Bromocriptine: old drug, new formulation and new indication

R.I.G. Holt, A.H. Barnett, C.J. Bailey

Research output: Contribution to journalArticle

Abstract

Bromocriptine is an ergot alkaloid dopamine D receptor agonist that has been used extensively in the past to treat hyperprolactinaemia, galactorrhoea and Parkinsonism. It is known that hypothalamic hypodopaminergic states and disturbed circadian rhythm are associated with the development of insulin resistance, obesity and diabetes in animals and humans. When administered in the early morning at the start of the light phase, a new quick release (QR) formulation of bromocriptine appears to act centrally to reset circadian rhythms of hypothalamic dopamine and serotonin and improve insulin resistance and other metabolic abnormalities. Phase II and III clinical studies show that QR-bromocriptine lowers glycated haemoglobin by 0.6-1.2% (7-13 mmol/mol) either as monotherapy or in combination with other antidiabetes medications. Apart from nausea, the drug is well tolerated. The doses used to treat diabetes (up to 4.8 mg daily) are much lower than those used to treat Parkinson's disease and have not been associated with retroperitoneal fibrosis or heart valve abnormalities. QR-bromocriptine (Cycloset™) has recently been approved in the USA for the treatment of type 2 diabetes mellitus (T2DM). Thus, a QR formulation of bromocriptine timed for peak delivery in the early morning may provide a novel neurally mediated approach to the control of hyperglycaemia in T2DM.
Original languageEnglish
Pages (from-to)1048-1057
Number of pages10
JournalDiabetes, Obesity and Metabolism
Volume12
Issue number12
Early online date26 Oct 2010
DOIs
Publication statusPublished - Dec 2010

Keywords

  • antidiabetes drug
  • bromocriptine
  • circadian rhythms
  • clinical trials
  • diabetes mellitus
  • drug mechanism
  • glycaemic control
  • treatment

Fingerprint Dive into the research topics of 'Bromocriptine: old drug, new formulation and new indication'. Together they form a unique fingerprint.

  • Cite this