Comparative Pharmacology
Head-to-head clinical analysis: APOKYN versus MIRAPEX ER.
Peer-Reviewed Evidence
Head-to-head clinical analysis: APOKYN versus MIRAPEX ER.
APOKYN vs MIRAPEX ER
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.
Non-ergot dopamine agonist with high affinity for D2 and D3 receptor subtypes; stimulates dopamine receptors in the striatum.
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).
Oral, start 0.375 mg once daily, titrate weekly by 0.375 mg/dose to 1.5 mg once daily (immediate-release); ER: same total daily dose once daily.
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: 8–12 hours in young healthy adults; prolonged to 16–40 hours in elderly (≥65 years) and up to 30 hours in moderate renal impairment (CrCl 20–50 mL/min).
Renal (approx. 90% as metabolites and unchanged drug; <5% unchanged in urine); biliary/fecal (minor, <10%)
Renal excretion of unchanged drug and metabolites: ~90% in urine (pramipexole: ~70% unchanged; N-desmethyl metabolite: ~20%). Fecal excretion: ~2%. Biliary elimination: minimal.
Category C
Category C
Dopamine Agonist
Dopamine Agonist