Pergolide


Concise Prescribing Info
Indications/Uses
Parkinson's disease.
Dosage/Direction for Use
Adult : PO As monotherapy: Initial: 50 mcg in the evening on day 1, then increased to 50 mcg bid on days 2-4. Then, increased by 100-250 mcg every 3-4 days, given in 3 divided doses, up to a daily dose of 1.5 mg at day 28. Then, after day 30, dose is increased by a max of 250 mcg twice wkly, until optimum response is attained. Maintenance dose: 2.1-2.5 mg daily, given in 3 divided doses. Max: 3 mg daily. As adjunct to levodopa: Initial: 50 mcg daily for 2 days, then increased by 100-150 mcg, in 3 divided doses every 3 days over the next for 12 days. Then, increased by 250 mcg every 3 days, concurrently decrease levodopa dose until an optimum response is attained. Max: 3 mg daily.
Dosage Details
Oral
Parkinson's disease
Adult: As monotherapy: Initially, 50 mcg in the evening on day 1, then increased to 50 mcg bid on days 2-4. Then, increased by 100-250 mcg every 3-4 days, given in 3 divided doses, up to a daily dose of 1.5 mg at day 28. Then, after day 30, dose is increased by a max of 250 mcg twice wkly, until optimum response is attained. Maintenance dose: 2.1-2.5 mg daily, given in 3 divided doses. Max: 3 mg daily. As adjunct to levodopa: Initially, 50 mcg daily for 2 days, then increased by 100-150 mcg, given in 3 divided doses every 3 days over the next for 12 days. Then, increased by 250 mcg every 3 days, concurrently decrease levodopa dose until an optimum response is attained. Max: 3 mg daily.
Contraindications
History of cardiac valvulopathy and fibrotic disorders.
Special Precautions
Patient w/ history of psychosis, confusional states, hallucination, somnolence; risk factor for cardiac dysrhythmias; sleep disorders. Pregnancy and lactation. Avoid abrupt withdrawal.
Adverse Reactions
Significant: Fibrotic complications (e.g. pulmonary, pleural, retroperitoneal fibrosis; pericarditis, pleuritis, pericardial and pleural effusion); exacerbate confusion, hallucinations, somnolence, sudden sleep onset, dyskinesia, impulse control disorders (e.g. pathological gambling, increased libido, hypersexuality, compulsive spending or buying, binge eating, compulsive eating), atrial premature contractions, sinus tachycardia, orthostatic and sustained hypotension.
Nervous: Headache, dizziness, asthenia, paraesthesia, extra pyramidal syndrome, akinesia, dystonia, hypertonia, neuralgia, speech disorder, tremor, abnormal gait, anxiety, depression, psychosis, incoordination flu-syndrome.
CV: Chest pain, palpitations, syncope, HTN, vasodilation, arrhthymia, MI, peripheral oedema.
GI: Nausea, vomiting, constipation, diarrhoea, dyspepsia, abdominal pain, dry mouth, dysphagia.
Resp: Rhinitis, dyspnoea, hiccups, epistaxis.
Genitourinary: UTI, urinary frequency, haematuria.
Haematologic: Anaemia.
Musculoskeletal: Back and neck pain, arthralgia, myalgia, twitching, dystonia.
Ophthalmologic: Abnormal vision, diplopia, eye disorder.
Dermatologic: Sweating, rash, facial oedema.
Others: Pain, chills, infection.
Potentially Fatal: Cardiac valvulopathy.
Patient Counseling Information
This drug may cause somnolence and sudden sleep onset, if affected, do not drive or operate machinery.
MonitoringParameters
Assess CV status including ECG before initiation of treatment and periodically thereafter. Perform baseline evaluation of ESR, other inflammatory markers, lung function/chest X-ray, serum creatine, renal function and monitor thereafter. Monitor for signs and symptoms of valvulopathy (e.g. dyspnoea, oedema, CHF, cardiac murmurs), fibrotic disorders (e.g. cough, dyspnoea, oedema, CHF, cardiac rub, urinary tract obstruction), development of impulse control disorders.
Overdosage
Symptoms: Vomiting, hypotension, agitation, severe hallucinations, severe involuntary movements, tingling in arms and legs, palpitations, ventricular extrasystoles. Management: Symptomatic and supportive treatment. Maintain arterial BP. May give antiarrhythmic agent if necessary. Give phenothiazine or butyrophenone neuroleptic agent for CNS stimulation. Establish patient’s airway and support ventilation and perfusion. May employ activated charcoal instead of or in addition to gastric emptying to hasten elimination of absorbed drug.
Drug Interactions
Increased risk of sudden sleep onset w/ sedating agents. May increase risk of hypotension w/ antihypertensive agents. Exacerbation of confusion, hallucination and dyskinesia w/ levodopa. Decreased effectiveness w/ dopamine antagonists (e.g. metoclopramide, neuroleptics).
Action
Description: Pergolide, an ergot derivative, is a potent dopamine agonist at D1, D2 and D3 receptor sites. In Parkinson’s disease, it directly stimulates postsynaptic dopamine receptors in the nigrostriatal system.
Pharmacokinetics:
Absorption: Absorbed from the GI tract.
Distribution: Plasma protein binding: Approx 90%.
Metabolism: Extensively metabolised into at least 10 metabolites including N-despropylpergolide, pergolide sulfone and pergolide sulfoxide.
Excretion: Mainly via urine (approx 55%, as metabolites); faeces (40%, as metabolites); expired CO2 (5%, as metabolites).
Chemical Structure

Click on icon to see table/diagram/image
Storage
Store below 25°C.
ATC Classification
N04BC02 - pergolide ; Belongs to the class of dopamine agonist. Used in the management of Parkinson's disease.
Disclaimer: This information is independently developed by MIMS based on Pergolide from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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