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
[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
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 The drug was withdrawn from the US market in March 2007 and from the Canadian market in August 2007.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 Date1.33487998E12 |
|||
Primary | Unknown Approved UseUnknown |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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 |
|
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 |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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 |
|
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 |
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 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) Sources: Page: p.123Syncope (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 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%) Sources: Page: p.863Dyskinesia (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: 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) Sources: Page: p.11Tingling (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 |
Other AEs: Hallucinations... Other AEs: Hallucinations (grade 3) Sources: Page: p.11 |
60 mg single, oral Overdose Dose: 60 mg Route: oral Route: single Dose: 60 mg Sources: Page: p.11 |
healthy n = 1 Health Status: healthy Population Size: 1 Sources: Page: p.11 |
Other AEs: Vomiting, Hypotension... Other AEs: Vomiting Sources: Page: p.11Hypotension Agitation |
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... Other AEs: Palpitations Sources: Page: p.11Hypotension |
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... Other AEs: Ventricular extrasystoles Sources: Page: p.11-12 |
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%) Sources: Page: p.7Confusion (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.4 |
unhealthy Health Status: unhealthy Condition: Parkinson’s disease Sources: Page: p.4 |
Other AEs: Daytime sleepiness, Hypotension symptomatic... Other AEs: Daytime sleepiness Sources: Page: p.4Hypotension 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: Somnolence Sources: Page: p.4 |
Other AEs: Daytime sleepiness... Other AEs: Daytime sleepiness (common) 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.4-5 |
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) Sources: Page: p.5Pleural effusion (rare) Pleural fibrosis (rare) Pericarditis (rare) Pericardial effusion (rare) Cardiac valvulopathy (rare) Retroperitoneal fibrosis (rare) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
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 Health Status: healthy Population Size: 1 Sources: Page: p.11 |
|
Hypotension | 60 mg single, oral Overdose Dose: 60 mg Route: oral Route: single Dose: 60 mg Sources: Page: p.11 |
healthy n = 1 Health Status: healthy Population Size: 1 Sources: Page: p.11 |
|
Vomiting | 60 mg single, oral Overdose Dose: 60 mg Route: oral Route: single Dose: 60 mg Sources: Page: p.11 |
healthy n = 1 Health Status: healthy Population Size: 1 Sources: Page: p.11 |
|
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
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 |
|
[Dopaminergic agonists in the treatment of Parkinson's disease]. | 2000 Dec |
|
Are dopamine receptor agonists neuroprotective in Parkinson's disease? | 2001 |
|
Tourette syndrome: clinical characteristics and current management strategies. | 2001 |
|
Switching from pergolide to pramipexole in patients with Parkinson's disease. | 2001 |
|
Functional neuroanatomy of the ventral striopallidal GABA pathway. New sites of intervention in the treatment of schizophrenia. | 2001 Aug 15 |
|
Dopamine interacts directly with its D3 and D2 receptors on normal human T cells, and activates beta1 integrin function. | 2001 Dec |
|
Efficacy and tolerability of dopamine agonists in a parkinsonian population. | 2001 Feb |
|
Pleuropulmonary disease due to pergolide use for restless legs syndrome. | 2001 Jul |
|
Cost-effectiveness of pergolide compared to bromocriptine in the treatment of Parkinson's disease: a decision-analytic model. | 2001 Jul-Aug |
|
[A 64-year-old man with parkinsonism as an initial symptom followed by dementia associated with marked abnormal behaviours]. | 2001 Nov |
|
Daytime sleepiness and other sleep disorders in Parkinson's disease. | 2001 Oct 23 |
|
The effect of a dopamine agonist on dysarthric speech production: a case study. | 2001 Sep-Oct |
|
Pergolide mesilate may improve fatigue in patients with Parkinson's disease. | 2001-2002 |
|
[Use of dopamine agonists in the treatment of Parkinson's disease]. | 2002 |
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DA agonists -- ergot derivatives: pergolide: management of Parkinson's disease. | 2002 |
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Choosing the right dopamine agonist for patients with Parkinson's disease. | 2002 |
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[Treatment of Parkinson's syndrome]. | 2002 |
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[Pergolide-induced pleural effusion in a patient with juvenile parkinsonism]. | 2002 Aug |
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Neuroleptic malignant-like syndrome after rapid switch from bromocriptine to pergolide. | 2002 Dec |
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Polysomnographic characterization of pergolide-induced sleep attacks in idiopathic PD. | 2002 Feb 12 |
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Restless legs syndrome: treatment with dopaminergic agents. | 2002 Feb 26 |
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Long-term studies of dopamine agonists. | 2002 Feb 26 |
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Penile erections and hypersexuality induced by pergolide treatment in advanced, fluctuating Parkinson's disease. | 2002 Jan |
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Chronic pericardial constriction linked to the antiparkinsonian dopamine agonist pergolide. | 2002 Jan |
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Pergolide protects SH-SY5Y cells against neurodegeneration induced by H(2)O(2). | 2002 Jan 2 |
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Delayed visual loss following pergolide treatment of a prolactinoma. | 2002 Jun |
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[Multiple latency test in a patient with episodes of sleep induced by pergolide]. | 2002 Jun 16-30 |
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Sleep attacks in patients taking dopamine agonists: review. | 2002 Jun 22 |
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Antiparkinsonian treatment in pregnancy. | 2002 Mar |
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Plasma adrenocorticotropin (ACTH) concentrations and clinical response in horses treated for equine Cushing's disease with cyproheptadine or pergolide. | 2002 Nov |
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Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. II. Agonist and antagonist properties at subtypes of dopamine D(2)-like receptor and alpha(1)/alpha(2)-adrenoceptor. | 2002 Nov |
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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 |
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Treatment with pergolide or cyproheptadine of pituitary pars intermedia dysfunction (equine Cushing's disease). | 2002 Nov-Dec |
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An evidence-based review of dopamine receptor agonists in the treatment of Parkinson's disease. | 2002 Oct |
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Muscarinic agonist-mediated increases in serum corticosterone levels are abolished in m(2) muscarinic acetylcholine receptor knockout mice. | 2002 Oct |
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[Cutaneous vasculitis during pergolide mesylate treatment]. | 2002 Sep |
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Cognitive effects of the dopamine receptor agonist pergolide. | 2003 |
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Dopamine agonists induce episodes of irresistible daytime sleepiness. | 2003 |
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[Gilles de la tourette syndrome: clinical spectrum and management]. | 2003 Apr 1-15 |
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The in vitro transport of pergolide from surfactant-based elastic vesicles through human skin: a suggested mechanism of action. | 2003 Jan 9 |
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The modulatory effects of dopamine D1 and D2 receptor function on object working memory in humans. | 2003 Mar |
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[(123)I]beta-CIT SPECT is a useful method for monitoring dopaminergic degeneration in early stage Parkinson's disease. | 2003 Mar |
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The initial drug treatment of older patients with Parkinson's disease - consider an agonist, but don't demonise dopa. | 2003 May |
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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 |
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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Wed Jul 05 23:13:53 UTC 2023
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Record UNII |
24MJ822NZ9
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Validated (UNII)
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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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M8547
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CHEMBL531
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DB01186
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PERGOLIDE
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C61886
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SUB09725MIG
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TARGET -> AGONIST |
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ACTIVE MOIETY |
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Biological Half-life | PHARMACOKINETIC |
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