cabergoline ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

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

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • cabergoline
  • dostinex
  • galastop
  • cabaser
  • cabaseril
An ergoline derivative and dopamine D2-agonist that inhibits PROLACTIN secretion. It is used in the management of HYPERPROLACTINEMIA, and to suppress lactation following childbirth for medical reasons. Cabergoline is also used in the management of PARKINSON DISEASE.
  • Molecular weight: 451.62
  • Formula: C26H37N5O2
  • CLOGP: 4.17
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 2
  • TPSA: 71.68
  • ALOGS: -3.85
  • ROTB: 8

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.50 mg O
3 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 3 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.01 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 65 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
Dec. 23, 1996 FDA

FDA Adverse Event Reporting System (Female)

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
Blood growth hormone increased 180.28 18.51 34 7210 403 50597477
Insulin-like growth factor increased 159.02 18.51 34 7210 784 50597096
Aortic valve incompetence 114.26 18.51 39 7205 5437 50592443
Insulin-like growth factor decreased 86.80 18.51 18 7226 356 50597524
Ovarian hyperstimulation syndrome 83.21 18.51 27 7217 3217 50594663
Pituitary tumour 81.84 18.51 20 7224 845 50597035
Blood prolactin increased 76.28 18.51 25 7219 3074 50594806
Needle issue 61.98 18.51 27 7217 7248 50590632
Coronary artery dissection 59.68 18.51 15 7229 712 50597168
Mitral valve incompetence 57.30 18.51 34 7210 17437 50580443
Blood prolactin decreased 55.99 18.51 9 7235 37 50597843
Pituitary haemorrhage 50.06 18.51 9 7235 80 50597800
Inappropriate schedule of product administration 49.34 18.51 56 7188 71775 50526105
Pituitary tumour benign 46.39 18.51 15 7229 1766 50596114
Pulmonary pain 46.38 18.51 16 7228 2299 50595581
Acromegaly 40.05 18.51 7 7237 52 50597828
Cardiac valve disease 38.72 18.51 16 7228 3770 50594110
Mediastinal fibrosis 37.66 18.51 6 7238 23 50597857
Tricuspid valve incompetence 37.10 18.51 23 7221 12747 50585133
Bite 37.02 18.51 9 7235 372 50597508
Prolactin-producing pituitary tumour 36.30 18.51 7 7237 94 50597786
Pneumocephalus 33.72 18.51 7 7237 139 50597741
Cerebrospinal fluid leakage 33.31 18.51 10 7234 922 50596958
Overweight 31.42 18.51 13 7231 3073 50594807
Hypogonadism 30.49 18.51 6 7238 90 50597790
Diabetes mellitus 29.93 18.51 36 7208 48997 50548883
Neoplasm progression 29.51 18.51 28 7216 29129 50568751
Urine calcium/creatinine ratio increased 29.16 18.51 6 7238 114 50597766
Blood pressure increased 27.99 18.51 60 7184 133072 50464808
Mastitis 27.72 18.51 11 7233 2336 50595544
Kounis syndrome 26.99 18.51 9 7235 1166 50596714
Compulsive shopping 26.94 18.51 8 7236 710 50597170
Gambling disorder 26.85 18.51 9 7235 1185 50596695
Abortion spontaneous 26.04 18.51 31 7213 41741 50556139
Injection site mass 26.01 18.51 20 7224 15660 50582220
Urethral caruncle 24.88 18.51 5 7239 84 50597796
Aortic valve sclerosis 24.03 18.51 8 7236 1032 50596848
Camptocormia 23.66 18.51 6 7238 295 50597585
Cholelithiasis 23.37 18.51 28 7216 37945 50559935
Delusion 23.26 18.51 16 7228 10553 50587327
Memory impairment 23.04 18.51 41 7203 79319 50518561
Death 22.88 18.51 9 7235 325370 50272510
Blood growth hormone abnormal 22.51 18.51 4 7240 33 50597847
Empty sella syndrome 22.41 18.51 4 7240 34 50597846
Blood parathyroid hormone increased 22.39 18.51 10 7234 2844 50595036
Ovarian rupture 22.10 18.51 4 7240 37 50597843
Blood thyroid stimulating hormone decreased 21.65 18.51 11 7233 4161 50593719
Application site mass 21.56 18.51 4 7240 43 50597837
Dopamine dysregulation syndrome 21.48 18.51 5 7239 171 50597709
Chikungunya virus infection 21.23 18.51 5 7239 180 50597700
Hypopituitarism 21.12 18.51 7 7237 890 50596990
Blood sodium increased 20.73 18.51 9 7235 2393 50595487
Neoplasm 20.65 18.51 12 7232 5916 50591964
Toxicity to various agents 20.52 18.51 3 7241 212496 50385384
Arteriovenous fistula 19.98 18.51 5 7239 233 50597647
Galactorrhoea 19.86 18.51 10 7234 3713 50594167
Headache 19.84 18.51 132 7112 506403 50091477
Pituitary tumour recurrent 19.75 18.51 4 7240 70 50597810
Dengue fever 19.42 18.51 6 7238 609 50597271
Vitamin B12 decreased 19.36 18.51 9 7235 2806 50595074
Normal newborn 19.30 18.51 12 7232 6679 50591201
Nocturia 19.24 18.51 12 7232 6718 50591162
Adjacent segment degeneration 18.73 18.51 3 7241 12 50597868
Blood gonadotrophin decreased 18.73 18.51 3 7241 12 50597868
Mitral valve disease 18.68 18.51 8 7236 2058 50595822

