Oral Antidiabetic Drugs: Classes and Mechanisms
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Questions and Answers

What is the primary advantage of metformin over insulin or sulfonylureas in treating hyperglycemia?

  • It increases weight
  • It provokes hypoglycemia
  • It is more expensive
  • It is an insulin-sparing agent and does not increase weight or provoke hypoglycemia (correct)

    • What is the effect of metformin therapy on macrovascular disease?

  • It increases the risk
  • It has no effect
  • It decreases the risk (correct)
  • It is still unknown

    • What is the mechanism of action of thiazolidinediones (Tzds)?

  • Inhibition of peroxisome proliferator-activated receptor-gamma (PPAR-γ)
  • Inhibition of glucose metabolism
  • Activation of peroxisome proliferator-activated receptor-gamma (PPAR-γ) (correct)
  • Stimulation of insulin secretion

    • What is the effect of metformin on the absorption of vitamin B12?

    <p>It may interfere with the absorption</p> Signup and view all the answers

    What is the primary action of thiazolidinediones (Tzds)?

    <p>Nuclear regulation of genes involved in glucose and lipid metabolism and adipocyte differentiation</p> Signup and view all the answers

    What is the indication of metformin in combination with insulin secretagogues or thiazolidinediones?

    <p>Type 2 diabetes in whom oral monotherapy is inadequate</p> Signup and view all the answers

    What is the effect of metformin on the prevention of type 2 diabetes?

    <p>It is efficacious in preventing the new onset of type 2 diabetes</p> Signup and view all the answers

    What is the commonest unwanted effect of metformin?

    <p>Dose-related gastrointestinal disturbances</p> Signup and view all the answers

    What is the underlying reason for secondary failure to sulfonylurea therapy in type 2 diabetes?

    <p>Progressive decrease in B-cell mass</p> Signup and view all the answers

    Which of the following drugs can displace sulfonylureas from protein binding sites?

    <p>Salicylates</p> Signup and view all the answers

    What is the mechanism of action of alpha glucosidase inhibitors like acarbose and miglitol?

    <p>Competitive inhibition of intestinal alpha glucosidase</p> Signup and view all the answers

    What is the recommended timing of taking alpha glucosidase inhibitors like acarbose and miglitol?

    <p>Just prior to ingesting the first portion of a meal</p> Signup and view all the answers

    What is a contraindication for the use of alpha glucosidase inhibitors like acarbose and miglitol?

    <p>Inflammatory bowel disease</p> Signup and view all the answers

    What is a potential adverse effect of alpha glucosidase inhibitors like acarbose and miglitol when used with sulfonylureas?

    <p>Hypoglycemia</p> Signup and view all the answers

    What is the effects of alpha glucosidase inhibitors like acarbose and miglitol on the absorption of starches and disaccharides?

    <p>Reduce the absorption of starches and disaccharides</p> Signup and view all the answers

    What is the approved use of alpha glucosidase inhibitors like acarbose and miglitol?

    <p>In combination with sulfonylureas for type 2 diabetes</p> Signup and view all the answers

    What is the effect of Acarbose on hepatic enzyme levels?

    <p>Reversible elevation</p> Signup and view all the answers

    What is the primary function of GIP in the body?

    <p>Stimulating glucose-dependent insulin release</p> Signup and view all the answers

    What is the effect of dipeptidyl peptidase-4 on incretins?

    <p>Rapidly degrades active incretins</p> Signup and view all the answers

    What is the difference between GLP-1 and GIP in terms of their secretion site?

    <p>GLP-1 is secreted by the distal GI tract, while GIP is secreted by the proximal GI tract</p> Signup and view all the answers

    What is the effect of Exenatide on insulin release?

    <p>Increases insulin release</p> Signup and view all the answers

    What is the effect of Sitaglaptin on endogenous incretins?

    <p>Increases their activity by inhibiting dipeptidyl peptidase-4</p> Signup and view all the answers

    What is the characteristic of GLP-1 in type 2 diabetes?

    <p>Levels are decreased</p> Signup and view all the answers

    What is the difference between the insulinotropic response to GLP-1 and GIP in type 2 diabetes?

    <p>GIP response is diminished but not absent, while GLP-1 response is absent</p> Signup and view all the answers

    What is the effect of PPAR-γ activation on insulin sensitivity in adipocytes, hepatocytes, and skeletal muscle?

    <p>Increased insulin sensitivity</p> Signup and view all the answers

    Which of the following is a characteristic of thiazolidinediones?

    <p>Slow onset and offset of activity over weeks or months</p> Signup and view all the answers

    What is the effect of pioglitazone on triglyceride levels compared to rosiglitazone?

    <p>More significant triglyceride-lowering effect</p> Signup and view all the answers

    What is a common adverse effect of thiazolidinediones, especially when used with insulin or insulin secretagogues?

