chemistry

Pergolide

Pergolide is a chemistry topic covered in the lgStudy science library. This page brings together a partial reference excerpt, illustrations, worked examples, real-world applications and a short study plan, so you can understand Pergolide rather than just read about it. In short: Pergolide, sold under the brand name Permax and Prascend (veterinary) among others, is an ergoline-based dopamine receptor agonist used in some countries for the treatment of Parkinson's disease. Parkinson's disease is associated with reduced dopamine synthesis in the substantia nigra of the brain.

Key takeaways

Pergolide belongs to chemistry; place it in that map before memorising details.
Learn the definition first, then one example that makes the definition concrete.
Connect Pergolide to a quantity you can measure, compute or draw — that is where exam questions come from.
Reproduce the core statement of Pergolide from memory before moving on to harder problems.

Reference excerpt

Pergolide, sold under the brand name Permax and Prascend (veterinary) among others, is an ergoline-based dopamine receptor agonist used in some countries for the treatment of Parkinson's disease. Parkinson's disease is associated with reduced dopamine synthesis in the substantia nigra of the brain. Pergolide acts on many of the same receptors as dopamine to increase receptor activity. It was patented in 1978 and approved for medical use in 1989. In 2007, pergolide was withdrawn from the U.S. market for human use after several published studies revealed a link between the drug and increased rates of valvular heart disease. However, a veterinary form of pergolide, marketed under the trade name Prascend, is permitted for the treatment of pituitary pars intermedia dysfunction (PPID) also known as equine Cushing's syndrome (ECS) in horses.

Medical uses Pergolide is no longer available for use by humans in the United States, however, it is still used in various other countries, such as in the EU, where it is only recommended for patients who cannot take other treatments. Pergolide has also been tested for use in treatment of restless leg syndrome and hyperprolactinemia. Pergolide is currently available for veterinary use. Under the trade name Prascend, manufactured by Boehringer Ingelheim, it is commonly used in horses for the treatment of pituitary hyperplasia at the pars intermedia, also known as Equine Cushing's Syndrome (ECS).

Pharmacology

Pharmacodynamics Pergolide acts as an agonist of dopamine D2 and 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. Although pergolide is more potent as an agonist of the D2 receptor, it has high D1 receptor affinity and is one of the most potent D1 receptor agonists of the dopamine receptor agonists that are clinically available. The agonist activity of pergolide at the D1 receptor somewhat alters its clinical and side effect profile in the treatment of Parkinson's disease. Pergolide has been said to be hallucinogenic due to activation of 5-HT2A receptors. However, other sources have stated that the drug is non-hallucinogenic. It has been associated with cardiac valvulopathy due to activation of 5-HT2B receptors.

Side effects In 2003, pergolide was reported to be associated with a form of heart disease called cardiac fibrosis. In March 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. This damage 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. Among similar antiparkinsonian drugs, cabergoline, but not lisuride, exhibit this same type of serotonin receptor binding and, in January 2007, cabergoline (Dostinex) was also reported to be associated with valvular proliferation heart damage. Pergolide has also been shown to impair associative learning, and can rarely cause Raynaud's phenomenon.

Addictive behaviors At least one British pergolide user has attracted some media attention with claims that it has caused him to develop a gambling addiction. 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 problems they claim are the result of the drug's side effects.

Chemistry

Analogues Analogues of pergolide include LY-116467 (LY-062, 6-methylpergolide), LY-158A (6-ethylpergolide), and tiomergine (CF 25-397), among others.

Society and culture

Brand names Brand names of pergolide include Permax and Prascend (veterinary), among others.

Research Pergolide has been studied in the treatment of social anxiety disorder in one small study but was found to be ineffective.

See also Substituted ergoline Non-hallucinogenic 5-HT2A receptor agonist

References

Illustrations

Worked examples

Example 1 — a first encounter with Pergolide

Start with the simplest possible case. Write down what Pergolide claims or describes in one sentence, then invent the smallest concrete situation in which that sentence is true. In chemistry, the smallest case is usually a single object, a single equation or a single measurement. Check that every symbol or term in your sentence has a meaning in that case.

Example 2 — changing one variable

Take the situation from Example 1 and change exactly one quantity: double it, halve it, or set it to zero. Predict what should happen to Pergolide before you calculate. Comparing your prediction with the result is the fastest way to find out whether you understand the idea or only the words.

Example 3 — an exam-style question

Typical questions about Pergolide ask you to (a) state it precisely, (b) apply it to given data, and (c) explain a limitation. Practise writing all three answers in under five minutes; the third part is what separates a full-mark answer from an average one.

Applications of Pergolide

In research: Pergolide appears in chemistry research whenever the underlying quantities have to be modelled precisely. Papers usually cite it as a starting assumption and then explore where it breaks down.
In technology and industry: Engineering practice reuses Pergolide in design rules, simulations and safety margins. Knowing the idea lets you read a specification sheet and understand why the numbers look the way they do.
In the classroom: Pergolide is common in secondary-school and first-year university syllabi. It links to neighbouring topics 5-HT2B agonists, Cardiotoxins, D2 receptor agonists, so understanding it makes those chapters shorter.
In everyday life: Look for Pergolide outside the textbook — in sport, cooking, traffic, electronics or the sky above you. An example you found yourself is remembered far longer than one you were given.

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How to study Pergolide in 20 minutes

Read the reference excerpt below once, without taking notes.
Close the page and write down what Pergolide means in your own words.
Compare your version with the excerpt and mark what you missed.
Work through the three examples above with pen and paper.
Explain Pergolide out loud to somebody else — or to Teacher Smith in the lgStudy chat.

Frequently asked questions

What is Pergolide in simple terms?

Why does Pergolide matter?

Because it connects several chemistry ideas at once: it gives you a definition you can apply, a quantity you can calculate, and a way to check whether a result is plausible.

How should I study Pergolide?

Read the excerpt, restate it from memory, then work through the examples and applications listed on this page. The five-step study plan above takes about twenty minutes.

What does this page cover?

It gives you a compact reference excerpt plus original lgStudy explanations, examples, applications and study material on Pergolide.