FDA Adverse Event Reporting System (Male)

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
Cerebrospinal fluid leakage 260.63 20.53 46 4240 361 29569880
Gambling disorder 182.70 20.53 43 4243 1532 29568709
Insulin-like growth factor increased 127.09 20.53 30 4256 1081 29569160
Aortic valve incompetence 101.48 20.53 35 4251 4978 29565263
Pneumocephalus 89.17 20.53 15 4271 85 29570156
Mitral valve incompetence 77.39 20.53 38 4248 13255 29556986
Visual pathway disorder 76.37 20.53 11 4275 16 29570225
Pituitary haemorrhage 73.22 20.53 14 4272 177 29570064
Needle issue 55.26 20.53 22 4264 4661 29565580
Empty sella syndrome 55.14 20.53 9 4277 41 29570200
Secondary hypogonadism 50.45 20.53 11 4275 275 29569966
Blood growth hormone increased 50.37 20.53 11 4275 277 29569964
Neoplasm progression 49.95 20.53 32 4254 18580 29551661
Jealous delusion 47.99 20.53 10 4276 200 29570041
Prolactin-producing pituitary tumour 44.25 20.53 7 4279 25 29570216
Cardiac valve disease 42.96 20.53 16 4270 2832 29567409
Hormone level abnormal 42.85 20.53 10 4276 342 29569899
Pituitary tumour 39.10 20.53 10 4276 503 29569738
Pleural effusion 39.02 20.53 50 4236 71858 29498383
Tricuspid valve incompetence 37.25 20.53 20 4266 8374 29561867
Intracranial hypotension 36.28 20.53 8 4278 211 29570030
Cortisol free urine increased 34.05 20.53 5 4281 9 29570232
Pleural fibrosis 33.65 20.53 11 4275 1324 29568917
Blood corticotrophin increased 32.06 20.53 6 4280 67 29570174
Glucose tolerance decreased 31.59 20.53 6 4280 73 29570168
Gambling 31.55 20.53 7 4279 190 29570051
Impulse-control disorder 30.50 20.53 10 4276 1215 29569026
Acromegaly 29.62 20.53 5 4281 29 29570212
Therapeutic response decreased 29.18 20.53 26 4260 24685 29545556
Autoimmune thyroiditis 28 20.53 9 4277 1027 29569214
Dopamine dysregulation syndrome 27.98 20.53 7 4279 322 29569919
Borderline personality disorder 27.75 20.53 7 4279 333 29569908
Hemianopia 27.60 20.53 8 4278 645 29569596
Injection site pain 26.72 20.53 28 4258 32418 29537823
Priapism 26.61 20.53 13 4273 4475 29565766
IIIrd nerve paralysis 25.76 20.53 7 4279 446 29569795
Hypersexuality 25.62 20.53 9 4277 1347 29568894
Persecutory delusion 25.05 20.53 10 4276 2131 29568110
Injection site erosion 24.99 20.53 5 4281 81 29570160
Blood prolactin increased 24.54 20.53 9 4277 1525 29568716
Reversible cerebral vasoconstriction syndrome 24.26 20.53 6 4280 263 29569978
Cardiomegaly 23.61 20.53 18 4268 13758 29556483
Death 22.19 20.53 11 4275 342073 29228168
Blood testosterone decreased 22.15 20.53 11 4275 3919 29566322
Aortic valve sclerosis 21.83 20.53 7 4279 793 29569448
Therapeutic product effect decreased 21.76 20.53 24 4262 29427 29540814
Renal haematoma 20.83 20.53 6 4280 473 29569768

FDA Adverse Event Reporting System (Geriatric)

