Cabergon – Cabergoline 125 mcg – 25 tab

Description

Pharmacological category:
Dopamine D2 receptor agonist

Mechanism of action:
Cabergoline is a long-acting, ergot-derived dopamine D2 receptor agonist that suppresses pituitary lactotroph activity. By activating D2 receptors, it inhibits adenylate cyclase, decreases intracellular cAMP, and reduces prolactin gene expression and secretion. This results in dose-dependent reductions in serum prolactin and restoration of gonadotropin pulsatility.
Its prolonged pharmacologic effect reflects its long elimination half-life and strong receptor binding affinity.
In prolactinomas, cabergoline not only reduces prolactin hypersecretion but can also induce tumor shrinkage through antiproliferative and pro-apoptotic actions on lactotroph cells, thereby improving clinical manifestations of hyperprolactinemia.

Side effects:
Cabergoline may cause nausea, abdominal discomfort, constipation, headache, dizziness, and orthostatic hypotension, especially at treatment initiation or after dose escalation. Central nervous system effects include somnolence, insomnia, agitation, and, rarely, impulse-control disorders such as pathological gambling or hypersexuality. Decreased prolactin levels may alter libido and reproductive function. Less commonly, peripheral edema, nasal congestion, and digital vasospasm occur. With prolonged use or higher cumulative doses, ergot-derived dopamine agonists have been associated with valvular heart disease. Concomitant use of dopaminergic or hypotensive agents may potentiate neuropsychiatric effects or hypotension.

Dosage:
Take 125-500 mcg orally once or twice a week.