Bromocriptine: old drug, new formulation and new indication

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Bromocriptine: old drug, new formulation and new indication. / Holt, RIG; Barnett, Anthony; Bailey, CJ.

In: Diabetes, Obesity and Metabolism, Vol. 12, No. 12, 01.12.2010, p. 1048-1057.

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@article{0e0634ad92984044badcf3af8b563681,
title = "Bromocriptine: old drug, new formulation and new indication",
abstract = "Bromocriptine is an ergot alkaloid dopamine D-2 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 (TM)) 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.",
keywords = "drug mechanism, diabetes mellitus, treatment, glycaemic control, circadian rhythms, bromocriptine, clinical trials, antidiabetes drug",
author = "RIG Holt and Anthony Barnett and CJ Bailey",
year = "2010",
month = dec,
day = "1",
doi = "10.1111/j.1463-1326.2010.01304.x",
language = "English",
volume = "12",
pages = "1048--1057",
journal = "Diabetes, obesity & metabolism",
issn = "1462-8902",
publisher = "Wiley",
number = "12",

}

RIS

TY - JOUR

T1 - Bromocriptine: old drug, new formulation and new indication

AU - Holt, RIG

AU - Barnett, Anthony

AU - Bailey, CJ

PY - 2010/12/1

Y1 - 2010/12/1

N2 - Bromocriptine is an ergot alkaloid dopamine D-2 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 (TM)) 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.

AB - Bromocriptine is an ergot alkaloid dopamine D-2 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 (TM)) 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.

KW - drug mechanism

KW - diabetes mellitus

KW - treatment

KW - glycaemic control

KW - circadian rhythms

KW - bromocriptine

KW - clinical trials

KW - antidiabetes drug

U2 - 10.1111/j.1463-1326.2010.01304.x

DO - 10.1111/j.1463-1326.2010.01304.x

M3 - Article

C2 - 20977575

VL - 12

SP - 1048

EP - 1057

JO - Diabetes, obesity & metabolism

JF - Diabetes, obesity & metabolism

SN - 1462-8902

IS - 12

ER -