IUPAC_name = (6a"R",9"R",10a"R")-9-(methylthiomethyl)-7-propyl--4,6,6a,7,8,9,10,10a-octahydroindolo [4,3-"fg"] quinoline
width = 180
CAS_number = 66104-22-1
ATC_prefix = N04
ATC_suffix = BC02
PubChem = 47811
DrugBank = APRD00663
C = 19 | H = 26 | N = 2 | S = 1
molecular_weight = 314.489 g/mol
protein_bound = 90%
metabolism = Extensively hepatic
elimination_half-life = 27 hours
pregnancy_category = B
legal_status = Withdrawn (U.S.)
routes_of_administration = Oral
Pergolide is an
ergoline-based dopamine receptor agonistused for the treatment of Parkinson's disease.
Parkinson's disease is associated with low levels of the
neurotransmitter dopaminein the brain. Pergolide has some of the same effects as dopamine in the body.
Pergolide is also 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 intermediahyperplasia or Equine Cushing's Syndrome (ECS) in horses. [cite web |url=http://www.wedgewoodpharmacy.com/monographs/pergolide.asp |title=Pergolide For Veterinary Use |author=Barbara Forney, VMD ]
The drug is in decreasing use, as it was reported in 2003 to be associated with a form of heart disease called
cardiac fibrosis. [cite journal | url = http://www.tga.gov.au/adr/aadrb/aadr0408.htm | year = 2004 | month = August | title = Cardiac valvulopathy with pergolide | author = ADRAC | journal = Aust Adv Drug React Bull | volume = 23 | issue = 4 [http://www.tga.gov.au/adr/aadrb/aadr0408.htm Free full text] from the Australian Therapeutic Goods Administration] 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, cabergolinebut not lisurideexhibit this same type of serotonin receptor binding. [ Jähnichen S, Horowski R, Pertz H. PDFlink| [http://userpage.fu-berlin.de/~hpertz/Presentation001.pdf "Pergolide and Cabergoline But not Lisuride Exhibit Agonist Efficacy at Serotonin 5-HT2B Receptors".] |515 KiB Presentation. Retrieved on 2007-03-30.] In January, 2007, cabergoline(Dostinex) was reported also to be associated with valvular proliferation heart damage. [cite journal |author=Schade R, Andersohn F, Suissa S, Haverkamp W, Garbe E |title=Dopamine agonists and the risk of cardiac-valve regurgitation |journal=N Engl J Med |volume=356 |issue=1 |pages=29–38 |year=2007 |pmid=17202453 |doi=10.1056/NEJMoa062222] In March 2007, pergolide was withdrawn from the U.S. market due to serious valvular damage that was shown in two independent studies.cite web | url = http://www.fda.gov/medwatch/safety/2007/safety07.htm#Pergolide | title = MedWatch - 2007 Safety Information Alerts. Permax (pergolide) and generic equivalents | publisher = U.S. Food and Drug Administration| date = March 29, 2007 | accessdate = 2007-03-30]
Pergolide has also been shown to impair associative learning. [cite journal |author=Breitenstein C "et al". |title=Tonic dopaminergic stimulation impairs associative learning in healthy subjects |journal=Neuropsychopharmacology |volume=31 |issue=11 |pages=2552–64 |year=2006 |pmid=16880771 |doi=10.1038/sj.npp.1301167]
On March 30th, 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. [ [http://www.medscape.com/viewarticle/554347?sssdmh=dm1.259053&src=ddd Pergolide Withdrawn From US Market] ] However, Pergolide is still available in many other countries including Canada.
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