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Identification
NameCabergoline
Accession NumberDB00248  (APRD00836)
TypeSmall Molecule
GroupsApproved
DescriptionCabergoline, an ergot derivative, is a long-acting dopamine agonist and prolactin inhibitor. It is used to treat hyperprolactinemic disorders and Parkinsonian Syndrome. Cabergoline possesses potent agonist activity on dopamine D2 receptors.
Structure
Thumb
Synonyms
(8beta)-N-[3-(dimethylamino)Propyl]-N-[(ethylamino)carbonyl]-6-(2-propenyl)-ergoline-8-carboxamide
(8R)-6-Allyl-N-[3-(dimethylamino)propyl]-N-(ethylcarbamoyl)ergoline-8-carboxamide
1-((6-Allylergolin-8beta-yl)carbonyl)-1-(3-(dimethylamino)propyl)-3-ethylurea
1-[(6-Allylergoline-8beta-yl)carbonyl]-1-[3-(dimethylamino)propyl]-3-ethylurea
1-Ethyl-3-(3'-dimethylamionpropyl)-2-(6'-allylergoline-8'beta-carbonyl)urea
Cabergolina
Cabergoline
Cabergolinum
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Act CabergolineTablet0.5 mgOralActavis Pharma Company2007-11-06Not applicableCanada
CabergolineTablet0.5 mgOralCobalt Pharmaceuticals CompanyNot applicableNot applicableCanada
CabergolineTablet.5 mg/1OralGreenstone LLC2014-09-22Not applicableUs
DostinexTablet0.5 mgOralPfizer Canada Inc2000-06-30Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-cabergolineTablet0.5 mgOralApotex IncNot applicableNot applicableCanada
CabergolineTablet.5 mg/1OralTeva Pharmaceuticals USA Inc2007-03-07Not applicableUs
CabergolineTablet.5 mg/1OralApotex Corp.2013-03-08Not applicableUs
CabergolineTablet.5 mg/1OralMylan Pharmaceuticals Inc.2013-12-02Not applicableUs
CabergolineTablet.5 mg/1OralAvera Mc Kennan Hospital2015-04-14Not applicableUs
CabergolineTablet.5 mg/1OralCobalt Laboratories2008-04-21Not applicableUs
CabergolineTablet.5 mg/1OralPar Pharmaceutical, Inc.2005-12-29Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
CabaserPfizer
Brand mixturesNot Available
SaltsNot Available
Categories
UNIILL60K9J05T
CAS number81409-90-7
WeightAverage: 451.6043
Monoisotopic: 451.294725453
Chemical FormulaC26H37N5O2
InChI KeyKORNTPPJEAJQIU-KJXAQDMKSA-N
InChI
InChI=1S/C26H37N5O2/c1-5-11-30-17-19(25(32)31(26(33)27-6-2)13-8-12-29(3)4)14-21-20-9-7-10-22-24(20)18(16-28-22)15-23(21)30/h5,7,9-10,16,19,21,23,28H,1,6,8,11-15,17H2,2-4H3,(H,27,33)/t19-,21-,23-/m1/s1
IUPAC Name
1-[3-(dimethylamino)propyl]-3-ethyl-1-[(2R,4R,7R)-6-(prop-2-en-1-yl)-6,11-diazatetracyclo[7.6.1.0²,⁷.0¹²,¹⁶]hexadeca-1(16),9,12,14-tetraene-4-carbonyl]urea
SMILES
[H][C@@]12CC3=CNC4=CC=CC(=C34)[C@@]1([H])C[[email protected]](CN2CC=C)C(=O)N(CCCN(C)C)C(=O)NCC
Pharmacology
IndicationFor the treatment of hyperprolactinemic disorders, either idiopathic or due to prolactinoma (prolactin-secreting adenomas). May also be used to manage symptoms of Parkinsonian Syndrome as monotherapy during initial symptomatic management or as an adjunct to levodopa therapy during advanced stages of disease.
Structured Indications
PharmacodynamicsCabergoline 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, which are associated with dyskinesias. The dopaminergic D2 receptor subfamily consists of D2, D3 and D4 subreceptors, which are 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 (in order of decreasing binding affinities) on 5-hydroxytryptamine (5-HT)2B, 5-HT2A, 5-HT1D, dopamine D4, 5-HT1A, dopamine D1, 5-HT1B and 5-HT2C receptors and antagonist activity on α2B, α2A, and α2C 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.
Mechanism of actionThe dopamine D2 receptor is a 7-transmembrane G-protein coupled receptor associated with Gi proteins. In lactotrophs, stimulation of dopamine D2 causes inhibition of adenylyl cyclase, which decreases intracellular cAMP concentrations and blocks IP3-dependent release of Ca2+ from intracellular stores. Decreases in intracellular calcium levels may also be brought about via inhibition of calcium influx through voltage-gated calcium channels, rather than via inhibition of adenylyl cyclase. Additionally, receptor activation blocks phosphorylation of p42/p44 MAPK and decreases MAPK/ERK kinase phosphorylation. Inhibition of MAPK appears to be mediated by c-Raf and B-Raf-dependent inhibition of MAPK/ERK kinase. Dopamine-stimulated growth hormone release from the pituitary gland is mediated by a decrease in intracellular calcium influx through voltage-gated calcium channels rather than via adenylyl cyclase inhibition. Stimulation of dopamine D2 receptors in the nigrostriatal pathway leads to improvements in coordinated muscle activity in those with movement disorders. Cabergoline is a long-acting dopamine receptor agonist with a high affinity for D2 receptors. Receptor-binding studies indicate that cabergoline has low affinity for dopamine D1, α1,- and α2- adrenergic, and 5-HT1- and 5-HT2-serotonin receptors.
TargetKindPharmacological actionActionsOrganismUniProt ID
D(2) dopamine receptorProteinyes
agonist
HumanP14416 details
5-hydroxytryptamine receptor 2BProteinunknown
agonist
HumanP41595 details
D(3) dopamine receptorProteinunknown
agonist
HumanP35462 details
5-hydroxytryptamine receptor 2AProteinunknown
agonist
HumanP28223 details
Alpha-2B adrenergic receptorProteinunknown
antagonist
HumanP18089 details
5-hydroxytryptamine receptor 1DProteinunknown
agonist
HumanP28221 details
D(4) dopamine receptorProteinunknown
agonist
HumanP21917 details
Alpha-2A adrenergic receptorProteinunknown
antagonist
HumanP08913 details
5-hydroxytryptamine receptor 1AProteinunknown
agonist
HumanP08908 details
Alpha-2C adrenergic receptorProteinunknown
antagonist
HumanP18825 details
D(1B) dopamine receptorProteinunknown
agonist
HumanP21918 details
D(1A) dopamine receptorProteinunknown
agonist
HumanP21728 details
5-hydroxytryptamine receptor 1BProteinunknown
agonist
HumanP28222 details
5-hydroxytryptamine receptor 2CProteinunknown
agonist
HumanP28335 details
5-hydroxytryptamine receptor 7Proteinunknown
antagonist
HumanP34969 details
Alpha-1A adrenergic receptorProteinunknown
binder
HumanP35348 details
Alpha-1B adrenergic receptorProteinunknown
binder
HumanP35368 details
Alpha-1D adrenergic receptorProteinunknown
binder
HumanP25100 details
Beta-1 adrenergic receptorProteinunknown
binder
HumanP08588 details
Beta-2 adrenergic receptorProteinunknown
binder
HumanP07550 details
D(1) dopamine receptorProtein groupunknown
agonist
Humannot applicabledetails
D(2S) dopamine receptorProteinunknown
agonist
Humannot applicabledetails
D(2L) dopamine receptorProteinunknown
agonist
Humannot applicabledetails
Related Articles
AbsorptionFirst-pass effect is seen, however the absolute bioavailability is unknown.
Volume of distributionNot Available
Protein bindingModerately bound (40% to 42%) to human plasma proteins in a concentration-independent manner.
Metabolism

Hepatic. Cabergoline is extensively metabolized, predominately via hydrolysis of the acylurea bond of the urea moiety. Cytochrome P-450 mediated metabolism appears to be minimal. The main metabolite identified in urine is 6-allyl-8b-carboxy-ergoline (4-6% of dose). Three other metabolites were identified urine (less than 3% of dose).

