Podcast
Questions and Answers
What method is primarily used to administer glucagon during hypoglycemic emergencies?
What method is primarily used to administer glucagon during hypoglycemic emergencies?
- Intramuscular route (correct)
- Oral route
- Subcutaneous route
- Intravenous route
What is a significant limitation of glucagon when hepatic glycogen stores are depleted?
What is a significant limitation of glucagon when hepatic glycogen stores are depleted?
- It cannot be administered intramuscularly
- It causes renal toxicity
- It leads to severe gastrointestinal distress
- Its hyperglycemic action is transient (correct)
What is a common side effect associated with glucagon use?
What is a common side effect associated with glucagon use?
- Dizziness
- Nausea and vomiting (correct)
- Hypotension
- Diarrhea
What mechanism underlies the hyperglycemic effect of diazoxide?
What mechanism underlies the hyperglycemic effect of diazoxide?
Which of the following properties does glucagon share with diazoxide?
Which of the following properties does glucagon share with diazoxide?
Which channel does diazoxide interact with to exert its effects?
Which channel does diazoxide interact with to exert its effects?
What is the primary mechanism of action of metformin in the liver?
What is the primary mechanism of action of metformin in the liver?
Which of the following effects is NOT associated with the activation of AMPK?
Which of the following effects is NOT associated with the activation of AMPK?
What is a common side effect of thiazolidinediones?
What is a common side effect of thiazolidinediones?
What is the primary action of α-glucosidase inhibitors in the intestinal tract?
What is the primary action of α-glucosidase inhibitors in the intestinal tract?
Which process is NOT facilitated by the binding of thiazolidinediones to PPARγ?
Which process is NOT facilitated by the binding of thiazolidinediones to PPARγ?
Which statement regarding metformin's pharmacokinetics is true?
Which statement regarding metformin's pharmacokinetics is true?
Which of the following is a common side effect of α-glucosidase inhibitors?
Which of the following is a common side effect of α-glucosidase inhibitors?
The primary effect of activated AMPK includes all of the following EXCEPT:
The primary effect of activated AMPK includes all of the following EXCEPT:
What mechanism do gliflozins utilize to lower blood glucose levels?
What mechanism do gliflozins utilize to lower blood glucose levels?
What is a notable pharmacokinetic characteristic of acarbose?
What is a notable pharmacokinetic characteristic of acarbose?
How do thiazolidinediones primarily affect glucose metabolism?
How do thiazolidinediones primarily affect glucose metabolism?
Which patient demographic is particularly at higher risk for urinary tract infections due to gliflozin use?
Which patient demographic is particularly at higher risk for urinary tract infections due to gliflozin use?
The transport of metformin into cells is primarily mediated through which of the following?
The transport of metformin into cells is primarily mediated through which of the following?
What type of reaction can occur with acarbose regarding hepatic transaminases?
What type of reaction can occur with acarbose regarding hepatic transaminases?
Which of the following correctly describes the administration method of liraglutide?
Which of the following correctly describes the administration method of liraglutide?
Which of the following statements about exenatide is true?
Which of the following statements about exenatide is true?
Which alteration in the amino acid sequence of insulin results in increased stability and solubility?
Which alteration in the amino acid sequence of insulin results in increased stability and solubility?
What is the primary mechanism by which glucose stimulates insulin secretion?
What is the primary mechanism by which glucose stimulates insulin secretion?
Which of the following combinations represents a mixed insulin formulation?
Which of the following combinations represents a mixed insulin formulation?
Which of the following is NOT a common side effect of insulin therapy?
Which of the following is NOT a common side effect of insulin therapy?
What distinguishes the first generation sulphonylureas from the second generation?
What distinguishes the first generation sulphonylureas from the second generation?
Which insulin formulation is characterized by prolonged action and a predictable kinetic profile?
Which insulin formulation is characterized by prolonged action and a predictable kinetic profile?
Which glucose transporter is activated by the binding of insulin to its receptor?
Which glucose transporter is activated by the binding of insulin to its receptor?
What effect does insulin have that contributes to weight gain?
What effect does insulin have that contributes to weight gain?
What is a significant side effect of Thiazolidinediones that could exacerbate a specific cardiovascular condition?
What is a significant side effect of Thiazolidinediones that could exacerbate a specific cardiovascular condition?