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
Cerebrospinal fluid leakage 235.76 16.04 52 10114 1260 64487306
Insulin-like growth factor increased 213.26 16.04 50 10116 1602 64486964
Blood growth hormone increased 182.70 16.04 37 10129 585 64487981
Aortic valve incompetence 159.60 16.04 57 10109 8244 64480322
Gambling disorder 151.40 16.04 39 10127 1855 64486711
Pneumocephalus 124.03 16.04 23 10143 222 64488344
Pituitary haemorrhage 113.21 16.04 22 10144 278 64488288
Mitral valve incompetence 106.29 16.04 60 10106 25478 64463088
Needle issue 100.59 16.04 42 10124 9230 64479336
Blood prolactin increased 90.24 16.04 30 10136 3498 64485068
Pituitary tumour 84.63 16.04 22 10144 1084 64487482
Ovarian hyperstimulation syndrome 80.04 16.04 26 10140 2819 64485747
Insulin-like growth factor decreased 72.59 16.04 17 10149 541 64488025
Visual pathway disorder 70.93 16.04 12 10154 64 64488502
Empty sella syndrome 70.62 16.04 12 10154 66 64488500
Acromegaly 69.73 16.04 12 10154 72 64488494
Tricuspid valve incompetence 68.18 16.04 39 10127 16964 64471602
Prolactin-producing pituitary tumour 58.96 16.04 11 10155 110 64488456
Cardiac valve disease 57.92 16.04 24 10142 5171 64483395
Coronary artery dissection 54.90 16.04 15 10151 895 64487671
Pulmonary pain 54.44 16.04 19 10147 2565 64486001
Neoplasm progression 52.84 16.04 47 10119 40917 64447649
Intracranial hypotension 52.45 16.04 12 10154 344 64488222
Secondary hypogonadism 52.38 16.04 12 10154 346 64488220
Diabetes mellitus 46.77 16.04 55 10111 66419 64422147
Hormone level abnormal 45.51 16.04 15 10151 1702 64486864
Pituitary tumour benign 45.02 16.04 16 10150 2277 64486289
Blood pressure increased 42.71 16.04 88 10078 172464 64316102
Acute kidney injury 41.42 16.04 10 10156 449230 64039336
Jealous delusion 40.79 16.04 9 10157 218 64488348
Blood growth hormone abnormal 40.68 16.04 7 10159 42 64488524
Dopamine dysregulation syndrome 38.94 16.04 10 10156 469 64488097
Toxicity to various agents 37.89 16.04 6 10160 363507 64125059
Mediastinal fibrosis 37.74 16.04 6 10160 20 64488546
Death 35.31 16.04 16 10150 482689 64005877
Bite 35.11 16.04 9 10157 419 64488147
Gambling 33.40 16.04 8 10158 281 64488285
Inappropriate schedule of product administration 32.78 16.04 55 10111 92231 64396335
Pituitary enlargement 32.53 16.04 6 10160 56 64488510
Delusion 32.25 16.04 25 10141 17989 64470577
Aortic valve sclerosis 30.93 16.04 11 10155 1568 64486998
Glucose tolerance decreased 30.86 16.04 6 10160 76 64488490
Pleural fibrosis 29.88 16.04 14 10152 4036 64484530
Mitral valve disease 28.77 16.04 12 10154 2626 64485940
Headache 28.55 16.04 161 10005 529306 63959260
Cardiomegaly 28.22 16.04 26 10140 23658 64464908
Hallucination 28.03 16.04 45 10121 72743 64415823
Neoplasm 27.84 16.04 16 10150 7015 64481551
Injection site pain 27.75 16.04 57 10109 111351 64377215
Urine calcium/creatinine ratio increased 27.32 16.04 6 10160 142 64488424
Priapism 27.07 16.04 13 10153 3957 64484609
Reversible cerebral vasoconstriction syndrome 26.71 16.04 11 10155 2331 64486235
Injection site mass 26.71 16.04 22 10144 17248 64471318
Tricuspid valve disease 26.17 16.04 7 10159 385 64488181
Visual field defect 25.66 16.04 16 10150 8130 64480436
Carotid aneurysm rupture 25.24 16.04 4 10162 13 64488553
Urethral caruncle 24.99 16.04 5 10161 74 64488492
Hypersexuality 24.12 16.04 9 10157 1470 64487096
Blood pressure systolic increased 23.91 16.04 34 10132 49419 64439147
Persecutory delusion 23.55 16.04 12 10154 4146 64484420
Aortic valve disease 23.47 16.04 9 10157 1584 64486982
Cardiac valve sclerosis 23.25 16.04 5 10161 107 64488459
Sleep apnoea syndrome 23.19 16.04 26 10140 29806 64458760
Injection site erosion 22.82 16.04 5 10161 117 64488449
Ovarian rupture 22.47 16.04 4 10162 30 64488536
Pituitary tumour recurrent 22.32 16.04 5 10161 130 64488436
Blindness 22.12 16.04 22 10144 21997 64466569
Pleural effusion 21.82 16.04 56 10110 126503 64362063
Mastitis 21.69 16.04 9 10157 1945 64486621
Compulsive shopping 21.45 16.04 7 10159 770 64487796
Drug resistance 21.36 16.04 27 10139 35075 64453491
Heart rate decreased 21.14 16.04 34 10132 55033 64433533
Blood testosterone decreased 20.96 16.04 9 10157 2116 64486450
Body temperature decreased 20.84 16.04 23 10143 25905 64462661
Cortisol free urine increased 20.77 16.04 4 10162 48 64488518
Camptocormia 20.31 16.04 6 10160 475 64488091
Normal newborn 20.17 16.04 12 10154 5605 64482961
Pneumonia 20.08 16.04 36 10130 559540 63929026
Impulse-control disorder 19.97 16.04 8 10158 1580 64486986
Sepsis 19.55 16.04 6 10160 230335 64258231
Autoimmune thyroiditis 19.46 16.04 10 10156 3518 64485048
IIIrd nerve paralysis 19.23 16.04 7 10159 1067 64487499
Memory impairment 19.20 16.04 42 10124 85640 64402926
Mitral valve sclerosis 18.89 16.04 5 10161 264 64488302
Blood prolactin decreased 18.89 16.04 5 10161 264 64488302
Oncologic complication 18.79 16.04 5 10161 270 64488296
Performance enhancing product use 18.63 16.04 4 10162 85 64488481
Adjacent segment degeneration 18.44 16.04 3 10163 12 64488554
Hyperprolactinaemia 18.12 16.04 10 10156 4055 64484511
Kounis syndrome 17.92 16.04 9 10157 3016 64485550
Renal haematoma 17.91 16.04 6 10160 716 64487850
Cholelithiasis 17.33 16.04 28 10138 45478 64443088
Movement disorder 16.80 16.04 19 10147 21981 64466585
Hemianopia 16.78 16.04 7 10159 1532 64487034
Mass 16.72 16.04 16 10150 15260 64473306
Blood corticotrophin increased 16.58 16.04 4 10162 145 64488421
Arteriovenous fistula 16.57 16.04 6 10160 900 64487666
Infusion related reaction 16.48 16.04 3 10163 164464 64324102
Rheumatoid arthritis 16.46 16.04 3 10163 164291 64324275
Cardiac murmur 16.37 16.04 14 10152 11549 64477017
Carcinoid tumour 16.37 16.04 5 10161 443 64488123
Tumour compression 16.32 16.04 4 10162 155 64488411
Thyroid disorder 16.24 16.04 14 10152 11678 64476888