SubstrateEnzymesProduct
Cabergoline
Not Available
6-allyl-8b-carboxy-ergolineDetails
Route of eliminationAfter oral dosing of radioactive cabergoline to five healthy volunteers, approximately 22% and 60% of the dose was excreted within 20 days in the urine and feces, respectively. Less than 4% of the dose was excreted unchanged in the urine.
Half lifeThe elimination half-life is estimated from urinary data of 12 healthy subjects to range between 63 to 69 hours.
Clearance
  • renal cl=0,008 L/min
  • nonrenal cl=3.2 L/min
ToxicityOverdosage might be expected to produce nasal congestion, syncope, or hallucinations.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
1,10-PhenanthrolineThe serum concentration of Cabergoline can be increased when it is combined with 1,10-Phenanthroline.Experimental
3,4-DichloroisocoumarinThe serum concentration of Cabergoline can be increased when it is combined with 3,4-Dichloroisocoumarin.Experimental
4-(2-AMINOETHYL)BENZENESULFONYL FLUORIDEThe serum concentration of Cabergoline can be increased when it is combined with 4-(2-AMINOETHYL)BENZENESULFONYL FLUORIDE.Experimental
7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINEThe metabolism of Cabergoline can be decreased when combined with 7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE.Experimental
AcebutololAcebutolol may increase the vasoconstricting activities of Cabergoline.Approved
AcepromazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Acepromazine.Approved, Vet Approved
AceprometazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Aceprometazine.Approved
AcetophenazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Acetophenazine.Approved
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Cabergoline.Approved
AdrafinilCabergoline may increase the hypertensive activities of Adrafinil.Withdrawn
AlmotriptanCabergoline may increase the vasoconstricting activities of Almotriptan.Approved, Investigational
AlogliptinThe serum concentration of Cabergoline can be increased when it is combined with Alogliptin.Approved
Alpha-1-proteinase inhibitorThe serum concentration of Cabergoline can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved
AlprenololAlprenolol may increase the vasoconstricting activities of Cabergoline.Approved, Withdrawn
AmiodaroneThe metabolism of Cabergoline can be decreased when combined with Amiodarone.Approved, Investigational
AmisulprideThe therapeutic efficacy of Amisulpride can be decreased when used in combination with Cabergoline.Approved, Investigational
AmitrazCabergoline may increase the hypertensive activities of Amitraz.Vet Approved
AmitriptylineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Amitriptyline.Approved
AmoxapineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Amoxapine.Approved
AmperozideThe risk or severity of adverse effects can be increased when Cabergoline is combined with Amperozide.Experimental
AmprenavirThe serum concentration of Cabergoline can be increased when it is combined with Amprenavir.Approved
AnisodamineCabergoline may increase the hypertensive activities of Anisodamine.Investigational
Antithrombin III humanThe serum concentration of Cabergoline can be increased when it is combined with Antithrombin III human.Approved
AnvirzelAnvirzel may decrease the cardiotoxic activities of Cabergoline.Investigational
Aop200704Aop200704 may increase the vasoconstricting activities of Cabergoline.Investigational
ApixabanThe serum concentration of Cabergoline can be increased when it is combined with Apixaban.Approved
ApomorphineCabergoline may increase the vasoconstricting activities of Apomorphine.Approved, Investigational
ApraclonidineCabergoline may increase the hypertensive activities of Apraclonidine.Approved
AprepitantThe serum concentration of Cabergoline can be increased when it is combined with Aprepitant.Approved, Investigational
AprotininThe serum concentration of Cabergoline can be increased when it is combined with Aprotinin.Approved, Withdrawn
ArbutamineCabergoline may increase the hypertensive activities of Arbutamine.Approved
ArformoterolCabergoline may increase the hypertensive activities of Arformoterol.Approved, Investigational
ArgatrobanThe serum concentration of Cabergoline can be increased when it is combined with Argatroban.Approved, Investigational
AripiprazoleThe risk or severity of adverse effects can be increased when Cabergoline is combined with Aripiprazole.Approved, Investigational
ArotinololArotinolol may increase the vasoconstricting activities of Cabergoline.Approved
AsenapineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Asenapine.Approved
AsunaprevirThe serum concentration of Cabergoline can be increased when it is combined with Asunaprevir.Approved, Investigational
AtazanavirThe serum concentration of Cabergoline can be increased when it is combined with Atazanavir.Approved, Investigational
AtenololAtenolol may increase the vasoconstricting activities of Cabergoline.Approved
AtomoxetineThe metabolism of Cabergoline can be decreased when combined with Atomoxetine.Approved
AzaperoneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Azaperone.Vet Approved
BatimastatThe serum concentration of Cabergoline can be increased when it is combined with Batimastat.Experimental
BefunololCabergoline may increase the hypertensive activities of Befunolol.Experimental
BenazeprilThe serum concentration of Cabergoline can be increased when it is combined with Benazepril.Approved, Investigational
BenmoxinThe metabolism of Cabergoline can be decreased when combined with Benmoxin.Withdrawn
BenperidolThe risk or severity of adverse effects can be increased when Cabergoline is combined with Benperidol.Investigational
BenzamidineThe serum concentration of Cabergoline can be increased when it is combined with Benzamidine.Experimental
BetaxololBetaxolol may increase the vasoconstricting activities of Cabergoline.Approved
BevacizumabBevacizumab may increase the cardiotoxic activities of Cabergoline.Approved, Investigational
BevantololBevantolol may increase the vasoconstricting activities of Cabergoline.Approved
BexaroteneThe serum concentration of Cabergoline can be decreased when it is combined with Bexarotene.Approved, Investigational
Bi201335The serum concentration of Cabergoline can be increased when it is combined with Bi201335.Investigational
BifeprunoxThe risk or severity of adverse effects can be increased when Cabergoline is combined with Bifeprunox.Investigational
BisoprololBisoprolol may increase the vasoconstricting activities of Cabergoline.Approved
BitolterolCabergoline may increase the hypertensive activities of Bitolterol.Withdrawn
BivalirudinThe serum concentration of Cabergoline can be increased when it is combined with Bivalirudin.Approved, Investigational
BoceprevirThe serum concentration of Cabergoline can be increased when it is combined with Boceprevir.Approved
BopindololBopindolol may increase the vasoconstricting activities of Cabergoline.Approved
BortezomibThe metabolism of Cabergoline can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Cabergoline can be decreased when it is combined with Bosentan.Approved, Investigational
BrexpiprazoleThe risk or severity of adverse effects can be increased when Cabergoline is combined with Brexpiprazole.Approved
BrimonidineCabergoline may increase the hypertensive activities of Brimonidine.Approved
BromocriptineCabergoline may increase the vasoconstricting activities of Bromocriptine.Approved, Investigational
BromperidolThe risk or severity of adverse effects can be increased when Cabergoline is combined with Bromperidol.Investigational
BucindololBucindolol may increase the vasoconstricting activities of Cabergoline.Investigational
BufuralolBufuralol may increase the vasoconstricting activities of Cabergoline.Experimental, Investigational
BupranololBupranolol may increase the vasoconstricting activities of Cabergoline.Approved
BuspironeThe risk or severity of adverse effects can be increased when Cabergoline is combined with Buspirone.Approved, Investigational
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Cabergoline.Approved
CandoxatrilThe serum concentration of Cabergoline can be increased when it is combined with Candoxatril.Experimental
CandoxatrilatThe serum concentration of Cabergoline can be increased when it is combined with Candoxatrilat.Experimental
CaptoprilThe serum concentration of Cabergoline can be increased when it is combined with Captopril.Approved
CarbamazepineThe metabolism of Cabergoline can be increased when combined with Carbamazepine.Approved, Investigational
CarbomycinThe serum concentration of Cabergoline can be increased when it is combined with Carbomycin.Vet Approved
CariprazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Cariprazine.Approved
CaroxazoneThe metabolism of Cabergoline can be decreased when combined with Caroxazone.Withdrawn
CarteololCarteolol may increase the vasoconstricting activities of Cabergoline.Approved
CarvedilolCarvedilol may increase the vasoconstricting activities of Cabergoline.Approved, Investigational
CeliprololCeliprolol may increase the vasoconstricting activities of Cabergoline.Approved, Investigational
CeritinibThe serum concentration of Cabergoline can be increased when it is combined with Ceritinib.Approved
ChlorpromazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Chlorpromazine.Approved, Vet Approved
ChlorprothixeneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Chlorprothixene.Approved, Withdrawn
ChymostatinThe serum concentration of Cabergoline can be increased when it is combined with Chymostatin.Experimental
CilastatinThe serum concentration of Cabergoline can be increased when it is combined with Cilastatin.Approved
CilazaprilThe serum concentration of Cabergoline can be increased when it is combined with Cilazapril.Approved
CirazolineCabergoline may increase the hypertensive activities of Cirazoline.Experimental
CitalopramThe risk or severity of adverse effects can be increased when Citalopram is combined with Cabergoline.Approved
ClarithromycinThe serum concentration of Cabergoline can be increased when it is combined with Clarithromycin.Approved
ClemastineThe metabolism of Cabergoline can be decreased when combined with Clemastine.Approved
ClenbuterolCabergoline may increase the hypertensive activities of Clenbuterol.Approved, Vet Approved
ClomipramineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Clomipramine.Approved, Vet Approved
ClonidineCabergoline may increase the hypertensive activities of Clonidine.Approved
ClotrimazoleThe metabolism of Cabergoline can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Clozapine.Approved
CobicistatThe metabolism of Cabergoline can be decreased when combined with Cobicistat.Approved
ConivaptanThe serum concentration of Cabergoline can be increased when it is combined with Conivaptan.Approved, Investigational
CrizotinibThe metabolism of Cabergoline can be decreased when combined with Crizotinib.Approved
CyamemazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Cyamemazine.Approved
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Cyclobenzaprine.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Cabergoline.Approved, Investigational
CyclosporineThe metabolism of Cabergoline can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
Dabigatran etexilateThe serum concentration of Cabergoline can be increased when it is combined with Dabigatran etexilate.Approved
DabrafenibThe serum concentration of Cabergoline can be decreased when it is combined with Dabrafenib.Approved
DapiprazoleThe risk or severity of adverse effects can be increased when Cabergoline is combined with Dapiprazole.Approved
DapoxetineThe risk or severity of adverse effects can be increased when Dapoxetine is combined with Cabergoline.Investigational
DarunavirThe serum concentration of Cabergoline can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Cabergoline can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Cabergoline can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Cabergoline can be decreased when combined with Delavirdine.Approved
DesipramineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Desipramine.Approved
DeslanosideDeslanoside may decrease the cardiotoxic activities of Cabergoline.Approved
DesvenlafaxineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Desvenlafaxine.Approved
DetomidineCabergoline may increase the hypertensive activities of Detomidine.Vet Approved
DexamethasoneThe serum concentration of Cabergoline can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DexmedetomidineCabergoline may increase the hypertensive activities of Dexmedetomidine.Approved, Vet Approved
DextromethorphanThe risk or severity of adverse effects can be increased when Cabergoline is combined with Dextromethorphan.Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Cabergoline.Approved
DigoxinDigoxin may decrease the cardiotoxic activities of Cabergoline.Approved
DihydroergotamineCabergoline may increase the vasoconstricting activities of Dihydroergotamine.Approved
DiltiazemThe metabolism of Cabergoline can be decreased when combined with Diltiazem.Approved
DipivefrinCabergoline may increase the hypertensive activities of Dipivefrin.Approved
DobutamineCabergoline may increase the hypertensive activities of Dobutamine.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Cabergoline.Approved, Investigational
DolasetronDolasetron may increase the serotonergic activities of Cabergoline.Approved
DoxepinThe risk or severity of adverse effects can be increased when Cabergoline is combined with Doxepin.Approved
DoxycyclineThe metabolism of Cabergoline can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Cabergoline can be decreased when combined with Dronedarone.Approved
DroperidolThe risk or severity of adverse effects can be increased when Cabergoline is combined with Droperidol.Approved, Vet Approved
DroxidopaCabergoline may increase the hypertensive activities of Droxidopa.Approved, Investigational
DuloxetineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Duloxetine.Approved
EcabetThe serum concentration of Cabergoline can be increased when it is combined with Ecabet.Approved, Investigational
EcopipamThe risk or severity of adverse effects can be increased when Cabergoline is combined with Ecopipam.Investigational
EdoxabanThe serum concentration of Cabergoline can be increased when it is combined with Edoxaban.Approved
EfavirenzThe serum concentration of Cabergoline can be decreased when it is combined with Efavirenz.Approved, Investigational
ElafinThe serum concentration of Cabergoline can be increased when it is combined with Elafin.Investigational
EletriptanCabergoline may increase the vasoconstricting activities of Eletriptan.Approved, Investigational
EnalaprilThe serum concentration of Cabergoline can be increased when it is combined with Enalapril.Approved, Vet Approved
EnalaprilatThe serum concentration of Cabergoline can be increased when it is combined with Enalaprilat.Approved
EnalkirenThe serum concentration of Cabergoline can be increased when it is combined with Enalkiren.Experimental
EnzalutamideThe serum concentration of Cabergoline can be decreased when it is combined with Enzalutamide.Approved
EphedrineCabergoline may increase the hypertensive activities of Ephedrine.Approved
EpinephrineCabergoline may increase the hypertensive activities of Epinephrine.Approved, Vet Approved
Ergoloid mesylateErgoloid mesylate may increase the vasoconstricting activities of Cabergoline.Approved
ErgonovineErgonovine may increase the vasoconstricting activities of Cabergoline.Approved
ErgotamineCabergoline may increase the hypertensive activities of Ergotamine.Approved
ErythromycinThe serum concentration of Cabergoline can be increased when it is combined with Erythromycin.Approved, Vet Approved
EscitalopramThe risk or severity of adverse effects can be increased when Cabergoline is combined with Escitalopram.Approved, Investigational
Eslicarbazepine acetateThe serum concentration of Cabergoline can be decreased when it is combined with Eslicarbazepine acetate.Approved
EsmololEsmolol may increase the vasoconstricting activities of Cabergoline.Approved
EtilefrineCabergoline may increase the hypertensive activities of Etilefrine.Withdrawn
EtravirineThe serum concentration of Cabergoline can be decreased when it is combined with Etravirine.Approved
FencamfamineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Fencamfamine.Approved, Illicit, Withdrawn
FenoterolCabergoline may increase the hypertensive activities of Fenoterol.Approved
FentanylThe risk or severity of adverse effects can be increased when Cabergoline is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FluconazoleThe metabolism of Cabergoline can be decreased when combined with Fluconazole.Approved
FluoxetineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe risk or severity of adverse effects can be increased when Cabergoline is combined with Flupentixol.Approved, Withdrawn
FluphenazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Fluphenazine.Approved
FluspirileneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Fluspirilene.Approved
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Cabergoline.Approved, Investigational
FormoterolCabergoline may increase the hypertensive activities of Formoterol.Approved, Investigational
FosamprenavirThe serum concentration of Cabergoline can be increased when it is combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Cabergoline can be increased when it is combined with Fosaprepitant.Approved
FosinoprilThe serum concentration of Cabergoline can be increased when it is combined with Fosinopril.Approved
FosphenytoinThe metabolism of Cabergoline can be increased when combined with Fosphenytoin.Approved
FrovatriptanCabergoline may increase the vasoconstricting activities of Frovatriptan.Approved, Investigational
FurazolidoneThe metabolism of Cabergoline can be decreased when combined with Furazolidone.Approved, Vet Approved
Fusidic AcidThe serum concentration of Cabergoline can be increased when it is combined with Fusidic Acid.Approved
GabexateThe serum concentration of Cabergoline can be increased when it is combined with Gabexate.Investigational
GeldanamycinThe serum concentration of Cabergoline can be increased when it is combined with Geldanamycin.Experimental
GM6001The serum concentration of Cabergoline can be increased when it is combined with GM6001.Experimental
GranisetronGranisetron may increase the serotonergic activities of Cabergoline.Approved, Investigational
