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
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
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 The drug was withdrawn from the US market in March 2007 and from the Canadian market in August 2007.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 |
---|---|---|
Sleep attacks and Parkinson's disease treatment. | 2000 Apr 15 |
|
Dopamine agonists. | 2001 |
|
[Parkinson's disease]. | 2001 Mar 3 |
|
DA agonists -- ergot derivatives: pergolide: management of Parkinson's disease. | 2002 |
|
DA agonists -- ergot derivatives: bromocriptine: management of Parkinson's disease. | 2002 |
|
Choosing the right dopamine agonist for patients with Parkinson's disease. | 2002 |
|
Clinical pharmacokinetic and pharmacodynamic properties of drugs used in the treatment of Parkinson's disease. | 2002 |
|
A new design of a polysomnography-based multi-center treatment study for the restless legs syndrome. | 2002 Apr |
|
Valvular heart disease in patients taking pergolide. | 2002 Dec |
|
Penile erections and hypersexuality induced by pergolide treatment in advanced, fluctuating Parkinson's disease. | 2002 Jan |
|
Delayed visual loss following pergolide treatment of a prolactinoma. | 2002 Jun |
|
Long term tolerability of high dose ergoline derived dopamine agonist therapy for the treatment of Parkinson's disease. | 2002 Nov |
|
Dopamine agonist monotherapy in Parkinson's disease. | 2002 Nov 30 |
|
Treatment with pergolide or cyproheptadine of pituitary pars intermedia dysfunction (equine Cushing's disease). | 2002 Nov-Dec |
|
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 |
|
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 |
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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 |
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.
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C38149
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C66884
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ACTIVE MOIETY
SUBSTANCE RECORD