Drugs for Diabetes Flashcards
Rapid-acting Insulins
Aspart
Lispro
Glulisine
Short-acting Insulin
Regular Insulin
Intermediate-acting Insulin
Neutral Protamine Hagerdorn (NPH)
Long-acting Insulin
Detemir
Glargine
Amylin Analog name
Pramlintide
GLP-1 agonists
Exantide
Liraglutide
DPP-4 Inhibitors
-liptins Sitagliptin Linagliptin Saxagliptin Alogliptin
First gen K-channel blockers (Sulfonylureas)
-amides
Chlorpropamide
Tolbutamide
Tolazamide
Second-gen K channel blockers
Glipizide
Glyburide
Glimepiride
Meglitinides (Non-sulfonylurea K channel blocker)
-inide
Nateglinide
Repaglinide
Thiazolidinediones
-azones
Pioglitazone
Rosiglitazone
SGLT2 inhibitors
-flozin
Canagliflozin
Dapagliflozin
Empagliflozin
a-glycosidase inhibitors
Acarbose
Miglitol
What is the diagnostic criteria for Diabetes Mellitus?
Fasting plasma glucose over 125 mg/dl
Is insulin anabolic or catabolic?
only anabolic hormone that lowers blood glucose
2 pathways that insulin activates to increase glucose transport into cell and promote growth
PI3K-Akt- GLUT4 insertion into membrane
MAP kinase- proliferation
How does Insulin act as a antihyperglycemic?
Activation of glycolysis and glycogen synthesis
Inhibition of gluconeogenesis and glycogenolysis
How do the short acting insulins increase pharmacokinetics?
mutated to block formation of dimers and hexamers which allows faster absorption
When are short acting insulins used?
Postprandial hyperglycemia
When is regular insulin used?
Basal insulin maintenance
Overnight maintenance
Can be given IV in emergencies
A patient wants to stabilize their blood sugar throughout the day with 1-2 injections. What can be prescribed?
Long acting insulins Detemir or Glargine
Can insulins be used for TIDM and TIIDM?
Yes, compared to regulators of insulin secretion which works only on TIIDM
What BMP abnormality can be corrected with insulin?
Hyperkalemia- Insulin drives K+ into cells via activation of Na/K ATPase
Adverse effects of Insulin
Hypoglycemia if over-dosed (most common) Lipodistrophy at injection site Insulin resistance Type I hypersensitivity reaction Hypokalemia
What hormone released by B-cells of the pancreas enhances insulin action?
Amylin
When is Pramlintide indicated?
Adjunct to Post prandial insulin
What endogenous factors increase insulin release?
B2 agonists (Terbutaline, Albuterol) Incretins (GLP-1 agonists)
What endogenous factors decrease insulin release?
Somatostatin
a2-agonists (Clonidine)
4 targets to regulate insulin secretion
- Gs (stimulate insulin)
- Gi (decrease)
- K+ channel (block to decrease)
- Ca2+ channel
What are incretins?
GI hormones that decrease blood glucose
Glucagon-Like Peptide-1 (GLP-1) MOA
Promotes B-cell proliferation
Insulin gene expression
Increases glucose-dependent insulin secretion
Promotes satiety
What is the action of Dipeptidyl Peptidase-4?
Breaks down GLP-1
How do the Sulfonylureas work to increase insulin release?
Blocks K+ channel by binding to SUR1 which depolarizes the cell
Adverse affects of Sulfonylureas
Hypoglycemia
Weight gain
CYP inhibitor
What other drugs increase the efficacy of sulfonylureas leading to hypoglycemia risk?
NSAIDS!!
When are the meglitinides recommended to take?
Orally before a meal
What are advantages of Metformin?
Doesn’t cause hypoglycemia
No weight gain
Not metabolized (excreted unchanged)
Side effects of Metformin
GI issues
Lactic Acidosis under hypoxic conditions
Thiazolidinediones MOA
PPARy ligand that increases Glut4
Use of Thiazolidinediones
T2DM and is a euglycemic drug (will not cause hypoglycemia)
Adverse effects of Thiazolidinediones
Increased vascular permeability
Increased ENaC expression leading to edema
Osteoporosis risk
How do the SGLT2 inhibitors work?
Block reabsorption of Glucose in the PCT
If you’re patient is hypotensive/hypovolemic, should you use SGLT2 inhibitors
Only after correcting volume due to the osmotic diuresis effect the -flozins
a-glycosidade inhibitor MOA
Blocks breakdown of polysaccharides into mono’s, which inhibits their absorption.