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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 CS M0007652 Ergolines
CHEBI has role CHEBI:35610 antineoplastic agents
CHEBI has role CHEBI:48407 antiparkinson agent
CHEBI has role CHEBI:51065 Dopamine receptor agonist
MeSH PA D018726 Anti-Dyskinesia 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
FDA EPC N0000175827 Ergot Derivative

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Hyperprolactinemia indication 237662005 DOID:12700
Heart valve disorder contraindication 368009 DOID:4079
Severe pre-eclampsia contraindication 46764007
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




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

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:

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

External reference:

IDSource
4021014 VUID
N0000148483 NUI
D00987 KEGG_DRUG
134895 RXNORM
C0107994 UMLSCUI
CHEBI:3286 CHEBI
CHEMBL1201087 ChEMBL_ID
D000077465 MESH_DESCRIPTOR_UI
DB00248 DRUGBANK_ID
37 IUPHAR_LIGAND_ID
5860 INN_ID
LL60K9J05T UNII
54746 PUBCHEM_CID
4317 MMSL
6425 MMSL
73532 MMSL
d04112 MMSL
005446 NDDF
109139002 SNOMEDCT_US
386979007 SNOMEDCT_US
4021014 VANDF

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Cabergoline HUMAN PRESCRIPTION DRUG LABEL 1 0093-5420 TABLET 0.50 mg ORAL ANDA 25 sections
Cabergoline HUMAN PRESCRIPTION DRUG LABEL 1 49884-673 TABLET 0.50 mg ORAL ANDA 21 sections
Cabergoline HUMAN PRESCRIPTION DRUG LABEL 1 50090-3157 TABLET 0.50 mg ORAL ANDA 25 sections
Cabergoline HUMAN PRESCRIPTION DRUG LABEL 1 50090-3951 TABLET 0.50 mg ORAL ANDA 21 sections
Cabergoline HUMAN PRESCRIPTION DRUG LABEL 1 50090-5834 TABLET 0.50 mg ORAL ANDA 22 sections
Cabergoline HUMAN PRESCRIPTION DRUG LABEL 1 50742-118 TABLET 0.50 mg ORAL ANDA 23 sections
Cabergoline HUMAN PRESCRIPTION DRUG LABEL 1 59762-1005 TABLET 0.50 mg ORAL NDA AUTHORIZED GENERIC 22 sections