U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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
Structure of PERGOLIDE

SMILES

[H][C@@]12CC3=CNC4=CC=CC(=C34)[C@@]1([H])C[C@@H](CSC)CN2CCC

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

HIDE SMILES / InChI

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

Description
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 The drug was withdrawn from the US market in March 2007 and from the Canadian market in August 2007.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.

Originator

Curator's Comment: # Eli Lilly

Approval Year

Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
209 ng/mL
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
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
127 ng/mL
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
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
1094 ng × h/mL
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
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
573 ng × h/mL
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
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
22.8 h
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

Funbound

ValueDoseCo-administeredAnalytePopulation
9%
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

Doses

DosePopulationAdverse events​
0.05 mg single, oral
Recommended
Dose: 0.05 mg
Route: oral
Route: single
Dose: 0.05 mg
Co-administed with::
levodopa oral
Sources: Page: p.123
unhealthy, 46 - 75
n = 14
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: 46 - 75
Sex: M+F
Population Size: 14
Sources: Page: p.123
Disc. AE: Rash, Syncope...
AEs leading to
discontinuation/dose reduction:
Rash (grade 2-3)
Syncope (grade 3)
Sources: Page: p.123
1 mg 3 times / day steady, oral
Recommended
Dose: 1 mg, 3 times / day
Route: oral
Route: steady
Dose: 1 mg, 3 times / day
Co-administed with::
levodopa oral
Sources: Page: p.123
unhealthy, 46 - 75
n = 14
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: 46 - 75
Sex: M+F
Population Size: 14
Sources: Page: p.123
2.2 mg multiple, oral (mean)
Recommended
Dose: 2.2 mg
Route: oral
Route: multiple
Dose: 2.2 mg
Co-administed with::
levodopa oral(562.5 mg/day)
Sources: Page: p.863
unhealthy, 65.5 ± 9.5
n = 102
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: 65.5 ± 9.5
Sex: M+F
Population Size: 102
Sources: Page: p.863
Disc. AE: Diarrhea, Dyskinesia...
AEs leading to
discontinuation/dose reduction:
Diarrhea (1%)
Dyskinesia (1%)
Dystonia (1%)
Headache (1%)
Liver disorder (1%)
Nausea and vomiting (2.9%)
Parkinsonism aggravated (1%)
Sleep disorder (1%)
Urinary incontinence (1%)
Sources: Page: p.863
14 mg multiple, oral
Overdose
Dose: 14 mg
Route: oral
Route: multiple
Dose: 14 mg
Sources: Page: p.11
unhealthy
n = 1
Health Status: unhealthy
Condition: Parkinson’s disease
Population Size: 1
Sources: Page: p.11
Other AEs: Movements involuntary, Tingling...
