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QuickView for Cabergoline (compound)

Name: cabergoline
PubChem Compound ID: 2512
Molecular formula: C26H37N5O2
Molecular weight: 451.604 g/mol
Name: cabergoline
Name (isomeric): DB00248
Drug Type: small molecule
Cabergolinum [Latin]; Cabergolina [Spanish]
Brand: Cabaser, Dostinex
Category: Antineoplastic Agents, Antiparkinson Agents, Dopamine Agonists
CAS number: 81409-90-7
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.
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 are associated with dyskinesias. The dopaminergic ...
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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. Decr...
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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.
Biotransformation: 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).
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: renal cl=0,008 L/min nonrenal cl=3.2 L/min
Toxicity: Overdosage might be expected to produce nasal congestion, syncope, or hallucinations.
Affected organisms: Humans and other mammals
Food interaction:
Take with food to improve tolerance.
Absorption is not affected by food.
Drug interaction:
VenlafaxineIncreased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
TramadolIncreased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
VoriconazoleVoriconazole may increase the serum concentration of cabergoline likely by decreasing its metabolism. Concomitant therapy is contraindicated.
TrimipramineIncreased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
ZolmitriptanConcomitant use of the serotonin 5-HT1D receptor agonist, zolmitriptan, and the ergot derivative, carbergoline, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated. Use of two serotonin modulators, such as zolmitriptan and carbergoline, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
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