Bromocriptine: old drug, new formulation and new indication
Bromocriptine: old drug, new formulation and new indication
Bromocriptine is an ergot alkaloid dopamine D2 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
antidiabetes drug, bromocriptine, circadian rhythms, clinical trials, diabetes mellitus, drug mechanism, glycaemic control, treatment
1048-1057
Holt, R. I. G.
d54202e1-fcf6-4a17-a320-9f32d7024393
Barnett, A. H.
88f0298d-bb5e-452d-93c2-1517dcf312a6
Bailey, C. J.
b7a2ff9b-90a8-4ecb-baa6-55be224384b6
December 2010
Holt, R. I. G.
d54202e1-fcf6-4a17-a320-9f32d7024393
Barnett, A. H.
88f0298d-bb5e-452d-93c2-1517dcf312a6
Bailey, C. J.
b7a2ff9b-90a8-4ecb-baa6-55be224384b6
Abstract
Bromocriptine is an ergot alkaloid dopamine D2 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
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Published date: December 2010
Keywords:
antidiabetes drug, bromocriptine, circadian rhythms, clinical trials, diabetes mellitus, drug mechanism, glycaemic control, treatment
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Local EPrints ID: 167747
URI: http://eprints.soton.ac.uk/id/eprint/167747
ISSN: 1462-8902
PURE UUID: f9b1d443-923d-4b49-89ce-fd01ddac7afb
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Date deposited: 18 Nov 2010 08:13
Last modified: 14 Mar 2024 02:45
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Author:
A. H. Barnett
Author:
C. J. Bailey
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