Other AEs:
Movements involuntary (grade 3)
Tingling (grade 3)
Sources: Page: p.11
19 mg multiple, oral
Overdose
Dose: 19 mg
Route: oral
Route: multiple
Dose: 19 mg
Sources: Page: p.11
unhealthy
n = 1
Health Status: unhealthy
Condition: Parkinson’s disease
Population Size: 1
Sources: Page: p.11
Other AEs: Hallucinations...
60 mg single, oral
Overdose
Dose: 60 mg
Route: oral
Route: single
Dose: 60 mg
Sources: Page: p.11
healthy
n = 1
Other AEs: Vomiting, Hypotension...
7 mg single, oral
Overdose
Dose: 7 mg
Route: oral
Route: single
Dose: 7 mg
Sources: Page: p.11
unhealthy
n = 1
Health Status: unhealthy
Condition: Parkinson’s disease
Population Size: 1
Sources: Page: p.11
Other AEs: Palpitations, Hypotension...
7 mg single, oral
Overdose
Dose: 7 mg
Route: oral
Route: single
Dose: 7 mg
Sources: Page: p.11-12
unhealthy
n = 1
Health Status: unhealthy
Condition: Parkinson’s disease
Population Size: 1
Sources: Page: p.11-12
Other AEs: Ventricular extrasystoles...
1 mg 3 times / day multiple, oral
Recommended
Dose: 1 mg, 3 times / day
Route: oral
Route: multiple
Dose: 1 mg, 3 times / day
Co-administed with::
l-dopa/carbidopa oral(650 mg/day)
Sources: Page: p.7
unhealthy
n = 1200
Health Status: unhealthy
Condition: Parkinson’s disease
Population Size: 1200
Sources: Page: p.7
Other AEs: Hallucinations, Confusion...
Other AEs:
Hallucinations (7.8%)
Confusion (1.8%)
Sources: Page: p.7
1 mg 3 times / day multiple, oral
Recommended
Dose: 1 mg, 3 times / day
Route: oral
Route: multiple
Dose: 1 mg, 3 times / day
Co-administed with::
l-dopa/carbidopa oral(650 mg/day)
Sources: Page: p.4
unhealthy
Health Status: unhealthy
Condition: Parkinson’s disease
Sources: Page: p.4
Other AEs: Daytime sleepiness, Hypotension symptomatic...
Other AEs:
Daytime sleepiness
Hypotension symptomatic (10%)
Sources: Page: p.4
1 mg 3 times / day multiple, oral
Recommended
Dose: 1 mg, 3 times / day
Route: oral
Route: multiple
Dose: 1 mg, 3 times / day
Co-administed with::
l-dopa/carbidopa oral(650 mg/day)
Sources: Page: p.4
unhealthy
Health Status: unhealthy
Condition: Somnolence
Sources: Page: p.4
Other AEs: 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
Co-administed with::
l-dopa/carbidopa oral(650 mg/day)
Sources: Page: p.4-5
unhealthy
Health Status: unhealthy
Condition: Parkinson’s disease
Sources: Page: p.4-5
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: Page: p.4-5
1 mg 3 times / day multiple, oral
Recommended
Dose: 1 mg, 3 times / day
Route: oral
Route: multiple
Dose: 1 mg, 3 times / day
Co-administed with::
l-dopa/carbidopa oral(650 mg/day)
Sources: Page: p.5
unhealthy
Health Status: unhealthy
Condition: Parkinson’s disease
Sources: Page: p.5
Other AEs: Pleuritis, Pleural effusion...
Other AEs:
Pleuritis (rare)
Pleural effusion (rare)
Pleural fibrosis (rare)
Pericarditis (rare)
Pericardial effusion (rare)
Cardiac valvulopathy (rare)
Retroperitoneal fibrosis (rare)
Sources: Page: p.5
AEs

