Podcast
Questions and Answers
What is a contraindication for SGLT-2 inhibitors?
What is a contraindication for SGLT-2 inhibitors?
Which of the following is an adverse effect associated with thiazolidinediones?
Which of the following is an adverse effect associated with thiazolidinediones?
What therapeutic action do GLP-1 agonists primarily perform?
What therapeutic action do GLP-1 agonists primarily perform?
Which drug should not be taken with gemfibrozil?
Which drug should not be taken with gemfibrozil?
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What therapy is indicated for the treatment of hypoglycemia?
What therapy is indicated for the treatment of hypoglycemia?
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Which class of medications is primarily effective in decreasing insulin resistance?
Which class of medications is primarily effective in decreasing insulin resistance?
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What is an important caution when using human amylin?
What is an important caution when using human amylin?
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A patient with type 1 diabetes should avoid which therapeutic agents?
A patient with type 1 diabetes should avoid which therapeutic agents?
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Which adverse effect is associated with SGLT-2 inhibitors?
Which adverse effect is associated with SGLT-2 inhibitors?
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What is the primary indication for GLP-1 agonists?
What is the primary indication for GLP-1 agonists?
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What action do glucose-elevating agents perform?
What action do glucose-elevating agents perform?
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What precaution should be taken concerning thiazolidinediones?
What precaution should be taken concerning thiazolidinediones?
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Which of the following is a major adverse effect of GLP-1 agonists?
Which of the following is a major adverse effect of GLP-1 agonists?
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Which of these agents requires monitoring for severe renal impairment before administration?
Which of these agents requires monitoring for severe renal impairment before administration?
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Which sign or symptom is commonly associated with hyperglycemia?
Which sign or symptom is commonly associated with hyperglycemia?
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What is the primary action of insulin in the body?
What is the primary action of insulin in the body?
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In which scenario is the use of sulfonylureas contraindicated?
In which scenario is the use of sulfonylureas contraindicated?
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What potential adverse effect can occur from the use of insulin?
What potential adverse effect can occur from the use of insulin?
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Which of the following correctly describes the indications for insulin use?
Which of the following correctly describes the indications for insulin use?
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What effect do thiazide diuretics have when used with insulin?
What effect do thiazide diuretics have when used with insulin?
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What is a main therapeutic action of sulfonylureas?
What is a main therapeutic action of sulfonylureas?
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Which of the following is NOT a common symptom of hyperglycemia?
Which of the following is NOT a common symptom of hyperglycemia?
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How are sulfonylureas metabolized in the body?
How are sulfonylureas metabolized in the body?
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Which statement accurately depicts a caution for using insulin?
Which statement accurately depicts a caution for using insulin?
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What advantage do second-generation sulfonylureas have over first-generation sulfonylureas?
What advantage do second-generation sulfonylureas have over first-generation sulfonylureas?
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In which scenario would alpha-glucosidase inhibitors be indicated?
In which scenario would alpha-glucosidase inhibitors be indicated?
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What is a key therapeutic action of biguanides?
What is a key therapeutic action of biguanides?
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What potential adverse effect is associated with the use of biguanides?
What potential adverse effect is associated with the use of biguanides?
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Which statement is true regarding DPP-4 inhibitors?
Which statement is true regarding DPP-4 inhibitors?
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What is a common side effect associated with meglitinides?
What is a common side effect associated with meglitinides?
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Which of the following is a contraindication for using alpha-glucosidase inhibitors?
Which of the following is a contraindication for using alpha-glucosidase inhibitors?
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Why should caution be exercised when administering biguanides?
Why should caution be exercised when administering biguanides?
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What indicates the need for immediate assessment in a patient taking DPP-4 inhibitors?
What indicates the need for immediate assessment in a patient taking DPP-4 inhibitors?
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Which adverse effect is more common with alpha-glucosidase inhibitors?
Which adverse effect is more common with alpha-glucosidase inhibitors?
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What is a principal therapeutic action of meglitinides?
What is a principal therapeutic action of meglitinides?
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What constitutes a contraindication for DPP-4 inhibitors?
What constitutes a contraindication for DPP-4 inhibitors?
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What is a key pharmacokinetic property of biguanides?
What is a key pharmacokinetic property of biguanides?
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What should be monitored in patients taking alpha-glucosidase inhibitors?
What should be monitored in patients taking alpha-glucosidase inhibitors?
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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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Description
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.
