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Details

Stereochemistry ABSOLUTE
Molecular Formula C19H26N2S.CH4O3S
Molecular Weight 410.594
Optical Activity UNSPECIFIED
Defined Stereocenters 3 / 3
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of PERGOLIDE MESYLATE

SMILES

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

InChI

InChIKey=UWCVGPLTGZWHGS-ZORIOUSZSA-N
InChI=1S/C19H26N2S.CH4O3S/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;1-5(2,3)4/h4-6,10,13,16,18,20H,3,7-9,11-12H2,1-2H3;1H3,(H,2,3,4)/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

Molecular Formula CH4O3S
Molecular Weight 96.106
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

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 The drug was withdrawn from the US market in March 2007 and from the Canadian market in August 2007.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
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
[Dopaminergic agonists in the treatment of Parkinson's disease].
2000 Dec
Are dopamine receptor agonists neuroprotective in Parkinson's disease?
2001
Neostriatal muscarinic receptor subtypes involved in the generation of tremulous jaw movements in rodents implications for cholinergic involvement in parkinsonism.
2001 Apr 27
Functional neuroanatomy of the ventral striopallidal GABA pathway. New sites of intervention in the treatment of schizophrenia.
2001 Aug 15
[Sleep attacks and pergolide mesylate].
2001 Feb
Cost-effectiveness of pergolide compared to bromocriptine in the treatment of Parkinson's disease: a decision-analytic model.
2001 Jul-Aug
[Pharmacological effects of cabergoline against parkinsonism].
2001 Jun
Pergolide mesilate may improve fatigue in patients with Parkinson's disease.
2001-2002
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: bromocriptine: management of Parkinson's disease.
2002
Elastic vesicles: interaction with human skin and drug transport.
2002
The potential of dopamine agonists in drug addiction.
2002 Apr
[The evolution of use of anti-Parkinson drugs in Spain].
2002 Apr 1-15
[Pergolide-induced pleural effusion in a patient with juvenile parkinsonism].
2002 Aug
Discrimination of morphine- and haloperidol-induced muscular rigidity and akinesia/catalepsy in simple tests in rats.
2002 Aug 21
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
Pergolide protects SH-SY5Y cells against neurodegeneration induced by H(2)O(2).
2002 Jan 2
Pergolide-induced lung disease in patients with Parkinson's disease.
2002 Jul
Dopamine receptor agonists for treating prolactinomas.
2002 Jun
Sleep attacks in patients taking dopamine agonists: review.
2002 Jun 22
Antiparkinsonian treatment in pregnancy.
2002 Mar
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
Muscarinic agonist-mediated increases in serum corticosterone levels are abolished in m(2) muscarinic acetylcholine receptor knockout mice.
2002 Oct
The effect of pergolide on cognitive performance of young and middle-aged rats.
2002 Sep
Gateways to Clinical Trials.
2002 Sep
[Cutaneous vasculitis during pergolide mesylate treatment].
2002 Sep
Pergolide-induced pleuropulmonary fibrosis.
2002 Sep-Oct
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
Dopamine D1 rather than D2 receptor agonists disrupt prepulse inhibition of startle in mice.
2003 Jan
The in vitro transport of pergolide from surfactant-based elastic vesicles through human skin: a suggested mechanism of action.
2003 Jan 9
The modulatory effects of dopamine D1 and D2 receptor function on object working memory in humans.
2003 Mar
[(123)I]beta-CIT SPECT is a useful method for monitoring dopaminergic degeneration in early stage Parkinson's disease.
2003 Mar
The initial drug treatment of older patients with Parkinson's disease - consider an agonist, but don't demonise dopa.
2003 May
Dihydroergocriptine in Parkinson's disease: clinical efficacy and comparison with other dopamine agonists.
2003 May