AEs

AESignificanceDosePopulation
Rash grade 2-3
Disc. AE
0.05 mg single, oral
Recommended
Dose: 0.05 mg
Route: oral
Route: single
Dose: 0.05 mg
Co-administed with::
levodopa oral
Sources: Page: p.123
unhealthy, 46 - 75
n = 14
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: 46 - 75
Sex: M+F
Population Size: 14
Sources: Page: p.123
Syncope grade 3
Disc. AE
0.05 mg single, oral
Recommended
Dose: 0.05 mg
Route: oral
Route: single
Dose: 0.05 mg
Co-administed with::
levodopa oral
Sources: Page: p.123
unhealthy, 46 - 75
n = 14
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: 46 - 75
Sex: M+F
Population Size: 14
Sources: Page: p.123
Diarrhea 1%
Disc. AE
2.2 mg multiple, oral (mean)
Recommended
Dose: 2.2 mg
Route: oral
Route: multiple
Dose: 2.2 mg
Co-administed with::
levodopa oral(562.5 mg/day)
Sources: Page: p.863
unhealthy, 65.5 ± 9.5
n = 102
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: 65.5 ± 9.5
Sex: M+F
Population Size: 102
Sources: Page: p.863
Dyskinesia 1%
Disc. AE
2.2 mg multiple, oral (mean)
Recommended
Dose: 2.2 mg
Route: oral
Route: multiple
Dose: 2.2 mg
Co-administed with::
levodopa oral(562.5 mg/day)
Sources: Page: p.863
unhealthy, 65.5 ± 9.5
n = 102
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: 65.5 ± 9.5
Sex: M+F
Population Size: 102
Sources: Page: p.863
Dystonia 1%
Disc. AE
2.2 mg multiple, oral (mean)
Recommended
Dose: 2.2 mg
Route: oral
Route: multiple
Dose: 2.2 mg
Co-administed with::
levodopa oral(562.5 mg/day)
Sources: Page: p.863
unhealthy, 65.5 ± 9.5
n = 102
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: 65.5 ± 9.5
Sex: M+F
Population Size: 102
Sources: Page: p.863
Headache 1%
Disc. AE
2.2 mg multiple, oral (mean)
Recommended
Dose: 2.2 mg
Route: oral
Route: multiple
Dose: 2.2 mg
Co-administed with::
levodopa oral(562.5 mg/day)
Sources: Page: p.863
unhealthy, 65.5 ± 9.5
n = 102
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: 65.5 ± 9.5
Sex: M+F
Population Size: 102
Sources: Page: p.863
Liver disorder 1%
Disc. AE
2.2 mg multiple, oral (mean)
Recommended
Dose: 2.2 mg
Route: oral
Route: multiple
Dose: 2.2 mg
Co-administed with::
levodopa oral(562.5 mg/day)
Sources: Page: p.863
unhealthy, 65.5 ± 9.5
n = 102
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: 65.5 ± 9.5
Sex: M+F
Population Size: 102
Sources: Page: p.863
Parkinsonism aggravated 1%
Disc. AE
2.2 mg multiple, oral (mean)
Recommended
Dose: 2.2 mg
Route: oral
Route: multiple
Dose: 2.2 mg
Co-administed with::
levodopa oral(562.5 mg/day)
Sources: Page: p.863
unhealthy, 65.5 ± 9.5
n = 102
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: 65.5 ± 9.5
Sex: M+F
Population Size: 102
Sources: Page: p.863
Sleep disorder 1%
Disc. AE
2.2 mg multiple, oral (mean)
Recommended
Dose: 2.2 mg
Route: oral
Route: multiple
Dose: 2.2 mg
Co-administed with::
levodopa oral(562.5 mg/day)
Sources: Page: p.863
unhealthy, 65.5 ± 9.5
n = 102
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: 65.5 ± 9.5
Sex: M+F
Population Size: 102
Sources: Page: p.863
Urinary incontinence 1%
Disc. AE
2.2 mg multiple, oral (mean)
Recommended
Dose: 2.2 mg
Route: oral
Route: multiple
Dose: 2.2 mg
Co-administed with::
levodopa oral(562.5 mg/day)
Sources: Page: p.863
unhealthy, 65.5 ± 9.5
n = 102
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: 65.5 ± 9.5
Sex: M+F
Population Size: 102
Sources: Page: p.863
Nausea and vomiting 2.9%
Disc. AE
2.2 mg multiple, oral (mean)
Recommended
Dose: 2.2 mg
Route: oral
Route: multiple
Dose: 2.2 mg
Co-administed with::
levodopa oral(562.5 mg/day)
Sources: Page: p.863
unhealthy, 65.5 ± 9.5
n = 102
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: 65.5 ± 9.5
Sex: M+F
Population Size: 102
Sources: Page: p.863
Movements involuntary grade 3
14 mg multiple, oral
Overdose
Dose: 14 mg
Route: oral
Route: multiple
Dose: 14 mg
Sources: Page: p.11
unhealthy
n = 1
Health Status: unhealthy
Condition: Parkinson’s disease
Population Size: 1
Sources: Page: p.11
Tingling grade 3
14 mg multiple, oral
Overdose
Dose: 14 mg
Route: oral
Route: multiple
Dose: 14 mg
Sources: Page: p.11
unhealthy
n = 1
Health Status: unhealthy
Condition: Parkinson’s disease
Population Size: 1
Sources: Page: p.11
Hallucinations grade 3
19 mg multiple, oral
Overdose
Dose: 19 mg
Route: oral
Route: multiple
Dose: 19 mg
