SGLT-2 Inhibitors Overview
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Questions and Answers

What is a contraindication for SGLT-2 inhibitors?

  • Type 2 diabetes
  • High cholesterol
  • DKA or type 1 diabetes (correct)
  • Hypertension

Which of the following is an adverse effect associated with thiazolidinediones?

  • Upper respiratory infections (correct)
  • Dehydration
  • Nausea
  • Hypoglycemia

What therapeutic action do GLP-1 agonists primarily perform?

  • Increase insulin release (correct)
  • Increase glucagon release
  • Accelerate gastric emptying
  • Decrease insulin release

Which drug should not be taken with gemfibrozil?

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

What therapy is indicated for the treatment of hypoglycemia?

<p>Glucose-elevating agents (A)</p> Signup and view all the answers

Which class of medications is primarily effective in decreasing insulin resistance?

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

What is an important caution when using human amylin?

<p>Decrease insulin dosing when starting (A)</p> Signup and view all the answers

A patient with type 1 diabetes should avoid which therapeutic agents?

<p>GLP-1 agonists (B), SGLT-2 inhibitors (C)</p> Signup and view all the answers

Which adverse effect is associated with SGLT-2 inhibitors?

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

What is the primary indication for GLP-1 agonists?

<p>Managing type 2 diabetes (A)</p> Signup and view all the answers

What action do glucose-elevating agents perform?

<p>Increase blood glucose levels (B)</p> Signup and view all the answers

What precaution should be taken concerning thiazolidinediones?

<p>Monitor liver function (C)</p> Signup and view all the answers

Which of the following is a major adverse effect of GLP-1 agonists?

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

Which of these agents requires monitoring for severe renal impairment before administration?

<p>SGLT-2 inhibitors (D)</p> Signup and view all the answers

Which sign or symptom is commonly associated with hyperglycemia?

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

What is the primary action of insulin in the body?

<p>Transportation of glucose into cells (B)</p> Signup and view all the answers

In which scenario is the use of sulfonylureas contraindicated?

<p>History of allergy to sulfonylureas (D)</p> Signup and view all the answers

What potential adverse effect can occur from the use of insulin?

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

Which of the following correctly describes the indications for insulin use?

<p>For both type 1 and type 2 diabetes, if other treatments fail (A)</p> Signup and view all the answers

What effect do thiazide diuretics have when used with insulin?

<p>They increase blood glucose levels (C)</p> Signup and view all the answers

What is a main therapeutic action of sulfonylureas?

<p>Stimulate insulin release from pancreatic beta cells (C)</p> Signup and view all the answers

Which of the following is NOT a common symptom of hyperglycemia?

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

How are sulfonylureas metabolized in the body?

<p>Rapidly absorbed and undergo hepatic metabolism (A)</p> Signup and view all the answers

Which statement accurately depicts a caution for using insulin?

<p>Consideration must be given during pregnancy and lactation (A)</p> Signup and view all the answers

What advantage do second-generation sulfonylureas have over first-generation sulfonylureas?

<p>They do not interact with as many protein-bound drugs. (A)</p> Signup and view all the answers

In which scenario would alpha-glucosidase inhibitors be indicated?

<p>In combination with other agents for uncontrolled glucose levels. (B)</p> Signup and view all the answers

What is a key therapeutic action of biguanides?

<p>Decrease hepatic glucose production. (B)</p> Signup and view all the answers

What potential adverse effect is associated with the use of biguanides?

<p>Lactic acidosis. (D)</p> Signup and view all the answers

Which statement is true regarding DPP-4 inhibitors?

<p>They slow the inactivation of incretin hormones. (A)</p> Signup and view all the answers

What is a common side effect associated with meglitinides?

<p>Upper respiratory infection. (A)</p> Signup and view all the answers

Which of the following is a contraindication for using alpha-glucosidase inhibitors?

<p>History of GI disorders. (C)</p> Signup and view all the answers

Why should caution be exercised when administering biguanides?

