RESEARCH MONOGRAPH · KDC-MN-318
Cabergoline
Cabergoline, sold as Dostinex, is a long-acting ergot dopamine agonist with a half-life measured in days rather than hours, allowing once or twice dosing. It is the first-line drug for prolactinomas (pituitary tumors that secrete the hormone prolactin), where it normalizes hormone levels and shrinks tumors in most patients. The principal safety concern is heart valve damage from chronic 5-HT2B receptor activation, which has been documented at high cumulative doses used in Parkinson disease. At the lower doses used for prolactinomas the valve risk appears small but is not zero, and patients on long-term therapy receive periodic echocardiograms. Not stocked by Kodiac. This monograph is provided for research and educational reference.
Intrigue 0–100 blends mechanism novelty, evidence strength, and translational potential. Kodiac editorial, not peer-reviewed.
Long-acting ergoline D2 dopamine agonist
A long-acting ergoline D2 dopamine receptor agonist; first-line for prolactinoma and used off-label for Parkinson disease maintenance.
Abstract
Cabergoline ((6aR,9R,10aS)-N-[3-(dimethylamino)propyl]-N-[(ethylamino)carbonyl]-7-(2-propenyl)-ergoline-8-beta-carboxamide; CAS 81409-90-7; molecular formula C26H37N5O2; molecular weight 451.61) is a long-acting ergoline D2 dopamine receptor agonist developed at Pharmacia and approved by the FDA in 1996 under the trade name Dostinex. The compound has high D2 affinity (Ki approximately 0.6 nM) with minimal activity at non-dopaminergic receptors compared to bromocriptine. Plasma half-life is approximately 60 to 100 hours, the longest of any clinical dopamine agonist, supporting oral dosing. Approved for hyperprolactinemia (prolactinoma, idiopathic hyperprolactinemia). Off-label use in Parkinson disease (less common since the introduction of non-ergot agonists), cocaine dependence, and dopamine-deficiency syndromes. The 5-HT2B partial agonism produces a recognized but rare risk of cardiac valvulopathy at high cumulative doses (Parkinson dose ranges); the lower prolactinoma doses are not associated with this risk. Used as the canonical long-acting ergoline dopamine agonist.
Mechanism of action
Long-acting ergoline D2 dopamine agonist; high D2 affinity with minimal off-target activity. 5-HT2B partial agonism produces cardiac valvulopathy risk at high cumulative dose.
Reported research dose ranges
Clinical 0.25 to 1 mg (prolactinoma); 1 to 6 mg (Parkinson, off-label).
References
- Webster J, et al. A comparison of cabergoline and bromocriptine in the treatment of hyperprolactinemic amenorrhea. N Engl J Med 1994.
- Schade R, et al. Dopamine agonists and the risk of cardiac-valve regurgitation. N Engl J Med 2007.
- Andreotti F, et al. Cabergoline and cardiac valvulopathy. Heart 2008.
Read the full monograph
The full reference document is available as a research-use-only PDF download. Note: PDFs for newly added compounds may take a few hours to propagate after this article was published.
The full reference document is provided strictly for research use only. It reports research dose ranges from the published literature, not instructions for use in humans or animals.
FOR RESEARCH USE ONLY. Not for medical, diagnostic, or therapeutic purposes. Not for human consumption. All information is provided for research and educational purposes only.