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pergolide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| dopamine receptor agonists, ergoline derivatives | 2105 | 66104-22-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A long-acting dopamine agonist which has been used to treat PARKINSON DISEASE and HYPERPROLACTINEMIA but withdrawn from some markets due to potential for HEART VALVE DISEASES.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 3 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.14 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 38 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 3.441 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.555 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 33.343 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 39.719 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 7.110 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 15.610 | % | High | 1 |
| herg | hERG pIC50 | 5.554 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 29.648 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 183.654 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 5.660 | % | High | 1 |
| kinase-safety-class | ACVR2B,AKT1,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP2K6,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPKAPK2,MET,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,TEK,TGFBR1,TTK,ZAP70 | 46 | |||
| kinase-selectivity-class | AXL,BRAF,EIF2AK3 | 3 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.716 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 280.543 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 9.480 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 1.782 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 24.490 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 294.442 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 37.870 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 6.170 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 211.349 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 30, 1988 | FDA |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Gambling disorder | 105.96 | 79.63 | 16 | 180 | 1760 | 42619379 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Gambling disorder | 116.39 | 93.04 | 16 | 198 | 2175 | 110586910 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N04BC02 | NERVOUS SYSTEM ANTI-PARKINSON DRUGS DOPAMINERGIC AGENTS Dopamine agonists |
| FDA CS | M0007656 | Ergot Alkaloids |
| FDA MoA | N0000000117 | Dopamine Agonists |
| MeSH PA | D015259 | Dopamine Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018491 | Dopamine Agonists |
| FDA EPC | N0000175767 | Ergot-derived Dopamine Receptor Agonist |
| CHEBI has role | CHEBI:48407 | antiparkinson drug |
| CHEBI has role | CHEBI:51065 | dopamine agonist |
| CHEBI has role | CHEBI:176497 | geroprotector |
Related Drugs by ATC class:
N04BC Dopamine agonists 8 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Parkinsonism | indication | 32798002 | |
| Heart valve disorder | contraindication | 368009 | DOID:4079 |
| Pericarditis | contraindication | 3238004 | DOID:1787 |
| Orthostatic hypotension | contraindication | 28651003 | |
| Conduction disorder of the heart | contraindication | 44808001 | |
| Retroperitoneal fibrosis | contraindication | 49120005 | |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Pleurisy | contraindication | 196075003 | |
| Renal fibrosis | contraindication | 197660000 | |
| Pericardial effusion | contraindication | 373945007 | DOID:118 |
| Breastfeeding (mother) | contraindication | 413712001 | |
| Fibrosis of pleura | contraindication | 442110002 | |
| Pleural Effusions | contraindication |
🐶 Veterinary Drug Use
| Species | Use | Relation |
|---|---|---|
| Horses | Control of clinical signs associated with pituitary pars intermedia dysfunction (Equine Cushings Disease) | Indication |
🐶 Veterinary products
| Product | Applicant | Ingredients |
|---|---|---|
| Prascend | Boehringer lngelheim Animal Health USA Inc. | 1 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 12.41 | acidic |
| pKa2 | 7.67 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| D(2) dopamine receptor | GPCR | AGONIST | EC50 | 8.30 | WOMBAT-PK | DRUG LABEL | |||
| D(1A) dopamine receptor | GPCR | AGONIST | Ki | 6.47 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| 5-hydroxytryptamine receptor 1A | GPCR | Ki | 8.50 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 2A | GPCR | EC50 | 8.10 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 2B | GPCR | EC50 | 8.20 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 2C | GPCR | EC50 | 6.50 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 6 | GPCR | Ki | 7.75 | CHEMBL | |||||
| Alpha-1A adrenergic receptor | GPCR | Ki | 5.98 | PDSP | |||||
| Alpha-2B adrenergic receptor | GPCR | Ki | 7.50 | WOMBAT-PK | |||||
| D(3) dopamine receptor | GPCR | AGONIST | EC50 | 9 | WOMBAT-PK | ||||
| D(1B) dopamine receptor | GPCR | AGONIST | Ki | 6.76 | WOMBAT-PK | ||||
| 5-hydroxytryptamine receptor 1B | GPCR | EC50 | 6.60 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 1D | GPCR | Ki | 7.90 | WOMBAT-PK | |||||
| Alpha-2C adrenergic receptor | GPCR | Ki | 7.20 | WOMBAT-PK | |||||
| Cytochrome P450 2D6 | Enzyme | IC50 | 6.70 | DRUG MATRIX | |||||
| D(4) dopamine receptor | GPCR | AGONIST | Ki | 7.25 | WOMBAT-PK | ||||
| Alpha-1D adrenergic receptor | GPCR | Ki | 6.13 | DRUG MATRIX | |||||
| Alpha-2A adrenergic receptor | GPCR | Ki | 7.30 | WOMBAT-PK | |||||
| Alpha-synuclein | Transporter | IC50 | 5.10 | CHEMBL | |||||
| Alpha-1B adrenergic receptor | GPCR | Ki | 6.16 | PDSP | |||||
| Potassium voltage-gated channel subfamily H member 2 | Ion channel | IC50 | 6.92 | CHEMBL | |||||
| Alpha-1B adrenergic receptor | GPCR | Ki | 5.84 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 1B | GPCR | Ki | 7.40 | DRUG MATRIX | |||||
| Alpha-1A adrenergic receptor | GPCR | IC50 | 5.71 | CHEMBL | |||||
| D(2) dopamine receptor | GPCR | Kd | 8.40 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | IC50 | 7.82 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 7 | GPCR | AGONIST | Ki | 9 | IUPHAR | ||||
| D(2) dopamine receptor | GPCR | IC50 | 7.32 | CHEMBL | |||||
| D(3) dopamine receptor | GPCR | IC50 | 8.62 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 6 | GPCR | AGONIST | Ki | 7.50 | IUPHAR | ||||
| Adrenergic receptor alpha-2 | GPCR | IC50 | 7.39 | CHEMBL | |||||
| Dopamine receptor | GPCR | IC50 | 7.74 | CHEMBL | |||||
| Dopamine receptor | GPCR | IC50 | 8.51 | CHEMBL | |||||
| Cerebral cortex alpha adrenergic receptor | GPCR | IC50 | 7.39 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D00502 | KEGG_DRUG |
| 66104-23-2 | SECONDARY_CAS_RN |
| 4019530 | VANDF |
| 4019883 | VANDF |
| C0031007 | UMLSCUI |
| CHEBI:63617 | CHEBI |
| CHEMBL531 | ChEMBL_ID |
| CHEMBL1275 | ChEMBL_ID |
| DB01186 | DRUGBANK_ID |
| D010479 | MESH_DESCRIPTOR_UI |
| 47811 | PUBCHEM_CID |
| 48 | IUPHAR_LIGAND_ID |
| 4651 | INN_ID |
| 24MJ822NZ9 | UNII |
| 203553 | RXNORM |
| 2257 | MMSL |
| 45580 | MMSL |
| 5259 | MMSL |
| d00977 | MMSL |
| 003442 | NDDF |
| 003443 | NDDF |
| 108468004 | SNOMEDCT_US |
| 108469007 | SNOMEDCT_US |
| 372498008 | SNOMEDCT_US |
| 24MJ822NZ9 | INXIGHT DRUGS |
Pharmaceutical products:
None