<p>Risk of lactic acidosis in certain patients. (D)</p> Signup and view all the answers

What indicates the need for immediate assessment in a patient taking DPP-4 inhibitors?

<p>Signs of pancreatitis. (D)</p> Signup and view all the answers

Which adverse effect is more common with alpha-glucosidase inhibitors?

<p>GI effects. (B)</p> Signup and view all the answers

What is a principal therapeutic action of meglitinides?

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

What constitutes a contraindication for DPP-4 inhibitors?

<p>History of pancreatitis. (B)</p> Signup and view all the answers

What is a key pharmacokinetic property of biguanides?

<p>Not metabolized and excreted primarily in urine. (A)</p> Signup and view all the answers

What should be monitored in patients taking alpha-glucosidase inhibitors?

<p>HbA1c levels. (C)</p> Signup and view all the answers

Study Notes

Gemfibrozil

  • Should not be administered with repaglinide

Meglitinide Prototype

  • Not specified in text

SGLT-2 Inhibitors

  • Block cotransporter system so glucose is not reabsorbed but lost in urine
  • Used as an adjunct to diet and exercise to treat Type 2 diabetes
  • Research is ongoing regarding benefits and risks in Type 1 diabetes
  • Absorbed from the GI tract
  • Metabolized in the liver and excreted via kidneys and feces

Contraindications for SGLT-2 Inhibitors

  • DKA or type 1 diabetes
  • Severe renal impairment
  • Second or third trimester of pregnancy

Cautions for SGLT-2 Inhibitors

  • Patients should not breast or chestfeed

Adverse Effects of SGLT-2 Inhibitors

  • Dehydration and hypotension
  • UTIs and genital fungal infections
  • DKA
  • Canagliflozin:
    • Loss of bone density
    • Bone fractures
  • Lower limb amputation

Drug-Drug Interactions with SGLT-2 Inhibitors

  • Medications that enhance metabolism of SGLT-2 inhibitors

Thiazolidinediones

  • Decrease insulin resistance in peripheral cells and liver
  • Increase responsiveness to insulin
  • Used as an adjunct to diet and exercise to lower blood glucose in type 2 diabetes
  • Absorbed orally
  • Metabolized by the liver and excreted via kidneys and feces

Contraindications for Thiazolidinediones

  • Moderate or severe heart failure

Cautions for Thiazolidinediones

  • Monitor for changes in liver function

Adverse Effects of Thiazolidinediones

  • Upper respiratory infections
  • Headaches
  • Muscle pains
  • Increased total cholesterol
  • Rare: hepatic injury
  • Rapid weight gain and edema due to fluid retention

Drug-Drug Interactions with Thiazolidinediones

  • Insulin
  • CYP2C8 inhibitors

Human Amylin

  • Slows gastric emptying
  • Suppresses glucagon secretion from the liver
  • Regulates food intake by modulating appetite
  • Used in patients with both type 1 and type 2 diabetes who are also treated with insulin
  • Rapid onset of action; peaks in 20 minutes
  • Should be injected before each major meal

Contraindications for Human Amylin

  • Hypersensitivity
  • Gastroparesis

Cautions for Human Amylin

  • When starting, insulin dosing should be decreased

Adverse Effects of Human Amylin

  • Nausea, vomiting, anorexia, headache, injection site reactions
  • Severe hypoglycemia

Drug-Drug Interactions with Human Amylin

  • Pramlintide and insulin or other antidiabetic medications
  • Absorption of oral medications may be inhibited
  • Gastric-slowing medications (e.g., opioids)

GLP-1 Agonists

  • Increase insulin release
  • Decrease glucagon release
  • Slow GI emptying
  • Used as an adjunct to diet and exercise for people with type 2 diabetes
  • Some are used to reduce the risk of major CV events in people with type 2 diabetes and CV disease

Pharmacokinetics of GLP-1 Agonists

  • Most are administered via subcutaneous injection
  • Metabolism and excretion vary

