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Old Drug, New Trick – Cycloset

May 11, 2009

FDA Approves A New First In Class Diabetes Drug – Cycloset™ People with Type 2 diabetes may soon get a very different treatment approach

Old Drug, New Trick – Cyclosert
Robert Fredenrich, PharmD Candidate
University of Florida: College of Pharmacy


Bromocriptine has historically been used for Parkinsons, but this old drug has a new trick. Marketed under the name Cyclosert, it was approved by the FDA for treating Type 2 diabetes on May 6th, 2009. It is a once daily quick release low dose form of bromocriptine, acts on the central nervous system to improve glucose tolerance and insulin resistance centrally.  This is accomplished through resetting the neuroendocrine rhythms, which have been shown to be associated changes in metabolism leading to obesity and insulin resistance.  These metabolic changes likely occur in the suprachiasmatic nuclei located in the hypothalamus, and are regulated by dopamine and serotonin. The agonist activity at dopamine receptors of bromocriptine act on the suprachiasmatic nuclei and inhibits the serotonin effects to reset the neuronal activities, and resulting in improved glucose tolerance and insulin resistance.

Bromocriptine also reduces catecholamine levels by decreasing sympathetic tone, resulting in decreased lipolysis and free fatty acids.  There is also an increase in protein synthesis and breakdown into amino acids, coupled with reduced breakdown of amino acids leaving them for the increased protein synthesis.  This causes an increase in energy usage resulting in loss of body fat. Paraventricular hypothalamic reduction also results in deceased glucose production from the liver.

In short, Cyclosert once daily every morning can regulate metabolism improving glucose tolerance and insulin resistance, as well as reducing body fat through a decrease in sympathetic tone and increased energy usage.  It will be interesting to see how helpful this drug will be as we learn more about this new trick and how it works in the days to come.

Robert is in touch with the developers of this new drug and will have an indepth

Cincotta, A. H., MacEachern, T. A., and Meier, A. H. Bromocriptine Redirects Metabolism and Prevents Seasonal Onset of Obese Hyperinsulinemic State in Syrian Hamsters. Am J Physiol. 1993 Feb;264(2 Pt 1):E285-93.

Pijl H, Ohashi S, Matsuda M, Et Al. Bromocriptine: a novel approach to the treatment of type 2 diabetes. Diabetes Care. 2000 Aug;23(8):1154-61.

Scranton, R. E., Gaziano, J. M., Rutty, D., et. al. A Randomized, Double-Blind, Placebo-Controlled Trial to Assess Safety and Tolerability During Treatment of Type 2 Diabetes with Usual Diabetes Therapy and Either Cycloset or Placebo.

Put Courtesy of Diabetesincontrol.com at the bottom of the feature.