MOA OF DIABETES DRUGS
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Questions and Answers

Which of the following is NOT a known effect of metformin?

  • Reduction of serum glucose levels
  • Fluid retention
  • Increased insulin release from the pancreas (correct)
  • Reduced transcription of leptin
  • What is the main mechanism of action of GLP-1 Agonists (Incretinmimetics)?

  • Enhancement of insulin secretion in the presence of glucose (correct)
  • Inhibition of insulin secretion
  • Enhancement of fatty acid utilization
  • Stimulation of glucagon release
  • Which of the following is a side effect associated with pioglitazone?

  • Reduced subcutaneous fat
  • Increased risk of bladder cancer (correct)
  • Decreased risk of bone fractures
  • Enhanced leptin transcription
  • How does metformin affect fatty acid utilization in cells?

    <p>Inhibits cells from utilizing fatty acids as an energy source</p> Signup and view all the answers

    Which antidiabetic medication is contraindicated in pregnancy and breastfeeding?

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

    Which medication can lower HbA1c by approximately 0.8% when used as monotherapy?

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

    Which medication prevents sucrose breakdown into glucose, making only glucose or dextrose usable during a hypoglycemic episode?

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

    Which medication is contraindicated in patients with irritable bowel syndrome (IBS) and obstruction?

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

    Which medication increases the effectiveness of insulin and can reduce the amount of external insulin required by 30%?

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

    Which medication has a slow onset of approximately 2 months for maximum effect and requires regular liver function tests?

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

    What is the main mechanism of action of Biguanides like metformin?

    <p>Inhibition of hepatic glucose production by inhibiting gluconeogenesis</p> Signup and view all the answers

    Which insulin has a peakless duration of action greater than 42 hours?

    <p>Detemir insulins</p> Signup and view all the answers

    Which of the following hypoglycemic agents is suitable for patients with sulfa allergy?

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

    What is the main adverse effect associated with Nateglinide (Starlix) use?

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

    Which of the following medications can be mixed with rapid-acting insulins without altering kinetics?

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

    Which enzyme do Dipeptidyl-peptidase-4 (DPP4) Inhibitors inhibit?

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

    What is the primary effect of Saxagliptin (Onglyza)?

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

    What side effect is NOT commonly associated with DPP-4 inhibitors?

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

    Which DPP-4 inhibitor can be used in all stages of renal impairment without dose adjustment?

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

    What is the mechanism of action of SGLT2 inhibitors?

    <p>Inhibit the sodium-glucose transporter type 2 in the kidney</p> Signup and view all the answers

    Why is it important to take other drugs at least 1 hour before or 2 hours after the administration of Linagliptin (Tradjenta)?

    <p>To enhance drug absorption</p> Signup and view all the answers

    Which adverse effect is NOT associated with SGLT2 inhibitors use?

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

    Which GLP-1 agonist drug is eliminated hepatically?

    <p>Liraglutide (Victoza)</p> Signup and view all the answers

    Which drug acts by slowing gastric emptying, suppressing post-prandial glucagon concentration, and increasing satiety?

    <p>Pramlintide (Symlin)</p> Signup and view all the answers

    Which GLP-1 agonist is available as an oral formulation?

    <p>Semaglutide (Rybelsus)</p> Signup and view all the answers

    What is the main indication for Pramlintide (Symlin) use?

    <p>Type-1 diabetic patients who use insulin at mealtime</p> Signup and view all the answers

    Which GLP-1 receptor agonist is specifically marketed as a treatment for obesity?

    <p>Semaglutide (Ozempic)</p> Signup and view all the answers

    Which drug class is associated with an increased risk of heart failure, particularly in patients with preexisting heart or kidney disease?

    <p>SGLT2 Inhibitors</p> Signup and view all the answers

    Which adverse effect is a common side effect of GLP-1 agonist drugs?

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

    In which CKD stages are liraglutide, albiglutide, and dulaglutide contraindicated?

    <p>Stages 4 and 5</p> Signup and view all the answers

    What is the key difference between insulin detemir (Levemir) and glargine in terms of duration of action?

    <p>Detemir has a peakless 22-hour duration of action, while glargine has a shorter duration of action.</p> Signup and view all the answers

    What is the mechanism of action for sulfonylureas like glyburide (Micronase)?

    <p>They bind to and close the K+ATP channel on pancreatic β-cells.</p> Signup and view all the answers

    Which medication should not be used in patients with renal or liver failure due to its metabolism and excretion profile?