Sources: Page: p.11
unhealthy
n = 1
Health Status: unhealthy
Condition: Parkinson’s disease
Population Size: 1
Sources: Page: p.11
Agitation
60 mg single, oral
Overdose
Dose: 60 mg
Route: oral
Route: single
Dose: 60 mg
Sources: Page: p.11
healthy
n = 1
Hypotension
60 mg single, oral
Overdose
Dose: 60 mg
Route: oral
Route: single
Dose: 60 mg
Sources: Page: p.11
healthy
n = 1
Vomiting
60 mg single, oral
Overdose
Dose: 60 mg
Route: oral
Route: single
Dose: 60 mg
Sources: Page: p.11
healthy
n = 1
Hypotension
7 mg single, oral
Overdose
Dose: 7 mg
Route: oral
Route: single
Dose: 7 mg
Sources: Page: p.11
unhealthy
n = 1
Health Status: unhealthy
Condition: Parkinson’s disease
Population Size: 1
Sources: Page: p.11
Palpitations
7 mg single, oral
Overdose
Dose: 7 mg
Route: oral
Route: single
Dose: 7 mg
Sources: Page: p.11
unhealthy
n = 1
Health Status: unhealthy
Condition: Parkinson’s disease
Population Size: 1
Sources: Page: p.11
Ventricular extrasystoles
7 mg single, oral
Overdose
Dose: 7 mg
Route: oral
Route: single
Dose: 7 mg
Sources: Page: p.11-12
unhealthy
n = 1
Health Status: unhealthy
Condition: Parkinson’s disease
Population Size: 1
Sources: Page: p.11-12
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
Co-administed with::
l-dopa/carbidopa oral(650 mg/day)
Sources: Page: p.7
unhealthy
n = 1200
Health Status: unhealthy
Condition: Parkinson’s disease
Population Size: 1200
Sources: Page: p.7
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
Co-administed with::
l-dopa/carbidopa oral(650 mg/day)
Sources: Page: p.7
unhealthy
n = 1200
Health Status: unhealthy
Condition: Parkinson’s disease
Population Size: 1200
Sources: Page: p.7
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
Co-administed with::
l-dopa/carbidopa oral(650 mg/day)
Sources: Page: p.4
unhealthy
Health Status: unhealthy
Condition: Parkinson’s disease
Sources: Page: p.4
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
Co-administed with::
l-dopa/carbidopa oral(650 mg/day)
Sources: Page: p.4
unhealthy
Health Status: unhealthy
Condition: Parkinson’s disease
Sources: Page: p.4
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
Co-administed with::
l-dopa/carbidopa oral(650 mg/day)
Sources: Page: p.4
unhealthy
Health Status: unhealthy
Condition: Somnolence
Sources: Page: p.4
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
Co-administed with::
l-dopa/carbidopa oral(650 mg/day)
Sources: Page: p.4-5
unhealthy
Health Status: unhealthy
Condition: Parkinson’s disease
Sources: Page: p.4-5
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
Co-administed with::
l-dopa/carbidopa oral(650 mg/day)
Sources: Page: p.4-5
unhealthy
Health Status: unhealthy
Condition: Parkinson’s disease
Sources: Page: p.4-5
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
Co-administed with::
l-dopa/carbidopa oral(650 mg/day)
Sources: Page: p.5
unhealthy
Health Status: unhealthy
Condition: Parkinson’s disease
Sources: Page: p.5
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
Co-administed with::
l-dopa/carbidopa oral(650 mg/day)
Sources: Page: p.5
unhealthy
Health Status: unhealthy
Condition: Parkinson’s disease
Sources: Page: p.5
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
Co-administed with::
l-dopa/carbidopa oral(650 mg/day)
Sources: Page: p.5
unhealthy
Health Status: unhealthy
Condition: Parkinson’s disease
Sources: Page: p.5
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
Co-administed with::
l-dopa/carbidopa oral(650 mg/day)
Sources: Page: p.5
unhealthy
Health Status: unhealthy
Condition: Parkinson’s disease
Sources: Page: p.5
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
Co-administed with::
l-dopa/carbidopa oral(650 mg/day)
Sources: Page: p.5
unhealthy
Health Status: unhealthy
Condition: Parkinson’s disease
Sources: Page: p.5
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
Co-administed with::
l-dopa/carbidopa oral(650 mg/day)
Sources: Page: p.5
unhealthy
Health Status: unhealthy
Condition: Parkinson’s disease
Sources: Page: p.5
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
Co-administed with::
l-dopa/carbidopa oral(650 mg/day)
Sources: Page: p.5
unhealthy
Health Status: unhealthy
Condition: Parkinson’s disease
Sources: Page: p.5
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG



