Endocrine Pharmacology Flashcards
(33 cards)
Name short-acting insulin (meal related).
regular
lisper
aspirate
glulisine
Name short-acting insulin (meal related).
regular
lisper
aspirate
glulisine
Name short-acting insulin (meal related).
regular
lisper
aspirate
glulisine
List intermediate/long acting basal insulin.
NPH
glargine
detemir
What are the advantages and disadvantages of insulin analogs.
disadvantages: hypoglycemia, local reactions, weight gain
advantages: no dose limit, rapidly effective
What is the mechanism of sulfonylureas?
PO drugs like glipizide, glyburide or glimepiride bind to the sulfonylurea receptor on beta cells leading to increased insulin secretion (A1c 1-2% decrease)
What are the risks of sulfonylureas?
BID dosing can cause hypoglycemia, weight gain and should be used with caution in elderly, renal failure, and liver failure due to risk of hypoglycemia
What are the risks of sulfonylureas?
BID dosing can cause hypoglycemia, weight gain and should be used with caution in elderly, renal failure, and liver failure due to risk of hypoglycemia
Contrast sulfonylurea and meglitinides.
meglitinides have a similar MOA but shorter acting, dosed at meal times (A1c 0.5-1.5%- less potent)
What are the adverse effects of meglitinides?
hypoglycemia, weight gain, use with caution in those with renal or liver failure, can be cost limited
In what ways does metformin (broad mechanisms) reduce blood sugar?
.
In what ways does metformin (broad mechanisms) reduce blood sugar?
increases insulin sensitivity and decreases hepatic glucose production
What are the advantages and disadvantages of metformin?
can produce weight loss or be weight neutral, does not produce hypoglycemia
can cause GI symptoms: metallic taste, nausea, diarrhea and lactic acidosis
When is use of metformin contraindicated?
renal insufficiency liver disease or alcohol abuse heart failure serious acute illness age >80yo
Give examples of thiazolidineiones and their mechanism of action.
Piolitazone and rosiglitazone (restricted)
acts as an agonist of the PPAR gamma nuclear receptor family, it sensitizes skeletal muscle to insulin leading to increased glucose uptake AND decreases hepatic glucose production (A1c 0.5-1.4%)
What are the advantages and disadvantages of thiazolidinediones?
advantage: no hypoglycemia, pioglitazone improves lipid profile
disadvantages: delayed onset of action (6-12 weeks till full effect); can result in weight gain, edema/fluid retention, increased risk of fractures, contraindicated in heart failure, caution with liver failure
What are the advantages and disadvantages of thiazolidinediones?
advantage: no hypoglycemia, pioglitazone improves lipid profile
disadvantages: delayed onset of action (6-12 weeks till full effect); can result in weight gain, edema/fluid retention, increased risk of fractures, contraindicated in heart failure, caution with liver failure
What is the mechanism of a-Glucsidase?
acarbose inhibits alpha gluconsidase enzyme which delays digestion and absorption of carbs and subsequent conversion into glucose
**can cause major flatulence and diarrhea as a result
How do incretin mimetics aim to address high blood glucose?
the promote glucose mediated insulin secretion and decrease hepatic glucose production (slows gastric emptying, improves satiety) (A1c 0.5-1%)
What are the advantages and disadvantages of uncertain mimetics?
reduction in appetite can lead to weight loss
does not cause hypoglycemia when used alone
may support beta cell mass/survival
adverse effects include GI symptoms (nausea and vomiting) and use with caution in renal insufficiency
Describe the how DPP-4 inhibitors are effective in treating high blood glucose.
DPP4 is an enzyme that is responsible for degrading GLP-1, GLP-1 normally acts as a powerful limiter of blood glucose
DPP-4 inhibitiors increase endogenous GLP-1 and also increase insulin secretion (A1c 05-0.8%)
Describe the how DPP-4 inhibitors are effective in treating high blood glucose.
DPP4 is an enzyme that is responsible for degrading GLP-1, GLP-1 normally acts as a powerful limiter of blood glucose
DPP-4 inhibitiors increase endogenous GLP-1 and also increase insulin secretion (A1c 05-0.8%)
Name examples of SGLT2 inhibitors and describe how they work to decrease blood sugar.
canagliflozin, dapagliflozin, empagliflozin
inhibit the SGLT2 sodium-glucose cotransporter in the proximal renal tubule
What are the advantages and disadvantages of SGLT2 inhibitors?
advantages: weight loss, decrease in SBP and low risk of hypoglycemia
adverse effects: genital and urinary tract infections (candida), and othostatic hypertension, contraindicated in liver or renal insufficiency