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

    What is the main adverse effect associated with sulfonylureas like glyburide?

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

    How does insulin degludec (Tresiba) differ from insulin detemir (Levemir) in terms of dosing?

    <p>Detemir requires twice-daily dosing, while degludec is dosed once daily.</p> Signup and view all the answers

    What is the primary difference between the mechanism of action of biguanides like metformin and sulfonylureas like glyburide?

    <p>Biguanides potentiate insulin effects in adipose and muscle tissue, while sulfonylureas bind to and close K+ATP channels on pancreatic β-cells.</p> Signup and view all the answers

    Which medication is 100 times more potent than 1st generation agents in terms of hypoglycemic effects?

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

    What side effect is common to both 1st and 2nd generation sulfonylureas?

    <p>Weight gain</p> Signup and view all the answers

    What adverse reactions are rarely associated with sulfonylureas?

    <p>Rash/puritis (sulfa allergies)</p> Signup and view all the answers

    Which medication's weakly active metabolites are excreted by the kidney, leading to a higher incidence of hypoglycemia in elderly patients with kidney disease?

    <p>Insulin degludec</p> Signup and view all the answers

    Study Notes

    Thiazolidinediones (TZDs)

    • Also known as "glitazones"
    • Examples: Rosiglitazone (Avandia), Pioglitazone (Actos)
    • Increase tissue insulin sensitivity
    • Enhance insulin-dependent uptake of fatty acids and glucose from plasma into fat/muscle
    • Can cause weight gain (2-10 lbs), fluid retention, and increased incidence of CHF
    • May increase risk of bladder cancer with pioglitazone
    • Can cause GI disturbances, fatigue, headache, and increased risk of bone fractures in women
    • Contraindicated in pregnancy and breast-feeding

    GLP-1 Agonists (Incretin Mimetics)

    • Examples: Exenatide (Byetta), Liraglutide (Victoza), Dulaglutide (Trulicity), Lixisenatide (Adlyxin), Semaglutide (Ozempic), Tirzepatide (Mounjaro)
    • Enhance secretion of insulin in the presence of glucose
    • Slow the rate of absorption of glucose and other nutrients by delaying gastric emptying
    • Reduce appetite and inhibit glucagon release
    • Stimulate beta cell differentiation and proliferation
    • Do not affect glucose, lactose, or fructose absorption

    Biguanides

    • Example: Metformin
    • Decrease hepatic glucose production by inhibiting gluconeogenesis
    • Activate AMP-dependent kinase (AMPK) which inhibits the expression of hepatic gluconeogenic genes
    • Used orally, QD, for diabetes treatment
    • Can cause GI upset, diarrhea, and lactic acidosis in rare cases

    Meglitinides

    • Examples: Repaglinide (Prandin), Nateglinide (Starlix)
    • Hypoglycemic agents that stimulate insulin release by closing K+ ATP channel
    • Used before meals to reduce post-prandial glucose levels
    • Can cause weight gain, GI upset, headache, and hypoglycemia

    Dipeptidyl-Peptidase-4 (DPP-4) Inhibitors

    • Examples: Sitagliptin (Januvia), Saxagliptin (Onglyza), Linagliptin (Tradjenta), Alogliptin (Nesina)
    • Inhibit the metabolism of endogenous GLP-1 and GIP, increasing their duration of effectiveness
    • Used as add-on therapy for type 2 diabetes
    • Can cause angioedema, urticaria, localized skin exfoliation, bronchial hyperreactivity, and runny nose

    Insulin

    • Examples: Detemir (Levemir), Degludec (Tresiba), Glipizide (Glucotrol), Glimepiride (Amaryl)
    • Hypoglycemic agents that stimulate insulin release by closing K+ ATP channel
    • Used for diabetes treatment, can cause weight gain, hypoglycemia, and hypersensitivity reactions

    SGLT2 Inhibitors

    • Examples: Canagliflozin (Invokana), Ertugliflozin (Steglatro), Dapagliflozin (Farxiga), Empagliflozin (Jardiance), Bexagliflozin (Brenzavvy)
    • Inhibit the sodium-glucose transporter type 2 (SGLT2) in the proximal tubule of the kidney
    • Increase urinary glucose excretion, causing weight loss and reducing HbA1c
    • Can cause genital yeast infections, urinary tract infections, and volume depletion

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    Description

    Learn about the impact of weight gain on insulin release, glucose levels, and appetite regulation. Understand how weight gain leads to fluid retention, activation of PPAR-γ, and changes in transcription factors involved in fat storage and energy production.

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