Comparative Pharmacology
Head-to-head clinical analysis: APOKYN versus REQUIP.
Peer-Reviewed Evidence
Head-to-head clinical analysis: APOKYN versus REQUIP.
APOKYN vs REQUIP
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Apomorphine is a non-ergoline dopamine agonist that stimulates dopamine D2 and D1 receptors. It also activates D3, D4, and D5 receptors and has some serotonergic and adrenergic activity.
Dopamine receptor agonist; exhibits high affinity for D2 and D3 receptors, and moderate affinity for D1 and D4 receptors.
Subcutaneous injection: 0.2 mL (2 mg) as a test dose, then 0.1-0.6 mL (1-6 mg) as needed for episodes of hypomobility; maximum single dose: 0.6 mL (6 mg); maximum daily dose: 2.0 mL (20 mg).
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 approximately 30–60 minutes (range 0.5–1 hour); clinically, rapid clearance necessitates continuous or frequent dosing for sustained effect
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 (approx. 90% as metabolites and unchanged drug; <5% unchanged in urine); biliary/fecal (minor, <10%)
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