Pergolide
Drug Info:
Top
Pergolide
Brand names: Permax, Permax®
Chemical formula:
- Espa�ol:
- Mesilato de pergolida, Tableta oral
Pergolide Mesylate Oral tablet
What is this medicine?
PERGOLIDE (PER go lide) is used to control the signs and symptoms of Parkinson's disease. It helps to improve muscle control and movement difficulties.
NOTE: This drug is being removed from the US market. If you are currently taking Pergolide, contact your doctor about stopping this medicine and finding an alternative therapy. Do not stop taking this medicine without first speaking to your doctor. Abruptly stopping this medicine can be dangerous.
This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.
What should I tell my health care provider before I take this medicine?
They need to know if you have any of these conditions:
•history of heart disease or heart valve disease
•low blood pressure
•an unusual or allergic reaction to pergolide, ergot alkaloids, or other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding
How should I use this medicine?
Take this medicine by mouth with a glass of water. Follow the directions on the prescription label. Take your doses at regular intervals. Do not take your medicine more often than directed. Do not stop taking except on the advice of your doctor or health care professional.
Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.
Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.
What may interact with this medicine?
•medicines for mental problems and psychotic disturbances
•metoclopramide
This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.
What should I watch for while using this medicine?
Visit your doctor or health care professional for regular checks on your progress. It may be several weeks or months before you feel the full effect of this medicine.
You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you. You may experience flushing, nausea, vomiting, pale skin, or sweating before dizziness or fainting occurs. Do not get up too quickly from a lying or sitting position. Report any dizziness or related symptoms to your health care provider as soon as possible. Alcohol may increase dizziness and drowsiness. Avoid alcoholic drinks. Do not take any medications that cause drowsiness without first checking with your health care provider.
If you find that you have sudden feelings of wanting to sleep during normal activities, like cooking, watching television, or while driving or riding in a car, you should contact your health care professional.
Your mouth may get dry. Chewing sugarless gum or sucking hard candy, and drinking plenty of water may help. Contact your doctor if the problem does not go away or is severe.
What side effects may I notice from receiving this medicine?
Side effects that you should report to your doctor or health care professional as soon as possible:
•anxiety, restlessness
•chest pain
•confusion
•difficulty breathing or catching your breath
•double vision, or other vision problems
•fainting spells
•falling asleep during normal activities like driving
•fast, irregular heartbeat
•hallucination, loss of contact with reality
•lower back pain, or chest or neck pain
•mental changes
•palpitations
•uncontrollable movements of the arms, face, hands, head, mouth, shoulders, or upper body
•unusually weak or tired
Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•constipation or diarrhea
•difficulty sleeping
•headache
•loss of appetite
•nausea
•runny or stuffy nose
•stomach pain
•vomiting
•weight change
This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
Where should I keep my medicine?
Keep out of the reach of children.
Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Throw away any unused medicine after the expiration date.
Last updated: 7/1/2002
Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.
Oxford A-Z of Medicinal Drugs:
Top
pergolide
A dopamine receptor agonist, similar to bromocriptine, used alone or as an adjunct to levodopa in the treatment of Parkinson's disease. It is available as tablets on prescription only.
Side effects:
include hallucinations, confusion, involuntary abnormal movements, somnolence, abdominal pain, nausea, dyspepsia, double vision, breathlessness, lung problems, and insomnia.
Precautions:
pergolide should not be taken by people with heart-valve disease and should be used with caution in people with abnormal heart rhythms (see arrhythmia) or a history of confusion or hallucinations and in women who are pregnant or breastfeeding (it stops production of breast milk). Dosage should be reduced gradually at the end of treatment.
Interactions with other drugs:
Antipsychotics: antagonize the effect of pergolide.
Metoclopramide antagonizes the effect of pergolide.
Proprietary preparation:
Celance.
| peppermint oil, pentoxifylline, pentostatin | |
| pericyazine, perindopril, permethrin |
Wikipedia on Answers.com:
Top
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 | eMolecules & PubChem |
|
|
 (what is this?) (verify) |
|
Pergolide (Permax, Pergotoliderived) 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.
|
Contents
|
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-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
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-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.[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]
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. On March 30, 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.[11] However, Pergolide is still available in many other countries.
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-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. 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
- ^ Pergolide Withdrawn From US Market
|
|||||||||||||||||||||||||||||||||
|
|||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
|
||||||||||||||
|
|||||
This entry is from Wikipedia, the leading user-contributed encyclopedia. It may not have been reviewed by professional editors (see full disclaimer)
Post a question - any question - to the WikiAnswers community:
Copyrights:
Oxford A-Z of Medicinal Drugs
Market University Press. © 2000, 2003, 2010 An A-Z of Medicinal Drugs. All rights reserved.
Read more