GuanabenzCabergoline may increase the hypertensive activities of Guanabenz.Approved
GuanfacineCabergoline may increase the hypertensive activities of Guanfacine.Approved, Investigational
HaloperidolThe risk or severity of adverse effects can be increased when Cabergoline is combined with Haloperidol.Approved
HexoprenalineCabergoline may increase the hypertensive activities of Hexoprenaline.Approved, Withdrawn
HigenamineCabergoline may increase the hypertensive activities of Higenamine.Investigational
HirulogThe serum concentration of Cabergoline can be increased when it is combined with Hirulog.Experimental
HydracarbazineThe metabolism of Cabergoline can be decreased when combined with Hydracarbazine.Approved
IdelalisibThe serum concentration of Cabergoline can be increased when it is combined with Idelalisib.Approved
idraparinuxThe serum concentration of Cabergoline can be increased when it is combined with idraparinux.Investigational
IloperidoneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Iloperidone.Approved
ImatinibThe metabolism of Cabergoline can be decreased when combined with Imatinib.Approved
ImidaprilThe serum concentration of Cabergoline can be increased when it is combined with Imidapril.Investigational
ImipramineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Imipramine.Approved
IndenololIndenolol may increase the vasoconstricting activities of Cabergoline.Withdrawn
IndinavirThe serum concentration of Cabergoline can be increased when it is combined with Indinavir.Approved
IproclozideThe metabolism of Cabergoline can be decreased when combined with Iproclozide.Withdrawn
IproniazidThe metabolism of Cabergoline can be decreased when combined with Iproniazid.Withdrawn
IsavuconazoniumThe metabolism of Cabergoline can be decreased when combined with Isavuconazonium.Approved, Investigational
IsocarboxazidThe metabolism of Cabergoline can be decreased when combined with Isocarboxazid.Approved
IsoetarineCabergoline may increase the hypertensive activities of Isoetarine.Approved
IsoflurophateThe serum concentration of Cabergoline can be increased when it is combined with Isoflurophate.Approved, Withdrawn
IsoprenalineCabergoline may increase the hypertensive activities of Isoprenaline.Approved
IsoxsuprineCabergoline may increase the hypertensive activities of Isoxsuprine.Approved, Withdrawn
IsradipineThe metabolism of Cabergoline can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Cabergoline can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Cabergoline can be increased when it is combined with Ivacaftor.Approved
IxazomibThe serum concentration of Cabergoline can be increased when it is combined with Ixazomib.Approved
JosamycinThe serum concentration of Cabergoline can be increased when it is combined with Josamycin.Approved
KetoconazoleThe metabolism of Cabergoline can be decreased when combined with Ketoconazole.Approved, Investigational
KitasamycinThe serum concentration of Cabergoline can be increased when it is combined with Kitasamycin.Experimental
LabetalolLabetalol may increase the vasoconstricting activities of Cabergoline.Approved
LepirudinThe serum concentration of Cabergoline can be increased when it is combined with Lepirudin.Approved
LevobunololLevobunolol may increase the vasoconstricting activities of Cabergoline.Approved
LevomilnacipranThe risk or severity of adverse effects can be increased when Cabergoline is combined with Levomilnacipran.Approved
LinagliptinThe serum concentration of Cabergoline can be increased when it is combined with Linagliptin.Approved
LinezolidThe risk or severity of adverse effects can be increased when Cabergoline is combined with Linezolid.Approved, Investigational
LisinoprilThe serum concentration of Cabergoline can be increased when it is combined with Lisinopril.Approved, Investigational
LisurideCabergoline may increase the vasoconstricting activities of Lisuride.Approved
LithiumThe risk or severity of adverse effects can be increased when Cabergoline is combined with Lithium.Approved
LofexidineCabergoline may increase the hypertensive activities of Lofexidine.Approved, Investigational
LopinavirThe serum concentration of Cabergoline can be increased when it is combined with Lopinavir.Approved
LorcaserinThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Cabergoline.Approved
LovastatinThe metabolism of Cabergoline can be decreased when combined with Lovastatin.Approved, Investigational
LoxapineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Loxapine.Approved
Lu AA21004Cabergoline may increase the vasoconstricting activities of Lu AA21004.Investigational
LuliconazoleThe serum concentration of Cabergoline can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Cabergoline can be increased when combined with Lumacaftor.Approved
LurasidoneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Lurasidone.Approved
MaprotilineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Maprotiline.Approved
MebanazineThe metabolism of Cabergoline can be decreased when combined with Mebanazine.Withdrawn
MedetomidineCabergoline may increase the hypertensive activities of Medetomidine.Vet Approved
MelperoneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Melperone.Approved
MephentermineCabergoline may increase the hypertensive activities of Mephentermine.Approved
MesoridazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Mesoridazine.Approved
MetaraminolCabergoline may increase the hypertensive activities of Metaraminol.Approved, Investigational
MethadoneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Methadone.Approved
MethotrimeprazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Methotrimeprazine.Approved
MethoxamineCabergoline may increase the hypertensive activities of Methoxamine.Approved
MethyldopaCabergoline may increase the hypertensive activities of Methyldopa.Approved
Methylene blueThe metabolism of Cabergoline can be decreased when combined with Methylene blue.Investigational
MetipranololMetipranolol may increase the vasoconstricting activities of Cabergoline.Approved
MetoclopramideThe risk or severity of adverse effects can be increased when Cabergoline is combined with Metoclopramide.Approved, Investigational
MetoprololMetoprolol may increase the vasoconstricting activities of Cabergoline.Approved, Investigational
MidodrineCabergoline may increase the hypertensive activities of Midodrine.Approved
MifepristoneThe serum concentration of Cabergoline can be increased when it is combined with Mifepristone.Approved, Investigational
MilnacipranThe risk or severity of adverse effects can be increased when Cabergoline is combined with Milnacipran.Approved
MinaprineThe metabolism of Cabergoline can be decreased when combined with Minaprine.Approved
MirabegronCabergoline may increase the hypertensive activities of Mirabegron.Approved
MirtazapineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Mirtazapine.Approved
MitotaneThe serum concentration of Cabergoline can be decreased when it is combined with Mitotane.Approved
MoclobemideThe metabolism of Cabergoline can be decreased when combined with Moclobemide.Approved
ModafinilThe serum concentration of Cabergoline can be decreased when it is combined with Modafinil.Approved, Investigational
MoexiprilThe serum concentration of Cabergoline can be increased when it is combined with Moexipril.Approved
MolindoneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Molindone.Approved
N-(3-Propylcarbamoyloxirane-2-Carbonyl)-Isoleucyl-ProlineThe serum concentration of Cabergoline can be increased when it is combined with N-(3-Propylcarbamoyloxirane-2-Carbonyl)-Isoleucyl-Proline.Experimental
NadololNadolol may increase the vasoconstricting activities of Cabergoline.Approved
NafamostatThe serum concentration of Cabergoline can be increased when it is combined with Nafamostat.Investigational
NafcillinThe serum concentration of Cabergoline can be decreased when it is combined with Nafcillin.Approved
NaphazolineCabergoline may increase the hypertensive activities of Naphazoline.Approved
NaratriptanCabergoline may increase the vasoconstricting activities of Naratriptan.Approved, Investigational
NCX 4016The serum concentration of Cabergoline can be increased when it is combined with NCX 4016.Investigational
NebivololCabergoline may increase the hypertensive activities of Nebivolol.Approved, Investigational
NefazodoneThe metabolism of Cabergoline can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Cabergoline can be increased when it is combined with Nelfinavir.Approved
NetupitantThe serum concentration of Cabergoline can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Cabergoline can be increased when combined with Nevirapine.Approved
NialamideThe metabolism of Cabergoline can be decreased when combined with Nialamide.Withdrawn
NilotinibThe metabolism of Cabergoline can be decreased when combined with Nilotinib.Approved, Investigational
NitroaspirinThe serum concentration of Cabergoline can be increased when it is combined with Nitroaspirin.Investigational
NitroglycerinCabergoline may decrease the vasodilatory activities of Nitroglycerin.Approved, Investigational
NorepinephrineCabergoline may increase the hypertensive activities of Norepinephrine.Approved
NortriptylineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Nortriptyline.Approved
