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Quick-Release Bromocriptine for Treatment of Type 2 Diabetes

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Quick-release bromocriptine (bromocriptine-QR) (Cycloset) was approved in 2009 for the treatment of type 2 diabetes. The exact anti-diabetic mechanism of action of bromocriptine-QR has not been elucidated, but the drug may help resetting the circadian dopamine signal. Randomized placebo-controlled trials showed that the mean reduction in hemoglobin A1c (HbA1c) levels by bromocriptine-QR was 0.0-0.2% when compared to baseline and 0.4-0.5% when compared with placebo after 24 weeks of therapy. Withdrawal rates due to adverse effects in patients receiving bromocriptine- QR and placebo were 24% and 11%, respectively. The most common adverse effect of bromocriptine-QR was nausea reported by 32% of patients compared with 7% of patients randomized to placebo. The advantages of bromocriptine- QR were minimal risk of hypoglycemia, neutral effect on weight, and reassuring cardiovascular safety over 1 year of use. However, the drug had multiple drawbacks including modest efficacy, high rates of nausea, lack of long-term efficacy and safety data, and considerable cost. Bromocriptine-QR may be used in patients with type 2 diabetes with mild hyperglycemia (HbA1c close to 7.5%) either as adjunctive treatment to metformin and sulfonylurea (SU) or as monotherapy in patients who are intolerant to both agents.

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Keywords: Type 2 diabetes; bromocriptine; cabergoline; circadian rhythm; diabetes; dizziness; dopamine agonists; hyperglycemia; hyperprolactinemia; insulin resistance; nausea; obesity; prolactin

Document Type: Research Article

Publication date: September 1, 2011

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  • The aim of Current Drug Delivery is to publish peer-reviewed articles, short communications, short and in-depth reviews in the rapidly developing field of drug delivery. Modern drug research aims to build in delivery properties of a drug at the design phase, however in many cases this ideal cannot be met and the development of delivery systems becomes as important as the development as the drugs themselves.

    The journal aims to cover the latest outstanding developments in drug and vaccine delivery employing physical, physico-chemical and chemical methods. The drugs include a wide range of bioactive compounds from simple pharmaceuticals to peptides, proteins, nucleotides, nucleosides and sugars. The journal will also report progress in the fields of transport routes and mechanisms including efflux proteins and multi-drug resistance.

    The journal is essential for all pharmaceutical scientists involved in drug design, development and delivery.
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