Comparative Pharmacology
Head-to-head clinical analysis: CABERGOLINE versus CYCLOSET.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CABERGOLINE versus CYCLOSET.
CABERGOLINE vs CYCLOSET
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Cabergoline is a long-acting dopamine D2 receptor agonist that inhibits prolactin secretion by the anterior pituitary gland.
Cycloset (bromocriptine mesylate) is a dopamine D2 receptor agonist. It improves glycemic control in type 2 diabetes by resetting hypothalamic circadian rhythms, thereby reducing hepatic glucose production and increasing insulin sensitivity. It also suppresses the release of very low-density lipoprotein from the liver.
0.25 mg orally twice weekly, up to 1 mg twice weekly; for hyperprolactinemia, initial 0.25 mg twice weekly, titrate by 0.25 mg every 4 weeks based on prolactin levels.
1.6 mg to 2.4 mg administered orally once daily at bedtime. Titrate by 0.8 mg every 2 weeks based on glycemic response and tolerability.
None Documented
None Documented
Clinical Note
moderateCabergoline + Digoxin
"Cabergoline may decrease the cardiotoxic activities of Digoxin."
Clinical Note
moderateCabergoline + Digitoxin
"Cabergoline may decrease the cardiotoxic activities of Digitoxin."
Clinical Note
moderateCabergoline + Deslanoside
"Cabergoline may decrease the cardiotoxic activities of Deslanoside."
Clinical Note
moderateCabergoline + Acetyldigitoxin
"Cabergoline may decrease the cardiotoxic activities of Acetyldigitoxin."
Terminal elimination half-life is 63-68 hours in healthy subjects, allowing for once- or twice-weekly dosing. In hepatic impairment, half-life may be prolonged.
Terminal elimination half-life is 4–6 hours in patients with normal renal function; clinically, steady-state is reached within 24 hours.
Approximately 60-70% of the dose is excreted in feces (primarily as unchanged drug and metabolites), with about 20-30% excreted renally (mostly as metabolites).
Renal: ~90% (30% unchanged, rest as inactive metabolites); fecal: ~10%.
Category A/B
Category C
Dopamine Agonist
Dopamine Agonist / Antidiabetic