cabergoline indications/contra

Stem definitionDrug idCAS RN
ergot alkaloid derivatives 460 81409-90-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • cabergoline
  • dostinex
  • galastop
  • cabaser
  • cabaseril
also acts as prolactin antagonist
  • Molecular weight: 451.62
  • Formula: C26H37N5O2
  • CLOGP: 4.17
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 2
  • TPSA: 71.68
  • ALOGS: -3.85
  • ROTB: 8

Drug dosage:

DoseUnitRoute
0.50 mg O
3 mg O

Approvals:

DateAgencyCompanyOrphan
Dec. 23, 1996 FDA

FDA Adverse Event Reporting System

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MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Aortic valve incompetence 562.39 34.61 96 1465 1421 3382877
Mitral valve incompetence 465.13 34.61 95 1466 3839 3380459
Cardiac valve disease 324.26 34.61 58 1503 1125 3383173
Tricuspid valve incompetence 250.11 34.61 53 1508 2532 3381766
Gambling disorder 233.69 34.61 39 1522 490 3383808
Pleural effusion 196.37 34.61 66 1495 18713 3365585
Aortic valve sclerosis 165.74 34.61 27 1534 288 3384010
Cerebrospinal fluid leakage 164.16 34.61 27 1534 307 3383991
Parkinson's disease 155.01 34.61 35 1526 2236 3382062
Exposure during pregnancy 150.35 34.61 60 1501 27503 3356795
Hallucination 143.65 34.61 48 1513 13292 3371006
Blood prolactin increased 136.76 34.61 29 1532 1379 3382919
Mitral valve disease 132.33 34.61 24 1537 499 3383799
Cardiac failure 128.00 34.61 49 1512 20056 3364242
Pneumocephalus 113.71 34.61 17 1544 97 3384201
Pleural fibrosis 112.47 34.61 20 1541 370 3383928
Condition aggravated 105.40 34.61 52 1509 39181 3345117
Headache 93.95 34.61 65 1496 91915 3292383
Abortion spontaneous 93.36 34.61 33 1528 10752 3373546
Neoplasm progression 90.15 34.61 27 1534 5217 3379081
Pituitary haemorrhage 89.40 34.61 14 1547 113 3384185
Pulmonary hypertension 88.53 34.61 28 1533 6482 3377816
Oedema peripheral 87.64 34.61 44 1517 34317 3349981
Delusion 82.02 34.61 23 1538 3522 3380776
Heart valve incompetence 81.98 34.61 16 1545 498 3383800
Hypersexuality 77.77 34.61 15 1546 438 3383860
Interstitial lung disease 67.56 34.61 28 1533 13988 3370310
Visual pathway disorder 66.73 34.61 10 1551 58 3384240
Dyspnoea 65.65 34.61 55 1506 102879 3281419
Dopamine dysregulation syndrome 64.91 34.61 11 1550 151 3384147

Pharmacologic Action:

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SourceCodeDescription
ATC G02CB03 GENITO URINARY SYSTEM AND SEX HORMONES
OTHER GYNECOLOGICALS
OTHER GYNECOLOGICALS
Prolactine inhibitors
ATC N04BC06 NERVOUS SYSTEM
ANTI-PARKINSON DRUGS
DOPAMINERGIC AGENTS
Dopamine agonists
FDA Chemical/Ingredient N0000007618 Ergolines
FDA EPC N0000175827 Ergot Derivative
MeSH PA D018726 Anti-Dyskinesia Agents
MeSH PA D000970 Antineoplastic Agents
MeSH PA D000978 Antiparkinson Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D015259 Dopamine Agents
MeSH PA D018491 Dopamine Agonists
MeSH PA D018377 Neurotransmitter Agents
CHEBI has role CHEBI:51065 dopamine agonist
CHEBI has role CHEBI:48407 antiparkinson drug
CHEBI has role CHEBI:35610 antineoplastic agent

