Comparative Pharmacology
Head-to-head clinical analysis: APOKYN versus CYCLOSET.
Peer-Reviewed Evidence
Head-to-head clinical analysis: APOKYN versus CYCLOSET.
APOKYN vs CYCLOSET
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.
Cycloset (bromocriptine mesylate) is a dopamine D2 receptor agonist. It improves glycemic control in type 2 diabetes by resetting hypothalamic circadian rhythms, thereby reducing hepatic glucose production and increasing insulin sensitivity. It also suppresses the release of very low-density lipoprotein from the liver.
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).
1.6 mg to 2.4 mg administered orally once daily at bedtime. Titrate by 0.8 mg every 2 weeks based on glycemic response and tolerability.
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 is 4–6 hours in patients with normal renal function; clinically, steady-state is reached within 24 hours.
Renal (approx. 90% as metabolites and unchanged drug; <5% unchanged in urine); biliary/fecal (minor, <10%)
Renal: ~90% (30% unchanged, rest as inactive metabolites); fecal: ~10%.
Category C
Category C
Dopamine Agonist
Dopamine Agonist / Antidiabetic