Comparative Pharmacology
Head-to-head clinical analysis: NEUPRO versus PERGOLIDE MESYLATE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: NEUPRO versus PERGOLIDE MESYLATE.
NEUPRO vs PERGOLIDE MESYLATE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Rotigotine is a non-ergoline dopamine agonist with high affinity for dopamine D1, D2, D3, D4, and D5 receptors; also binds to serotonin 5-HT1A and alpha2-adrenergic receptors.
Ergoline-derived dopamine D2 receptor agonist; also activates D1 and D3 receptors, and has antagonist activity at α2-adrenergic and 5-HT2B receptors.
Apply transdermally once daily; initial dose 2 mg/24h, titrated weekly by 2 mg/24h up to 6 mg/24h, maximum 8 mg/24h.
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
Single dose: 5-7 hours (transdermal); steady state: 7-10 hours; effective half-life for dosing is 8 hours due to reservoir in skin
Terminal elimination half-life: 15-27 hours (mean 21 hours); clinically relevant for once-daily dosing
Renal: 45% (metabolites), Fecal: 40% (metabolites), Biliary: 15%
Renal: 50-60% as metabolites; Fecal: 40-50%; Biliary: minor (<5%)
Category C
Category C
Dopamine Agonist
Dopamine Agonist