The P-I-E-N-O Parkinsn's List Drug Database
pergolide / PermaxTM
ANTIPARKINSON:
Dopamine agonist
Description: Pergolide is an oral, semisynthetic ergot alkaloid derivative used in the management of Parkinson's disease. Pergolide is similar in action to other drugs in this class such as bromocriptine and lisuride. Pergolide has 10 to 1000 times the potency of bromocriptine on a milligram basis and may be effective in patients who have become tolerant to bromocriptine. Pergolide was approved by the FDA in December 1988.
Mechanism of Action: As a potent dopaminergic agonist, pergolide directly stimulates postsynaptic dopamine receptors in the nigrostriatal system. Like apomorphine and lisuride, the dopamine-agonist properties of pergolide are not associated with presynaptic dopamine synthesis or stores; pergolide is an agonist at postsynaptic receptors. Pergolide is one of the most potent dopaminergic agonists. Unlike bromocriptine, pergolide stimulates both DA and DA receptors. Pergolide also causes less nausea and orthostatic hypotension than does bromocriptine and may be effective in patients who have become tolerant to bromocriptine.
Pergolide inhibits the secretion of prolactin in humans and causes transient increases in serum growth hormone and decreases in luteinizing hormone. The effects on prolactin secretion persist much longer than antiparkinsonian action.
Pharmacokinetics: Pergolide is administered orally and is well absorbed. It is approximately 90% bound to plasma proteins. The drug undergoes metabolism to 10 metabolites, some of which are pharmacologically active. Elimination of the drug is primarily renal. The elimination half-life has been reported as 27 hours.
CONTRAINDICATIONS/PRECAUTIONS: Pergolide is contraindicated in patients who are known to have ergot alkaloid hypersensitivity.
Pergolide can cause symptomatic orthostatic hypotension or sustained hypotension, especially during initial administration. Tolerance to these effects will develop if doses are titrated gradually. Patients should be warned of this risk. Initial doses should be small, gradually increasing over a 3-to 4-week period.
Hallucinations have occurred in patients receiving pergolide, requiring discontinuation of therapy in some patients. Patients should be warned of this adverse reaction.
Pergolide is classified as pregnancy category B. No adequate studies have examined the effects of pergolide on the human fetus. Animal reproduction studies have shown no adverse fetal effects.
DRUG INTERACTIONS: Pergolide is a potent dopamine-receptor agonist. Dopamine-receptor antagonists, including the neuroleptics (phenothiazines, haloperidol, and thiothixene), or metoclopramide should not be administered concurrently because they can antagonize the effects of pergolide.
ADVERSE REACTIONS: Pergolide is administered as adjunctive therapy to levodopa/carbidopa. The adverse effect profile reported from clinical trials reflect either combined therapy with pergolide/levodopa/carbidopa or placebo/levodopa/carbidopa.
Adverse CNS effects associated with pergolide administration occur frequently. Those seen more often in pergolide-treated patients as opposed to those treated with placebo are dyskinesias (involuntary movements of the head, face, tongue, upper arms and body), dystonia, hallucinations, drowsiness, anxiety and insomnia. Less frequent CNS reactions include akathisia, confusion, dizziness, psychosis, and personality changes. Sudden withdrawal of pergolide therapy can precipitate CNS adverse effects such as hallucinations and confusion in patients remaining on levodopa/carbidopa. For these patients a gradual decrease in dosage is recommended.
In clinical trials symptomatic orthostatic hypotension and/or sustained hypotension occurred in more than 10% of patients, compared to 7% taking placebo (both taken in conjunction with levodopa/carbidopa). Careful dosage titration can improve this profile, and tolerance can develop with continued therapy. Patients need to be aware of the risk of syncope and the need for gradual dosage increase. Other cardiovascular adverse events include occasional hypertension, palpitations and the possibility of myocardial infarction. Vasodilatation may occur. There have been rare cases of CNS hemorrhage. Diplopia and headache may be symptomatic of cerebrovascular hemorrhage.
Gastrointestinal complaints with pergolide were frequently reported in clinical trials, usually at a rate about twice that for placebo. They include abdominal pain, constipation, diarrhea, dyspepsia, anorexia, nausea/vomiting and less frequently xerostomia.
For the body as a whole, pain has been reported at a variety of sites while taking pergolide. These include chest, neck and back pain. A flu-like syndrome occurs infrequently with fever and chills. Rhinitis was reported by 12% of patients taking pergolide as opposed to 5% taking placebo. Dyspnea occurred in 4.8% vs 1.1% on placebo.
Other less frequent adverse reactions with pergolide include myalgia, weakness, weight gain or weight loss.
PATIENT INFORMATION:
What do pergolide tablets do?
Pergolide (PermaxTM ) can help correct an imbalance of chemicals in the brain thought to be responsible for Parkinson's disease. Pergolide helps to improve muscle control and movement difficulties. Pergolide will not cure Parkinson's disease, but will help to control the symptoms and slow down the progression of the disease. Pergolide tablets are taken together with other tablets that control parkinsonian symptoms. Generic pergolide tablets are not yet available.
What should my doctor, dentist, or pharmacist know before I take pergolide?
They need to know if you have any of these conditions:
How should I take this medicine?
Take pergolide tablets by mouth. Follow the directions on the prescription label. Swallow the tablets with a drink of water. Take your doses at regular intervals. Do not take your medicine more often than directed.
Special precautions for use in children:
This medicine is not for children.
What if I miss a dose?
If you miss a dose, take it as soon as you can. If it is almost time for your next dose, take only that dose. Do not take double or extra doses.
What other medicines can interact with pergolide?
Tell your doctor or pharmacist: about all other medicines you are taking, including non-prescription medicines; if you are a frequent user of drinks with caffeine or alcohol; if you smoke; or if you use illegal drugs. These may affect the way your medicine works. Check before stopping or starting any of your medicines.
What side effects may I notice from taking pergolide?
Serious side effects with pergolide include:
Call your doctor as soon as you can if you get any of these side effects.
Minor side effects with pergolide include:
Let your doctor know about these side effects if they do not go away or if they annoy you.
What do I need to watch for while I take pergolide?
Visit your doctor for regular checks on your progress. It may be several weeks or months before you feel the full effect of pergolide. Continue to take your medicine on a regular schedule and do not stop taking except on your doctor's advice.
You may get dizzy or have difficulty controlling your movements. Do not drive, use machinery, or do anything that needs mental alertness until you know how pergolide affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. Alcohol can increase possible dizziness; avoid alcoholic drinks. If you are going to have surgery, tell your doctor or dentist that you are taking pergolide.
Pergolide may make your mouth dry. Chewing sugarless gum, sucking hard candy and drinking plenty of water may help. Visit your dentist regularly.
Where can I keep my medicine?
Keep out of the reach of children in a container that small children cannot open.
Store at room temperature between 15 and 30C (59 and 86F). Keep container tightly closed. Throw away any unused medicine after the expiration date.
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