Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C19H26N2S |
Molecular Weight | 314.488 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 3 / 3 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CCCN1C[C@H](CSC)C[C@H]2[C@H]1CC3=CNC4=C3C2=CC=C4
InChI
InChIKey=YEHCICAEULNIGD-MZMPZRCHSA-N
InChI=1S/C19H26N2S/c1-3-7-21-11-13(12-22-2)8-16-15-5-4-6-17-19(15)14(10-20-17)9-18(16)21/h4-6,10,13,16,18,20H,3,7-9,11-12H2,1-2H3/t13-,16-,18-/m1/s1
Molecular Formula | C19H26N2S |
Molecular Weight | 314.488 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 3 / 3 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionCurator's Comment: Description was created based on several sources, including http://www.scripintelligence.jp/wp-content/uploads/2014/05/12-January-2005-Heart-valve-disease-warning-for-pergolide-in-Europe.pdf | https://www.medicines.org.uk/emc/PIL.2413.latest.pdf?isAttachment=true&documentid=2413 | https://www.ncbi.nlm.nih.gov/pubmed/23769407
Curator's Comment: Description was created based on several sources, including http://www.scripintelligence.jp/wp-content/uploads/2014/05/12-January-2005-Heart-valve-disease-warning-for-pergolide-in-Europe.pdf | https://www.medicines.org.uk/emc/PIL.2413.latest.pdf?isAttachment=true&documentid=2413 | https://www.ncbi.nlm.nih.gov/pubmed/23769407
Pergolide is a long-acting dopamine agonist approved in 1982 for the treatment of Parkinson’s Disease. It is an ergot derivative that acts on the dopamine D2 and D3, alpha2- and alpha1-adrenergic, and 5-hydroxytryptamine (5-HT) receptors. It was indicated as adjunct therapy with levodopa/carbidopa in the symptomatic treatment of parkinsonian syndrome. It was later found that pergolide increased the risk of cardiac valvulopathy. The drug was withdrawn from the US market in March 2007 and from the Canadian market in August 2007. Pergolide stimulates centrally-located dopaminergic receptors resulting in a number of pharmacologic effects. Five dopamine receptor types from two dopaminergic subfamilies have been identified. The dopaminergic D1 receptor subfamily consists of D1 and D5 subreceptors and are associated with dyskinesias. The dopaminergic D2 receptor subfamily consists of D2, D3 and D4 subreceptors and has been associated with improvement of symptoms of movement disorders. Thus, agonist activity specific for D2 subfamily receptors, primarily D2 and D3 receptor subtypes, are the primary targets of dopaminergic antiparkinsonian agents. It is thought that postsynaptic D2 stimulation is primarily responsible for the antiparkinsonian effect of dopamine agonists, while presynaptic D2 stimulation confers neuroprotective effects. This semisynthetic ergot derivative exhibits potent agonist activity on dopamine D2- and D3-receptors. It also exhibits agonist activity on dopamine D4, D1, and D5, 5-hydroxytryptamine (5-HT)1A, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2B, 5-HT2C, α2A-, α2B-, α2C-, α1A-, α1B-, and α1D-adrenergic receptors. Parkinsonian Syndrome manifests when approximately 80% of dopaminergic activity in the nigrostriatal pathway of the brain is lost. As this striatum is involved in modulating the intensity of coordinated muscle activity (e.g. movement, balance, walking), loss of activity may result in dystonia (acute muscle contraction), Parkinsonism (including symptoms of bradykinesia, tremor, rigidity, and flattened affect), akathesia (inner restlessness), tardive dyskinesia (involuntary muscle movements usually associated with long-term loss of dopaminergic activity), and neuroleptic malignant syndrome, which manifests when complete blockage of nigrostriatal dopamine occurs. High dopaminergic activity in the mesolimbic pathway of the brain causes hallucinations and delusions; these side effects of dopamine agonists are manifestations seen in patients with schizophrenia who have overractivity in this area of the brain. The hallucinogenic side effects of dopamine agonists may also be due to 5-HT2A agonism. The tuberoinfundibular pathway of the brain originates in the hypothalamus and terminates in the pituitary gland. In this pathway, dopamine inhibits lactotrophs in anterior pituitary from secreting prolactin. Increased dopaminergic activity in the tuberoinfundibular pathway inhibits prolactin secretion. Pergolide also causes transient increases in somatotropin (growth hormone) secretion and decreases in luteinizing hormone (LH) concentrations. Pergolide is not available for use by humans in the United States, but approved for veterinary use; it was used in various other countries for the treatment of various conditions including Parkinson's disease, hyperprolactinemia, and restless leg syndrome. Pergolide in Europe was indicated for Parkinson's disease only when other dopaminergic agonist treatments had failed, and treatment had to be initiated by a
neurologist. The label warned against using doses of more than 5mg a day, whether alone or in combination with levodopa. However the marketing of this drug finally stopped in France in May 2011 and sales elsewhere in Europe ceased eventually.
