Comparative Pharmacology
Head-to-head clinical analysis: CYCLOSET versus FORTAMET.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CYCLOSET versus FORTAMET.
CYCLOSET vs FORTAMET
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.
Metformin decreases hepatic glucose production, decreases intestinal absorption of glucose, and improves insulin sensitivity by increasing peripheral glucose uptake and utilization.
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.
Initial: 500 mg orally twice daily or 1000 mg orally once daily; titrate in increments of 500 mg weekly; maximum daily dose: 2000 mg.
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 is approximately 6.2 hours (range 4–9 hours) in patients with normal renal function; half-life is prolonged in renal impairment (up to 18 hours in moderate impairment and 24 hours in severe impairment).
Renal: ~90% (30% unchanged, rest as inactive metabolites); fecal: ~10%.
Renal excretion of unchanged drug accounts for approximately 90% of elimination; the remainder is excreted fecally (via bile).
Category C
Category C
Dopamine Agonist / Antidiabetic
Antidiabetic