Glucose-Lowering Medications: Sulfonylureas & Meglitinides

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Questions and Answers

What is the mechanism of action for sulfonylureas?

Block reabsorption of glucose in the kidneys

Increase insulin secretion by closing potassium channels (correct)

Inhibit glucagon release from pancreatic alpha cells

Increase gastric emptying to reduce postprandial glucose levels

Which of the following is a common side effect associated with GLP-1 analogues?

Urinary infections

Weight gain

Nausea (correct)

Dehydration

Which medication inhibits the DPP-4 enzyme?

Sitagliptin (correct)

Nateglinide

Liraglutide

Glipizide

What is a significant contraindication for the use of sulfonylureas?

Renal insufficiency Signup and view all the answers

What is a side effect of sodium-glucose co-transporter 2 inhibitors?

Dehydration and orthostatic hypotension Signup and view all the answers

Which of the following is NOT a characteristic of DPP-4 inhibitors?

They promote weight loss Signup and view all the answers

What is the primary action of GLP-1 analogues related to insulin?

Stimulate insulin secretion only when blood glucose levels are elevated Signup and view all the answers

Which of the following examples is a first-generation sulfonylurea?

Chlorpropamide Signup and view all the answers

Which of the following is considered an effect of sodium-glucose co-transporter 2 inhibitors?

Increased urinary glucose excretion Signup and view all the answers

Which mechanism of action is associated with thionamides?

Blocking of thyroid peroxidase and 5'-deiodinase Signup and view all the answers

What is a key contraindication for the use of methimazole?

Administration during the first trimester of pregnancy Signup and view all the answers

Which medication is used for mineralocorticoid replacement in primary adrenal insufficiency?

Fludrocortisone Signup and view all the answers

Which of the following is a common side effect of levothyroxine?

Heat intolerance Signup and view all the answers

What condition is cinacalcet primarily used to treat?

Hyperparathyroidism in CKD Signup and view all the answers

Which of these medications should not be used concurrently with levothyroxine?

All of the above Signup and view all the answers

Which statement about propylthiouracil (PTU) is correct?

It can be used during the first trimester of pregnancy. Signup and view all the answers

What is the primary action of fludrocortisone in the body?

Reabsorption of sodium in the kidneys Signup and view all the answers

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

Hypocalcemia Signup and view all the answers

Which of the following medications is misused for weight loss?

Levothyroxine Signup and view all the answers

Study Notes

Glucose-Lowering Medications

Sulfonylureas and Meglitinides

Mechanism: Stimulate insulin secretion by closing K+ channels in pancreatic β cells, increasing calcium influx and insulin release.
Side Effects: Hypoglycemia, weight gain, and disulfiram-like reactions with first-generation sulfonylureas.
Contraindications: Risk of hypoglycemia increases with renal insufficiency.
Examples:
- Sulfonylureas (1st Generation): Chlorpropamide, Tolbutamide
- Sulfonylureas (2nd Generation): Glipizide, Glyburide
- Meglitinides: Nateglinide, Repaglinide

GLP-1 Analogues

Mechanism: Mimics the GLP-1 hormone, decreasing glucagon release, delaying gastric emptying, and enhancing glucose-dependent insulin secretion.
Side Effects: Nausea, vomiting, pancreatitis, significant weight loss, and increased satiety.
Examples: Exenatide, Liraglutide, Semaglutide

DPP-4 Inhibitors ("gliptin")

Mechanism: Inhibit Dipeptidyl peptidase-4 enzyme, prolonging GLP-1 action, leading to decreased glucagon, increased insulin secretion, and delayed gastric emptying.
Side Effects: Respiratory and urinary infections, no significant weight change, increased satiety.
Examples: Linagliptin, Saxagliptin, Sitagliptin

Sodium-Glucose Co-transporter 2 Inhibitors

Mechanism: Block glucose reabsorption in renal proximal convoluted tubules, promoting glucose excretion through urine.
Side Effects: Increased risk of urinary tract infections (UTIs), vulvovaginal candidiasis, dehydration, and orthostatic hypotension.

Thyroid Hormone Medications

Thionamides

Mechanism: Inhibit thyroid peroxidase, blocking thyroid hormone synthesis; PTU also inhibits T4 to T3 conversion.
Clinical Use: Treat hyperthyroidism.
Side Effects: Skin rash, agranulocytosis, aplastic anemia, hepatotoxicity, teratogenicity potential.
Examples: Methimazole, Propylthiouracil (PTU)

Levothyroxine and Liothyronine

Mechanism: Synthetic forms of thyroid hormones (T4 and T3).
Clinical Use: Treat hypothyroidism, myxedema, and weight loss.
Side Effects: Tachycardia, heat intolerance, tremors, arrhythmias.
Contraindications: May be affected by antacids, bile acid resins, and ferrous sulfate.

Fludrocortisone (Aldosterone Analogue)

Mechanism: Synthetic mineralocorticoid promoting sodium reabsorption in kidneys; mimics aldosterone's effects.
Clinical Use: Mineralocorticoid replacement in primary adrenal insufficiency.
Side Effects: Fluid retention (edema), heart failure exacerbation, and hyperpigmentation.

Cinacalcet

Mechanism: Activates calcium-sensing receptor in the parathyroid gland, reducing parathyroid hormone synthesis.
Clinical Use: Treats secondary hyperparathyroidism in CKD patients on dialysis and hypercalcemia associated with primary hyperparathyroidism.

Sevelamer

Mechanism: Non-absorbable phosphate binder that prevents phosphate absorption from the gastrointestinal tract.

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Description

This quiz explores the mechanisms of action, clinical uses, side effects, and contraindications of sulfonylureas and meglitinides. Understand how these medications increase insulin secretion and their implications for treatment. Test your knowledge on examples and adverse reactions associated with these drugs.