Diabetes Pharmacology: Insulin and Drugs

Questions and Answers

Which of the following is a short-acting insulin example?

Insulin aspart (correct)

Neutral Protamine Hagedorn (NPH) insulin

Insulin glargine

Insulin detemir

What is the primary mechanism of action of insulin in the body?

Promotes uptake of glucose by cells (correct)

Increases blood glucose levels

Releases glycogen from liver

Inhibits glucose transporters

Which of the following drugs is classified as a long-acting insulin?

Insulin lispro

Insulin Lente

Insulin ultralente (correct)

Insulin aspart

What is NOT a function of insulin in the body?

Enhances gluconeogenesis Signup and view all the answers

Which insulin form is characterized by the longest duration of action?

Insulin glargine Signup and view all the answers

What is a key action of thiazolidinediones in relation to glucose uptake?

Stimulates glucose uptake specifically in adipose and muscle tissue Signup and view all the answers

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

Fractures due to osteoblast impairment Signup and view all the answers

How do thiazolidinediones affect sodium and glomerular filtration rate?

They increase sodium reabsorption and reduce GFR Signup and view all the answers

What hormonal effect does adiponectin have that is mediated by thiazolidinediones?

Stimulates glucose uptake in muscle Signup and view all the answers

What is the primary mechanism of action for SGLT2 inhibitors?

Inhibit glucose reabsorption in the kidney Signup and view all the answers

Which of the following is considered a potential adverse effect of SGLT2 inhibitors?

Mycotic genital infections Signup and view all the answers

Thiazolidinediones are contraindicated in which of the following conditions?

Heart failure Signup and view all the answers

What is a characteristic of α-Glucosidase Inhibitors?

They inhibit carbohydrate breakdown in the gut Signup and view all the answers

Which of the following statements about Dapagliflozin is accurate?

It inhibits SGLT2-mediated glucose reabsorption Signup and view all the answers

How do α-Glucosidase Inhibitors affect post-meal blood sugar levels?

They delay carbohydrate absorption Signup and view all the answers

What is a unique feature of the SGLT2 inhibitors compared to some other diabetes medications?

They lead to urinary glucose excretion Signup and view all the answers

How do AGIs manage postprandial blood glucose levels?

By inhibiting digestive enzymes in the gut Signup and view all the answers

Which of the following diabetes medications carries a risk of increased incidence of certain cancers?

Dapagliflozin Signup and view all the answers

What is the primary indication for α-glucosidase inhibitors such as acarbose?

Management of postprandial hyperglycemia in type 2 diabetes Signup and view all the answers

What side effect is commonly associated with α-glucosidase inhibitors?

Flatulence Signup and view all the answers

Which of the following conditions contraindicates the use of α-glucosidase inhibitors?

Irritable bowel syndrome Signup and view all the answers

How does miglitol function pharmacologically?

Inhibits isomaltase and β-glucosidases Signup and view all the answers

What is the mechanism of action of GLP-1 in patients with type 2 diabetes?

Stimulates insulin release from pancreatic beta cells Signup and view all the answers

What management is recommended for hypoglycemia associated with α-glucosidase inhibitors?

Glucose Signup and view all the answers

Which of these drugs is a Dipeptidyl Peptidase (DPP)-4 inhibitor?

Sitagliptin Signup and view all the answers

What effect does prolonged use of α-glucosidase inhibitors have on gastrointestinal side effects?

They are reduced due to enzyme up-regulation Signup and view all the answers

What is the primary mechanism of action of biguanides like Metformin?

Reduce blood glucose without stimulating insulin secretion Signup and view all the answers

What causes lipoatrophy and lipohypertrophy related to insulin use?

Immune response and fat cell generation Signup and view all the answers

Which of the following describes the pharmacokinetics of NPH insulin?

Slow, even absorption due to protamine and zinc Signup and view all the answers

Which side effect is associated with Metformin use?

Abdominal pain and diarrhea Signup and view all the answers

What is the primary action of sulfonylureas in treating diabetes?

Increase insulin secretion from pancreatic beta cells Signup and view all the answers

What characterizes the pharmacokinetics of second-generation sulfonylureas?

Short half-lives of 3 to 5 hours Signup and view all the answers

What condition is a contraindication for the use of Metformin?

Renal impairment Signup and view all the answers

What aspect of SGLT2 inhibitors contributes to their mechanism of action?