CNS Activity
Originator
Sources: http://adisinsight.springer.com/drugs/800000655
Curator's Comment: # Eli Lilly
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
26.0 nM [Ki] | |||
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | PRASCEND Approved UseFor the control of clinical signs associated with Pituitary Pars Intermedia Dysfunction (Equine Cushing’s Disease) in horses. Launch Date2012 |
|||
Primary | Unknown Approved UseUnknown |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
127 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15965310/ |
0.25 mg 3 times / day steady-state, oral dose: 0.25 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
PERGOLIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
209 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15965310/ |
0.5 mg 3 times / day steady-state, oral dose: 0.5 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
PERGOLIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
472 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15965310/ |
1 mg 3 times / day steady-state, oral dose: 1 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
PERGOLIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
573 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15965310/ |
0.25 mg 3 times / day steady-state, oral dose: 0.25 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
PERGOLIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
1094 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15965310/ |
0.5 mg 3 times / day steady-state, oral dose: 0.5 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
PERGOLIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
2392 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15965310/ |
1 mg 3 times / day steady-state, oral dose: 1 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
PERGOLIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
22.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15965310/ |
0.5 mg 3 times / day steady-state, oral dose: 0.5 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
PERGOLIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
9% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/6113911/ |
138 μg single, oral dose: 138 μg route of administration: Oral experiment type: SINGLE co-administered: |
PERGOLIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
Doses
Dose | Population | Adverse events |
---|---|---|
0.05 mg single, oral Recommended |
unhealthy, 46 - 75 |
Disc. AE: Rash, Syncope... AEs leading to discontinuation/dose reduction: Rash (grade 2-3) Sources: Syncope (grade 3) |
1 mg 3 times / day steady, oral Recommended Dose: 1 mg, 3 times / day Route: oral Route: steady Dose: 1 mg, 3 times / day Sources: |
unhealthy, 46 - 75 |
|
2.2 mg multiple, oral Recommended |
unhealthy, 65.5 ± 9.5 Health Status: unhealthy Age Group: 65.5 ± 9.5 Sex: M+F Sources: |
Disc. AE: Diarrhea, Dyskinesia... AEs leading to discontinuation/dose reduction: Diarrhea (1%) Sources: Dyskinesia (1%) Dystonia (1%) Headache (1%) Liver disorder (1%) Nausea and vomiting (2.9%) Parkinsonism aggravated (1%) Sleep disorder (1%) Urinary incontinence (1%) |
14 mg multiple, oral Overdose Dose: 14 mg Route: oral Route: multiple Dose: 14 mg Sources: |
unhealthy Health Status: unhealthy Sources: |
Other AEs: Movements involuntary, Tingling... Other AEs: Movements involuntary (grade 3) Sources: Tingling (grade 3) |
19 mg multiple, oral Overdose Dose: 19 mg Route: oral Route: multiple Dose: 19 mg Sources: |
unhealthy Health Status: unhealthy Sources: |
Other AEs: Hallucinations... Other AEs: Hallucinations (grade 3) Sources: |
60 mg single, oral Overdose Dose: 60 mg Route: oral Route: single Dose: 60 mg Sources: |
healthy Health Status: healthy Sources: |
