- Molecular NameCabergoline
- SynonymCabergolina [Spanish]; Cabergolinum [Latin]
- Weight451.615
- Drugbank_IDDB00248
- ACS_NO81409-90-7
- Show 3D model
- LogP (experiment)2.855
- LogP (predicted, AB/LogP v2.0)3.91
- pkaN/A
- LogD (pH=7, predicted)1.27
- Solubility (experiment)Insoluble
- LogS (predicted, ACD/Labs)(ph=7)-1.95
- LogSw (predicted, AB/LogsW2.0)0.05
- Sw (mg/ml) (predicted, ACD/Labs)0.04
- No.of HBond Donors2
- No.of HBond Acceptors7
- No.of Rotatable Bonds8
- TPSA71.68
- StatusFDA approved
- AdministrationN/A
- PharmacologyAn ergot 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.
- Absorption_valueN/A
- Absorption (description)Cabergoline is absorbed after oral administration and undergoes significant first-pass metabolism.
- Caco_2N/A
- Bioavailability65.0
- Protein binding45.0
- Volume of distribution (VD)N/A
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmHepatic. Cabergoline is extensively metabolized, predominately via hydrolysis of the acylurea bond or the urea moiety. Other important metabolite is a product of the 29-N dealkylation. Cytochrome P-450 mediated metabolism appears to be minimal.
- Half life63~68 h (in healthy subjects); 79~115 h (in hyperprolactinaemic subjects)
- ExcretionIt is widely distributed and extensively metabolised, mainly by hydrolysis, to several inactive metabolites. The drug is mainly eliminated via faeces with a small proportion excreted in urine. Less than 4% is excreted unchanged; 1% as the parent drug.
- Urinary ExcretionN/A
- CleranceN/A
- ToxicityOverdosage might be expected to produce nasal congestion, syncope, or hallucinations.
- LD50 (rat)N/A
- LD50 (mouse)N/A