Pergolide

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Pergolide

Pergolide is an ergoline

Ergoline

Ergoline is a chemical Chemical compound whose structural skeleton is contained in a diverse range of alkaloids and a few psychedelic Psychoactive drug ....
-based dopamine receptor

Dopamine receptor

Dopamine receptors are a class of metabotropic receptor G protein-coupled receptors that are prominent in the vertebrate central nervous system ....
agonist

Agonist

An agonist is a term used to describe a type of Ligand or drug that binds and alters the activity of a Receptor . The ability to alter the activity of a receptor, also known as the agonist's efficacy is a property that distinguishes it from receptor antagonist, a type of receptor ligand which also binds a receptor but which does not alter t...
used for the treatment of Parkinson's disease

Parkinson's disease

Parkinson's disease is a degenerative disorder of the central nervous system that often impairs the sufferer's motor skills and speech, as well as other functions....
.

Parkinson's disease is associated with low levels of the neurotransmitter

Neurotransmitter

Neurotransmitters are chemistry which relay, amplify and modulate signals between a neuron and another cell . Neurotransmitters are packaged into vesicles that cluster beneath the membrane on the presynaptic side of a synapse, and are released into the synaptic cleft, where they bind to receptors in the membrane on the postsynaptic side of...
dopamine

Dopamine

Dopamine is a neurotransmitter occurring in a wide variety of animals, including both vertebrates and invertebrates. In the human brain, this phenethylamine functions as a neurotransmitter, activating the five types of dopamine receptors ? D1, D2, D3, D4 and D5, and their variants....
in the brain. Pergolide has some of the same effects as dopamine in the body.

olide 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.

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Encyclopedia

Pergolide is an ergoline

Ergoline

Ergoline is a chemical Chemical compound whose structural skeleton is contained in a diverse range of alkaloids and a few psychedelic Psychoactive drug ....
-based dopamine receptor

Dopamine receptor

Dopamine receptors are a class of metabotropic receptor G protein-coupled receptors that are prominent in the vertebrate central nervous system ....
agonist

Agonist

Parkinson's disease

Neurotransmitter

Dopamine

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. Since Pergolide can reduce prolactin levels, it is often used to treat hyperprolactinemia.

Furthermore, pergolide may also be used for veterinary purposes. It is commonly used for the treatment of pituitary pars intermedia

Pars intermedia

Pars intermedia is the boundary between the anterior and posterior lobes of the pituitary. It contains three types of cells - Anterior pituitary basophils, chromophobes, and colloid-filled cysts....
hyperplasia or Equine Cushing's Syndrome

Cushing's syndrome

Cushing's syndrome is a hormone disorder caused by high levels of cortisol in the blood. This can be caused by taking glucocorticoid drugs, or by tumors that produce cortisol or adrenocorticotropic hormone ....
(ECS) in horses.

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

Cardiac fibrosis

Cardiac fibrosis refers to an abnormal thickening of the heart valves due to inappropriate proliferation of cardiac fibroblasts.Fibrocyte cells normally secrete collagen, and function to provide structural support for the heart....
. 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

Ergotamine

Ergotamine is an ergopeptine and part of the ergot family of alkaloids; it is structurally and biochemically closely related to ergoline. It possesses structural similarity to several neurotransmitters, and has biological activity as a vasoconstrictor....
, methysergide

Methysergide

Methysergide is a prescription drug used for prophylaxis of migraine and is sold under the brand names Sansert and Deseril in 2mg dosages....
, fenfluramine

Fenfluramine

Fenfluramine is a drug that was part of the Fen-Phen anti-obesity medication . Also known as Pondimin, fenfluramine was introduced on the U.S....
, and other serotonin 5-HT_2B agonists, including serotonin itself when elevated in the blood in carcinoid syndrome

Carcinoid syndrome

Carcinoid syndrome refers to the array of symptoms that occur secondary to carcinoid.Carcinoid tumors are discrete, yellow, well-circumscribed tumors that can occur anywhere along the gastrointestinal tract and in the lung....
. Pergolide can rarely cause Raynaud's phenomenon

Raynaud's phenomenon

Raynaud's phenomenon , in medicine, is a vasospasm disorder causing discoloration of the fingers, toes, and occasionally other extremities. This condition can also cause nails to become brittle with longitudinal ridges....
. Among similar antiparkinsonian drugs, cabergoline

Cabergoline

Lisuride

Lisuride is an anti-Parkinson's disease drug of the iso-ergoline class, chemically related to the dopaminergic ergoline Parkinson's drugs. Lisuride is described as free base and as hydrogenmaleate salt....
exhibit this same type of serotonin receptor binding. In January, 2007, cabergoline

Cabergoline

Cabergoline , an ergot derivative, is a potent dopamine Receptor agonist on D2 receptors. It also acts on dopamine receptors in lactophilic hypothalamus Cell to suppress prolactin production in the pituitary gland....
(Dostinex) was reported also to be associated with valvular proliferation heart damage. In March 2007, pergolide was withdrawn from the U.S. market due to serious valvular damage that was shown in two independent studies.

Pergolide has also been shown to impair associative learning.

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. However, Pergolide is still available in many other countries including Canada.