Detail

Cabergoline

Description

Name: Cabergoline
Type: small molecule
Groups: approved
Indication: For 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.
Accession Number: DB00248 ( APRD00836)
Description: Cabergoline, 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:
Prescription Products:
NameDosageStrengthRouteMarketing StartMarketing EndCountry
Act Cabergolinetablet0.5 mgoral06-11-2007Canada
Cabergolinetablet0.5 mgoral01-01-1970Canada
Cabergolinetablet.5 mg/1oral22-09-2014US
Dostinextablet0.5 mgoral30-06-2000Canada

Generic Prescription Products:
NameDosageStrengthRouteMarketing StartMarketing EndCountry
Cabergolinetablet.5 mg/1oral02-12-2013US
Cabergolinetablet.5 mg/1oral21-04-2008US
Cabergolinetablet.5 mg/1oral07-03-2007US
Cabergolinetablet.5 mg/1oral08-03-2013US
Cabergolinetablet.5 mg/1oral14-04-2015US
Cabergolinetablet.5 mg/1oral29-12-2005US

Over the Counter Products: Not Available
International Brands
  • No Brands

Brand Names
  • No Brands

Brand Mixtures
Brand NameIngredients
CabergolineCabergoline
CabergolineCabergoline
CabergolineCabergoline
CabergolineCabergoline
CabergolineCabergoline
CabergolineCabergoline
CabergolineCabergoline
DostinexCabergoline
Act CabergolineCabergoline
CabergolineCabergoline

Categories
  • Antineoplastic Agents
  • Antiparkinson Agents
  • Dopamine Agonists
  • Ergot Derivatives

Pharmacology

Indication: For 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.
Pharmacodynamics: Not Available
Mechanism of action: The 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.
Absorption: First-pass effect is seen, however the absolute bioavailability is unknown.
Volume of distribution: Not Available
Protein binding: Moderately bound (40% to 42%) to human plasma proteins in a concentration-independent manner.
Metabolism: Not Available
Route of elimination: After 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 life: The elimination half-life is estimated from urinary data of 12 healthy subjects to range between 63 to 69 hours.
Clearance: Not Available
Toxicity: Overdosage might be expected to produce nasal congestion, syncope, or hallucinations.
Affected organisms
  • Not Available

SNP Mediated Adverse Drug Reactions
  • Not Available

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 tablet$37.39tablet

Patents
CountryPatent NumberApprovedExpires (estimated)

