Rasagiline


Concise Prescribing Info
Indications/Uses
Idiopathic parkinsonism.
Dosage/Direction for Use
Adult : PO 1 mg once daily as monotherapy or as adjunctive therapy to levodopa.
Dosage Details
Oral
Idiopathic parkinsonism
Adult: 1 mg once daily as monotherapy or as adjunctive therapy to levodopa.
Hepatic Impairment
Mild: 0.5 mg once daily.
Administration
May be taken with or without food. Avoid tyramine-rich foods, beverages or dietary supplements & amines (from cough/cold prep).
Contraindications
Severe hepatic impairment. Concomitant use w/ other MAOIs and pethidine w/in 14 days after discontinuation of therapy; St John's wort.
Special Precautions
Mild to moderate hepatic impairment. Pregnancy and lactation
Adverse Reactions
Headache, flu-like syndrome, malaise, neck pain, angina pectoris, dyspepsia, anorexia, leucopenia, arthralgia, arthritis, depression, vertigo, rhinitis, conjunctivitis, skin rashes, melanoma, and urinary urgency. Rarely, CVA and MI.
Patient Counseling Information
Avoid tobacco smoking.
MonitoringParameters
Monitor BP, symptoms of parkinsonism, new or worsening mental status and behavioural changes, somnolence and falling asleep during daily activities and skin examination for presence of melanoma.
Overdosage
Symptoms: Dysphoria, hypomania, hypertensive crisis and serotonin syndrome. Management: Symptomatic and supportive therapy.
Drug Interactions
Increased plasma levels w/ potent CYP1A2 inhibitors (e.g. ciprofloxacin). Increased clearance w/ entacapone.
Potentially Fatal: Increased risk of non-selective MAO inhibition w/ other MAOIs and pethidine that may lead to hypertensive crises.
Food Interaction
Increased risk of hypertensive crises w/ St John's wort. May reduce plasma concentration w/ tobacco smoking.
Action
Description: Rasagiline is a potent, irreversible monoamine oxidase (MAO)-B selective inhibitor which may cause an increase in extracellular levels of dopamine in the striatum, leading to reduced symptomatic motor deficits of Parkinson's disease.
Duration: Approx 1 wk (irreversible inhibition).
Pharmacokinetics:
Absorption: Rapidly absorbed from the GI tract. Absolute bioavailability: Approx 36%. Time to peak plasma concentration: Approx 30-60 min.
Distribution: Plasma protein binding: Approx 60-70%.
Metabolism: Undergoes extensive hepatic metabolism via N-dealkylation and/or hydroxylation to yield 1-aminoindan (major metabolite), 3-hydroxy-N-propargyl-1 aminoindan and 3-hydroxy-1-aminoindan by CYP1A2 isoenzyme, and conjugation to yield glucuronides.
Excretion: Mainly in the urine (<1% as unchanged drug) and partly in the faeces. Terminal half-life: 0.6-2 hr.
Chemical Structure

Chemical Structure Image
Rasagiline

Source: National Center for Biotechnology Information. PubChem Database. Rasagiline, CID=3052776, https://pubchem.ncbi.nlm.nih.gov/compound/Rasagiline (accessed on Jan. 22, 2020)

Storage
Store below 25°C.
ATC Classification
N04BD02 - rasagiline ; Belongs to the class of dopaminergic agents, monoamine oxidase B inhibitors. Used in the management of Parkinson's disease.
References
Anon. Rasagiline. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 04/04/2016.

Buckingham R (ed). Rasagiline Mesilate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/04/2016.

Joint Formulary Committee. Rasagiline. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/04/2016.

McEvoy GK, Snow EK, Miller J et al (eds). Rasagiline Mesylate. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 01/04/2016.

Disclaimer: This information is independently developed by MIMS based on Rasagiline from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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