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MOA OF DIABETES DRUGS

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40 Questions

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

Increased insulin release from the pancreas

What is the main mechanism of action of GLP-1 Agonists (Incretinmimetics)?

Enhancement of insulin secretion in the presence of glucose

Which of the following is a side effect associated with pioglitazone?

Increased risk of bladder cancer

How does metformin affect fatty acid utilization in cells?

Inhibits cells from utilizing fatty acids as an energy source

Which antidiabetic medication is contraindicated in pregnancy and breastfeeding?

Pioglitazone

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

Nateglinide

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

Acarbose

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

Miglitol

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

Rosiglitazone

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

Pioglitazone

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

Inhibition of hepatic glucose production by inhibiting gluconeogenesis

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

Detemir insulins

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

Metformin

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

Hypoglycemia

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

Degludec

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

Protease

What is the primary effect of Saxagliptin (Onglyza)?

Promotes insulin release

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

Hypertension

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

Linagliptin

What is the mechanism of action of SGLT2 inhibitors?

Inhibit the sodium-glucose transporter type 2 in the kidney

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

To enhance drug absorption

Which adverse effect is NOT associated with SGLT2 inhibitors use?

Hypertension

Which GLP-1 agonist drug is eliminated hepatically?

Liraglutide (Victoza)

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

Pramlintide (Symlin)

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

Semaglutide (Rybelsus)

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

Type-1 diabetic patients who use insulin at mealtime

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

Semaglutide (Ozempic)

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

SGLT2 Inhibitors

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

Nausea

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

Stages 4 and 5

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

Detemir has a peakless 22-hour duration of action, while glargine has a shorter duration of action.

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

They bind to and close the K+ATP channel on pancreatic β-cells.

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

Glyburide

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

Hypoglycemia

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

Detemir requires twice-daily dosing, while degludec is dosed once daily.

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

Biguanides potentiate insulin effects in adipose and muscle tissue, while sulfonylureas bind to and close K+ATP channels on pancreatic β-cells.

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

Glyburide

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

Weight gain

What adverse reactions are rarely associated with sulfonylureas?

Rash/puritis (sulfa allergies)

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

Insulin degludec

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

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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