Comparative Pharmacology
Head-to-head clinical analysis: BROMOCRIPTINE MESYLATE versus REQUIP XL.
Head-to-head clinical analysis: BROMOCRIPTINE MESYLATE versus REQUIP XL.
BROMOCRIPTINE MESYLATE vs REQUIP XL
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
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.
Ropinirole is a non-ergoline dopamine agonist with high relative in vitro specificity and full intrinsic activity at the D2 subfamily of dopamine receptors, binding with higher affinity to D3 than to D2 or D4 receptor subtypes. The relevance of D3 receptor binding in Parkinson's disease is unknown.
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).
Initial: 2 mg orally once daily for weeks 1-2, then titrate as needed; maintenance: 8-24 mg orally once daily.
None Documented
None Documented
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.
Approximately 6 hours (range 4-8 hours) for ropinirole; terminal half-life in elderly or hepatic impairment may be prolonged up to 10-12 hours. Clinically, steady-state achieved within 2 days of dosing.
Primarily hepatic metabolism with 85-90% fecal excretion via bile; <5% renal excretion as unchanged drug and metabolites.
Renal: 60% (mainly metabolites, <10% unchanged); fecal/biliary: 20%; total excretion accounts for >80% of dose.
Category A/B
Category C
Dopamine Agonist
Dopamine Agonist