Pergolide


Thông tin thuốc gốc
Chỉ định và Liều dùng
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.
Chống chỉ định
History of cardiac valvulopathy and fibrotic disorders.
Thận trọng
Patient w/ history of psychosis, confusional states, hallucination, somnolence; risk factor for cardiac dysrhythmias; sleep disorders. Pregnancy and lactation. Avoid abrupt withdrawal.
Phản ứng phụ
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.
Thông tin tư vấn bệnh nhân
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.
Quá liều
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.
Tương tác
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).
Tác dụng
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).
Đặc tính

Chemical Structure Image
Pergolide

Source: National Center for Biotechnology Information. PubChem Database. Pergolide, CID=47811, https://pubchem.ncbi.nlm.nih.gov/compound/Pergolide (accessed on Jan. 22, 2020)

Bảo quản
Store below 25°C.
Phân loại MIMS
Phân loại ATC
N04BC02 - pergolide ; Belongs to the class of dopamine agonist. Used in the management of Parkinson's disease.
References
Buckingham R (ed). Pergolide Mesilate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 05/10/2017.

Joint Formulary Committee. Pergolide. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 05/10/2017.

Pergolide 1 mg Tablets (Norton Healthcare Limited). MHRA. https://products.mhra.gov.uk/. Accessed 05/10/2017.

Pergolide 250 mcg Tablets (Norton Healthcare Limited). MHRA. https://products.mhra.gov.uk/. Accessed 05/10/2017.

Pergolide 50 mcg Tablets (Norton Healthcare Limited). MHRA. https://products.mhra.gov.uk/. Accessed 05/10/2017.

Permax Tablet (Valeant Pharmaceuticals, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 05/10/2017.

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