Comparative Pharmacology
Head-to-head clinical analysis: APOKYN versus BROMOCRIPTINE MESYLATE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: APOKYN versus BROMOCRIPTINE MESYLATE.
APOKYN vs BROMOCRIPTINE MESYLATE
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.
Bromocriptine mesylate is a dopamine D2 receptor agonist that also exhibits partial agonist activity at D1 receptors. By stimulating dopamine receptors in the tuberoinfundibular pathway, it inhibits prolactin secretion from the anterior pituitary. It also activates postsynaptic dopamine receptors in the striatum, improving motor function in Parkinson disease. Additionally, it has been shown to improve glycemic control in type 2 diabetes by modulating central dopaminergic tone and reducing hepatic glucose production.
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: 1.25-2.5 mg twice daily, increased gradually as tolerated. Maximum 100 mg/day. Also used intravaginally for hyperprolactinemia (2.5 mg 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 is approximately 6-8 hours in healthy individuals, but may be prolonged to 12-14 hours in patients with hepatic impairment or in the elderly.
Renal (approx. 90% as metabolites and unchanged drug; <5% unchanged in urine); biliary/fecal (minor, <10%)
Primarily hepatic metabolism with 85-90% fecal excretion via bile; <5% renal excretion as unchanged drug and metabolites.
Category C
Category A/B
Dopamine Agonist
Dopamine Agonist