Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/09/09 14:03:26」(JST)
wiki en
| 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| Legal status | Withdrawn (U.S.) |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 Y |
| ATC code | N04BC02 |
| PubChem | CID 47811 |
| IUPHAR ligand | 48 |
| DrugBank | DB01186 |
| ChemSpider | 43503 Y |
| UNII | 24MJ822NZ9 Y |
| KEGG | D08339 Y |
| ChEMBL | CHEMBL531 Y |
| 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
|
|
|
InChI
|
|
| Y (what is this?) (verify) |
|
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In 2007, pergolide was withdrawn from the U.S. market for human use, after several published studies revealed a link between the drug and increased rates of valvular heart disease.[1]
However, a veterinary form of pergolide (trade name Prascend) is permitted for the treatment of equine Cushing's syndrome (ECS) in horses.[2]
Contents
- 1 Indications
- 2 Pharmacology
- 3 Side effects
- 3.1 Claimed side effects
- 4 References
Indications[edit source | edit]
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.
Furthermore, pergolide may also be used for veterinary purposes. Under the trade name Prascend, manufactured by Boehringer Ingelheim,[3] it is commonly used for the treatment of pituitary pars intermedia hyperplasia or Equine Cushing's Syndrome (ECS) in horses.[4]
Pharmacology[edit source | edit]
Pergolide functions as an agonist at the dopamine D2, D1 and serotonin 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, and 5-HT2C 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[edit source | edit]
The drug is in decreasing use, as it was reported in 2003 to be associated with a form of heart disease called cardiac fibrosis.[5] 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.[6] 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-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, cabergoline but not lisuride exhibit this same type of serotonin receptor binding.[7] In January, 2007, cabergoline (Dostinex) was reported also to be associated with valvular proliferation heart damage.[8] 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.[9]
Pergolide has also been shown to impair associative learning.[10]
Claimed side effects[edit source | edit]
At least one British pergolide user has attracted some media attention with claims that it has caused him to develop a gambling addiction.[11][12] 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[13] problems they claim are the result of the drug's side effects.
References[edit source | edit]
- ^ [http://web.archive.org/web/20070408111551/http://www.fda.gov/cder/drug/advisory/pergolide.htm FDA Public Health Advisory: Pergolide (marketed as Permax)
- ^ [1]
- ^ http://www.valleyvet.com/ct_detail.html?pgguid=e0f4888c-86de-4ce9-9013-6d947df697a8&gas=pergolide%20mesylate
- ^ Barbara Forney, VMD. "Pergolide For Veterinary Use".
- ^ ADRAC (August 2004). "Cardiac valvulopathy with pergolide". Aust Adv Drug React Bull 23 (4). 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-HT2B 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. 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
全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.
- 1. パーキンソン病の薬理学的治療 pharmacologic treatment of parkinson disease
- 2. Management of hyperprolactinemia
- 3. 薬剤誘発性の弁膜症 valvular heart disease induced by drugs
- 4. 多系統萎縮症：予後および治療 multiple system atrophy prognosis and treatment
- 5. トゥレット症候群 tourette syndrome
English Journal
- Reversible Hypotony and Choroidal Effusion Following the Use of Pergolide for Parkinson's Disease.
- Andreatta W1, Shah P.
- Seminars in ophthalmology.Semin Ophthalmol.2015 Aug 21:1-3. [Epub ahead of print]
- PURPOSE: To alert clinicians of the possibility of reversible drug-induced occult hypotony and choroidal effusion following the long-term use of pergolide.METHODS: Annotations were made while the case was observed. The clinical records of the patient were reviewed retrospectively.RESULTS: A 74-year-
- PMID 24251433
- Trends in inpatient antiparkinson drug use in the USA, 2001-2012.
- Crispo JA1, Fortin Y, Thibault DP, Emons M, Bjerre LM, Kohen DE, Perez-Lloret S, Mattison D, Willis AW, Krewski D.
- European journal of clinical pharmacology.Eur J Clin Pharmacol.2015 Aug;71(8):1011-9. doi: 10.1007/s00228-015-1881-4. Epub 2015 Jun 18.
- PURPOSE: Although therapeutic options and clinical guidelines for Parkinson's disease (PD) have changed significantly in the past 15 years, prescribing trends in the USA remain unknown. The purpose of this population-based cohort study was to examine patterns of inpatient antiparkinson drug use bet
- PMID 26081062
- Effectiveness of risk minimization measures for cabergoline-induced cardiac valve fibrosis in clinical practice in Italy.
- Italiano D1, Bianchini E, Ilardi M, Cilia R, Pezzoli G, Zanettini R, Vacca L, Stocchi F, Bramanti P, Ciurleo R, Di Lorenzo G, Polimeni G, de Luise C, Ross D, Rijnbeek P, Sturkenboom M, Trifirò G.
- Journal of neural transmission (Vienna, Austria : 1996).J Neural Transm.2015 Jun;122(6):799-808. doi: 10.1007/s00702-014-1314-z. Epub 2014 Sep 18.
- On June 2008, the European Medicines Agency (EMA) introduced changes to the Summary of Product Characteristics (SPC) for cabergoline and pergolide, to reduce the risk of cardiac valvulopathy in users of these drugs. To assess the effectiveness of EMA recommendations in Italian clinical practice, we
- PMID 25230720
Japanese Journal
- 医薬品のリスク・マネジメントにおけるエビデンス診療ギャップ：レセプト分析からの視点
- 中山 健夫
- 薬学雑誌. 乙号 132(5), 549-554, 2012
- … The receipt analysis showed that more than 70% of Parkinson's disease patients prescribed with cabergoline or pergolide did not undergo echocardiography despite the revision of the product label recommendation. …
- NAID 130001888669
- Echocardiography for the Detection of Valvulopathy Associated with the Use of Ergot-Derived Dopamine Agonists in Patients with Parkinson's Disease
- Nakaoka Sachiko,Ishizaki Tatsuro,Urushihara Hisashi,Satoh Toshihiko,Ikeda Shunya,Morikawa Kaoru,Nakayama Takeo
- Internal Medicine 50(7), 687-694, 2011
- … Objective The ergot-derived dopamine agonists, cabergoline and pergolide, are associated with valvulopathy risk. … This study assessed changes in echocardiography evaluation of patients with Parkinson's disease (PD) taking cabergoline or pergolide before and after the label revision and examined the factors related with echocardiography performance. …
- NAID 130000650040
- Retroperitoneal Fibrosis Secondary to Pergolide Therapy
- Fukae Jiro,Tanaka Shigeki,Hattori Nobutaka
- Internal Medicine 49(15), 1687-1687, 2010
- NAID 130000299610
Related Links
- Pergolide official prescribing information for healthcare professionals. Includes: indications, dosage, adverse reactions, pharmacology and more. ... Events Observed During the Premarketing Evaluation of Pergolide Mesylate 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 ...
Related Pictures
★リンクテーブル★
| リンク元 | 「ペルゴリド」「Permax」 |
| 拡張検索 | 「pergolide mesilate」 |