Which statement best describes the metabolism of Thiazolidinediones?
Which statement best describes the metabolism of Thiazolidinediones?
What effect does co-administration of rifampin have on Thiazolidinediones?
What effect does co-administration of rifampin have on Thiazolidinediones?
What is the primary action of Dipeptidyl peptidase-4 (DPP-4) inhibitors like sitagliptin?
What is the primary action of Dipeptidyl peptidase-4 (DPP-4) inhibitors like sitagliptin?
Which of the following statements about GLP-1 agonists is TRUE?
Which of the following statements about GLP-1 agonists is TRUE?
What is the primary pharmacokinetic characteristic of Gliptins?
What is the primary pharmacokinetic characteristic of Gliptins?
Which of the following is NOT a reported side effect of Gliptins?
Which of the following is NOT a reported side effect of Gliptins?
Which group of patients should avoid the use of Thiazolidinediones?
Which group of patients should avoid the use of Thiazolidinediones?
Study Notes
Insulin Variants and Mechanisms
- Alterations in human insulin's amino acid sequence enhance stability and modify action duration, such as insulin lispro from reversing proline and lysine.
- Mixed insulin formulations include 70:30 combinations of NPH and regular insulin, as well as lispro protamine/lispro in ratios of 50/50 and 75/25.
- Insulin glargine offers prolonged effects with a predictable kinetic profile.
Insulin Secretion Regulation
- Glucose serves as the primary insulin secretagogue.
- ATP-sensitive potassium channels contribute to membrane depolarization, initiating insulin release from storage vesicles.
- Insulin binds to enzyme-linked transmembrane receptors, activating glucose transport processes via Glut-4 in adipose and muscle tissues.
Insulin Side Effects
- Common side effects include hypoglycemia, weight gain, allergic reactions, injection site reactions, lipoatrophy, and lipohypertrophy.
Oral Hypoglycemic Agents
Sulphonylureas
- Substituted arylsulphonylureas, divided into first-generation (e.g., tolbutamide, chlorpropamide) rarely used due to severe hypoglycemia risk.
- Second-generation includes glibenclamide, gliclazide, glipizide, and glimepiride, with less severe hypoglycemic effects.
Metformin
- Acts primarily by suppressing hepatic gluconeogenesis and is best absorbed in the small intestine; does not bind plasma proteins.
- Common side effects include gastrointestinal disturbances (anorexia, diarrhea, nausea) and lactic acidosis, with a rare incidence of hypoglycemia.
Thiazolidinediones (Glitazones)
- Rosiglitazone and pioglitazone bind to PPARγ in adipose tissue, enhancing glucose and fatty acid uptake but contributing to weight gain.
- Slow onset of blood glucose-lowering effects, with significant side effects including weight gain and fluid retention, potentially exacerbating heart failure.
Dipeptidyl Peptidase-4 (DPP-4) Inhibitors (Gliptins)
- Inhibit DPP-4 enzyme, enhancing bioavailability of incretins like GLP-1 and GIP to lower blood glucose levels.
- Common side effects include nausea, stomach pain, and flu-like symptoms.
GLP-1 Agonists
- These agents activate GLP-1 receptors, stimulating insulin biosynthesis and release.
- Administered via subcutaneous injections, with side effects including nausea, vomiting, and delayed gastric emptying.
α-Glucosidase Inhibitors
- Inhibit α-glucosidase in the intestine, reducing starch and disaccharide absorption, resulting in decreased postprandial plasma glucose.
- Examples include acarbose and miglitol, with common gastrointestinal side effects such as flatulence and diarrhea.
SGLT-2 Inhibitors (Gliflozins)
- Agents like dapagliflozin and canagliflozin block sodium-glucose co-transport in kidneys, reducing glucose absorption and blood glucose levels.
- Short half-life and plasma protein binding; they increase urinary tract infection risk.
Glucagon and Diazoxide for Hypoglycemia
- Glucagon, produced via recombinant DNA, treats severe hypoglycemia, administered intravenously, intramuscularly, or subcutaneously.
- Diazoxide, an oral vasodilator with hyperglycemic effects, prevents insulin secretion through KATP channel interaction.
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Description
This quiz explores the structural modifications of human insulin, including its amino acid sequence and protein structure alterations. Learn about various insulin types such as insulin lispro, NPH, and glargine, and their effects on solubility and action duration.
