Pergolide

Pergolide

Clinical data
AHFS/Drugs.com	Monograph
Pregnancy category	B
Routes of administration	Oral
ATC code	N04BC02 (WHO)
Legal status
Legal status	US: veterinary use only, withdrawn for human use
Pharmacokinetic data
Protein binding	90%
Metabolism	Extensively hepatic
Biological half-life	27 hours
Identifiers
IUPAC name (8β)-8-[(methylthio)methyl]-6-propylergoline
Synonyms	(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
Chemical and physical data
Formula	C19H26N2S
Molar mass	314.489 g/mol
3D model (Jmol)	Interactive image
SMILES S(C)C[C@@H]2C[C@@H]3c4cccc1c4c(cn1)C[C@H]3N(C2)CCC
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?)

Pergolide (trade names Permax, Prascend) 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In 2007 pergolide was withdrawn from the U.S. market for human use after several published studies revealed a link between the drug and increased rates of valvular heart disease. 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.

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.

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

Pergolide acts as an agonist of dopamine D₂ and D₁ and serotonin 5-HT_1A, 5-HT_1B, 5-HT_2A, 5-HT_2B, and 5-HT_2C receptors. It may possess agonist activity at other dopamine receptor subtypes as well, similar to cabergoline. Although pergolide is more potent as an agonist of the D₂ receptor, it has high D₁ receptor affinity and is one of the most potent D₁ receptor agonists of the dopamine receptor agonists that are clinically available. The agonist activity of pergolide at the D₁ receptor somewhat alters its clinical and side effect profile in the treatment of Parkinson's disease.