Comparative Tolerability Profiles of Oral Antidiabetic Agents View Full Text


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Article Info

DATE

1994-10

AUTHORS

Andrew J. Krentz, Robin E. Ferner, Clifford J. Bailey

ABSTRACT

The sulphonylureas and the biguanides are widely used as adjuncts to dietary measures in the treatment of non-insulin-dependent (type 2) diabetes mellitus (NIDDM). Adverse effect profiles differ markedly between the sulphonylureas and biguanides, reflecting differences in chemical structure and mode of action. Sulphonylureas are generally well tolerated, although pharmacokinetic differences between these agents have important clinical implications. The main adverse effect associated with sulphonylureas is hypoglycaemia. This effect is a predictable consequence of the principal pharmacological effect of these drugs, i.e. sensitisation of the islet β-cell to glucose, resulting in enhanced endogenous insulin secretion. Sulphonylurea-induced suppression of hepatic glucose production may cause profound and protracted hypoglycaemia, especially in elderly patients, in individuals with intercurrent illnesses and reduced caloric intake, or when taken in combination with other compounds with hypoglycaemic potential, e.g. alcohol (ethanol). Sulphonylureas with a longer duration of action, notably chlorpropamide and glibenclamide (glyburide), are more liable to induce serious hypoglycaemia, particularly when drug elimination is reduced by renal impairment. Other drugs such as salicylates may potentiate the actions of sulphonylureas, thereby increasing the risk of hypoglycaemia.Biguanide therapy is associated with alterations in lactate homeostasis which under certain clinical circumstances may result in fatal lactic acidosis. Phen-formin is associated with a markedly greater risk of lactic acidosis than metformin. Phenformin has been withdrawn in many countries for this reason. All biguanides must be avoided in patients with renal impairment, hepatic dysfunction and cardiac failure — conditions where drug accumulation or disordered lactate metabolism may predispose to lactic acidosis. Phenformin should not be given to individuals who exhibit a severe, genetically conferred hepatic defect of hydroxylation which impedes metabolism of this drug. Less seriously, the biguanides are associated with a relatively high incidence of gastrointestinal adverse effects which limit compliance.Acarbose, a competitive inhibitor of intestinal α-glucosidases, has recently been introduced. In contrast to the sulphonylureas and biguanides, acarbose has not been associated with life-threatening adverse effects. This reflects the low systemic absorption of the drug and, predictably, its principal unwanted effects are gastrointestinal disturbances resulting from iatrogenic carbohydrate malabsorption. More... »

PAGES

223-241

References to SciGraph publications

  • 1977-04. Comparative effects of phenformin, metformin and glibenclamide on metabolic rhythms in maturity-onset diabetics in DIABETOLOGIA
  • 1984-01. Roles of chlorpropamide, alcohol and acetaldehyde in determining the chlorpropamide-alcohol flush in DIABETOLOGIA
  • 1983-12. Influence of oxidation polymorphism on phenformin kinetics and dynamics in CLINICAL PHARMACOLOGY & THERAPEUTICS
  • 1992-10. The fiftieth anniversary of hypoglycaemic sulphonamides. How did the mother compound work? in DIABETOLOGIA
  • 1983-06. Glibenclamide-associated hypoglycaemia: A report on 57 cases in DIABETOLOGIA
  • 1978-02. Biguanides in DIABETOLOGIA
  • 1978-02. Lactic acidosis in biguanide-treated diabetics in DIABETOLOGIA
  • 1989-01. Sulphonylurea Antidiabetic Drugs in DRUGS
  • 1988-03. Acarbose in DRUGS
  • 1980-03. The crux of the UGDP in DIABETOLOGIA
  • 1983-06. UK prospective study of therapies of maturity-onset diabetes in DIABETOLOGIA
  • 1982-06. Type 2 (non-insulin-dependent) diabetes — An epidemiological overview in DIABETOLOGIA
  • 1991-02. The relationships between dose and concentration of tolbutamide and insulin and glucose responses in patients with non-insulin-dependent diabetes in EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY
  • 1992-10. Safety Profile of Acarbose, an α-Glucosidase Inhibitor in DRUGS
  • 1988. Acarbose Monotherapy in the Treatment of Non-insulin-Dependent Diabetes Mellitus — a Review in ACARBOSE FOR THE TREATMENT OF DIABETES MELLITUS
  • 1988. Toxicology of Acarbose, with Special Reference to Long-term Carcinogenicity Studies in ACARBOSE FOR THE TREATMENT OF DIABETES MELLITUS
  • 1985-11. Sulphonylurea therapy doubles B-cell response to glucose in Type 2 diabetic patients in DIABETOLOGIA
  • 1987-06. The Relationship Between the Pharmacokinetics and Pharmacodynamic Effects of Oral Hypoglycaemic Drugs in CLINICAL PHARMACOKINETICS
  • 1981-09. Clinical Pharmacology of Sulphonylurea Hypoglycaemic Agents: Part 1 in DRUGS
  • Identifiers

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    http://scigraph.springernature.com/pub.10.2165/00002018-199411040-00002

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    41 schema:description The sulphonylureas and the biguanides are widely used as adjuncts to dietary measures in the treatment of non-insulin-dependent (type 2) diabetes mellitus (NIDDM). Adverse effect profiles differ markedly between the sulphonylureas and biguanides, reflecting differences in chemical structure and mode of action. Sulphonylureas are generally well tolerated, although pharmacokinetic differences between these agents have important clinical implications. The main adverse effect associated with sulphonylureas is hypoglycaemia. This effect is a predictable consequence of the principal pharmacological effect of these drugs, i.e. sensitisation of the islet β-cell to glucose, resulting in enhanced endogenous insulin secretion. Sulphonylurea-induced suppression of hepatic glucose production may cause profound and protracted hypoglycaemia, especially in elderly patients, in individuals with intercurrent illnesses and reduced caloric intake, or when taken in combination with other compounds with hypoglycaemic potential, e.g. alcohol (ethanol). Sulphonylureas with a longer duration of action, notably chlorpropamide and glibenclamide (glyburide), are more liable to induce serious hypoglycaemia, particularly when drug elimination is reduced by renal impairment. Other drugs such as salicylates may potentiate the actions of sulphonylureas, thereby increasing the risk of hypoglycaemia.Biguanide therapy is associated with alterations in lactate homeostasis which under certain clinical circumstances may result in fatal lactic acidosis. Phen-formin is associated with a markedly greater risk of lactic acidosis than metformin. Phenformin has been withdrawn in many countries for this reason. All biguanides must be avoided in patients with renal impairment, hepatic dysfunction and cardiac failure — conditions where drug accumulation or disordered lactate metabolism may predispose to lactic acidosis. Phenformin should not be given to individuals who exhibit a severe, genetically conferred hepatic defect of hydroxylation which impedes metabolism of this drug. Less seriously, the biguanides are associated with a relatively high incidence of gastrointestinal adverse effects which limit compliance.Acarbose, a competitive inhibitor of intestinal α-glucosidases, has recently been introduced. In contrast to the sulphonylureas and biguanides, acarbose has not been associated with life-threatening adverse effects. This reflects the low systemic absorption of the drug and, predictably, its principal unwanted effects are gastrointestinal disturbances resulting from iatrogenic carbohydrate malabsorption.
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