OverviewOther

Other InhibitorOther SubstrateOther Inducer




Drug as perpetrator​Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
PubMed

PubMed

TitleDatePubMed
Treatment of Parkinson's disease with ropinirole after pergolide-induced retroperitoneal fibrosis.
1999 Dec
Sleep attacks and Parkinson's disease treatment.
2000 Apr 15
Sleep attacks (sleep episodes) with pergolide.
2000 Apr 15
Are dopamine receptor agonists neuroprotective in Parkinson's disease?
2001
Tourette syndrome: clinical characteristics and current management strategies.
2001
Dopamine agonists.
2001
Switching from pergolide to pramipexole in patients with Parkinson's disease.
2001
Efficacy and tolerability of dopamine agonists in a parkinsonian population.
2001 Feb
[Sleep attacks and pergolide mesylate].
2001 Feb
Pleuropulmonary disease due to pergolide use for restless legs syndrome.
2001 Jul
[Pharmacological effects of cabergoline against parkinsonism].
2001 Jun
Long-term effects of pergolide in the treatment of restless legs syndrome.
2001 May 22
The effect of a dopamine agonist on dysarthric speech production: a case study.
2001 Sep-Oct
Restless legs syndrome in the older adult: diagnosis and management.
2002
[Use of dopamine agonists in the treatment of Parkinson's disease].
2002
DA agonists -- ergot derivatives: pergolide: management of Parkinson's disease.
2002
Choosing the right dopamine agonist for patients with Parkinson's disease.
2002
[Treatment of Parkinson's syndrome].
2002
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
Polysomnographic characterization of pergolide-induced sleep attacks in idiopathic PD.
2002 Feb 12
Long-term studies of dopamine agonists.
2002 Feb 26
[Validation of the French language version of the Parkinson's Disease Questionnaire - PDQ-39].
2002 Jan
Transdermal delivery of pergolide from surfactant-based elastic and rigid vesicles: characterization and in vitro transport studies.
2002 Jul
[Multiple system atrophy which had been treated as juvenile Parkinson's disease].
2002 Mar
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. III. Agonist and antagonist properties at serotonin, 5-HT(1) and 5-HT(2), receptor subtypes.
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
Treatment with pergolide or cyproheptadine of pituitary pars intermedia dysfunction (equine Cushing's disease).
2002 Nov-Dec
Muscarinic agonist-mediated increases in serum corticosterone levels are abolished in m(2) muscarinic acetylcholine receptor knockout mice.
2002 Oct
Gateways to Clinical Trials.
2002 Sep
[Cutaneous vasculitis during pergolide mesylate treatment].
2002 Sep
Double-blind, single-dose, cross-over study of the effects of pramipexole, pergolide, and placebo on rest tremor and UPDRS part III in Parkinson's disease.
2003 Feb
Tic reduction with pergolide in a randomized controlled trial in children.
2003 Feb 25
Both short- and long-acting D-1/D-2 dopamine agonists induce less dyskinesia than L-DOPA in the MPTP-lesioned common marmoset (Callithrix jacchus).
2003 Jan
Patents