Blocking glucose reabsorption in the proximal tubules Signup and view all the answers

Which of the following side effects is less common with second-generation sulfonylureas compared to first-generation agents?

Weight gain Signup and view all the answers

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

Tolbutamide Signup and view all the answers

What is the role of adenosine monophosphate (AMP) kinase in the action of Metformin?

Inhibits gluconeogenesis Signup and view all the answers

What effect does glucagon have on blood glucose levels?

Increases blood glucose levels by breaking down glycogen Signup and view all the answers

What is the risk associated with the use of first-generation sulfonylureas that is less prominent with second-generation drugs?

Hematologic toxicities Signup and view all the answers

What is the outcome of crystals varying in size on lente insulins?

Slower absorption and prolonged duration Signup and view all the answers

Study Notes

Drugs Used in Diabetes

Various drug classes are used in diabetes management, each with specific mechanisms of action.

Insulin

Forms include Regular insulin, NPH (Intermediate-acting), and Long-acting insulins like Insulin glargine and detemir.
Insulin promotes glucose uptake in cells by mobilizing glucose transporters (GLUT-4).
Increases glycogen storage in liver and muscle; inhibits gluconeogenesis.
Insulin also promotes protein synthesis and fat storage, and interacts with IGF-1 receptors for growth effects.

Pharmacokinetics of Insulin

Delivered mostly subcutaneously, with some formulations available for inhalation.
Variability exists among individuals regarding the peak hypoglycemic effect.
Lente insulins are absorbed slowly due to larger crystal sizes.

Indications and Side Effects of Insulin

Indicated for both Type 1 and Type 2 diabetes.
Common side effects include hypoglycemia, lipodystrophy (lipoatrophy and lipohypertrophy), and edema.

NPH Insulin

NPH is regular insulin modified with protamine and zinc to slow absorption.
Used in diabetes management for its steady effect.

Biguanides

Prototype: Metformin, which reduces blood glucose without stimulating insulin secretion.
Acts by reducing gluconeogenesis and enhancing insulin action through AMP kinase activation.
Helps delay glucose absorption from the gastrointestinal tract.

Pharmacology of Metformin

Excreted unchanged in urine; contraindicated in cases of metabolic acidosis.
Side effects include abdominal discomfort, nausea, diarrhea, and rare instances of lactic acidosis.

Sulfonylureas (SUs)

Oral agents that stimulate insulin secretion from pancreatic beta cells.
First-generation prototype: Tolbutamide; Second-generation prototype: Glyburide.

Mechanism of Action for SUs

Bind to cellular receptors on beta cells, leading to calcium influx and increased insulin release.
Reduce glucagon levels to lower glucose production.

Pharmacokinetics of SUs

Varying half-lives, with first-generation agents generally longer.
All are metabolized by the liver and excreted in urine; dosage adjustment may be necessary in liver impairment.

Indications and Side Effects of SUs

Indicated for Type 2 diabetes; potential hypoglycemia if taken with other agents.
Other side effects may include flushing (older agents), weight gain, and hematologic toxicities.

SGLT2 Inhibitors

Prototypes include Dapagliflozin, working by reducing glucose reabsorption in kidneys.
Actions lead to increased urinary glucose excretion without stimulating insulin secretion.

Adverse Effects of SGLT2 Inhibitors

Fatigue, increased urination, risk of genital/urinary infections, and rare hypoglycemia.

Alpha-Glucosidase Inhibitors (AGIs)

Prototype: Acarbose; reduce blood glucose by delaying carbohydrate absorption in the gut.
They competitively inhibit glucosidases, leading to lower post-meal glucose spikes.

Side Effects and Contraindications of AGIs

Side effects include flatulence, bloating, and diarrhea; contraindicated in IBS and inflammatory bowel disease.

Incretins

Prototypes: DPP-4 inhibitors like sitagliptin and incretin mimetics like exenatide.
Incretin hormones lower blood glucose by stimulating insulin and reducing glucagon.

Thiazolidinediones

Examples include rosiglitazone and pioglitazone; indicated for type 2 diabetes.
Contraindicated in cases of heart failure, with side effects including weight gain, edema, and potential heart issues.

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Description

Explore the various drug classes used in diabetes management with a focus on insulin. Learn about the mechanisms of action, pharmacokinetics, and indications for both Type 1 and Type 2 diabetes. This quiz covers essential concepts for understanding diabetes pharmacology.