    <p>Fluid retention</p> Signup and view all the answers

    Which of the following is a contraindication for thiazolidinedione use?

    <p>All of the above</p> Signup and view all the answers

    What is the average weight gain associated with thiazolidinedione use?

    <p>1-3 kg</p> Signup and view all the answers

    What is the effect of thiazolidinediones on HDL levels?

    <p>Increased HDL levels</p> Signup and view all the answers

    What percentage of new users respond to thiazolidinedione therapy?

    <p>70%</p> Signup and view all the answers

    What is the mechanism of action of metformin in reducing glucose absorption from the GIT?

    <p>Increased glucose to lactate conversion by enterocytes</p> Signup and view all the answers

    What is the consequence of metformin's blockade of gluconeogenesis?

    <p>Impaired hepatic metabolism of lactic acid</p> Signup and view all the answers

    Which of the following classes of oral antidiabetic drugs slow the absorption of starches?

    <p>Alpha-glucosidase inhibitors</p> Signup and view all the answers

    What is the primary mechanism of action of biguanides in reducing hepatic glucose production?

    <p>Reduced gluconeogenesis and glycogenolysis</p> Signup and view all the answers

    Which of the following drugs is not classified as an insulin secretagogue?

    <p>Metformin</p> Signup and view all the answers

    What is the primary mechanism of action of thiazolidinediones in reducing glucose levels?

    <p>Increased glucose uptake by adipose tissues</p> Signup and view all the answers

    What is the characteristic of metformin's excretion?

    <p>It is excreted by the kidneys as the active compound</p> Signup and view all the answers

    What is the risk associated with metformin use in patients with renal insufficiency?

    <p>Increased risk of lactic acidosis</p> Signup and view all the answers

    Study Notes

    Classes of Oral Antidiabetic Drugs

    • Drugs that sensitize the body to insulin and/or control hepatic glucose production
      • Biguanides (e.g., metformin)
        • Mechanism of action: direct stimulation of glycolysis, reduced hepatic and renal gluconeogenesis, slowing of glucose absorption from the GIT, and reduction of plasma glucagon levels
        • Metabolism and excretion: half-life of 1.5-3 hours, not bound to plasma proteins, not metabolized, and excreted by the kidneys as the active compound
        • Clinical use: first-line drug for the treatment of type II DM, decreases the risk of macrovascular and microvascular disease, and useful in preventing the new onset of type 2 diabetes
      • Thiazolidinediones (Tzds) (e.g., pioglitazone and rosiglitazone)
        • Mechanism of action: activates peroxisome proliferator-activated receptor-gamma (PPAR-γ), decreases insulin resistance, and regulates genes involved in glucose and lipid metabolism
        • Clinical use: decreases the risk of macrovascular and microvascular disease, improves hyperglycemia, hypertriglyceridemia, and elevated HbA1c
        • Adverse effects: fluid retention, weight gain, and increased risk of heart failure
    • Drugs that stimulate the pancreas to make more insulin (Insulin secretagogues)
      • Sulfonylureas
        • Mechanism of action: stimulates insulin release from pancreatic beta cells
        • Secondary failure: caused by progressive decrease in B-cell mass, reduction in physical activity, decline in lean body mass, and increase in ectopic fat deposition
        • Important drug interactions: displacement from protein binding sites, interference with hepatic metabolism, and reduction of renal elimination
    • Drugs that slow the absorption of starches
      • Alpha Glucosidase Inhibitors (e.g., acarbose and miglitol)
        • Mechanism of action: competitive inhibitors of intestinal alpha glucosidase, reducing the postprandial digestion and absorption of starch and disaccharides
        • Clinical use: approved for use in individuals with type 2 diabetes as monotherapy and in combination with sulfonylureas
        • Adverse effects: hypoglycemia, gas, and distention, and reversible hepatic enzyme elevation
    • Incretin Therapy
      • Incretins: naturally occurring hormones released by the gut, including GLP-1 and GIP
        • Physiologic activity: stimulates glucose-dependent insulin release, decreases glucagon production, and increases satiety
        • Diminished in type 2 diabetes: levels of GLP-1 are decreased, and insulinotropic response to GIP is diminished
      • Exenatide: synthetic analogue of GLP-1, used to increase insulin release
      • Sitaglaptin: drug that inhibits dipeptidyl peptidase-4, allowing endogenous incretins to act longer
    • Sodium Glucose Cotransporter 2 Inhibitors (SGLT-2)
      • Canagliflozin, Empagliflozin, and Dapagliflozin: drugs that inhibit SGLT-2, reducing glucose reabsorption in the kidneys and increasing glucose excretion in the urine

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    Description

    Learn about the different classes of oral antidiabetic drugs, their mechanisms of action, and metabolism. This quiz covers biguanides, such as metformin, and their effects on glucose production and absorption.

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