Contraindications for GLP-1 Agonists

  • Liraglutide and semaglutide: boxed warnings for risk of thyroid C-cell tumors in animals
  • Type 1 diabetes or DKA
  • Pregnancy and breast or chestfeeding

Adverse Effects of GLP-1 Agonists

  • Pancreatitis
  • GI effects

Drug-Drug Interactions with GLP-1 Agonists

  • Oral medications: effects may be slowed
  • Other antidiabetic agents

Glucose-Elevating Agents

  • Increase blood glucose levels by decreasing insulin release and accelerating the breakdown of glycogen in the liver to release glucose
  • Used in treatment of hypoglycemia
  • Rapidly absorbed and widely distributed throughout the body
  • Excreted in the urine

Contraindications for Glucose-Elevating Agents

  • Diazoxide:
    • Known allergies to sulfonamides or thiazides
    • Pregnancy
  • Glucagon: No adequate studies on pregnancy

Cautions for Glucose-Elevating Agents

  • Lactation
  • Hepatic dysfunction or CV disease

Adverse Effects of Glucose-Elevating Agents

  • Glucagon and dasiglucagon: GI upset, nausea, vomiting
  • Diazoxide: vascular effects

Drug-Drug Interactions with Glucose-Elevating Agents

  • Diazoxide: thiazide diuretics
  • Glucagon and dasiglucagon: oral anticoagulants

Alpha-Glucosidase Inhibitors

  • Inhibit alpha-glucosidase, which breaks down glucose for absorption
  • Delay absorption of glucose
  • Assist in lowering HbA1c levels
  • Used in combination with other agents for people whose glucose levels cannot be controlled with a single agent or with diet and exercise alone

Pharmacokinetics of Alpha-Glucosidase Inhibitors

  • Absorbed orally at variable amounts
  • Acarbose metabolized in the GI tract; miglitol excreted without being metabolized
  • Excreted by kidneys

Contraindications for Alpha-Glucosidase Inhibitors

  • Known hypersensitivity
  • DKA
  • GI disorders
  • Acarbose: cirrhosis

Cautions for Alpha-Glucosidase Inhibitors

  • Renal impairment

Adverse Effects of Alpha-Glucosidase Inhibitors

  • GI effects
  • Anemia

Drug-Drug Interactions for Alpha-Glucosidase Inhibitors

  • Other glucose-lowering agents
  • Medications that increase blood glucose

Biguanides

  • Decreases production and increases uptake of glucose
  • Lowers both basal and postprandial blood glucose levels
  • Decreases hepatic glucose production
  • Improves insulin sensitivity of peripheral cells
  • First-line standard of care for people with type 2 diabetes

Pharmacokinetics of Biguanides

  • Absorbed orally
  • Not metabolized; excreted primarily in urine
  • Absorption and elimination times vary based on type of formulation

Contraindications for Biguanides

  • Known hypersensitivity reactions
  • Metabolic acidosis
  • Severe renal impairment

Cautions for Biguanides

  • Hepatic impairment
  • Excessive alcohol intake
  • Patients not eating/drinking due to surgery
  • Patients undergoing radiologic studies with contrast
  • Age 65 years or older
  • Hypoxic state

Adverse Effects of Biguanides

  • Boxed warning: lactic acidosis
  • GI side effects
  • Dizziness
  • Headaches
  • Upper respiratory infection
  • Taste disturbance

Drug-Drug Interactions with Biguanides

  • Alcohol use
  • Carbonic anhydrase
  • Iodine-containing contrast media
  • Check drug interactions before administrating

DPP-4 Inhibitors

  • Slow inactivation of incretin hormones
  • Increase insulin release
  • Lower glucagon secretion
  • Used as an adjunct to diet and exercise to lower blood glucose levels in patients with type 2 diabetes

Pharmacokinetics for DPP-4 Inhibitors

  • Rapidly absorbed
  • Peak effects in 1 to 5 hours
  • Metabolism can vary
  • Excretion primarily via kidneys

