World Library  
Flag as Inappropriate
Email this Article


Article Id: WHEBN0000622942
Reproduction Date:

Title: Pergolide  
Author: World Heritage Encyclopedia
Language: English
Subject: Cabergoline, Apomorphine, Methysergide, LSM-775, Diallyllysergamide
Collection: Dopamine Agonists, Equine Medications, Ergolines, Thioethers, Withdrawn Drugs
Publisher: World Heritage Encyclopedia


Systematic (IUPAC) name
Clinical data
  • B
Legal status
Routes of
Pharmacokinetic data
Protein binding 90%
Metabolism Extensively hepatic
Biological half-life 27 hours
CAS Registry Number  Y
ATC code N04
PubChem CID:
DrugBank  Y
ChemSpider  Y
Synonyms (6aR,9R,10aR)-9-(methylthiomethyl)-7-propyl-4,6,6a,7,8,9,10,10a-octahydroindolo[4,3-fg]quinoline
Chemical data
Formula C19H26N2S
Molecular mass 314.489 g/mol

Pergolide (trade name Permax) is an ergoline-based dopamine receptor agonist used in some countries for the treatment of Parkinson's disease.

Parkinson's disease is associated with low levels of the neurotransmitter dopamine in the brain. Pergolide has some of the same effects as dopamine in the body.

In 2007 pergolide was withdrawn from the U.S. market for human use after several published studies revealed a link between the drug and increased rates of valvular heart disease.[1]

However, a veterinary form of pergolide (trade name Prascend) is permitted for the treatment of Pituitary Pars Intermedia Dysfunction (PPID) also known as equine Cushing's syndrome (ECS) in horses.[2]


  • Indications 1
  • Pharmacology 2
  • Side effects 3
    • Claimed side effects 3.1
  • References 4


Pergolide is not available for use by humans in the United States, however it is still used in various other countries, where it is used to treat various conditions including Parkinson's disease, hyperprolactinemia, and restless leg syndrome.

Furthermore, pergolide may also be used for veterinary purposes. Under the trade name Prascend, manufactured by Boehringer Ingelheim,[3] it is commonly used for the treatment of pituitary pars intermedia hyperplasia or Equine Cushing's Syndrome (ECS) in horses.[4]


Pergolide functions as an agonist at the dopamine D2, D1 and serotonin 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, and 5-HT2C receptors. It may possess agonist activity at other dopamine receptor subtypes as well, similar to cabergoline. The weak agonist activity of pergolide at D1 receptors somewhat alters its clinical and side effect profile in the treatment of Parkinson's disease.

Side effects

The drug is in decreasing use, as it was reported in 2003 to be associated with a form of heart disease called cardiac fibrosis.[5] In 2007, The United States Food and Drug Administration announced a voluntary withdrawal of the drug by manufacturers due to the possibility of heart valve damage.[6] Pergolide is not currently available in the United States for human use. This problem is thought to be due to pergolide's action at the 5-HT2B serotonin receptors of cardiac myocytes, causing proliferative valve disease by the same mechanism as ergotamine, methysergide, fenfluramine, and other serotonin 5-HT2B agonists, including serotonin itself when elevated in the blood in carcinoid syndrome. Pergolide can rarely cause Raynaud's phenomenon. Among similar antiparkinsonian drugs, cabergoline but not lisuride exhibit this same type of serotonin receptor binding.[7] In January, 2007, cabergoline (Dostinex) was reported also to be associated with valvular proliferation heart damage.[8] In March 2007, pergolide was withdrawn from the U.S. market for human use, due to serious valvular damage that was shown in two independent studies.[9]

Pergolide has also been shown to impair associative learning.[10]

Claimed side effects

At least one British pergolide user has attracted some media attention with claims that it has caused him to develop a gambling addiction.[11][12] In June 2010, it was reported that more than 100 Australian users of the drug are suing the manufacturer over both gambling and sex addiction[13] problems they claim are the result of the drug's side effects.


  1. ^ FDA Public Health Advisory: Pergolide (marketed as Permax)
  2. ^ [2]
  3. ^
  4. ^ Barbara Forney, VMD. "Pergolide For Veterinary Use". 
  5. ^   Free full text from the Australian Therapeutic Goods Administration
  6. ^ Public Health Advisory - Pergolide (marketed as Permax)
  7. ^ Jähnichen S, Horowski R, Pertz H. Receptors".2B"Pergolide and Cabergoline But not Lisuride Exhibit Agonist Efficacy at Serotonin 5-HT PDF (515 KiB) Presentation. Retrieved on 2007-03-30.
  8. ^ Schade R, Andersohn F, Suissa S, Haverkamp W, Garbe E (2007). "Dopamine agonists and the risk of cardiac-valve regurgitation".  
  9. ^ "MedWatch - 2007 Safety Information Alerts. Permax (pergolide) and generic equivalents". U.S.  
  10. ^ Breitenstein C, et al. (2006). "Tonic dopaminergic stimulation impairs associative learning in healthy subjects". Neuropsychopharmacology 31 (11): 2552–64.  
  11. ^ "Drug 'caused' gambling addiction" BBC TV 24 Jan. 2008
  12. ^ "Parkinson's Gambler" 5 Feb. 2008
  13. ^ "Parkinson's treatment linked to sex, gambling" 'The Age' 4 June 2010
This article was sourced from Creative Commons Attribution-ShareAlike License; additional terms may apply. World Heritage Encyclopedia content is assembled from numerous content providers, Open Access Publishing, and in compliance with The Fair Access to Science and Technology Research Act (FASTR), Wikimedia Foundation, Inc., Public Library of Science, The Encyclopedia of Life, Open Book Publishers (OBP), PubMed, U.S. National Library of Medicine, National Center for Biotechnology Information, U.S. National Library of Medicine, National Institutes of Health (NIH), U.S. Department of Health & Human Services, and, which sources content from all federal, state, local, tribal, and territorial government publication portals (.gov, .mil, .edu). Funding for and content contributors is made possible from the U.S. Congress, E-Government Act of 2002.
Crowd sourced content that is contributed to World Heritage Encyclopedia is peer reviewed and edited by our editorial staff to ensure quality scholarly research articles.
By using this site, you agree to the Terms of Use and Privacy Policy. World Heritage Encyclopedia™ is a registered trademark of the World Public Library Association, a non-profit organization.

Copyright © World Library Foundation. All rights reserved. eBooks from Project Gutenberg are sponsored by the World Library Foundation,
a 501c(4) Member's Support Non-Profit Organization, and is NOT affiliated with any governmental agency or department.