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Pergolide
Systematic (IUPAC) name
(8β)-8-[(methylthio)methyl]-6-propylergoline
Identifiers
CAS number 66104-22-1
ATC code N04BC02
PubChem 47811
DrugBank APRD00663
Chemical data
Formula C19H26N2S 
Mol. mass 314.489 g/mol
Synonyms (6aR,9R,10aR)-9-(methylthiomethyl)-7-propyl-4,6,6a,7,8,9,10,10a-octahydroindolo[4,3-fg]quinoline
Pharmacokinetic data
Protein binding 90%
Metabolism Extensively hepatic
Half life 27 hours
Therapeutic considerations
Pregnancy cat. B
Legal status Withdrawn (U.S.)
Routes Oral
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Pergolide (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.

Indications

Pergolide is not available in the United States. In some other countries, it is used to treat the stiffness, tremors, spasms, and poor muscle control of Parkinson's disease, although it has also been used to treat discomfort or pain in the lower extremities that can only be relieved by moving the legs. Pergolide is often used in conjunction with other medicines in the treatment of Parkinson's disease. Since Pergolide can reduce prolactin levels, it is often used to treat hyperprolactinemia.

Furthermore, pergolide may also be used for veterinary purposes. It is commonly used for the treatment of pituitary pars intermedia hyperplasia or Equine Cushing's Syndrome (ECS) in horses.[1]

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.[2] 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 [3]. Pergolide is not currently available in the United States. 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.[4] In January, 2007, cabergoline (Dostinex) was reported also to be associated with valvular proliferation heart damage.[5] In March 2007, pergolide was withdrawn from the U.S. market due to serious valvular damage that was shown in two independent studies.[6]

Pergolide has also been shown to impair associative learning.[7]

At least one British Pergolide user has attracted some media attention with claims that it has caused him to develop a gambling addiction.[8][9] On March 30, 2007, manufacturers of Pergolide agreed to withdraw the drug from the U.S. market after several published studies revealed a link between the drug and increased rates of valvular dysfunction.[10] However, Pergolide is still available in many other countries.

References

  1. ^ Barbara Forney, VMD. "Pergolide For Veterinary Use". http://www.wedgewoodpharmacy.com/monographs/pergolide.asp. 
  2. ^ ADRAC (August 2004). "Cardiac valvulopathy with pergolide". Aust Adv Drug React Bull 23 (4). http://www.tga.gov.au/adr/aadrb/aadr0408.htm.  Free full text from the Australian Therapeutic Goods Administration
  3. ^ Public Health Advisory - Pergolide (marketed as Permax)
  4. ^ Jähnichen S, Horowski R, Pertz H. "Pergolide and Cabergoline But not Lisuride Exhibit Agonist Efficacy at Serotonin 5-HT2B Receptors".PDF (515 KiB) Presentation. Retrieved on 2007-03-30.
  5. ^ Schade R, Andersohn F, Suissa S, Haverkamp W, Garbe E (2007). "Dopamine agonists and the risk of cardiac-valve regurgitation". N Engl J Med 356 (1): 29–38. doi:10.1056/NEJMoa062222. PMID 17202453. 
  6. ^ "MedWatch - 2007 Safety Information Alerts. Permax (pergolide) and generic equivalents". U.S. Food and Drug Administration. March 29, 2007. http://www.fda.gov/medwatch/safety/2007/safety07.htm#Pergolide. Retrieved 2007-03-30. 
  7. ^ Breitenstein C et al. (2006). "Tonic dopaminergic stimulation impairs associative learning in healthy subjects". Neuropsychopharmacology 31 (11): 2552–64. doi:10.1038/sj.npp.1301167. PMID 16880771. 
  8. ^ "Drug 'caused' gambling addiction" BBC TV 24 Jan. 2008
  9. ^ "Parkinson's Gambler" ITV.com 5 Feb. 2008
  10. ^ Pergolide Withdrawn From US Market







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