Cabergoline CAS: 81409-90-7 for Treatment of Parkinsonism (AREP)

Cabergoline

Alias: Cabaser, Dostinex; Dostine, 6-Allyl-N-[3-(dimethylamino)propyl]-N-(ethylcarbamoyl)ergoline-8-carboxamide
CAS: 81409-90-7
Molecular Formula: C26H37N5O2
Molecular Weight: 451.6
Melting Point: 102-104° C

 

Uses of Cabergoline:

1. hyperprolactinemia
2. adjunctive therapy of prolactin-producing pituitary gland tumors (prolactinomas);
3. monotherapy of Parkinson’s disease in the early phase;
4. combination therapy, together with levodopa and a decarboxylase inhibitor such as carbidopa, in progressive-phase Parkinson’s disease;
5. in some countries also: ablactation and dysfunctions associated with hyperprolactinemia (amenorrhea, oligomenorrhea, anovulation, nonpuerperal mastitis and galactorrhea);
6. treatment of uterine fibroids.
7. adjunctive therapy of acromegaly, cabergoline has low efficacy in suppressing levels and is highly efficient in suppressing hyperprolactinemia that is present in 20-30% of acromegaly cases;
8.and prolactin are similar structurally and have similar effects in many target tissues, therefore targeting prolactin may help symptoms when hormone secretion can not be sufficiently controlled by other methods;
9. Cushing’s disease – cabergoline may be used to lower ACTH levels and cause regression of ACTH producing pituitary adenomas;
10. other pituitary adenomas – cabergoline has demonstrated certain efficacy in controlling or reducing other kinds of pituitary adenomas, as well as silent or non-functional adenomas.

 

Description of Cabergoline: Pharmaceutical intermediates. This medication is used to treat high levels of prolactin hormone in your body. High levels of prolactin in women can cause symptoms such as unwanted breast milk and missed periods and can cause difficulty becoming pregnant. High levels of prolactin in men can cause symptoms such as enlarged breasts and decreased sexual ability/desire. Cabergoline is an ergot medication and works by blocking the release of prolactin from the pituitary gland.

 

History of Cabergoline: Cabergoline was first synthesized by scientists working for the Italian drug company Farmitalia-Carlo Erba SpA in Milan in 1981/82, who were experimenting with semisynthetic derivatives of the ergot alkaloids. Farmitalia-Carlo Erba was acquired by Pharmacia in 1992, which in turn was acquired  in 2002. The drug was approved by the FDA on December 23, 1996. It went generic in late 2005 following US patent expiration.

 

Properties of Cabergoline: White powder. Soluble in ethyl alcohol, chloroform, and N, Ndimethylformamide (DMF); Slightly soluble in 0.1N hydrochloric acid; Very slightly soluble in n-hexane; And insoluble in water.

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