関: pergolide

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/03/18 10:59:01」(JST)

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Pergolide (trade name 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.

In 2007, pergolide was withdrawn from the U.S. market for human use, after several published studies revealed a link between the drug and increased rates of valvular dysfunction.[11]

However Pergolide is allowed for veterinary use to treat Cushings Syndrome in horses.

Indications

Pergolide is not available 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.

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]

Pharmacology

Pergolide functions as an agonist at the dopamine D₂, 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. The weak agonist activity of pergolide at D₁ receptors somewhat alters its clinical and side effect profile in the treatment of Parkinson's disease.

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-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.^[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 for human use, due to serious valvular damage that was shown in two independent studies.^[6]

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

Claimed side effects

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] In June 2010, it was reported that more than 100 Australian users of the drug are suing the manufacturer over both gambling and sex addiction^[10] problems they claim are the result of the drug's side effects.

References

^ Barbara Forney, VMD. "Pergolide For Veterinary Use". http://www.wedgewoodpharmacy.com/monographs/pergolide.asp.
^ 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
^ Public Health Advisory - Pergolide (marketed as Permax)
^ Jähnichen S, Horowski R, Pertz H. "Pergolide and Cabergoline But not Lisuride Exhibit Agonist Efficacy at Serotonin 5-HT_2B Receptors". PDF (515 KiB) Presentation. Retrieved on 2007-03-30.
^ 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.
^ "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.
^ 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.
^ "Drug 'caused' gambling addiction" BBC TV 24 Jan. 2008
^ "Parkinson's Gambler" ITV.com 5 Feb. 2008
^ "Parkinson's treatment linked to sex, gambling" 'The Age' 4 June 2010

UpToDate Contents

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1. パーキンソン病の薬理学的治療 pharmacologic treatment of parkinson disease
2. 高プロラクチン血症のマネージメント management of hyperprolactinemia
3. 成人におけるむずむず脚症候群／ウィリス・エクボム病および周期性四肢運動障害の治療 treatment of restless legs syndrome willis ekbom disease and periodic limb movement disorder in adults
4. 薬剤誘発性の弁膜症 valvular heart disease induced by drugs
5. 多系統萎縮症：予後および治療 multiple system atrophy prognosis and treatment

English Journal

Anti-Parkinson's disease drugs and pharmacogenetic considerations.

Agúndez JA, García-Martín E, Alonso-Navarro H, Jiménez-Jiménez FJ.SourceUniversity of Extremadura, Department of Pharmacology , Avda. de la Universidad s/n, E-10071, Cáceres , Spain +34927257000 Ext 86897 ; +34924289676 ; jagundez@unex.es.
Expert opinion on drug metabolism & toxicology.Expert Opin Drug Metab Toxicol.2013 Apr 9. [Epub ahead of print]
Introduction: The development of pharmacogenetic-based clinical practice guidelines for the use of anti-Parkinson's disease drugs requires, as a pre-requisite, the identification and validation of genetic biomarkers. These biomarkers are then used as surrogate endpoints. This review analyzes potenti
PMID 23565891

Clinical features of dopamine agonist withdrawal syndrome in a movement disorders clinic.

Pondal M, Marras C, Miyasaki J, Moro E, Armstrong MJ, Strafella AP, Shah BB, Fox S, Prashanth LK, Phielipp N, Lang AE.SourceMovement Disorders Centre, Toronto Western Hospital, University of Toronto, Canada. mpondals@gmail.com
Journal of neurology, neurosurgery, and psychiatry.J Neurol Neurosurg Psychiatry.2013 Feb;84(2):130-5. doi: 10.1136/jnnp-2012-302684. Epub 2012 Aug 29.
BACKGROUND: Recently, symptoms similar to addictive drug withdrawal have been reported in a structured longitudinal study of patients with idiopathic Parkinson's Disease (PD) withdrawing from dopamine agonists (DA): the dopamine agonist withdrawal syndrome (DAWS).OBJECTIVES: The objective of this st
PMID 22933817

Pergolide block of the cloned Kv1.5 potassium channels.

Jeong I, Choi BH, Hahn SJ.SourceDepartment of Physiology, Cell Death and Disease Research Center, College of Medicine, The Catholic University of Korea, Seoul 137-701, South Korea.
Naunyn-Schmiedeberg's archives of pharmacology.Naunyn Schmiedebergs Arch Pharmacol.2013 Feb;386(2):125-33. doi: 10.1007/s00210-012-0776-5. Epub 2012 Jul 5.
Pergolide mesylate, an ergot-derivative dopamine receptor agonist, is prescribed for the management of patients with Parkinson's disease. Pergolide caused vasoconstriction in a pulmonary artery. Kv1.5 channel is highly expressed in pulmonary arterial smooth muscle cells, where it plays an important
PMID 22763615

「ペルゴリド」

Pergolide
Systematic (IUPAC) name
	(8β)-8-[(methylthio)methyl]-6-propylergoline
Clinical data
AHFS/Drugs.com	monograph
Pregnancy cat.	B
Legal status	Withdrawn (U.S.)
Routes	Oral
Pharmacokinetic data
Protein binding	90%
Metabolism	Extensively hepatic
Half-life	27 hours
Identifiers
CAS number	66104-22-1
ATC code	N04BC02
PubChem	CID 47811
IUPHAR ligand	48
DrugBank	DB01186
ChemSpider	43503
UNII	24MJ822NZ9
KEGG	D08339
ChEMBL	CHEMBL531
Synonyms	(6aR,9R,10aR)-9-(methylthiomethyl)-7-propyl-4,6,6a,7,8,9,10,10a-octahydroindolo[4,3-fg]quinoline
Chemical data
Formula	C19H26N2S
Mol. mass	314.489 g/mol
	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 ; Key:YEHCICAEULNIGD-MZMPZRCHSA-N ;
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　　[★]

英: pergolide
化: メシル酸ペルゴリド pergolide mesilate
商: ペルマックス Permax、ベセラール、ペルゴリン

[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-HT_2B 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.

[FDAwithdraw-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] "Parkinson's treatment linked to sex, gambling" 'The Age' 4 June 2010

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案内

Permax