Comparative Pharmacology
Head-to-head clinical analysis: PERGOLIDE MESYLATE versus REQUIP.
Peer-Reviewed Evidence
Head-to-head clinical analysis: PERGOLIDE MESYLATE versus REQUIP.
PERGOLIDE MESYLATE vs REQUIP
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Ergoline-derived dopamine D2 receptor agonist; also activates D1 and D3 receptors, and has antagonist activity at α2-adrenergic and 5-HT2B receptors.
Dopamine receptor agonist; exhibits high affinity for D2 and D3 receptors, and moderate affinity for D1 and D4 receptors.
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.
Immediate-release: Initial 0.25 mg orally three times daily; titrate weekly by 0.25 mg per dose to a total daily dose of 3 mg; max 24 mg/day. Extended-release: Initial 2 mg orally once daily; titrate by 2 mg/day at weekly intervals; max 24 mg/day.
None Documented
None Documented
Terminal elimination half-life: 15-27 hours (mean 21 hours); clinically relevant for once-daily dosing
Terminal elimination half-life: approximately 5-6 hours in young healthy adults, extending to 7-9 hours in elderly patients. Clinically, dosing is typically three times daily due to this short half-life.
Renal: 50-60% as metabolites; Fecal: 40-50%; Biliary: minor (<5%)
Primarily renal: approximately 90% of the dose is excreted in urine, with about 60% as unchanged drug and 30% as metabolites. Fecal excretion accounts for about 10%.
Category C
Category C
Dopamine Agonist
Dopamine Agonist