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.
Medical use
Lactation suppression
hyperprolactinemia
adjunctive therapy of prolactin-producing pituitary gland tumors (prolactinomas);
monotherapy of Parkinson's disease in the early phase;
combination therapy, together with levodopa and a decarboxylase inhibitor such as carbidopa, in progressive-phase Parkinson's disease;
in some countries also: ablactation and dysfunctions associated with hyperprolactinemia (amenorrhea, oligomenorrhea, anovulation, nonpuerperal mastitis and galactorrhea);
treatment of uterine fibroids.
adjunctive therapy of acromegaly, cabergoline has low efficacy in suppressing growth hormone levels and is highly efficient in suppressing hyperprolactinemia that is present in 20-30% of acromegaly cases; growth hormone and prolactin are similar structurally and have similar effects in many target tissues, therefore targeting prolactin may help symptoms when growth hormone secretion can not be sufficiently controlled by other methods.
COA OF Cabergoline 81409-90-7
| Item | Specifications | Results |
| Description | White or almost white crystalline powder | Conform |
Identity
|
1,IR complies
| Conform |
2,X-Ray complies
| Conform | |
3,HPLC complies
| Conform | |
| Optical rotation |
-77.0°~-83.0°
|
-78.0°
|
| Loss on drying | Not more than 0.5% | 0.32% |
| Related substances |
1,Cabergolin Imp A no more than0.15%
|
0.05%
|
2,Allylamide no more than 0.10%
| 0.03% | |
3,Allyl DHLA no more than 0.15%
| 0.06% | |
4,Cabergoline oxide no more than 0.10%
| 0.04% | |
5,Other impurities individually no more than 0.10%
| 0.03% | |
6,Total no more than 0.50%
| 0.21% | |
| Assay(HPLC) | 98.0%~102.0%(recalculated on anhydrous basis) | 99.4% |
Residual solvents
|
1,Dichloromethane no more than 100ppm
| 15ppm |
2,Acetone no more than 200ppm
| 15ppm | |
3,Tert-butylmethylether no more than 200ppm
| 11ppm | |
4,Xylene no more than 1500ppm
| 135ppm | |
5,Heptane no more than 1000ppm
| 20ppm | |
| Residue on ignition | No more than0.10% | 0.03% |
| Heavy metals | No more than 20ppm | 1ppm |
| Particle size | 90% of particles no more than 80um | Conform |
| Bulk density |
0.20~0.35g/cm3
|
0.33g/cm3
|
| Conclusion |
The results conforms with EP7.0/USP38 standard.
| |
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