Pergolide

Structural formula
General
Non-proprietary name	Pergolide
other names	8 β - (methylthiomethyl) -6-propylergoline ( IUPAC ) ; (6a R , 9 R , 10a R ) -9 - [(methylsulfanyl) methyl] -7-propyl-4,6,6a, 7,8,9,10,10a-octahydroindolo [4,3- fg ] quinoline;
Molecular formula	C 19 H 26 N 2 S (pergolide) ; C 19 H 26 N 2 S CH 3 SO 3 H (pergolide mesylate) ;
External identifiers / databases
ECHA InfoCard	100.241.322
PubChem	47811
DrugBank	DB01186
Wikidata	Q415752
Drug information
ATC code	N04 BC02
Drug class	Dopamine agonist
properties
Molar mass	314.49 g mol −1 (pergolide) ; 410.59 g mol −1 (pergolide mesylate) ;
Melting point	217.5 ° C (pergolide) ; 258–260 ° C (pergolide mesylate) ;
safety instructions
	Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed
GHS labeling of hazardous substances Mesylate; danger
H and P phrases	H: 300
	P: 264-301 + 310
Toxicological data	8.4 mg kg −1 ( LD 50 , rat , oral , pergolide mesilate)
	As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Pergolide is a drug that the therapy of the Parkinson's disease is used. This drug, which is derived from ergot alkaloids , mediates its pharmacological effects by activating dopamine receptors ( dopamine agonist ).

Clinical information

application

Pergolide is approved as a monotherapeutic agent and in combination with levodopa and a decarboxylase inhibitor (e.g. carbidopa ) for the treatment of Parkinson's disease. In veterinary medicine, pergolide is used as a monotherapeutic agent for the treatment of equine Cushing's syndrome in horses.

Interactions

Dopamine antagonists such as B. metoclopramide , reduce the effectiveness of pergolide. Pergolide increases the blood pressure lowering effect of antihypertensive drugs .

Side effects

Dyskinesia , hallucinations , sleep disorders, loss of appetite, nausea, hypotension and tachycardia were observed during therapy with pergolide . According to recent studies, pergolide can cause fibrotic heart valve damage, which is why it has already been withdrawn from the market in some countries (e.g. Sweden). The side effects of pergolide and other ergoline active ingredients can partly be explained by the fact that they are dirty drugs , that is, they do not act specifically on the dopamine receptors, but also on other receptors.

Pharmacological information

Mechanism of action

Pergolide is an agonist on the dopamine receptors D ₁ and D ₂ and their subtypes .

Trade names

Monopreparations

Parkotil (D), Permax (A, CH), numerous generics (D)

For horses: Prascend

Individual evidence

^ ^A ^b The Merck Index : An Encyclopedia of Chemicals, Drugs, and Biologicals , 14th Edition (Merck & Co., Inc.), Whitehouse Station, NJ, USA, 2006; P. 1236, ISBN 978-0-911910-00-1 .
↑ ^a ^b Data sheet Pergolide mesylate salt from Sigma-Aldrich , accessed on April 18, 2011 ( PDF ).
↑ Data sheet PERGOLIDE MESILATE CRS (PDF) at EDQM , accessed on March 14, 2009.
↑ Entry on Pergolid at Vetpharm, accessed on August 11, 2012.

[MERCK_Index-1] A ^b The Merck Index : An Encyclopedia of Chemicals, Drugs, and Biologicals , 14th Edition (Merck & Co., Inc.), Whitehouse Station, NJ, USA, 2006; P. 1236, ISBN 978-0-911910-00-1 .

[Sigma-2] Data sheet Pergolide mesylate salt from Sigma-Aldrich , accessed on April 18, 2011 ( PDF ).

[Ph._Eur.-3] Data sheet PERGOLIDE MESILATE CRS (PDF) at EDQM , accessed on March 14, 2009.

[vetpharm-4] Entry on Pergolid at Vetpharm, accessed on August 11, 2012.