Cabergoline
Dopamine Agonist | Prolactin Management
Cabergoline is a potent, long-acting dopamine D2 receptor agonist that powerfully suppresses prolactin secretion from the anterior pituitary. It is FDA-approved under the brand name Dostinex for the treatment of hyperprolactinemic disorders, including prolactin-secreting pituitary adenomas (prolactinomas). In the bodybuilding and performance enhancement community, cabergoline is considered an essential ancillary compound when running 19-nor anabolic steroids such as nandrolone (Deca-Durabolin, NPP) and trenbolone, both of which can elevate prolactin levels through progestogenic activity. Elevated prolactin causes a range of undesirable effects including gynecomastia (particularly the progesterone-mediated variant), sexual dysfunction (erectile dysfunction, decreased libido, anorgasmia), mood disturbances, and lactation. Cabergoline's exceptionally long half-life of 63-69 hours allows for convenient twice-weekly dosing, and its high affinity for D2 receptors makes it significantly more potent and better tolerated than the older dopamine agonist bromocriptine.
Moleküler Gösterim
M.W.: 451.60 Da
PubChem 2D yapı diyagramı
Referans Flakon
Referans illüstrasyonu — ürün listesi değildir
Etki Mekanizması
Cabergoline exerts its effects by acting as a potent agonist at dopamine D2 receptors on lactotroph cells in the anterior pituitary gland. Prolactin secretion is tonically inhibited by hypothalamic dopamine acting on these D2 receptors, and cabergoline mimics this inhibitory signal with high affinity and prolonged duration. By activating D2 receptors, cabergoline suppresses prolactin gene transcription, reduces prolactin synthesis, and inhibits prolactin release into the bloodstream. In patients with prolactinomas, cabergoline also induces tumor shrinkage by inhibiting lactotroph cell proliferation and promoting apoptosis. The drug's selectivity for D2 receptors over D1 receptors contributes to its favorable side effect profile compared to less selective dopamine agonists. In the context of 19-nor steroid use, nandrolone and trenbolone stimulate prolactin release through their progestogenic activity, and cabergoline directly counteracts this elevation by restoring dopaminergic inhibition at the pituitary level.
Cabergoline is a potent, long-acting dopamine D2 receptor agonist that powerfully suppresses prolactin secretion from the anterior pituitary. It is FDA-approved under the brand name Dostinex for the treatment of hyperprolactinemic disorders, including prolactin-secreting pituitary adenomas (prolactinomas). In the bodybuilding and performance enhancement community, cabergoline is considered an essential ancillary compound when running 19-nor anabolic steroids such as nandrolone (Deca-Durabolin, NPP) and trenbolone, both of which can elevate prolactin levels through progestogenic activity. Elevated prolactin causes a range of undesirable effects including gynecomastia (particularly the progesterone-mediated variant), sexual dysfunction (erectile dysfunction, decreased libido, anorgasmia), mood disturbances, and lactation. Cabergoline’s exceptionally long half-life of 63-69 hours allows for convenient twice-weekly dosing, and its high affinity for D2 receptors makes it significantly more potent and better tolerated than the older dopamine agonist bromocriptine.
Moleküler Veri
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| Hedef | Doz | Sıklık | Yol |
|---|---|---|---|
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Etkileşimler
Nandrolone (Deca-Durabolin / NPP)
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Kaynaklar
- A comparative study of cabergoline and bromocriptine in the treatment of hyperprolactinemia — Webster J, Piscitelli G, Polli A, Ferrari CI, Ismail I, Scanlon MF
- Cabergoline in the treatment of hyperprolactinemia: a study in 455 patients — Verhelst J, Abs R, Maiter D, van den Bruel A, Vandeweghe M, Velkeniers B, Mockel J, Lamberigts G, Petrossians P, Coremans P, Mahler C, Stevenaert A, Verlooy J, Raftopoulos C, Beckers A
- Prevalence of clinically significant valvular heart disease in patients treated with cabergoline for prolactinoma — Colao A, Galderisi M, Di Sarno A, Pardo M, Gaccione M, D'Andrea M, Guerra E, Pivonello R, Lerro G, Lombardi G
- Cabergoline: a review of its use in the treatment of pathological hyperprolactinemia — Biller BM, Molitch ME, Vance ML, Cannistraro KB, Davis KR, Simons JA, Schoenfelder JR, Klibanski A
- Diagnosis and treatment of hyperprolactinemia: an Endocrine Society clinical practice guideline — Melmed S, Casanueva FF, Hoffman AR, Kleinberg DL, Montori VM, Schlechte JA, Wass JA