Description

Simple

A medication used to treat high levels of a hormone called prolactin, which can cause infertility and other serious health conditions.

Clinical

A dopamine receptor agonist used for the treatment of hyperprolactinemic conditions due to various causes.

Overview

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.

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... Read more

Pharmacodynamic

Cabergoline 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... Read more

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... Read more

Absorption

First-pass effect is seen, however the absolute bioavailability is unknown.

Protein binding

Moderately bound (40% to 42%) to human plasma proteins in a concentration-independent manner.

Volume of distribution

Information currently not available.

Clearance

renal cl=0,008 L/minnonrenal cl=3.2 L/min

Half life

The elimination half-life is estimated from urinary data of 12 healthy subjects to range between 63 to 69 hours.

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.

Toxicity

Overdosage might be expected to produce nasal congestion, syncope, or hallucinations.

Adverse Effects

Contraindications

  • Regions: US
  • Patient Conditions:
      • Name: History of pericardial fibrosis
      • Drugbank Id: DBCOND0107529
  • Regions: US
  • Patient Conditions:
      • Name: History of retroperitoneal fibrosis
      • Drugbank Id: DBCOND0107530
  • Regions: US
  • Patient Conditions:
      • Name: History of cardiac valvular disorders
      • Drugbank Id: DBCOND0107527
  • Regions: US
  • Patient Conditions:
      • Name: History of pulmonary fibrosis
      • Drugbank Id: DBCOND0107528
  • Regions: US
  • Patient Conditions:
      • Name: Uncontrolled Hypertension
      • Drugbank Id: DBCOND0043537

Food Interactions

  • Take with food. Although absorption is not affected by food, food reduces irritation.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The serum concentration of (R)-warfarin can be increased when it is combined with Cabergoline.
(S)-Warfarin
The serum concentration of (S)-Warfarin can be increased when it is combined with Cabergoline.
1-benzylimidazole
The risk or severity of hypertension can be increased when Cabergoline is combined with 1-benzylimidazole.
2,5-Dimethoxy-4-ethylamphetamine
The risk or severity of serotonin syndrome can be increased when Cabergoline is combined with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamine
The risk or severity of adverse effects can be increased when Cabergoline is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
4-Bromo-2,5-dimethoxyamphetamine
The risk or severity of adverse effects can be increased when Cabergoline is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-Bromo-2,5-dimethoxyphenethylamine
Cabergoline may increase the hypertensive and vasoconstricting activities of 4-Bromo-2,5-dimethoxyphenethylamine.
4-hydroxycoumarin
The metabolism of 4-hydroxycoumarin can be decreased when combined with Cabergoline.
4-Methoxyamphetamine
Cabergoline may increase the hypertensive and vasoconstricting activities of 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamine
Cabergoline may increase the vasoconstricting activities of 5-methoxy-N,N-dimethyltryptamine.
6-Deoxyerythronolide B
The serum concentration of Cabergoline can be increased when it is combined with 6-Deoxyerythronolide B.
7-Nitroindazole
The risk or severity of adverse effects can be increased when Cabergoline is combined with 7-Nitroindazole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
The metabolism of Cabergoline can be decreased when combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
9-aminocamptothecin
The metabolism of 9-aminocamptothecin can be decreased when combined with Cabergoline.
Abediterol
Cabergoline may increase the hypertensive and vasoconstricting activities of Abediterol.
Acebutolol
Acebutolol may increase the vasoconstricting activities of Cabergoline.
Aceclofenac
The risk or severity of hypertension can be increased when Cabergoline is combined with Aceclofenac.
Acemetacin
The risk or severity of hypertension can be increased when Cabergoline is combined with Acemetacin.
Acenocoumarol
The serum concentration of Acenocoumarol can be increased when it is combined with Cabergoline.
Acepromazine
The risk or severity of adverse effects can be increased when Cabergoline is combined with Acepromazine.
4 References
  1. 1 . Pastor P, Tolosa E: [Cabergoline in the treatment of Parkinson's disease]. Neurologia. 2003 May;18(4):202-9.PubMed: 12721865
  2. 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. 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. 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