Comparative Pharmacology
Head-to-head clinical analysis: CABERGOLINE versus PERGOLIDE MESYLATE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CABERGOLINE versus PERGOLIDE MESYLATE.
CABERGOLINE vs PERGOLIDE MESYLATE
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.
Ergoline-derived dopamine D2 receptor agonist; also activates D1 and D3 receptors, and has antagonist activity at α2-adrenergic and 5-HT2B receptors.
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.
0.05 mg orally once daily for first 2 days, then increase by 0.1-0.15 mg/day every 3 days over 12 days, then by 0.25 mg/day every 3 days until optimal response; usual therapeutic range 2-3 mg/day divided 3 times daily; maximum 5 mg/day.
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: 15-27 hours (mean 21 hours); clinically relevant for once-daily dosing
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: 50-60% as metabolites; Fecal: 40-50%; Biliary: minor (<5%)
Category A/B
Category C
Dopamine Agonist
Dopamine Agonist