Contraindications for DPP-4 Inhibitors

  • DKA or type 1 diabetes
  • History of severe hypersensitivity reactions

Cautions for DPP-4 Inhibitors

  • Renal impairment

Adverse Effects of DPP-4 Inhibitors

  • Most people do not report adverse effects
  • Rare: pancreatitis, heart failure, severe arthralgia, hypersensitivity reactions, exfoliative skin conditions

Drug-Drug Interactions for DPP-4 Inhibitors

  • Other medications that lower blood glucose
  • May be other drug interactions based on individual drug’s metabolism

Meglitinides

  • Similar to sulfonylureas
  • Used as an adjunct to diet and exercise in treatment of type 2 diabetes
  • Rapidly absorbed
  • Extensively metabolized by liver
  • Quickly eliminated by kidneys

Contraindications for Meglitinides

  • Type 1 diabetes or DKA
  • Known hypersensitivity

Cautions for Meglitinides

  • No studies regarding pregnancy
  • Patients should not breast or chestfeed

Adverse Effects of Meglitinides

  • Upper respiratory infection
  • Headache
  • Arthralgia
  • Nausea
  • Diarrhea
  • Hypoglycemia

Drug-Drug Interactions for Meglitinides

  • Multiple; check for potential interactions.

Sites of Action of Drugs Used to Treat Diabetes

Insulin

  • Promotes the storage of the body’s fuels
  • Facilitates the transport of various metabolites and ions across cell membranes
  • Simulates the synthesis of glycogen from glucose, of fats from lipids, of proteins from amino acids
  • Reacts with specific receptor sites on the cells

Indications for Insulin

  • Treatment of Type 1 diabetes mellitus
  • Treatment of Type 2 diabetes mellitus in adults who have no response to diet, exercise, and other agents

Pharmacokinetics of Insulin

  • Various preparations available: short- and long-term coverage
  • Processed within the body like endogenous insulin
  • Peak, onset, and duration vary based on preparation

Contraindications for Insulin

  • None generally
  • Inhaled insulin: People with asthma, COPD, lung cancer or a history or lung cancer

Cautions for Insulin

  • Pregnancy and Lactation

Adverse Effects of Insulin

  • Hypoglycemia
  • Local reactions at injection sites
  • Decreased blood potassium levels

Drug-Drug Interactions for Insulin

  • Any drug that decreases glucose levels
  • Beta-blockers
  • Thiazide diuretics or glucocorticoids
  • Possible interactions with various herbal therapies

Sulfonylureas

  • Stimulate functioning beta cells in pancreatic islets to release insulin
  • May improve insulin binding to insulin receptors and increase the number of insulin receptors
  • Increase the effect of antidiuretic hormone on renal cells
  • Effective only in patients with functioning beta cells
  • May lose effectiveness over time
  • Second-generation sulfonylureas have several advantages over first-generation drugs

Therapeutic Actions of Sulfonylureas

  • Stimulate insulin release from the beta cells in the pancreas
  • They improve binding of insulin to insulin receptors

Indications for Sulfonylureas

  • Adjunct to diet and exercise to lower blood glucose levels in type 2 diabetes
  • Off-label use: Adjunct to insulin and metformin to improve glucose control

Pharmacokinetics of Sulfonylureas

  • Rapidly absorbed from the GI tract; undergo hepatic metabolism
  • Excreted in the urine
  • Glyburide also excreted via bile
  • Peak and duration vary with each drug

Contraindications for Sulfonylureas

  • Allergy
  • Diabetic complications
  • Type 1 diabetes
  • Pregnancy

Adverse Effects of Sulfonylureas

  • Hypoglycemia
  • GI distress
  • Allergic skin reactions

Drug-Drug Interactions for Sulfonylureas

  • Beta-blockers
  • Alcohol
  • Many herbal therapies

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This quiz explores SGLT-2 inhibitors, their mechanisms, contraindications, cautions, adverse effects, and drug interactions. It is designed for those studying diabetes treatments and their pharmacological implications. Test your knowledge on these crucial diabetes medications.

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