NylidrinCabergoline may increase the hypertensive activities of Nylidrin.Approved
OctamoxinThe metabolism of Cabergoline can be decreased when combined with Octamoxin.Withdrawn
OlanzapineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Olanzapine.Approved, Investigational
OlaparibThe metabolism of Cabergoline can be decreased when combined with Olaparib.Approved
OleandomycinThe serum concentration of Cabergoline can be increased when it is combined with Oleandomycin.Vet Approved
OlodaterolCabergoline may increase the hypertensive activities of Olodaterol.Approved
OmapatrilatThe serum concentration of Cabergoline can be increased when it is combined with Omapatrilat.Investigational
OndansetronOndansetron may increase the serotonergic activities of Cabergoline.Approved
OrciprenalineCabergoline may increase the hypertensive activities of Orciprenaline.Approved
OsanetantThe risk or severity of adverse effects can be increased when Cabergoline is combined with Osanetant.Investigational
OsimertinibThe serum concentration of Cabergoline can be increased when it is combined with Osimertinib.Approved
OtamixabanThe serum concentration of Cabergoline can be increased when it is combined with Otamixaban.Investigational
OuabainOuabain may decrease the cardiotoxic activities of Cabergoline.Approved
OxprenololOxprenolol may increase the vasoconstricting activities of Cabergoline.Approved
OxymetazolineCabergoline may increase the hypertensive activities of Oxymetazoline.Approved
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Cabergoline.Approved, Vet Approved
PalbociclibThe serum concentration of Cabergoline can be increased when it is combined with Palbociclib.Approved
PaliperidoneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Paliperidone.Approved
PalonosetronPalonosetron may increase the serotonergic activities of Cabergoline.Approved, Investigational
PargylineThe metabolism of Cabergoline can be decreased when combined with Pargyline.Approved
ParoxetineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Paroxetine.Approved, Investigational
PenbutololPenbutolol may increase the vasoconstricting activities of Cabergoline.Approved, Investigational
PentobarbitalThe metabolism of Cabergoline can be increased when combined with Pentobarbital.Approved, Vet Approved
PerazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Perazine.Investigational
PergolideCabergoline may increase the vasoconstricting activities of Pergolide.Approved, Vet Approved, Withdrawn
PerindoprilThe serum concentration of Cabergoline can be increased when it is combined with Perindopril.Approved
PerospironeThe risk or severity of adverse effects can be increased when Cabergoline is combined with Perospirone.Approved
PerphenazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Perphenazine.Approved
PethidineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Pethidine.Approved
PhenelzineThe metabolism of Cabergoline can be decreased when combined with Phenelzine.Approved
PheniprazineThe metabolism of Cabergoline can be decreased when combined with Pheniprazine.Withdrawn
PhenobarbitalThe metabolism of Cabergoline can be increased when combined with Phenobarbital.Approved
PhenoxypropazineThe metabolism of Cabergoline can be decreased when combined with Phenoxypropazine.Withdrawn
PhenylephrineCabergoline may increase the hypertensive activities of Phenylephrine.Approved
PhenylpropanolamineCabergoline may increase the hypertensive activities of Phenylpropanolamine.Approved, Vet Approved, Withdrawn
PhenytoinThe metabolism of Cabergoline can be increased when combined with Phenytoin.Approved, Vet Approved
PhosphoramidonThe serum concentration of Cabergoline can be increased when it is combined with Phosphoramidon.Experimental
PimozideThe risk or severity of adverse effects can be increased when Cabergoline is combined with Pimozide.Approved
PindololPindolol may increase the vasoconstricting activities of Cabergoline.Approved
PipamperoneThe therapeutic efficacy of Pipamperone can be decreased when used in combination with Cabergoline.Approved
PipotiazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Pipotiazine.Approved
PirbuterolCabergoline may increase the hypertensive activities of Pirbuterol.Approved
PirlindoleThe metabolism of Cabergoline can be decreased when combined with Pirlindole.Approved
PivhydrazineThe metabolism of Cabergoline can be decreased when combined with Pivhydrazine.Withdrawn
PosaconazoleThe metabolism of Cabergoline can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PractololPractolol may increase the vasoconstricting activities of Cabergoline.Approved
PrimidoneThe metabolism of Cabergoline can be increased when combined with Primidone.Approved, Vet Approved
PrinomastatThe serum concentration of Cabergoline can be increased when it is combined with Prinomastat.Investigational
ProcarbazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Procarbazine.Approved
ProcaterolCabergoline may increase the hypertensive activities of Procaterol.Approved
ProchlorperazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Prochlorperazine.Approved, Vet Approved
PromazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Promazine.Approved, Vet Approved
PromethazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Promethazine.Approved
PropericiazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Propericiazine.Approved
PropranololPropranolol may increase the vasoconstricting activities of Cabergoline.Approved, Investigational
ProthipendylThe risk or severity of adverse effects can be increased when Cabergoline is combined with Prothipendyl.Investigational
ProtriptylineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Protriptyline.Approved
PRX-00023Cabergoline may increase the vasoconstricting activities of PRX-00023.Investigational
PseudoephedrineCabergoline may increase the hypertensive activities of Pseudoephedrine.Approved
QuetiapineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Quetiapine.Approved
QuinaprilThe serum concentration of Cabergoline can be increased when it is combined with Quinapril.Approved, Investigational
RacecadotrilThe serum concentration of Cabergoline can be increased when it is combined with Racecadotril.Investigational
RacepinephrineCabergoline may increase the hypertensive activities of Racepinephrine.Approved
RacloprideThe risk or severity of adverse effects can be increased when Cabergoline is combined with Raclopride.Investigational
RactopamineCabergoline may increase the hypertensive activities of Ractopamine.Vet Approved
RamiprilThe serum concentration of Cabergoline can be increased when it is combined with Ramipril.Approved
RanolazineThe metabolism of Cabergoline can be decreased when combined with Ranolazine.Approved, Investigational
RasagilineThe metabolism of Cabergoline can be decreased when combined with Rasagiline.Approved
RemikirenThe serum concentration of Cabergoline can be increased when it is combined with Remikiren.Approved
RemoxiprideThe risk or severity of adverse effects can be increased when Cabergoline is combined with Remoxipride.Approved, Withdrawn
ReserpineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Reserpine.Approved
RifabutinThe metabolism of Cabergoline can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Cabergoline can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Cabergoline can be increased when combined with Rifapentine.Approved
RilmenidineCabergoline may increase the hypertensive activities of Rilmenidine.Investigational
RisperidoneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Risperidone.Approved, Investigational
RitanserinThe risk or severity of adverse effects can be increased when Cabergoline is combined with Ritanserin.Investigational
RitobegronCabergoline may increase the hypertensive activities of Ritobegron.Investigational
RitodrineCabergoline may increase the hypertensive activities of Ritodrine.Approved
RitonavirThe serum concentration of Cabergoline can be increased when it is combined with Ritonavir.Approved, Investigational
RivaroxabanThe serum concentration of Cabergoline can be increased when it is combined with Rivaroxaban.Approved
RizatriptanCabergoline may increase the vasoconstricting activities of Rizatriptan.Approved
RomifidineCabergoline may increase the hypertensive activities of Romifidine.Vet Approved
RopiniroleCabergoline may increase the vasoconstricting activities of Ropinirole.Approved, Investigational
RoxithromycinThe serum concentration of Cabergoline can be increased when it is combined with Roxithromycin.Approved, Withdrawn
SafrazineThe metabolism of Cabergoline can be decreased when combined with Safrazine.Withdrawn
SalbutamolCabergoline may increase the hypertensive activities of Salbutamol.Approved, Vet Approved
SalmeterolCabergoline may increase the hypertensive activities of Salmeterol.Approved
SaquinavirThe serum concentration of Cabergoline can be increased when it is combined with Saquinavir.Approved, Investigational
SaxagliptinThe serum concentration of Cabergoline can be increased when it is combined with Saxagliptin.Approved
SelegilineThe metabolism of Cabergoline can be decreased when combined with Selegiline.Approved, Investigational, Vet Approved
SertindoleThe risk or severity of adverse effects can be increased when Cabergoline is combined with Sertindole.Approved, Withdrawn
SertralineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Sertraline.Approved
SildenafilThe metabolism of Cabergoline can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Cabergoline can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Cabergoline can be increased when it is combined with Simeprevir.Approved
SitagliptinThe serum concentration of Cabergoline can be increased when it is combined with Sitagliptin.Approved, Investigational
SolabegronCabergoline may increase the hypertensive activities of Solabegron.Investigational
SolithromycinThe serum concentration of Cabergoline can be increased when it is combined with Solithromycin.Investigational
SotalolSotalol may increase the vasoconstricting activities of Cabergoline.Approved
SpiraprilThe serum concentration of Cabergoline can be increased when it is combined with Spirapril.Approved
SR 58611Cabergoline may increase the hypertensive activities of SR 58611.Investigational
St. John's WortThe serum concentration of Cabergoline can be decreased when it is combined with St. John's Wort.Nutraceutical
StiripentolThe serum concentration of Cabergoline can be increased when it is combined with Stiripentol.Approved
SulfisoxazoleThe metabolism of Cabergoline can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SulpirideThe therapeutic efficacy of Sulpiride can be decreased when used in combination with Cabergoline.Approved
SumatriptanCabergoline may increase the vasoconstricting activities of Sumatriptan.Approved, Investigational
SynephrineCabergoline may increase the hypertensive activities of Synephrine.Experimental
TapentadolThe risk or severity of adverse effects can be increased when Cabergoline is combined with Tapentadol.Approved
Tedizolid PhosphateTedizolid Phosphate may increase the serotonergic activities of Cabergoline.Approved
TelaprevirThe serum concentration of Cabergoline can be increased when it is combined with Telaprevir.Approved
TelithromycinThe metabolism of Cabergoline can be decreased when combined with Telithromycin.Approved
TemocaprilThe serum concentration of Cabergoline can be increased when it is combined with Temocapril.Experimental, Investigational
TerbutalineCabergoline may increase the hypertensive activities of Terbutaline.Approved
ThioproperazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Thioproperazine.Approved
ThioridazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Thioridazine.Approved
ThiorphanThe serum concentration of Cabergoline can be increased when it is combined with Thiorphan.Experimental
ThiothixeneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Thiothixene.Approved
TiaprideThe risk or severity of adverse effects can be increased when Cabergoline is combined with Tiapride.Investigational
TiclopidineThe metabolism of Cabergoline can be decreased when combined with Ticlopidine.Approved
TimololTimolol may increase the vasoconstricting activities of Cabergoline.Approved
TipranavirThe serum concentration of Cabergoline can be increased when it is combined with Tipranavir.Approved, Investigational
TizanidineCabergoline may increase the hypertensive activities of Tizanidine.Approved
TocilizumabThe serum concentration of Cabergoline can be decreased when it is combined with Tocilizumab.Approved
ToloxatoneThe metabolism of Cabergoline can be decreased when combined with Toloxatone.Approved
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Cabergoline.Approved, Investigational
TrandolaprilThe serum concentration of Cabergoline can be increased when it is combined with Trandolapril.Approved
Trans-2-PhenylcyclopropylamineThe metabolism of Cabergoline can be decreased when combined with Trans-2-Phenylcyclopropylamine.Experimental
TranylcypromineThe metabolism of Cabergoline can be decreased when combined with Tranylcypromine.Approved
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Cabergoline.Approved, Investigational
TrazodoneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Trazodone.Approved, Investigational
TrifluoperazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Trifluoperazine.Approved
TriflupromazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Triflupromazine.Approved, Vet Approved
TrimipramineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Trimipramine.Approved
TroleandomycinThe serum concentration of Cabergoline can be increased when it is combined with Troleandomycin.Approved
TropisetronTropisetron may increase the serotonergic activities of Cabergoline.Investigational
TulobuterolCabergoline may increase the hypertensive activities of Tulobuterol.Investigational
TylosinThe serum concentration of Cabergoline can be increased when it is combined with Tylosin.Vet Approved
UbenimexThe serum concentration of Cabergoline can be increased when it is combined with Ubenimex.Experimental
UlinastatinThe serum concentration of Cabergoline can be increased when it is combined with Ulinastatin.Investigational
VenlafaxineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Venlafaxine.Approved
VerapamilThe metabolism of Cabergoline can be decreased when combined with Verapamil.Approved
VilazodoneCabergoline may increase the vasoconstricting activities of Vilazodone.Approved
VildagliptinThe serum concentration of Cabergoline can be increased when it is combined with Vildagliptin.Approved, Investigational
VoriconazoleThe metabolism of Cabergoline can be decreased when combined with Voriconazole.Approved, Investigational
VortioxetineCabergoline may increase the vasoconstricting activities of Vortioxetine.Approved
XimelagatranThe serum concentration of Cabergoline can be increased when it is combined with Ximelagatran.Approved, Investigational, Withdrawn
XylazineCabergoline may increase the hypertensive activities of Xylazine.Vet Approved
YM-178Cabergoline may increase the hypertensive activities of YM-178.Investigational
Ym150The serum concentration of Cabergoline can be increased when it is combined with Ym150.Investigational
ZiprasidoneThe metabolism of Cabergoline can be decreased when combined with Ziprasidone.Approved
ZolmitriptanCabergoline may increase the vasoconstricting activities of Zolmitriptan.Approved, Investigational
ZotepineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Zotepine.Approved
ZuclopenthixolThe risk or severity of adverse effects can be increased when Cabergoline is combined with Zuclopenthixol.Approved, Investigational
Food Interactions
  • Absorption is not affected by food.
  • Take with food to improve tolerance.
References
Synthesis Reference

DrugSyn.org

US4526892
General References
  1. Pastor P, Tolosa E: [Cabergoline in the treatment of Parkinson's disease]. Neurologia. 2003 May;18(4):202-9. [PubMed:12721865 ]
  2. Curran MP, Perry CM: Cabergoline : a review of its use in the treatment of Parkinson's disease. Drugs. 2004;64(18):2125-41. [PubMed:15341508 ]
  3. Bracco F, Battaglia A, Chouza C, Dupont E, Gershanik O, Marti Masso JF, Montastruc JL: The long-acting dopamine receptor agonist cabergoline in early Parkinson's disease: final results of a 5-year, double-blind, levodopa-controlled study. CNS Drugs. 2004;18(11):733-46. [PubMed:15330687 ]
  4. Miyagi M, Arai N, Taya F, Itoh F, Komatsu Y, Kojima M, Isaji M: Effect of cabergoline, a long-acting dopamine D2 agonist, on reserpine-treated rodents. Biol Pharm Bull. 1996 Nov;19(11):1499-502. [PubMed:8951172 ]
External Links
ATC CodesN04BC06G02CB03
AHFS Codes
  • 28:36.20.04
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9383
Caco-2 permeable-0.6583
P-glycoprotein substrateSubstrate0.7972
P-glycoprotein inhibitor IInhibitor0.8903
P-glycoprotein inhibitor IIInhibitor0.7698
Renal organic cation transporterNon-inhibitor0.5339
CYP450 2C9 substrateNon-substrate0.812
CYP450 2D6 substrateNon-substrate0.7438
CYP450 3A4 substrateSubstrate0.6336
CYP450 1A2 substrateNon-inhibitor0.7733
CYP450 2C9 inhibitorNon-inhibitor0.7396
CYP450 2D6 inhibitorNon-inhibitor0.7124
CYP450 2C19 inhibitorNon-inhibitor0.8341
CYP450 3A4 inhibitorNon-inhibitor0.6476
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8712
Ames testNon AMES toxic0.5619
CarcinogenicityNon-carcinogens0.8542
BiodegradationNot ready biodegradable0.846
Rat acute toxicity2.8786 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.6224
hERG inhibition (predictor II)Non-inhibitor0.5309
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Impax laboratories inc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Par pharmaceutical inc
  • Watson laboratories inc
  • Pharmacia and upjohn co
Packagers
Dosage forms
FormRouteStrength
TabletOral.5 mg/1
TabletOral0.5 mg
Prices
Unit descriptionCostUnit
Cabergoline 0.5 mg tablet37.39USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point102-104 °CNot Available
water solubilityInsolubleNot Available
logP2.6Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.064 mg/mLALOGPS
logP2.97ALOGPS
logP2.58ChemAxon
logS-3.9ALOGPS
pKa (Strongest Acidic)15.25ChemAxon
pKa (Strongest Basic)9.32ChemAxon
Physiological Charge2ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area71.68 Å2ChemAxon
Rotatable Bond Count8ChemAxon
Refractivity133.5 m3·mol-1ChemAxon
Polarizability52.5 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as lysergic acids and derivatives. These are alkaloids with a structure based on the lysergic acid skeleton.