Other AEs: Vomiting, Hypotension... Other AEs: Vomiting Sources: Hypotension Agitation |
7 mg single, oral Overdose Dose: 7 mg Route: oral Route: single Dose: 7 mg Sources: |
unhealthy Health Status: unhealthy Sources: |
Other AEs: Palpitations, Hypotension... Other AEs: Palpitations Sources: Hypotension |
7 mg single, oral Overdose Dose: 7 mg Route: oral Route: single Dose: 7 mg Sources: |
unhealthy Health Status: unhealthy Sources: |
Other AEs: Ventricular extrasystoles... Other AEs: Ventricular extrasystoles Sources: |
1 mg 3 times / day multiple, oral Recommended Dose: 1 mg, 3 times / day Route: oral Route: multiple Dose: 1 mg, 3 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Other AEs: Daytime sleepiness, Hypotension symptomatic... Other AEs: Daytime sleepiness Sources: Hypotension symptomatic (10%) |
1 mg 3 times / day multiple, oral Recommended Dose: 1 mg, 3 times / day Route: oral Route: multiple Dose: 1 mg, 3 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Other AEs: Daytime sleepiness... Other AEs: Daytime sleepiness (common) Sources: |
1 mg 3 times / day multiple, oral Recommended Dose: 1 mg, 3 times / day Route: oral Route: multiple Dose: 1 mg, 3 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Disc. AE: Drug-induced hallucinosis... Other AEs: Drug-induced hallucinosis... AEs leading to discontinuation/dose reduction: Drug-induced hallucinosis (grade 3, 3%) Other AEs:Drug-induced hallucinosis (14%) Sources: |
1 mg 3 times / day multiple, oral Recommended Dose: 1 mg, 3 times / day Route: oral Route: multiple Dose: 1 mg, 3 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Other AEs: Pleuritis, Pleural effusion... Other AEs: Pleuritis (rare) Sources: Pleural effusion (rare) Pleural fibrosis (rare) Pericarditis (rare) Pericardial effusion (rare) Cardiac valvulopathy (rare) Retroperitoneal fibrosis (rare) |
1 mg 3 times / day multiple, oral Recommended Dose: 1 mg, 3 times / day Route: oral Route: multiple Dose: 1 mg, 3 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Other AEs: Hallucinations, Confusion... Other AEs: Hallucinations (7.8%) Sources: Confusion (1.8%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Rash | grade 2-3 Disc. AE |
0.05 mg single, oral Recommended |
unhealthy, 46 - 75 |
Syncope | grade 3 Disc. AE |
0.05 mg single, oral Recommended |
unhealthy, 46 - 75 |
Diarrhea | 1% Disc. AE |
2.2 mg multiple, oral Recommended |
unhealthy, 65.5 ± 9.5 Health Status: unhealthy Age Group: 65.5 ± 9.5 Sex: M+F Sources: |
Dyskinesia | 1% Disc. AE |
2.2 mg multiple, oral Recommended |
unhealthy, 65.5 ± 9.5 Health Status: unhealthy Age Group: 65.5 ± 9.5 Sex: M+F Sources: |
Dystonia | 1% Disc. AE |
2.2 mg multiple, oral Recommended |
unhealthy, 65.5 ± 9.5 Health Status: unhealthy Age Group: 65.5 ± 9.5 Sex: M+F Sources: |
Headache | 1% Disc. AE |
2.2 mg multiple, oral Recommended |
unhealthy, 65.5 ± 9.5 Health Status: unhealthy Age Group: 65.5 ± 9.5 Sex: M+F Sources: |
Liver disorder | 1% Disc. AE |
2.2 mg multiple, oral Recommended |
unhealthy, 65.5 ± 9.5 Health Status: unhealthy Age Group: 65.5 ± 9.5 Sex: M+F Sources: |
Parkinsonism aggravated | 1% Disc. AE |
2.2 mg multiple, oral Recommended |
unhealthy, 65.5 ± 9.5 Health Status: unhealthy Age Group: 65.5 ± 9.5 Sex: M+F Sources: |
Sleep disorder | 1% Disc. AE |
2.2 mg multiple, oral Recommended |
unhealthy, 65.5 ± 9.5 Health Status: unhealthy Age Group: 65.5 ± 9.5 Sex: M+F Sources: |
Urinary incontinence | 1% Disc. AE |
2.2 mg multiple, oral Recommended |
unhealthy, 65.5 ± 9.5 Health Status: unhealthy Age Group: 65.5 ± 9.5 Sex: M+F Sources: |
Nausea and vomiting | 2.9% Disc. AE |
2.2 mg multiple, oral Recommended |
unhealthy, 65.5 ± 9.5 Health Status: unhealthy Age Group: 65.5 ± 9.5 Sex: M+F Sources: |
