Comparative Pharmacology
Head-to-head clinical analysis: PERGOLIDE MESYLATE versus REQUIP XL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: PERGOLIDE MESYLATE versus REQUIP XL.
PERGOLIDE MESYLATE vs REQUIP XL
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.
Ropinirole is a non-ergoline dopamine agonist with high relative in vitro specificity and full intrinsic activity at the D2 subfamily of dopamine receptors, binding with higher affinity to D3 than to D2 or D4 receptor subtypes. The relevance of D3 receptor binding in Parkinson's disease is unknown.
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.
Initial: 2 mg orally once daily for weeks 1-2, then titrate as needed; maintenance: 8-24 mg orally once daily.
None Documented
None Documented
Terminal elimination half-life: 15-27 hours (mean 21 hours); clinically relevant for once-daily dosing
Approximately 6 hours (range 4-8 hours) for ropinirole; terminal half-life in elderly or hepatic impairment may be prolonged up to 10-12 hours. Clinically, steady-state achieved within 2 days of dosing.
Renal: 50-60% as metabolites; Fecal: 40-50%; Biliary: minor (<5%)
Renal: 60% (mainly metabolites, <10% unchanged); fecal/biliary: 20%; total excretion accounts for >80% of dose.
Category C
Category C
Dopamine Agonist
Dopamine Agonist