Sample Use Guides

In Vivo Use Guide
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
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
by admin
on Fri Dec 15 15:45:18 UTC 2023
Edited
by admin
on Fri Dec 15 15:45:18 UTC 2023
Record UNII
24MJ822NZ9
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
PERGOLIDE
INN   MI   VANDF   WHO-DD  
INN  
Official Name English
Pergolide [WHO-DD]
Common Name English
pergolide [INN]
Common Name English
PERGOLIDE [MI]
Common Name English
PERGOLIDE [VANDF]
Common Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 108197
Created by admin on Fri Dec 15 15:45:18 UTC 2023 , Edited by admin on Fri Dec 15 15:45:18 UTC 2023
LIVERTOX NBK548593
Created by admin on Fri Dec 15 15:45:18 UTC 2023 , Edited by admin on Fri Dec 15 15:45:18 UTC 2023
WHO-ATC N04BC02
Created by admin on Fri Dec 15 15:45:18 UTC 2023 , Edited by admin on Fri Dec 15 15:45:18 UTC 2023
NDF-RT N0000000117
Created by admin on Fri Dec 15 15:45:18 UTC 2023 , Edited by admin on Fri Dec 15 15:45:18 UTC 2023
NDF-RT N0000175767
Created by admin on Fri Dec 15 15:45:18 UTC 2023 , Edited by admin on Fri Dec 15 15:45:18 UTC 2023
CFR 21 CFR 520.1705
Created by admin on Fri Dec 15 15:45:18 UTC 2023 , Edited by admin on Fri Dec 15 15:45:18 UTC 2023
NCI_THESAURUS C66884
Created by admin on Fri Dec 15 15:45:18 UTC 2023 , Edited by admin on Fri Dec 15 15:45:18 UTC 2023
WHO-VATC QN04BC02
Created by admin on Fri Dec 15 15:45:18 UTC 2023 , Edited by admin on Fri Dec 15 15:45:18 UTC 2023
NDF-RT N0000007620
Created by admin on Fri Dec 15 15:45:18 UTC 2023 , Edited by admin on Fri Dec 15 15:45:18 UTC 2023
NCI_THESAURUS C38149
Created by admin on Fri Dec 15 15:45:18 UTC 2023 , Edited by admin on Fri Dec 15 15:45:18 UTC 2023
Code System Code Type Description
RXCUI
8047
Created by admin on Fri Dec 15 15:45:18 UTC 2023 , Edited by admin on Fri Dec 15 15:45:18 UTC 2023
PRIMARY RxNorm
DAILYMED
24MJ822NZ9
Created by admin on Fri Dec 15 15:45:18 UTC 2023 , Edited by admin on Fri Dec 15 15:45:18 UTC 2023
PRIMARY
PUBCHEM
47811
Created by admin on Fri Dec 15 15:45:18 UTC 2023 , Edited by admin on Fri Dec 15 15:45:18 UTC 2023
PRIMARY
MERCK INDEX
m8547
Created by admin on Fri Dec 15 15:45:18 UTC 2023 , Edited by admin on Fri Dec 15 15:45:18 UTC 2023
PRIMARY Merck Index
ChEMBL
CHEMBL531
Created by admin on Fri Dec 15 15:45:18 UTC 2023 , Edited by admin on Fri Dec 15 15:45:18 UTC 2023
PRIMARY
MESH
D010479
Created by admin on Fri Dec 15 15:45:18 UTC 2023 , Edited by admin on Fri Dec 15 15:45:18 UTC 2023
PRIMARY
DRUG BANK
DB01186
Created by admin on Fri Dec 15 15:45:18 UTC 2023 , Edited by admin on Fri Dec 15 15:45:18 UTC 2023
PRIMARY
WIKIPEDIA
PERGOLIDE
Created by admin on Fri Dec 15 15:45:18 UTC 2023 , Edited by admin on Fri Dec 15 15:45:18 UTC 2023
PRIMARY
NCI_THESAURUS
C61886
Created by admin on Fri Dec 15 15:45:18 UTC 2023 , Edited by admin on Fri Dec 15 15:45:18 UTC 2023
PRIMARY
EPA CompTox
DTXSID2023438
Created by admin on Fri Dec 15 15:45:18 UTC 2023 , Edited by admin on Fri Dec 15 15:45:18 UTC 2023
PRIMARY
IUPHAR
48
Created by admin on Fri Dec 15 15:45:18 UTC 2023 , Edited by admin on Fri Dec 15 15:45:18 UTC 2023
PRIMARY
INN
4651
Created by admin on Fri Dec 15 15:45:18 UTC 2023 , Edited by admin on Fri Dec 15 15:45:18 UTC 2023
PRIMARY
CAS
66104-22-1
Created by admin on Fri Dec 15 15:45:18 UTC 2023 , Edited by admin on Fri Dec 15 15:45:18 UTC 2023
PRIMARY
SMS_ID
100000082732
Created by admin on Fri Dec 15 15:45:18 UTC 2023 , Edited by admin on Fri Dec 15 15:45:18 UTC 2023
PRIMARY
DRUG CENTRAL
2105
Created by admin on Fri Dec 15 15:45:18 UTC 2023 , Edited by admin on Fri Dec 15 15:45:18 UTC 2023
PRIMARY
CHEBI
63617
Created by admin on Fri Dec 15 15:45:18 UTC 2023 , Edited by admin on Fri Dec 15 15:45:18 UTC 2023
PRIMARY
FDA UNII
24MJ822NZ9
Created by admin on Fri Dec 15 15:45:18 UTC 2023 , Edited by admin on Fri Dec 15 15:45:18 UTC 2023
PRIMARY
EVMPD
SUB09725MIG
Created by admin on Fri Dec 15 15:45:18 UTC 2023 , Edited by admin on Fri Dec 15 15:45:18 UTC 2023
PRIMARY
Related Record Type Details
TARGET -> AGONIST
BINDER->LIGAND
BINDING
TARGET -> AGONIST
SALT/SOLVATE -> PARENT
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC