Rivastigmine

Rivastigmine
Clinical data
Trade namesExelon, Prometax, others
AHFS/Drugs.comMonograph
MedlinePlusa602009
License data
Pregnancy
category
  • AU: B2
Routes of
administration
By mouth, transdermal patch
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability60 to 72%
Protein binding40%
MetabolismLiver, via pseudocholinesterase
Elimination half-life1.5 hours
Excretion97% in urine
Identifiers
  • (S)-3-[1-(dimethylamino)ethyl]phenyl N-ethyl-N-methylcarbamate
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.120.679 Edit this at Wikidata
Chemical and physical data
FormulaC14H22N2O2
Molar mass250.342 g·mol−1
3D model (JSmol)
  • O=C(Oc1cc(ccc1)[C@@H](N(C)C)C)N(CC)C
  • InChI=1S/C14H22N2O2/c1-6-16(5)14(17)18-13-9-7-8-12(10-13)11(2)15(3)4/h7-11H,6H2,1-5H3/t11-/m0/s1 checkY
  • Key:XSVMFMHYUFZWBK-NSHDSACASA-N checkY
 ☒NcheckY (what is this?)  (verify)

Rivastigmine (sold under the trade name Exelon among others) is a cholinesterase inhibitor used for the treatment of mild to moderate Alzheimer's disease.[4] The drug can be administered orally or via a transdermal patch; the latter form reduces the prevalence of side effects,[5] which typically include nausea and vomiting.[6]

The drug is eliminated through the urine, and appears to have relatively few drug-drug interactions.[6]

It was patented in 1985 and came into medical use in 1997.[7]

  1. ^ "Prescription medicines: registration of new generic medicines and biosimilar medicines, 2017". Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 30 March 2024.
  2. ^ Anvisa (2023-03-31). "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 2023-04-04). Archived from the original on 2023-08-03. Retrieved 2023-08-16.
  3. ^ "Product monograph brand safety updates". Health Canada. 7 July 2016. Retrieved 1 April 2024.
  4. ^ Khoury R, Rajamanickam J, Grossberg GT (March 2018). "An update on the safety of current therapies for Alzheimer's disease: focus on rivastigmine". Therapeutic Advances in Drug Safety. 9 (3). SAGE Publications: 171–178. doi:10.1177/2042098617750555. PMC 5810854. PMID 29492246.
  5. ^ Cite error: The named reference Winblad was invoked but never defined (see the help page).
  6. ^ a b Cite error: The named reference Inglis was invoked but never defined (see the help page).
  7. ^ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 540. ISBN 9783527607495.

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