Movements involuntary | grade 3 | 14 mg multiple, oral Overdose Dose: 14 mg Route: oral Route: multiple Dose: 14 mg Sources: |
unhealthy Health Status: unhealthy Sources: |
Tingling | grade 3 | 14 mg multiple, oral Overdose Dose: 14 mg Route: oral Route: multiple Dose: 14 mg Sources: |
unhealthy Health Status: unhealthy Sources: |
Hallucinations | grade 3 | 19 mg multiple, oral Overdose Dose: 19 mg Route: oral Route: multiple Dose: 19 mg Sources: |
unhealthy Health Status: unhealthy Sources: |
Agitation | 60 mg single, oral Overdose Dose: 60 mg Route: oral Route: single Dose: 60 mg Sources: |
healthy Health Status: healthy Sources: |
|
Hypotension | 60 mg single, oral Overdose Dose: 60 mg Route: oral Route: single Dose: 60 mg Sources: |
healthy Health Status: healthy Sources: |
|
Vomiting | 60 mg single, oral Overdose Dose: 60 mg Route: oral Route: single Dose: 60 mg Sources: |
healthy Health Status: healthy Sources: |
|
Hypotension | 7 mg single, oral Overdose Dose: 7 mg Route: oral Route: single Dose: 7 mg Sources: |
unhealthy Health Status: unhealthy Sources: |
|
Palpitations | 7 mg single, oral Overdose Dose: 7 mg Route: oral Route: single Dose: 7 mg Sources: |
unhealthy Health Status: unhealthy Sources: |
|
Ventricular extrasystoles | 7 mg single, oral Overdose Dose: 7 mg Route: oral Route: single Dose: 7 mg Sources: |
unhealthy Health Status: unhealthy Sources: |
|
Daytime sleepiness | 1 mg 3 times / day multiple, oral Recommended Dose: 1 mg, 3 times / day Route: oral Route: multiple Dose: 1 mg, 3 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
|
Hypotension symptomatic | 10% | 1 mg 3 times / day multiple, oral Recommended Dose: 1 mg, 3 times / day Route: oral Route: multiple Dose: 1 mg, 3 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Daytime sleepiness | common | 1 mg 3 times / day multiple, oral Recommended Dose: 1 mg, 3 times / day Route: oral Route: multiple Dose: 1 mg, 3 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Drug-induced hallucinosis | 14% | 1 mg 3 times / day multiple, oral Recommended Dose: 1 mg, 3 times / day Route: oral Route: multiple Dose: 1 mg, 3 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Drug-induced hallucinosis | grade 3, 3% Disc. AE |
1 mg 3 times / day multiple, oral Recommended Dose: 1 mg, 3 times / day Route: oral Route: multiple Dose: 1 mg, 3 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Cardiac valvulopathy | rare | 1 mg 3 times / day multiple, oral Recommended Dose: 1 mg, 3 times / day Route: oral Route: multiple Dose: 1 mg, 3 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Pericardial effusion | rare | 1 mg 3 times / day multiple, oral Recommended Dose: 1 mg, 3 times / day Route: oral Route: multiple Dose: 1 mg, 3 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Pericarditis | rare | 1 mg 3 times / day multiple, oral Recommended Dose: 1 mg, 3 times / day Route: oral Route: multiple Dose: 1 mg, 3 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Pleural effusion | rare | 1 mg 3 times / day multiple, oral Recommended Dose: 1 mg, 3 times / day Route: oral Route: multiple Dose: 1 mg, 3 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Pleural fibrosis | rare | 1 mg 3 times / day multiple, oral Recommended Dose: 1 mg, 3 times / day Route: oral Route: multiple Dose: 1 mg, 3 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Pleuritis | rare | 1 mg 3 times / day multiple, oral Recommended Dose: 1 mg, 3 times / day Route: oral Route: multiple Dose: 1 mg, 3 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Retroperitoneal fibrosis | rare | 1 mg 3 times / day multiple, oral Recommended Dose: 1 mg, 3 times / day Route: oral Route: multiple Dose: 1 mg, 3 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Confusion | 1.8% | 1 mg 3 times / day multiple, oral Recommended Dose: 1 mg, 3 times / day Route: oral Route: multiple Dose: 1 mg, 3 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Hallucinations | 7.8% | 1 mg 3 times / day multiple, oral Recommended Dose: 1 mg, 3 times / day Route: oral Route: multiple Dose: 1 mg, 3 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