Analysis of the effect of (-)-BPAP, a selective enhancer of the impulse propagation mediated release of catecholamines and serotonin in the brain.
2003 May 9
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 Wed Jul 05 22:50:01 UTC 2023
Edited
by admin
on Wed Jul 05 22:50:01 UTC 2023
Record UNII
55B9HQY616
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
PERGOLIDE MESYLATE
ORANGE BOOK   USAN   USP   USP-RS   VANDF  
USAN  
Official Name English
ERGOLINE, 8-((METHYLTHIO)METHYL)-6-PROPYL-, MONOMETHANESULPHONATE, (8.BETA.)-
Common Name English
ERGOLINE, 8-((METHYLTHIO)METHYL)-6-PROPYL-, MONOMETHANESULFONATE, (8.BETA.)-
Common Name English
PERGOLIDE MESYLATE [GREEN BOOK]
Common Name English
PERGOLIDE MESYLATE [USP MONOGRAPH]
Common Name English
Pergolide mesilate [WHO-DD]
Common Name English
8.BETA.-((METHYLTHIO)METHYL)-6-PROPYLERGOLINE MONOMETHANESULPHONATE
Common Name English
PERGOLIDE MESILATE [JAN]
Common Name English
PERMAX
Brand Name English
PERGOLIDE MESYLATE [VANDF]
Common Name English
NSC-758442
Code English
8β-[(Methylthio)methyl]-6-propylergoline monomethanesulfonate
Common Name English
PERGOLIDE MESILATE [EP MONOGRAPH]
Common Name English
PERGOLIDE MESYLATE [USAN]
Common Name English
PERGOLIDE MESILATE
EP   JAN   MART.   WHO-DD  
Common Name English
PERGOLIDE METHANESULFONATE [MI]
Common Name English
PERGOLIDE MESILATE [MART.]
Common Name English
PERGOLIDE MESYLATE [USP-RS]
Common Name English
LY-127809
Code English
PERGOLIDE MESYLATE [ORANGE BOOK]
Common Name English
PERGOLIDE METHANESULFONATE
MI  
Common Name English
NSC-319773
Code English
LY 127809
Code English
Classification Tree Code System Code
NCI_THESAURUS C38149
Created by admin on Wed Jul 05 22:50:01 UTC 2023 , Edited by admin on Wed Jul 05 22:50:01 UTC 2023
NCI_THESAURUS C66884
Created by admin on Wed Jul 05 22:50:01 UTC 2023 , Edited by admin on Wed Jul 05 22:50:01 UTC 2023
Code System Code Type Description
DAILYMED
55B9HQY616
Created by admin on Wed Jul 05 22:50:01 UTC 2023 , Edited by admin on Wed Jul 05 22:50:01 UTC 2023
PRIMARY
DRUG BANK
DBSALT002445
Created by admin on Wed Jul 05 22:50:01 UTC 2023 , Edited by admin on Wed Jul 05 22:50:01 UTC 2023
PRIMARY
CHEBI
8021
Created by admin on Wed Jul 05 22:50:01 UTC 2023 , Edited by admin on Wed Jul 05 22:50:01 UTC 2023
PRIMARY
NSC
758442
Created by admin on Wed Jul 05 22:50:01 UTC 2023 , Edited by admin on Wed Jul 05 22:50:01 UTC 2023
PRIMARY
RXCUI
8048
Created by admin on Wed Jul 05 22:50:01 UTC 2023 , Edited by admin on Wed Jul 05 22:50:01 UTC 2023
PRIMARY RxNorm
EVMPD
SUB03709MIG
Created by admin on Wed Jul 05 22:50:01 UTC 2023 , Edited by admin on Wed Jul 05 22:50:01 UTC 2023
PRIMARY
FDA UNII
55B9HQY616
Created by admin on Wed Jul 05 22:50:01 UTC 2023 , Edited by admin on Wed Jul 05 22:50:01 UTC 2023
PRIMARY
MERCK INDEX
M8547
Created by admin on Wed Jul 05 22:50:01 UTC 2023 , Edited by admin on Wed Jul 05 22:50:01 UTC 2023
PRIMARY Merck Index
PUBCHEM
47812
Created by admin on Wed Jul 05 22:50:01 UTC 2023 , Edited by admin on Wed Jul 05 22:50:01 UTC 2023
PRIMARY
EPA CompTox
DTXSID6040583
Created by admin on Wed Jul 05 22:50:01 UTC 2023 , Edited by admin on Wed Jul 05 22:50:01 UTC 2023
PRIMARY
NSC
319773
Created by admin on Wed Jul 05 22:50:01 UTC 2023 , Edited by admin on Wed Jul 05 22:50:01 UTC 2023
PRIMARY
RS_ITEM_NUM
1510845
Created by admin on Wed Jul 05 22:50:01 UTC 2023 , Edited by admin on Wed Jul 05 22:50:01 UTC 2023
PRIMARY
SMS_ID
100000085696
Created by admin on Wed Jul 05 22:50:01 UTC 2023 , Edited by admin on Wed Jul 05 22:50:01 UTC 2023
PRIMARY
NCI_THESAURUS
C47665
Created by admin on Wed Jul 05 22:50:01 UTC 2023 , Edited by admin on Wed Jul 05 22:50:01 UTC 2023
PRIMARY
ChEMBL
CHEMBL531
Created by admin on Wed Jul 05 22:50:01 UTC 2023 , Edited by admin on Wed Jul 05 22:50:01 UTC 2023
PRIMARY
CAS
66104-23-2
Created by admin on Wed Jul 05 22:50:01 UTC 2023 , Edited by admin on Wed Jul 05 22:50:01 UTC 2023
PRIMARY
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