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 activity in the substantia nigra of the brain. Pergolide acts on many of the same receptors as dopamine to increase receptor activity.

Quick Facts Clinical data, Trade names ...

Pergolide

Clinical data
Trade names	Permax, Prascend (veterinary), others
Other names	8β-[(Methylthio)methyl]-6-propylergoline
AHFS/Drugs.com	Monograph
Pregnancy category	B
Routes of administration	Oral
ATC code	N04BC02 (WHO)
Legal status
Legal status	BR: Class C1 (Other controlled substances)[1] CA: ℞-only US: WARNING[2] Veterinary use only, withdrawn for human use
Pharmacokinetic data
Protein binding	90%
Metabolism	Extensively Hepatic
Elimination half-life	27 hours
Identifiers
IUPAC name (6aR,9R,10aR)-9-(methylthiomethyl)-7-propyl-4,6,6a,7,8,9,10,10a-octahydroindolo[4,3-fg]quinoline
CAS Number	66104-22-1 Y
PubChem CID	47811
IUPHAR/BPS	48
DrugBank	DB01186 Y
ChemSpider	43503 Y
UNII	24MJ822NZ9
KEGG	D08339 Y
ChEBI	CHEBI:63617 N
ChEMBL	ChEMBL531 Y
CompTox Dashboard (EPA)	DTXSID2023438
ECHA InfoCard	100.241.322
Chemical and physical data
Formula	C19H26N2S
Molar mass	314.49 g·mol−1
3D model (JSmol)	Interactive image
SMILES [H][C@]12C[C@@H](CSC)CN(CCC)[C@]1([H])Cc3c[nH]c4cccc2c34
InChI 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 Y Key:YEHCICAEULNIGD-MZMPZRCHSA-N Y
NY (what is this?)  (verify)

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It was patented in 1978^[3] and approved for medical use in 1989.^[4] In 2007, pergolide was withdrawn from the U.S. market for human use after several published studies revealed a link between the drug and increased rates of valvular heart disease.^[5] However,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]

Pergolide is no longer 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.^{[citation needed]}

Pergolide is available for veterinary use. Under the trade name Prascend, manufactured by Boehringer Ingelheim,^[7] it is commonly used for the treatment of pituitary hyperplasia at the pars intermedia or Equine Cushing's Syndrome (ECS) in horses.^[6]

The drug is in decreasing use, as it was reported in 2003 to be associated with a form of heart disease called cardiac fibrosis.^[16] 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.^[17] 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-HT_2B serotonin receptors of cardiac myocytes, causing proliferative valve disease by the same mechanism as ergotamine, methysergide, fenfluramine, and other serotonin 5-HT_2B 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.^[18] In January 2007, cabergoline (Dostinex) was also reported to be associated with valvular proliferation heart damage.^[19] 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.^[20]

Pergolide has also been shown to impair associative learning.^[21]