Overview
| Generic Names: | Cabergolina [Spanish]; Cabergolinum [Latin] |
|---|---|
| Trade Names: | Cabaser; Dostinex |
| PharmGKB Accession Id: | PA448708 |
Description
Cabergoline, a lysergic acid amide derivative, is a potent dopamine receptor agonist on D2 receptors. It also acts on dopamine receptors in lactophilic hypothalamus cells to suppress prolactin production in the pituitary gland. It is frequently used as a second-line agent in the management of prolactinomas when bromocriptine is ineffective. Wikipedia (source: Drug Bank)
Indication
For the treatment of hyperprolactinemic disorders, either idiopathic or due to pituitary adenomas. (source: Drug Bank)
ATC Therapeutic Categories
- G02CB:Prolactine inhibitors
- N04BC:Dopamine agonists
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
The secretion of prolactin by the anterior pituitary is mainly under hypothalmic inhibitory control, likely exerted through release of dopamine by tuberoinfundibular neurons. Cabergoline is a long-acting dopamine receptor agonist with a high affinity for D2 receptors. Results of in vitro studies demonstrate that cabergoline exerts a direct inhibitory effect on the secretion of prolactin by rat pituitary lactotrophs. Cabergoline decreased serum prolactin levels in reserpinized rats. Receptor-binding studies indicate that cabergoline has low affinity for dopamine D1, α<sub>1</sub>,- and α<sub>2</sub>- adrenergic, and 5-HT<sub>1</sub>- and 5-HT<sub>2</sub>-serotonin receptors. (source: Drug Bank)
Pharmacology
Cabergoline is a dopamine receptor agonist and uncategorized drug which suppresses the production of prolactin in pituitary gland. It is an ergot-derivative. It has at times been used as an adjunct to SSRI antidepressants as there is some evidence that it counteracts certain side effects of those drugs such as reduced libido and anorgasmia. It also has been suggested online that it has a possible recreational use in reducing or eliminating the male refractory period. (source: Drug Bank)
Food Interactions
Absorption is not affected by food.
Take with food to improve tolerance.
(source:
Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Hepatic. Cabergoline is extensively metabolized, predominately via hydrolysis of the acylurea bond or the urea moiety. Cytochrome P-450 mediated metabolism appears to be minimal. (source: Drug Bank)
Protein Binding
Moderately bound (40% to 42%) to human plasma proteins in a concentration-independent manner. (source: Drug Bank)
Absorption
First-pass effect is seen, however the absolute bioavailability is unknown. (source: Drug Bank)
Toxicity
Overdosage might be expected to produce nasal congestion, syncope, or hallucinations. (source: Drug Bank)
Isomeric SMILES Code:
CCNC(=O)N(CCCN(C)C)C(=O)[C@@H]1C[C@@H]2c3cccc4c3c(c[nH]4)C[C@H]2N(C1)CC=C (source: Drug Bank)
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
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DRD2 |
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Publications |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| DRD2 |
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(source: Drug Bank) |
A list of non-curated publications that mention this drug along with other drugs is available.
Drug Interactions
| Drug | Description | |
|---|---|---|
| erythromycin |
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Erythromycin increases serum levels and toxicity of cabergoline (source: Drug Bank) |
Curated Information
The following diseases are in curated knowledge about this drug.
| Disease | Relationship | Evidence | |
|---|---|---|---|
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Heart Valve Diseases |
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Publications |
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Parkinson Disease |
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Publications |
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Pituitary adenoma |
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Publications |
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Prolactinoma |
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Publications |
LinkOuts
Common Searches
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Non-Curated Publications
A list of non-curated publications that mention this drug is available.