no | ||||
no | ||||
Sources: https://pubmed.ncbi.nlm.nih.gov/24227476/ |
no | |||
yes | ||||
Sources: https://pubmed.ncbi.nlm.nih.gov/24227476/ |
yes |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
PubMed
Title | Date | PubMed |
---|---|---|
Treatment of Parkinson's disease with ropinirole after pergolide-induced retroperitoneal fibrosis. | 1999 Dec |
|
Macrophage Fcgamma receptors expression is altered by treatment with dopaminergic drugs. | 1999 Mar |
|
Sleep attacks and Parkinson's disease treatment. | 2000 Apr 15 |
|
Sleep attacks (sleep episodes) with pergolide. | 2000 Apr 15 |
|
Adverse outcomes in a controlled trial of pergolide for cocaine dependence. | 2001 |
|
Switching from pergolide to pramipexole in patients with Parkinson's disease. | 2001 |
|
[Parkinson's disease]. | 2001 Mar 3 |
|
[A 64-year-old man with parkinsonism as an initial symptom followed by dementia associated with marked abnormal behaviours]. | 2001 Nov |
|
Pergolide mesilate may improve fatigue in patients with Parkinson's disease. | 2001-2002 |
|
Restless legs syndrome in the older adult: diagnosis and management. | 2002 |
|
[Treatment of Parkinson's syndrome]. | 2002 |
|
A new design of a polysomnography-based multi-center treatment study for the restless legs syndrome. | 2002 Apr |
|
Valvular heart disease in patients taking pergolide. | 2002 Dec |
|
Drug-related valvular heart disease: here we go again: will we do better this time? | 2002 Dec |
|
Neuroleptic malignant-like syndrome after rapid switch from bromocriptine to pergolide. | 2002 Dec |
|
Effects of pharmacological agents upon a transgenic model of Parkinson's disease in Drosophila melanogaster. | 2002 Jan |
|
Pergolide protects SH-SY5Y cells against neurodegeneration induced by H(2)O(2). | 2002 Jan 2 |
|
[Pergolide: a useful agonist for the treatment of Parkinson disease]. | 2002 Jul |
|
Dopamine agonist effects on startle and sensorimotor gating in normal male subjects: time course studies. | 2002 May |
|
Plasma adrenocorticotropin (ACTH) concentrations and clinical response in horses treated for equine Cushing's disease with cyproheptadine or pergolide. | 2002 Nov |
|
Long term tolerability of high dose ergoline derived dopamine agonist therapy for the treatment of Parkinson's disease. | 2002 Nov |
|
Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes. | 2002 Nov |
|
Dopamine agonist monotherapy in Parkinson's disease. | 2002 Nov 30 |
|
Treatment with pergolide or cyproheptadine of pituitary pars intermedia dysfunction (equine Cushing's disease). | 2002 Nov-Dec |
|
An evidence-based review of dopamine receptor agonists in the treatment of Parkinson's disease. | 2002 Oct |
|
The effect of pergolide on cognitive performance of young and middle-aged rats. | 2002 Sep |
|
Pergolide-induced pleuropulmonary fibrosis. | 2002 Sep-Oct |
|
Dopamine agonists induce episodes of irresistible daytime sleepiness. | 2003 |
|
The modulatory effects of dopamine D1 and D2 receptor function on object working memory in humans. | 2003 Mar |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.drugs.com/pro/pergolide.html
Administration of Pergolide mesylate tablets should be initiated with a daily dosage of 0.05 mg for the first 2 days. The dosage should then be gradually increased by 0.1 or 0.15 mg/day every third day over the next 12 days of therapy. The dosage may then be increased by 0.25 mg/day every third day until an optimal therapeutic dosage is achieved.
