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New prolonged-release metformin improves gastrointestinal tolerability
Jaime Davidson
University of Texas Southwestern Medical School, Dallas, Texas, USA
Harry Howlett
Merck Pharma UK, Harrier House, West Drayton, Middlesex, UB7 7QG, UK, hhowlett{at}merckpharma.co.uk
Current guidelines for the management of type 2 diabetes recommend initiating pharmacological therapy with metformin, particularly in overweight patients, but gastrointestinal side-effects and a complex administration regimen sometimes present barriers to its use. A novel, prolonged-release metformin formulation (Glucophage® SR*), given once-daily in double-blind, randomised, placebo-controlled trials, was associated with fewer gastrointestinal side-effects, than immediate-release metformin. A retrospective review of 468 metformin-treated patients in the USA found better gastrointestinal tolerability with prolonged-release metformin in patients new to metformin, or switched from the immediate-release formulation. The efficacy of the two formulations was similar. The improved tolerability associated with prolonged-release metformin probably arises from the tablet design, which releases metformin into the upper intestine by diffusion from a dual hydrophilic polymer matrix (GelShield diffusion system). This provides slower, smoother and longer drug delivery, without an initial rapid rise in plasma metformin. This novel metformin formulation may simplify the delivery of metformin-based therapy.
Key Words: metformin • type 2 diabetes • oral antidiabetic therapy • prolonged-release formulation • gastrointestinal tolerability • adherence.
References
- Howlett HC, Bailey CJ A risk-benefit assessment of metformin in type 2 diabetes mellitus. Drug Saf 1999;20:489-503.[CrossRef][Web of Science][Medline]
[Order article via Infotrieve]
- Campbell IW, Howlett HC Worldwide experience of metformin as an effective glucose-lowering agent: a meta-analysis. Diabetes Metab Rev 1995;11(suppl 1):S57-S62.[Web of Science][Medline]
[Order article via Infotrieve]
- UK Prospective Diabetes Study (UKPDS) Group. Effect of intensive blood glucose control with metformin on complications in overweight patients with type 2 diabetes (UKPDS 34). Lancet 1998;352:854-65.[CrossRef][Web of Science][Medline]
[Order article via Infotrieve]
- National Institute for Clinical Excellence. Management of type 2 diabetes - Management of blood glucose - NICE summary. Available at National Library for Health website, http://www.nelh.nhs.uk/guidelinesdb/html/fulltext-guidelines/Bloodglucose.html, last accessed by author January 29 2004.
- Davidson JA The treatment of type II diabetes in Texas: current issues for managed care and employers. Diabetes Care 1997;20:44-51.[Medline]
[Order article via Infotrieve]
- Davidson J. Revised standards for the treatment of type 2 diabetes in Texas. Diabetes Care 1999;22:1219-20.[Free Full Text]
- Garber AJ, Duncan TG, Goodman AM, Mills DJ, Rohlf JL Efficacy of metformin in type II diabetes: results of a double-blind, placebo-controlled, dose-response trial. Am J Med 1997;103:491-7.[CrossRef][Web of Science][Medline]
[Order article via Infotrieve]
- Scarpello Jhb. Optimal dosing strategies for maximising the clinical response to metformin in type 2 diabetes. Br J Vasc Dis 2001;1:28-36.
- Paes AHP, Bakker A., Soe-Agnie S-J. Impact of dosage frequency on patient compliance. Diabetes Care 1997;20:1512-17.[Abstract]
- Fujioka K., Bruce S., Joyal S., Swanink R., Pans M. Efficacy, dose-response relationship and safety of once-daily extended-release metformin (Glucophage® XR) in type 2 diabetic patients with inadequate glycemic control despite prior treatment with diet and exercise: results from two double-blind, placebo-controlled studies. Diabetes Obes Metab 2004 (in press).
- DeFronzo RA, Goodman AM Efficacy of metformin in patients with non-insulin dependent diabetes mellitus. N Engl J Med 1995;333:541-9.[Abstract/Free Full Text]
- Fujioka K., Joyal S., Bruce S. Type 2 diabetes patients switched from immediate-release metformin bid to an extended-release qd formulation in a randomized, controlled trial maintain comparable glycemic control. Clin Ther 2003;25:515-29.[CrossRef][Web of Science][Medline]
[Order article via Infotrieve]
- Blonde L., Dailey GE, Jabbour SA, Reasner CA, Mills DJ Gastrointestinal tolerability of extended-release metformin tablets compared to immediate-release metformin tablets - results of a retrospective cohort study. Curr Med Res Opin 2004;20:565-72.[CrossRef][Web of Science][Medline]
[Order article via Infotrieve]
- UK Prospective Diabetes Study (UKPDS) Group. Intensive blood-glucose control with sulphonylureas or insulin compared with conventional treatment and risk of complications in patients with type 2 diabetes (UKPDS 33). Lancet 1998;352:837-53.[CrossRef][Web of Science][Medline]
[Order article via Infotrieve]
- Timmins P., Donahue S., Meeker J., Marathe P. Steady-state pharmacokinetics of a novel extended-release metformin formulation. Clin Pharmacokinet 2004 (in press).
- Marathe P., Turner K. Steady-state pharmacokinetics of the metformin extended-release tablet versus immediate-release metformin in healthy subjects. Diabetes 2002;51(suppl 2):A474.[CrossRef]
The British Journal of Diabetes & Vascular Disease, Vol. 4, No. 4,
273-277 (2004)
DOI: 10.1177/14746514040040041101
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