KingdomOrganic compounds
Super ClassAlkaloids and derivatives
ClassErgoline and derivatives
Sub ClassLysergic acids and derivatives
Direct ParentLysergic acids and derivatives
Alternative Parents
Substituents
  • Lysergic acid or derivatives
  • Indoloquinoline
  • Benzoquinoline
  • Quinoline-3-carboxamide
  • Pyrroloquinoline
  • Quinoline
  • Piperidinecarboxylic acid
  • Piperidinecarboxamide
  • 3-piperidinecarboxamide
  • Isoindole or derivatives
  • Indole or derivatives
  • Indole
  • Aralkylamine
  • Ureide
  • Benzenoid
  • Piperidine
  • Heteroaromatic compound
  • Pyrrole
  • Urea
  • Tertiary aliphatic amine
  • Tertiary amine
  • Carboxamide group
  • Azacycle
  • Organoheterocyclic compound
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Potassium channel regulator activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name:
DRD2
Uniprot ID:
P14416
Molecular Weight:
50618.91 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Lombardi G, Varsaldi F, Miglio G, Papini MG, Battaglia A, Canonico PL: Cabergoline prevents necrotic neuronal death in an in vitro model of oxidative stress. Eur J Pharmacol. 2002 Dec 20;457(2-3):95-8. [PubMed:12464354 ]
  3. Kageyama K, Nigawara T, Kamata Y, Takahashi T, Anzai J, Suzuki S, Osamura YR, Suda T: A case of macroprolactinoma with subclinical growth hormone production. Endocr J. 2002 Feb;49(1):41-7. [PubMed:12008749 ]
  4. Pastor P, Tolosa E: [Cabergoline in the treatment of Parkinson's disease]. Neurologia. 2003 May;18(4):202-9. [PubMed:12721865 ]
  5. Curran MP, Perry CM: Cabergoline : a review of its use in the treatment of Parkinson's disease. Drugs. 2004;64(18):2125-41. [PubMed:15341508 ]
  6. Miyagi M, Arai N, Taya F, Itoh F, Komatsu Y, Kojima M, Isaji M: Effect of cabergoline, a long-acting dopamine D2 agonist, on reserpine-treated rodents. Biol Pharm Bull. 1996 Nov;19(11):1499-502. [PubMed:8951172 ]
  7. Ichikawa K, Kojima M: [Pharmacological effects of cabergoline against parkinsonism]. Nihon Yakurigaku Zasshi. 2001 Jun;117(6):395-400. [PubMed:11436517 ]
  8. Linazasoro G: Conversion from dopamine agonists to cabergoline: an open-label trial in 128 patients with advanced Parkinson disease. Clin Neuropharmacol. 2008 Jan-Feb;31(1):19-24. doi: 10.1097/wnf.0b013e318067bcc4. [PubMed:18303487 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various ergot alkaloid derivatives and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Beta-arrestin family members inhibit signaling via G proteins ...
Gene Name:
HTR2B
Uniprot ID:
P41595
Molecular Weight:
54297.41 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132 ]
  2. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
  3. Sharif NA: Serotonin-2 receptor agonists as novel ocular hypotensive agents and their cellular and molecular mechanisms of action. Curr Drug Targets. 2010 Aug;11(8):978-93. [PubMed:20426763 ]
  4. Sharif NA, McLaughlin MA, Kelly CR, Katoli P, Drace C, Husain S, Crosson C, Toris C, Zhan GL, Camras C: Cabergoline: Pharmacology, ocular hypotensive studies in multiple species, and aqueous humor dynamic modulation in the Cynomolgus monkey eyes. Exp Eye Res. 2009 Mar;88(3):386-97. doi: 10.1016/j.exer.2008.10.003. Epub 2008 Nov 1. [PubMed:18992242 ]
  5. Huang XP, Setola V, Yadav PN, Allen JA, Rogan SC, Hanson BJ, Revankar C, Robers M, Doucette C, Roth BL: Parallel functional activity profiling reveals valvulopathogens are potent 5-hydroxytryptamine(2B) receptor agonists: implications for drug safety assessment. Mol Pharmacol. 2009 Oct;76(4):710-22. doi: 10.1124/mol.109.058057. Epub 2009 Jul 1. [PubMed:19570945 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
G-protein coupled amine receptor activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.
Gene Name:
DRD3
Uniprot ID:
P35462
Molecular Weight:
44224.335 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132 ]
  2. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
  3. Sharif NA, McLaughlin MA, Kelly CR, Katoli P, Drace C, Husain S, Crosson C, Toris C, Zhan GL, Camras C: Cabergoline: Pharmacology, ocular hypotensive studies in multiple species, and aqueous humor dynamic modulation in the Cynomolgus monkey eyes. Exp Eye Res. 2009 Mar;88(3):386-97. doi: 10.1016/j.exer.2008.10.003. Epub 2008 Nov 1. [PubMed:18992242 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Virus receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates...
Gene Name:
HTR2A
Uniprot ID:
P28223
Molecular Weight:
52602.58 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132 ]
  2. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
  3. Sharif NA: Serotonin-2 receptor agonists as novel ocular hypotensive agents and their cellular and molecular mechanisms of action. Curr Drug Targets. 2010 Aug;11(8):978-93. [PubMed:20426763 ]
  4. Sharif NA, McLaughlin MA, Kelly CR, Katoli P, Drace C, Husain S, Crosson C, Toris C, Zhan GL, Camras C: Cabergoline: Pharmacology, ocular hypotensive studies in multiple species, and aqueous humor dynamic modulation in the Cynomolgus monkey eyes. Exp Eye Res. 2009 Mar;88(3):386-97. doi: 10.1016/j.exer.2008.10.003. Epub 2008 Nov 1. [PubMed:18992242 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Epinephrine binding
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine > norepinephrine > epinephrine = oxymetazoline > dopamine > p-tyramine = phenylephrine > serotonin > p-synephrine / p-octopamine. For antagonists, the rank order is yohimbine > chlorpromazine > phent...
Gene Name:
ADRA2B
Uniprot ID:
P18089
Molecular Weight:
49565.8 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132 ]
  2. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
  3. Sharif NA, McLaughlin MA, Kelly CR, Katoli P, Drace C, Husain S, Crosson C, Toris C, Zhan GL, Camras C: Cabergoline: Pharmacology, ocular hypotensive studies in multiple species, and aqueous humor dynamic modulation in the Cynomolgus monkey eyes. Exp Eye Res. 2009 Mar;88(3):386-97. doi: 10.1016/j.exer.2008.10.003. Epub 2008 Nov 1. [PubMed:18992242 ]
  4. Newman-Tancredi A, Cussac D, Audinot V, Nicolas JP, De Ceuninck F, Boutin JA, Millan MJ: 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. J Pharmacol Exp Ther. 2002 Nov;303(2):805-14. [PubMed:12388667 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate c...
Gene Name:
HTR1D
Uniprot ID:
P28221
Molecular Weight:
41906.38 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132 ]
  2. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Sh3 domain binding
Specific Function:
Dopamine receptor responsible for neuronal signaling in the mesolimbic system of the brain, an area of the brain that regulates emotion and complex behavior. Its activity is mediated by G proteins which inhibit adenylyl cyclase. Modulates the circadian rhythm of contrast sensitivity by regulating the rhythmic expression of NPAS2 in the retinal ganglion cells (By similarity).