Pergolide mesylate tablets are usually administered in divided doses 3 times per day. During dosage titration, the dosage of concurrent l-dopa/carbidopa may be cautiously decreased.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/16129789
Pergolide (10 umol/L) depolarized PASMC
membrane potential from 51.11.5 to 44.00.8 mV in
resistance PASMCs. In CHO cells, pergolide
(10(-7) to 10(-5) mol/L) inhibited heterologously expressed
rat BKCa channels in a dose-dependent manner.
Substance Class |
Chemical
Created
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on
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Record UNII |
24MJ822NZ9
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Record Status |
Validated (UNII)
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Record Version |
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Official Name | English | ||
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Preferred Name | English | ||
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Common Name | English | ||
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Common Name | English |
Classification Tree | Code System | Code | ||
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FDA ORPHAN DRUG |
108197
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LIVERTOX |
NBK548593
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WHO-ATC |
N04BC02
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NDF-RT |
N0000000117
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NDF-RT |
N0000175767
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CFR |
21 CFR 520.1705
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NCI_THESAURUS |
C66884
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WHO-VATC |
QN04BC02
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NDF-RT |
N0000007620
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NCI_THESAURUS |
C38149
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8047
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24MJ822NZ9
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47811
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m8547
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PRIMARY | Merck Index | ||
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CHEMBL531
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D010479
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DB01186
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PERGOLIDE
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C61886
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DTXSID2023438
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4651
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admin on Mon Mar 31 18:07:31 GMT 2025 , Edited by admin on Mon Mar 31 18:07:31 GMT 2025
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66104-22-1
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admin on Mon Mar 31 18:07:31 GMT 2025 , Edited by admin on Mon Mar 31 18:07:31 GMT 2025
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100000082732
Created by
admin on Mon Mar 31 18:07:31 GMT 2025 , Edited by admin on Mon Mar 31 18:07:31 GMT 2025
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2105
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admin on Mon Mar 31 18:07:31 GMT 2025 , Edited by admin on Mon Mar 31 18:07:31 GMT 2025
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63617
Created by
admin on Mon Mar 31 18:07:31 GMT 2025 , Edited by admin on Mon Mar 31 18:07:31 GMT 2025
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24MJ822NZ9
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admin on Mon Mar 31 18:07:31 GMT 2025 , Edited by admin on Mon Mar 31 18:07:31 GMT 2025
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SUB09725MIG
Created by
admin on Mon Mar 31 18:07:31 GMT 2025 , Edited by admin on Mon Mar 31 18:07:31 GMT 2025
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Related Record | Type | Details | ||
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TARGET -> AGONIST | |||
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BINDER->LIGAND |
BINDING
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TARGET -> AGONIST |
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SALT/SOLVATE -> PARENT |
Related Record | Type | Details | ||
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
---|---|---|---|---|---|---|
Biological Half-life | PHARMACOKINETIC |
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