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Pergolide


Pergolide
Systematic (IUPAC) name
?
Identifiers
CAS number	66104-22-1
ATC code	N04BC02
PubChem	47811
DrugBank	APRD00663
Chemical data
Formula	C₁₉H₂₆N₂S
Mol. mass	314.489 g/mol
Pharmacokinetic data
Bioavailability	?
Protein binding	90%
Metabolism	Extensively hepatic
Half life	27 hours
Excretion	?
Therapeutic considerations
Pregnancy cat.	B
Legal status	Withdrawn (U.S.)
Routes	Oral

Pergolide is an ergoline-based dopamine receptor agonist used for the treatment of Parkinson's disease.

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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.

Uses

Pergolide is also used to treat the stiffness, tremors, spasms, and poor muscle control of Parkinson's disease, although it has also been used to treat discomfort or pain in the lower extremities that can only be relieved by moving the legs. Pergolide is often used in conjunction with other medicines in the treatment of Parkinson's disease.

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]

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] 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.^[3] In January, 2007, cabergoline (Dostinex) was reported also to be associated with valvular proliferation heart damage.^[4] In March 2007, pergolide was withdrawn from the U.S. market due to serious valvular damage that was shown in two independent studies.^[5]

Pergolide has also been shown to impair associative learning.^[6]

On March 30th, 2007, manufacturers of Pergolide agreed to withdraw the drug from the U.S. market after several published studies revealed a link between the drug and increased rates of valvular dysfunction. ^[7]

References

^ 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
^ 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. PMID 17202453.
^ MedWatch - 2007 Safety Information Alerts. Permax (pergolide) and generic equivalents. U.S. Food and Drug Administration (March 29, 2007). Retrieved on 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.
^ http://www.medscape.com/viewarticle/554347?sssdmh=dm1.259053&src=ddd

v • d • e Ergolines
Lysergic acid derivatives	Bromocriptine, Cabergoline, Ergine,Ergonovine, Ergotamine, Lysergic acid, Lysergol, LSD, D-Lysergic acid hydroxyethylamide, Lisuride, Methergine, Methysergide, Pergolide
Hallucinogenic lysergamides	AL-LAD, ALD-52, BU-LAD, CYP-LAD, DAL, DAM-57, Ergonovine, ETH-LAD, LAE-32, LSD, LPD-824, LSM-775, D-Lysergic acid N-(α-hydroxyethyl)amide, Methylergonovine, MLD-41, PARGY-LAD, PRO-LAD
Other ergolines	Ergoline
Natural sources	Argyreia nervosa, Claviceps spp., Ipomoea tricolor, Ipomoea violacea, Rivea corymbosa

v • d • e Anti-parkinson drugs: dopaminergic agents (N04B)
Dopa and derivatives	Levodopa, Melevodopa, Etilevodopa
Adamantane derivatives	Amantadine
Dopamine agonists	Apomorphine, Bromocriptine, Cabergoline, Dihydrexidine, Dihydroergocryptine mesylate, Fenoldopam, Lisuride, Pergolide, Piribedil, Pramipexole, Quinpirole, Ropinirole, Rotigotine, SKF 38393, SKF 82958
MAOIs	Selegiline, Rasagiline
Other	Tolcapone, Entacapone, Budipine

Categories: Dopamine agonists | Withdrawn drugs

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Pergolide". A list of authors is available in Wikipedia.