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

Which antidiabetic medication is contraindicated in pregnancy and breastfeeding?

<p>Pioglitazone (A)</p> Signup and view all the answers

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

<p>Nateglinide (D)</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 (D)</p> Signup and view all the answers

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

<p>Miglitol (D)</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 (D)</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 (A)</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 (A)</p> Signup and view all the answers

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

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

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

<p>Metformin (C)</p> Signup and view all the answers

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

<p>Hypoglycemia (B)</p> Signup and view all the answers

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

<p>Degludec (B)</p> Signup and view all the answers

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

<p>Protease (A)</p> Signup and view all the answers

What is the primary effect of Saxagliptin (Onglyza)?

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

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

<p>Hypertension (D)</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 (B)</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 (B)</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 (B)</p> Signup and view all the answers

Which adverse effect is NOT associated with SGLT2 inhibitors use?

<p>Hypertension (B)</p> Signup and view all the answers

Which GLP-1 agonist drug is eliminated hepatically?

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

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

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

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

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

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

<p>Nausea (B)</p> Signup and view all the answers

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

<p>Stages 4 and 5 (A)</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. (A)</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. (B)</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 (C)</p> Signup and view all the answers

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

<p>Hypoglycemia (C)</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. (C)</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. (A)</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 (B)</p> Signup and view all the answers

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

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

What adverse reactions are rarely associated with sulfonylureas?

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

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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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