Rasagiline

Rasagiline
Clinical data
Trade namesAzilect, others
Other namesTVP-1012; TVP1012; R(+)-AGN-1135; N-Propargyl-(R)-1-aminoindan; N-Propargyl-1(R)-aminoindan; (R)-PAI
AHFS/Drugs.comMonograph
MedlinePlusa606017
License data
Pregnancy
category
  • AU: B3
Routes of
administration		By mouth[1][2]
Drug classMonoamine oxidase inhibitor; Antiparkinsonian
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability36%[2]
Protein binding88–94%[2]
MetabolismLiver (CYP1A2)[2]
Metabolites• (R)-1-Aminoindan[2]
• 3-OH-PAI[2]
• 3-OH-AI[2]
Elimination half-life3 hours[2]
ExcretionUrine: 62%[2]
Feces: 7%[2]
Identifiers
IUPAC name
  • (R)-N-(prop-2-ynyl)-2,3-dihydro-1H-inden-1-amine
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
PDB ligand
CompTox Dashboard (EPA)
ECHA InfoCard100.301.709
Chemical and physical data
FormulaC12H13N
Molar mass171.243 g·mol−1
3D model (JSmol)
SMILES
  • C#CCN[C@H]2c1ccccc1CC2
InChI
  • InChI=1S/C12H13N/c1-2-9-13-12-8-7-10-5-3-4-6-11(10)12/h1,3-6,12-13H,7-9H2/t12-/m1/s1 Y
  • Key:RUOKEQAAGRXIBM-GFCCVEGCSA-N Y
  (verify)

Rasagiline, sold under the brand name Azilect among others, is a medication which is used in the treatment of Parkinson's disease.[2][6] It is used as a monotherapy to treat symptoms in early Parkinson's disease or as an adjunct therapy in more advanced cases.[7] The drug is taken by mouth.[2]

Side effects of rasagiline include insomnia and orthostatic hypotension, among others.[2] Rasagiline acts as an inhibitor of the enzyme monoamine oxidase (MAO) and hence is a monoamine oxidase inhibitor (MAOI).[2] More specifically, it is a selective inhibitor of monoamine oxidase B (MAO-B).[2] The drug is thought to work by increasing levels of the monoamine neurotransmitter dopamine in the brain.[2] Rasagiline shows pharmacological differences from the related drug selegiline, including having no amphetamine-like metabolites, monoamine-releasing activity, or monoaminergic activity enhancer actions, which may result in clinical differences between the medications.[8][9]

Rasagiline was approved for medical use in the European Union in 2005[10] and in the United States in 2006.[2][11] Generic versions of rasagiline are available.[12][13][14]

  1. ^ Cite error: The named reference ChenSwope2005 was invoked but never defined (see the help page).
  2. ^ a b c d e f g h i j k l m n o p q r "Azilect- rasagiline mesylate tablet". DailyMed. 30 June 2020. Retrieved 23 July 2024.
  3. ^ "RASAGILINE JAMP/ RASAGILINE GXMED (AA-Med Pty Ltd) | Therapeutic Goods Administration (TGA)". Archived from the original on 7 July 2024. Retrieved 1 August 2025.
  4. ^ Anvisa (31 March 2023). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese). Diário Oficial da União (published 4 April 2023). Archived from the original on 3 August 2023. Retrieved 16 August 2023.
  5. ^ "Azilect EPAR". European Medicines Agency. 21 February 2005. Retrieved 23 July 2024.
  6. ^ Oldfield V, Keating GM, Perry CM (2007). "Rasagiline: a review of its use in the management of Parkinson's disease". Drugs. 67 (12): 1725–1747. doi:10.2165/00003495-200767120-00006. PMID 17683172. S2CID 195688993.
  7. ^ Gallagher DA, Schrag A (2008). "Impact of newer pharmacological treatments on quality of life in patients with Parkinson's disease". CNS Drugs. 22 (7): 563–586. doi:10.2165/00023210-200822070-00003. PMID 18547126. S2CID 29707067.
  8. ^ Cite error: The named reference GerlachReichmannRiederer2012 was invoked but never defined (see the help page).
  9. ^ Cite error: The named reference HarsingTimarMiklya2023 was invoked but never defined (see the help page).
  10. ^ Cite error: The named reference NRDD2005 was invoked but never defined (see the help page).
  11. ^ Cite error: The named reference OrgChemDD2014 was invoked but never defined (see the help page).
  12. ^ Cite error: The named reference Drugs@FDA was invoked but never defined (see the help page).
  13. ^ Cite error: The named reference GoodRx was invoked but never defined (see the help page).
  14. ^ Cite error: The named reference Drugs.com-Generics was invoked but never defined (see the help page).
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