OHAs Flashcards
Drug classes
- Meglitinides
- Alpha glucosidase inhibitors
- Sulfonylureas
- Thiazolidinediones/Glitazones
- Biguanides
- DPP-4 inhibitors
- GLP-1 analogs
- Sodium-glucose co-transporter 2 (SGLT2) inhibitors
Effect on weight
- Biguanides
- Sulfonylureas
- Glitazone
- GLP-1 analogs
- DPP-4 inhibitors
- Meglitinides
- Biguanides
- Loss
- Sulfonylureas
- Gain
- Glitazone
- Gain
- GLP-1 analogs
- Loss
- DPP-4 inhibitors
- Neutral
- Meglitinides
- Gain
First-line therapy in type 2 DM
Metformin
Which diabetes drugs can cause a disulfiram-like reaction?
First-generation sulfonylureas
To which class of diabetes drugs do pioglitazone and rosiglitazone belong?
Thiazolidinedione/Glitazones
Examples of 1st and 2nd generation sulfonylureas
- 1st generation
- Chlorpropamide
- Tolbutamide
- 2nd generation
- Glimepiride
- Glipizide
- Glyburide
Will sulfonylureas work in type 1 diabetes mellitus?
No; these drugs require islet cell function and the ability to secrete endogenous insulin (defective in type 1 diabetes)
Describe the mechanism of action of sulfonylureas
Close the K+ channel on the β-cell membrane
↓
Cell depolarization
↓
Insulin release by increased calcium influx
Memory aid:
- _S_ulfonyurea
-
_S_ecretion of insulin by beta-cells
- Require some islet function, so useless in type 1 DM
What is an adverse effect of second-generation sulfonylureas?
Hypoglycemia
Metformin drug class
Biguanides
What is the mechanism of action of metformin?
Unknown; may decrease gluconeogenesis, increase glycolysis, thereby decreasing serum glucose levels; overall, it acts as an insulin sensitizer
True or False: Metformin can be used in patients without islet function
True
Before prescribing metformin, it is important to assess the function of what organ?
Kidney; if metformin cannot be excreted it may build up leading to lactic acidosis
How do glitazones work?
They increase target cell response to insulin via the peroxisome proliferator-activated receptor-γ pathway
Memory aid:
- GLItazone
- Gains
- Lifts
- Increases
- insulin sensitivity
What are the side effects of glitazones?
- Weight gain
- Edema
- Hepatotoxicity
- Cardiovascular toxicity
Name two alpha-glucosidase inhibitors
- Acarbose
- Miglitol
T/F. Glitazones are safe to use in renal impairment
True; But they are hepatotoxic and cardiotoxic
Acarbose and miglitol mechanism of action
- Inhibit intestinal brush-border α-glucosidases
- Delayed carbohydrate hydrolysis and glucose absorption → decreased postprandial hyperglycemia
What is the principal toxicity of -glucosidase inhibitors?
GI disturbance
A peptide hormone that is cosecreted with insulin from the pancreatic β-cell and is thus deficient in diabetic people
Amylin
What is the mechanism of action of pramlintide?
Pramlintide is a mimetic of an endogenous hormone and acts by inhibiting glucagon
Actions of amylin
- Inhibits glucagon secretion
- Delays gastric emptying
- Acts as a satiety agent
Memory aid:
-
Decreases
- Glucagon
- Gastric emptying
- Gutom
What are some toxicities of pramlintide?
Hypoglycemia, nausea, diarrhea
Give an example of a glucagon-like peptide-1 mimetic drug
Exenatide
What is the mechanism of action of the GLP-1 mimetics?
Increases insulin and decreases glucagon
What are toxicities of exenatide use?
Nausea, vomiting and possibly pancreatitis
- Memory aid:*
- GLPancreatitis
Meglitinides examples
- Nateglinide
- Repaglinide
Meglitinides mechanism of action
Stimulate postprandial insulin release by binding to K+ channels on β cell membranes (site differs from sulfonylureas)
Memory aid:
-
MS summons insulin release
- Meglitinides
- Sulfonylureas
Drugs with suffix -gliptin are classified as ____
DPP-4 inhibitors
DPP-4 inhibitors mechanism of action
Inhibit DPP-4 enzyme that deactivates GLP-1, thereby increase glucose-dependent insulin release, decrease glucagon release, decrease gastric emptying, and increase satiety
SGLT2 inhibitors works by ____
Blocking reabsorption of glucose in PCT
SGLT2 inhibitors examples
- Canagliflozin
- Dapagliflozin
- Empagliflozin