Interactions

Drug Interactions
DrugInteraction
AcebutololAcebutolol may increase the vasoconstricting activities of Cabergoline.
AcepromazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Acepromazine.
AcetophenazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Acetophenazine.
AlmotriptanCabergoline may increase the vasoconstricting activities of Almotriptan.
AmisulprideThe therapeutic efficacy of Amisulpride can be decreased when used in combination with Cabergoline.
AripiprazoleThe risk or severity of adverse effects can be increased when Cabergoline is combined with Aripiprazole.
ArticaineCabergoline may increase the hypertensive activities of Articaine.
AtenololAtenolol may increase the vasoconstricting activities of Cabergoline.
BendroflumethiazideBendroflumethiazide may increase the vasoconstricting activities of Cabergoline.
BenzquinamideThe risk or severity of adverse effects can be increased when Cabergoline is combined with Benzquinamide.
BetaxololBetaxolol may increase the vasoconstricting activities of Cabergoline.
BisoprololBisoprolol may increase the vasoconstricting activities of Cabergoline.
CarphenazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Carphenazine.
CarteololCarteolol may increase the vasoconstricting activities of Cabergoline.
CarvedilolCarvedilol may increase the vasoconstricting activities of Cabergoline.
ChlormezanoneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Chlormezanone.
ChlorpromazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Chlorpromazine.
ChlorprothixeneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Chlorprothixene.
ClarithromycinThe serum concentration of Cabergoline can be increased when it is combined with Clarithromycin.
ClozapineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Clozapine.
DapoxetineThe risk or severity of adverse effects can be increased when Dapoxetine is combined with Cabergoline.
DipivefrinCabergoline may increase the hypertensive activities of Dipivefrin.
DopamineCabergoline may increase the hypertensive activities of Dopamine.
DroperidolThe risk or severity of adverse effects can be increased when Cabergoline is combined with Droperidol.
EletriptanCabergoline may increase the vasoconstricting activities of Eletriptan.
EphedrineCabergoline may increase the hypertensive activities of Ephedrine.
EpinephrineCabergoline may increase the hypertensive activities of Epinephrine.
EsmololEsmolol may increase the vasoconstricting activities of Cabergoline.
FencamfamineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Fencamfamine.
FlupentixolThe risk or severity of adverse effects can be increased when Cabergoline is combined with Flupentixol.
FluphenazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Fluphenazine.
FluspirileneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Fluspirilene.
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Cabergoline.
FrovatriptanCabergoline may increase the vasoconstricting activities of Frovatriptan.
GranisetronGranisetron may increase the serotonergic activities of Cabergoline.
HaloperidolThe risk or severity of adverse effects can be increased when Cabergoline is combined with Haloperidol.
LabetalolLabetalol may increase the vasoconstricting activities of Cabergoline.
LevobunololLevobunolol may increase the vasoconstricting activities of Cabergoline.
LevonordefrinCabergoline may increase the hypertensive activities of Levonordefrin.
LorcaserinThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Cabergoline.
LoxapineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Loxapine.
MepivacaineCabergoline may increase the hypertensive activities of Mepivacaine.
MesoridazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Mesoridazine.
MethotrimeprazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Methotrimeprazine.
MetipranololMetipranolol may increase the vasoconstricting activities of Cabergoline.
MetoclopramideThe risk or severity of adverse effects can be increased when Cabergoline is combined with Metoclopramide.
MetoprololMetoprolol may increase the vasoconstricting activities of Cabergoline.
MidodrineCabergoline may increase the hypertensive activities of Midodrine.
MolindoneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Molindone.
NadololNadolol may increase the vasoconstricting activities of Cabergoline.
NaphazolineCabergoline may increase the hypertensive activities of Naphazoline.
NaratriptanCabergoline may increase the vasoconstricting activities of Naratriptan.
NebivololNebivolol may increase the vasoconstricting activities of Cabergoline.
NitroglycerinCabergoline may decrease the vasodilatory activities of Nitroglycerin.
NorepinephrineCabergoline may increase the hypertensive activities of Norepinephrine.
OlanzapineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Olanzapine.
OndansetronThe risk or severity of adverse effects can be increased when Cabergoline is combined with Ondansetron.
OxymetazolineCabergoline may increase the hypertensive activities of Oxymetazoline.
PaliperidoneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Paliperidone.
PenbutololPenbutolol may increase the vasoconstricting activities of Cabergoline.
PerphenazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Perphenazine.
PhenelzinePhenelzine may increase the orthostatic hypotensive activities of Cabergoline.
PheniramineCabergoline may increase the hypertensive activities of Pheniramine.
PhenylephrineCabergoline may increase the hypertensive activities of Phenylephrine.
PimozideThe risk or severity of adverse effects can be increased when Cabergoline is combined with Pimozide.
PindololPindolol may increase the vasoconstricting activities of Cabergoline.
PipamperoneThe therapeutic efficacy of Pipamperone can be decreased when used in combination with Cabergoline.
PiperacetazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Piperacetazine.
ProchlorperazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Prochlorperazine.
PromazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Promazine.
PropranololPropranolol may increase the vasoconstricting activities of Cabergoline.
PropylhexedrineCabergoline may increase the hypertensive activities of Propylhexedrine.
PseudoephedrineCabergoline may increase the hypertensive activities of Pseudoephedrine.
QuetiapineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Quetiapine.
RacepinephrineCabergoline may increase the hypertensive activities of Racepinephrine.
RemoxiprideThe risk or severity of adverse effects can be increased when Cabergoline is combined with Remoxipride.
ReserpineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Reserpine.
RisperidoneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Risperidone.
RizatriptanCabergoline may increase the vasoconstricting activities of Rizatriptan.
SertindoleThe risk or severity of adverse effects can be increased when Cabergoline is combined with Sertindole.
SotalolSotalol may increase the vasoconstricting activities of Cabergoline.
SulpirideThe therapeutic efficacy of Sulpiride can be decreased when used in combination with Cabergoline.
SumatriptanCabergoline may increase the vasoconstricting activities of Sumatriptan.
Tedizolid PhosphateTedizolid Phosphate may increase the serotonergic activities of Cabergoline.
ThioridazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Thioridazine.
ThiothixeneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Thiothixene.
TimololTimolol may increase the vasoconstricting activities of Cabergoline.
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Cabergoline.
TranylcypromineTranylcypromine may increase the orthostatic hypotensive activities of Cabergoline.
TrifluoperazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Trifluoperazine.
TriflupromazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Triflupromazine.
TriprolidineCabergoline may increase the hypertensive activities of Triprolidine.
ZiprasidoneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Ziprasidone.
ZolmitriptanCabergoline may increase the vasoconstricting activities of Zolmitriptan.
ZuclopenthixolThe risk or severity of adverse effects can be increased when Cabergoline is combined with Zuclopenthixol.

