Comparative Pharmacology
Head-to-head clinical analysis: CYCLOSET versus REQUIP.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CYCLOSET versus REQUIP.
CYCLOSET vs REQUIP
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
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.
Dopamine receptor agonist; exhibits high affinity for D2 and D3 receptors, and moderate affinity for D1 and D4 receptors.
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.
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 is 4–6 hours in patients with normal renal function; clinically, steady-state is reached within 24 hours.
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: ~90% (30% unchanged, rest as inactive metabolites); fecal: ~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 / Antidiabetic
Dopamine Agonist