Gene Name:
DRD4
Uniprot ID:
P21917
Molecular Weight:
48359.86 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132 ]
  2. Newman-Tancredi A, Cussac D, Audinot V, Nicolas JP, De Ceuninck F, Boutin JA, Millan MJ: 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. J Pharmacol Exp Ther. 2002 Nov;303(2):805-14. [PubMed:12388667 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Thioesterase binding
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianser...
Gene Name:
ADRA2A
Uniprot ID:
P08913
Molecular Weight:
48956.275 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132 ]
  2. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
  3. Newman-Tancredi A, Cussac D, Audinot V, Nicolas JP, De Ceuninck F, Boutin JA, Millan MJ: 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. J Pharmacol Exp Ther. 2002 Nov;303(2):805-14. [PubMed:12388667 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Beta-arrestin family members inhibit signaling via G pro...
Gene Name:
HTR1A
Uniprot ID:
P08908
Molecular Weight:
46106.335 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132 ]
  2. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
  3. Sharif NA, McLaughlin MA, Kelly CR, Katoli P, Drace C, Husain S, Crosson C, Toris C, Zhan GL, Camras C: Cabergoline: Pharmacology, ocular hypotensive studies in multiple species, and aqueous humor dynamic modulation in the Cynomolgus monkey eyes. Exp Eye Res. 2009 Mar;88(3):386-97. doi: 10.1016/j.exer.2008.10.003. Epub 2008 Nov 1. [PubMed:18992242 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Protein homodimerization activity
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins.
Gene Name:
ADRA2C
Uniprot ID:
P18825
Molecular Weight:
49521.585 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132 ]
  2. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
  3. Newman-Tancredi A, Cussac D, Audinot V, Nicolas JP, De Ceuninck F, Boutin JA, Millan MJ: 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. J Pharmacol Exp Ther. 2002 Nov;303(2):805-14. [PubMed:12388667 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
G-protein coupled amine receptor activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
Gene Name:
DRD5
Uniprot ID:
P21918
Molecular Weight:
52950.5 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132 ]
  2. Kvernmo T, Hartter S, Burger E: A review of the receptor-binding and pharmacokinetic properties of dopamine agonists. Clin Ther. 2006 Aug;28(8):1065-78. [PubMed:16982285 ]
  3. Ichikawa K, Kojima M: [Pharmacological effects of cabergoline against parkinsonism]. Nihon Yakurigaku Zasshi. 2001 Jun;117(6):395-400. [PubMed:11436517 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
G-protein coupled amine receptor activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
Gene Name:
DRD1
Uniprot ID:
P21728
Molecular Weight:
49292.765 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132 ]
  2. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
  3. Kvernmo T, Hartter S, Burger E: A review of the receptor-binding and pharmacokinetic properties of dopamine agonists. Clin Ther. 2006 Aug;28(8):1065-78. [PubMed:16982285 ]
  4. Ichikawa K, Kojima M: [Pharmacological effects of cabergoline against parkinsonism]. Nihon Yakurigaku Zasshi. 2001 Jun;117(6):395-400. [PubMed:11436517 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances, such as lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of ...
Gene Name:
HTR1B
Uniprot ID:
P28222
Molecular Weight:
43567.535 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132 ]
  2. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-iodophenyl-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modul...
Gene Name:
HTR2C
Uniprot ID:
P28335
Molecular Weight:
51820.705 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132 ]
  2. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
  3. Sharif NA: Serotonin-2 receptor agonists as novel ocular hypotensive agents and their cellular and molecular mechanisms of action. Curr Drug Targets. 2010 Aug;11(8):978-93. [PubMed:20426763 ]
  4. Sharif NA, McLaughlin MA, Kelly CR, Katoli P, Drace C, Husain S, Crosson C, Toris C, Zhan GL, Camras C: Cabergoline: Pharmacology, ocular hypotensive studies in multiple species, and aqueous humor dynamic modulation in the Cynomolgus monkey eyes. Exp Eye Res. 2009 Mar;88(3):386-97. doi: 10.1016/j.exer.2008.10.003. Epub 2008 Nov 1. [PubMed:18992242 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that stimulate adenylate cyclase.
Gene Name:
HTR7
Uniprot ID:
P34969
Molecular Weight:
53554.43 Da
References
  1. Sharif NA, McLaughlin MA, Kelly CR, Katoli P, Drace C, Husain S, Crosson C, Toris C, Zhan GL, Camras C: Cabergoline: Pharmacology, ocular hypotensive studies in multiple species, and aqueous humor dynamic modulation in the Cynomolgus monkey eyes. Exp Eye Res. 2009 Mar;88(3):386-97. doi: 10.1016/j.exer.2008.10.003. Epub 2008 Nov 1. [PubMed:18992242 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Protein heterodimerization activity
Specific Function:
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine(PE)-stimulated ERK signaling in cardiac myocytes.
Gene Name:
ADRA1A
Uniprot ID:
P35348
Molecular Weight:
51486.005 Da
References
  1. Millan MJ, Maiofiss L, Cussac D, Audinot V, Boutin JA, Newman-Tancredi A: 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. J Pharmacol Exp Ther. 2002 Nov;303(2):791-804. [PubMed:12388666 ]
  2. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Protein heterodimerization activity
Specific Function:
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine (PE)-stimulated ERK signaling in cardiac myocytes.
Gene Name:
ADRA1B
Uniprot ID:
P35368
Molecular Weight:
56835.375 Da
References
  1. Millan MJ, Maiofiss L, Cussac D, Audinot V, Boutin JA, Newman-Tancredi A: 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. J Pharmacol Exp Ther. 2002 Nov;303(2):791-804. [PubMed:12388666 ]
  2. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Alpha1-adrenergic receptor activity
Specific Function:
This alpha-adrenergic receptor mediates its effect through the influx of extracellular calcium.
Gene Name:
ADRA1D
Uniprot ID:
P25100
Molecular Weight:
60462.205 Da
References
  1. Millan MJ, Maiofiss L, Cussac D, Audinot V, Boutin JA, Newman-Tancredi A: 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. J Pharmacol Exp Ther. 2002 Nov;303(2):791-804. [PubMed:12388666 ]
  2. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Receptor signaling protein activity
Specific Function:
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximately equal affinity. Mediates Ras activation through G(s)-alpha- and cAMP-mediated signaling.
Gene Name:
ADRB1
Uniprot ID:
P08588
Molecular Weight:
51322.1 Da
References
  1. Millan MJ, Maiofiss L, Cussac D, Audinot V, Boutin JA, Newman-Tancredi A: 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. J Pharmacol Exp Ther. 2002 Nov;303(2):791-804. [PubMed:12388666 ]
  2. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Protein homodimerization activity
Specific Function:
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. The beta-2-adrenergic receptor binds epinephrine with an approximately 30-fold greater affinity than it does norepinephrine.
Gene Name:
ADRB2
Uniprot ID:
P07550
Molecular Weight:
46458.32 Da
References
  1. Millan MJ, Maiofiss L, Cussac D, Audinot V, Boutin JA, Newman-Tancredi A: 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. J Pharmacol Exp Ther. 2002 Nov;303(2):791-804. [PubMed:12388666 ]
  2. PDSP Ki Database [Link]
Kind
Protein group
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
G-protein coupled amine receptor activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
Components:
NameUniProt IDDetails
D(1A) dopamine receptorP21728 Details
D(1B) dopamine receptorP21918 Details
References
  1. Millan MJ, Maiofiss L, Cussac D, Audinot V, Boutin JA, Newman-Tancredi A: 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. J Pharmacol Exp Ther. 2002 Nov;303(2):791-804. [PubMed:12388666 ]
  2. PDSP Ki Database [Link]
22. D(2S) dopamine receptor
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
References
  1. Millan MJ, Maiofiss L, Cussac D, Audinot V, Boutin JA, Newman-Tancredi A: 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. J Pharmacol Exp Ther. 2002 Nov;303(2):791-804. [PubMed:12388666 ]
  2. PDSP Ki Database [Link]
23. D(2L) dopamine receptor
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
References
  1. Millan MJ, Maiofiss L, Cussac D, Audinot V, Boutin JA, Newman-Tancredi A: 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. J Pharmacol Exp Ther. 2002 Nov;303(2):791-804. [PubMed:12388666 ]
  2. PDSP Ki Database [Link]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23