2012Expert Opinion on PharmacotherapyRequires access

Combination of glibenclamide–metformin HCl for the treatment of type 2 diabetes mellitus

Elizabeth M. Lamos, Stephanie Aleskow Stein, Stephen N. Davis

Open publisher page 18 citations

Abstract

INTRODUCTION: Combination of glibenclamide (glyburide in the U.S.) and metformin hydrochloride simultaneously addresses two different but complimentary mechanisms to improve glycemic control in type 2 diabetes. AREAS COVERED: The pharmacokinetics, efficacy, and side effect profile of the oral combination of glibenclamide-metformin are reviewed. EXPERT OPINION: Those patients, uncontrolled with single oral agent sulfonylurea or metformin alone, benefit from combination glibenclamide-metformin. There is improvement in fasting plasma glucose, HbA(1C), and post-prandial glucose control, and patients are more likely to achieve a HbA(1C) < 7%. Initiation should be started at the lowest doses and titrated to get the desired effect. Combination therapy allows for reduced pill burden while treating a multifactorial disease by two different mechanisms. Practitioners should be cognizant of risks of hypoglycemia and the theoretical potential for lactic acidosis in the elderly and those with renal impairment. We caution the use of glibenclamide-metformin in patients at risk for cardiovascular disease. Therapy should be individualized, but overall, combination of glibenclamide-metformin should be considered in patients, without renal or cardiovascular impairment, who are not controlled on monotherapy alone. Alternatively, practitioners may want to weigh the efficacy and safety of available dipeptidyl-peptidase-4 inhibitor-metformin combinations to those of glibenclamide-metformin when considering combination therapy.

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What this paper is about

INTRODUCTION: Combination of glibenclamide (glyburide in the U.S.) and metformin hydrochloride simultaneously addresses two different but complimentary mechanisms to improve glycemic control in type 2 diabetes. AREAS COVERED: The pharmacokinetics, efficacy, and side effect profile of the oral combination of glibenclamide-metformin are reviewed. EXPERT OPINION: Those patients, uncontrolled with single oral agent sulfonylurea or metformin alone, benefit from combination glibenclamide-metformin. There is improvement in fasting plasma glucose, HbA(1C), and post-prandial glucose control, and patients are more likely to achieve a HbA(1C) < 7%. Initiation should be started at the lowest doses and titrated to get the desired effect. Combination therapy allows for reduced pill burden while treating a multifactorial disease by two different mechanisms. Practitioners should be cognizant of risks of hypoglycemia and the theoretical potential for lactic acidosis in the elderly and those with renal impairment. We caution the use of glibenclamide-metformin in patients at risk for cardiovascular disease. Therapy should be individualized, but overall, combination of glibenclamide-metformin should be considered in patients, without renal or cardiovascular impairment, who are not controlled on monotherapy alone. Alternatively, practitioners may want to weigh the efficacy and safety of available dipeptidyl-peptidase-4 inhibitor-metformin combinations to those of glibenclamide-metformin when considering combination therapy.

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Available abstract

INTRODUCTION: Combination of glibenclamide (glyburide in the U.S.) and metformin hydrochloride simultaneously addresses two different but complimentary mechanisms to improve glycemic control in type 2 diabetes. AREAS COVERED: The pharmacokinetics, efficacy, and side effect profile of the oral combination of glibenclamide-metformin are reviewed. EXPERT OPINION: Those patients, uncontrolled with single oral agent sulfonylurea or metformin alone, benefit from combination glibenclamide-metformin. There is improvement in fasting plasma glucose, HbA(1C), and post-prandial glucose control, and patients are more likely to achieve a HbA(1C) < 7%. Initiation should be started at the lowest doses and titrated to get the desired effect. Combination therapy allows for reduced pill burden while treating a multifactorial disease by two different mechanisms. Practitioners should be cognizant of risks of hypoglycemia and the theoretical potential for lactic acidosis in the elderly and those with renal impairment. We caution the use of glibenclamide-metformin in patients at risk for cardiovascular disease. Therapy should be individualized, but overall, combination of glibenclamide-metformin should be considered in patients, without renal or cardiovascular impairment, who are not controlled on monotherapy alone. Alternatively, practitioners may want to weigh the efficacy and safety of available dipeptidyl-peptidase-4 inhibitor-metformin combinations to those of glibenclamide-metformin when considering combination therapy.

Key concepts: Glibenclamide, Metformin, Medicine, Gliclazide, Type 2 diabetes, Diabetes mellitus, Sulfonylurea, Hypoglycemia

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