Pergolide

Pergolide
Clinical data
Trade namesPermax, Prascend (veterinary), others
Other names8β-[(Methylthio)methyl]-6-propylergoline
AHFS/Drugs.comMonograph
Pregnancy
category
  • B
Routes of
administration		Oral
ATC code
Legal status
Legal status
Pharmacokinetic data
Protein binding90%
MetabolismExtensively Hepatic
Elimination half-life27 hours
Identifiers
  • (6aR,9R,10aR)-9-(methylthiomethyl)-7-propyl-4,6,6a,7,8,9,10,10a-octahydroindolo[4,3-fg]quinoline
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.241.322 Edit this at Wikidata
Chemical and physical data
FormulaC19H26N2S
Molar mass314.49 g·mol−1
3D model (JSmol)
  • [H][C@]12C[C@@H](CSC)CN(CCC)[C@]1([H])Cc3c[nH]c4cccc2c34
  • InChI=1S/C19H26N2S/c1-3-7-21-11-13(12-22-2)8-16-15-5-4-6-17-19(15)14(10-20-17)9-18(16)21/h4-6,10,13,16,18,20H,3,7-9,11-12H2,1-2H3/t13-,16-,18-/m1/s1 checkY
  • Key:YEHCICAEULNIGD-MZMPZRCHSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Pergolide, sold under the brand name Permax and Prascend (veterinary) among others, is an ergoline-based dopamine receptor agonist used in some countries for the treatment of Parkinson's disease. Parkinson's disease is associated with reduced dopamine synthesis in the substantia nigra of the brain. Pergolide acts on many of the same receptors as dopamine to increase receptor activity.

It was patented in 1978[3] and approved for medical use in 1989.[4] In 2007, pergolide was withdrawn from the U.S. market for human use after several published studies revealed a link between the drug and increased rates of valvular heart disease.[5] However, a veterinary form of pergolide, marketed under the trade name Prascend, is permitted for the treatment of pituitary pars intermedia dysfunction (PPID) also known as equine Cushing's syndrome (ECS) in horses.[6]

  1. ^ "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA. Retrieved 22 Oct 2023.
  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. ^ US patent 4166182A, Edmund C. Kornfeld & Nicholas J. Bach, "6-n-propyl-8-methoxymethyl or methylmercaptomethylergolines and related compounds", published 1979-08-28, issued 1979-08-28, assigned to Eli Lilly and Co 
  4. ^ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 533. ISBN 9783527607495.
  5. ^ "Pergolide (marketed as Permax)". FDA Public Health Advisory. Archived from the original on 2007-04-08. Retrieved 2019-12-16.{{cite web}}: CS1 maint: bot: original URL status unknown (link)
  6. ^ Forney B. "Pergolide for Veterinary Use".