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Hyperprolactinemia indication 237662005 DOID:12700
Heart valve disorder contraindication 368009 DOID:4079
Severe pre-eclampsia contraindication 46764007 DOID:10591
Retroperitoneal fibrosis contraindication 49120005
Fibrosis of lung contraindication 51615001 DOID:3770
Fibrosis of pericardium contraindication 194965002
Disease of liver contraindication 235856003 DOID:409
Breastfeeding (mother) contraindication 413712001
Hypertensive urgency contraindication 443482000
Occlusive Vascular Disease contraindication

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 12.83 acidic
pKa2 13.48 acidic
pKa3 7.88 Basic
pKa4 5.97 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
D(2) dopamine receptor GPCR AGONIST Ki 9.20 IUPHAR CHEMBL
D(3) dopamine receptor GPCR AGONIST Ki 9.10 IUPHAR
5-hydroxytryptamine receptor 2A GPCR AGONIST Ki 8.20 IUPHAR
5-hydroxytryptamine receptor 1D GPCR AGONIST Ki 8.10 IUPHAR
Alpha-2A adrenergic receptor GPCR ANTAGONIST Ki 7.90 IUPHAR
D(1B) dopamine receptor GPCR AGONIST Ki 7.70 IUPHAR
5-hydroxytryptamine receptor 1A GPCR AGONIST Ki 7.70 IUPHAR
Alpha-2C adrenergic receptor GPCR ANTAGONIST Ki 7.70 IUPHAR
D(4) dopamine receptor GPCR AGONIST Ki 7.30 IUPHAR
Alpha-2B adrenergic receptor GPCR ANTAGONIST Ki 7.10 IUPHAR
D(1A) dopamine receptor GPCR AGONIST Ki 6.70 IUPHAR
Alpha-1A adrenergic receptor GPCR ANTAGONIST Ki 6.50 IUPHAR
5-hydroxytryptamine receptor 1B GPCR AGONIST Ki 6.30 IUPHAR
5-hydroxytryptamine receptor 2C GPCR AGONIST Ki 6.20 IUPHAR
Alpha-1D adrenergic receptor GPCR Ki 6.78 PDSP
Alpha-1B adrenergic receptor GPCR Ki 7.22 PDSP
5-hydroxytryptamine receptor 2B GPCR Ki 8.85 CHEMBL

External reference:

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IDSource
DB00248 DRUGBANK_ID
37 IUPHAR_LIGAND_ID
4021014 VUID
N0000148483 NUI
C0107994 UMLSCUI
D00987 KEGG_DRUG
4021014 VANDF
73532 MMSL
N0000006339 NDFRT
N0000148483 NDFRT
005446 NDDF
d04112 MMSL
4317 MMSL
47579 RXNORM
109139002 SNOMEDCT_US
386979007 SNOMEDCT_US
54746 PUBCHEM_CID
CHEMBL1201087 ChEMBL_ID
C047047 MESH_SUPPLEMENTAL_RECORD_UI
LL60K9J05T UNII
5860 INN_ID
CHEBI:3286 CHEBI

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Cabergoline HUMAN PRESCRIPTION DRUG LABEL 1 0093-5420 TABLET 0.50 mg ORAL ANDA 11 sections
Cabergoline HUMAN PRESCRIPTION DRUG LABEL 1 49884-673 TABLET 0.50 mg ORAL ANDA 11 sections
Cabergoline HUMAN PRESCRIPTION DRUG LABEL 1 59762-1005 TABLET 0.50 mg ORAL NDA AUTHORIZED GENERIC 13 sections
CABERGOLINE HUMAN PRESCRIPTION DRUG LABEL 1 60505-2597 TABLET 0.50 mg ORAL ANDA 13 sections
Cabergoline HUMAN PRESCRIPTION DRUG LABEL 1 69189-5420 TABLET 0.50 mg ORAL ANDA 10 sections