Food Interactions:
  • Absorption is not affected by food.
  • Take with food to improve tolerance.

Taxonomy

Kingdom: Organic compounds
Super Class: Not Available
Class: Not Available
Sub Class: Not Available
Direct Parent: Not Available
Alternative Parents:
  • Aralkylamines
  • Azacyclic compounds
  • Benzenoids
  • Benzoquinolines
  • Carbonyl compounds
  • Carboxylic acid amides
  • Heteroaromatic compounds
  • Hydrocarbon derivatives
  • Indoles
  • Indoloquinolines
  • Isoindoles and derivatives
  • Piperidinecarboxamides
  • Piperidinecarboxylic acids
  • Pyrroles
  • Pyrroloquinolines
  • Quinoline-3-carboxamides
  • Trialkylamines
  • Ureides

substituent:
  • 3-piperidinecarboxamide
  • Amine
  • Aralkylamine
  • Aromatic heteropolycyclic compound
  • Azacycle
  • Benzenoid
  • Benzoquinoline
  • Carbonyl group
  • Carboxamide group
  • Carboxylic acid derivative
  • Heteroaromatic compound
  • Hydrocarbon derivative
  • Indole
  • Indole or derivatives
  • Indoloquinoline
  • Isoindole or derivatives
  • Lysergic acid or derivatives
  • Organoheterocyclic compound
  • Organonitrogen compound
  • Organooxygen compound
  • Piperidine
  • Piperidinecarboxamide
  • Piperidinecarboxylic acid
  • Pyrrole
  • Pyrroloquinoline
  • Quinoline
  • Quinoline-3-carboxamide
  • Tertiary aliphatic amine
  • Tertiary amine
  • Urea
  • Ureide

References

Synthesis Reference: "DrugSyn.org":http://www.drugsyn.org/Cabergoline.htm
General Reference: # Pastor P, Tolosa E: [Cabergoline in the treatment of Parkinson's disease] Neurologia. 2003 May;18(4):202-9. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/12721865 # Curran MP, Perry CM: Cabergoline : a review of its use in the treatment of Parkinson's disease. Drugs. 2004;64(18):2125-41. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15341508 # 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":http://www.ncbi.nlm.nih.gov/pubmed/15330687 # 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":http://www.ncbi.nlm.nih.gov/pubmed/8951172
External Links:
ResourceLink
RxListhttp://www.rxlist.com/cgi/generic/cabergoline.htm
Drugs.comhttp://www.drugs.com/cdi/cabergoline.html

ATC Codes:
  • Array
  • Array

AHFS Codes:
  • 28:36.20.04

MSDS: Download

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