cough
- Peripheral edema
- Headache
- Dizziness
- Dry mouth
- Loss of appetite
- Constipation/diarrhea
- Weight loss
Precautions & warnings
- May affect driving ability; do not drive if drowsy or dizzy
- Do not stop suddenly (may cause confusion, stiff muscles, high fever)
- Avoid foods high in tyramine (aged cheeses, air-dried meat, soy sauce, tap/draft beers, red wine) due to risk of hypertensive reaction
- Serotonin syndrome: Caution with SSRIs, SNRIs, TCAs
Contraindications
- Severe hepatic impairment
- Concomitant use with other MAOIs or within 14 days of discontinuation
- Concomitant use with pethidine (within 14 days of discontinuation)
- St. John's wort
Drug interactions
- Strong CYP1A2 inhibitors (ciprofloxacin): Increased plasma levels; do not exceed 0.5 mg/day
- Entacapone: Increased clearance
- Fluoxetine/fluvoxamine: Avoid concomitant use; wait 5 weeks after fluoxetine discontinuation to start rasagiline; wait 14 days after rasagiline discontinuation to start fluoxetine
- Dextromethorphan, sympathomimetics (ephedrine, pseudoephedrine): Not recommended
- Potentially fatal: Risk of non-selective MAO inhibition with other MAOIs and pethidine (hypertensive crisis)
Food interactions
Alcohol consumption with Rasagiline is unsafe.
Use in pregnancy
Use in Pregnancy: May be unsafe during pregnancy; animal studies have shown harmful effects; consult your doctor.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Probably unsafe; limited human data suggests drug may pass into breast milk; may inhibit prolactin secretion.
Pediatric use
Safety and efficacy not established in children under 18 years.
Geriatric use
No significant differences in safety profile between geriatric and non-geriatric patients.
Renal / hepatic impairment
Renal Impairment: Safe in kidney disease; dose adjustment may not be needed; not studied in severe renal impairment; consult your doctor.
Hepatic Impairment: Caution in liver disease; mild: 0.5 mg/day; moderate-severe: do not use; consult your doctor.
Overdose effects
Overdose: Drowsiness, dizziness, faintness, irritability, hyperactivity, agitation, severe headache, hallucinations, seizures, coma, hypertension/hypotension, respiratory depression, hyperpyrexia; no specific antidote; supportive care, tyramine-restricted diet for several weeks.
Storage conditions
Store at temperature not exceeding 30°C in a dry place; protect from light; keep out of reach of children.
Chemical structure
Rasagiline