Cabergoline

Cabergoline

Clinical data
Trade names	Cabaser, Dostinex
AHFS/Drugs.com	Monograph
License data	US FDA: CABERGOLINE
Pregnancy category	US: B (No risk in non-human studies)
Routes of administration	Oral
ATC code	G02CB03 (WHO) N04BC06 (WHO)
Legal status
Legal status	US: ℞-only
Pharmacokinetic data
Bioavailability	First-pass effect seen; absolute bioavailability unknown
Protein binding	Moderately bound (40–42%); concentration-independent
Metabolism	Hepatic, predominately via hydrolysis of the acylurea bond or the urea moiety
Biological half-life	63–69 hours (estimated)
Excretion	Urine (22%), feces (60%)
Identifiers
IUPAC name (6aR,9R,10aR)-N-[3-(dimethylamino)propyl]-N-(ethylcarbamoyl)-7-prop-2-enyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinoline-9-carboxamide
CAS Number	81409-90-7 Y
PubChem CID	54746
IUPHAR/BPS	37
DrugBank	DB00248 Y
ChemSpider	49452 Y
UNII	LL60K9J05T
KEGG	D00987 Y
ChEBI	CHEBI:3286 Y
ChEMBL	CHEMBL1201087 N
Chemical and physical data
Formula	C26H37N5O2
Molar mass	451.604 g/mol
3D model (Jmol)	Interactive image
SMILES O=C(NCC)N(C(=O)[C@@H]2C[C@@H]3c4cccc1c4c(cn1)C[C@H]3N(C2)C\C=C)CCCN(C)C
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 Y Key:KORNTPPJEAJQIU-KJXAQDMKSA-N Y
NY (what is this?)

Cabergoline (brand names Dostinex and others), an ergot derivative, is a potent dopamine receptor agonist on D₂ receptors. Rat studies show cabergoline has a direct inhibitory effect on pituitary lactotroph (prolactin) cells. It is frequently used as a first-line agent in the management of prolactinomas due to its higher affinity for D₂ receptor sites, less severe side effects, and more convenient dosing schedule than the older bromocriptine.

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, thereby allowing men to experience multiple ejaculatory orgasms in rapid succession, and at least one scientific study supports those speculations. Additionally, a systematic review and meta-analysis concluded that prophylactic treatment with cabergoline reduces the incidence, but not the severity, of ovarian hyperstimulation syndrome (OHSS), without compromising pregnancy outcomes, in females undergoing stimulated cycles of in vitro fertilization (IVF). Also, a study on rats found that cabergoline reduces voluntary alcohol consumption, possibly by increasing GDNF expression in the ventral tegmental area.