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Flashcards in Endocrine Pharmacology Deck (33):
1

Name short-acting insulin (meal related).

regular
lisper
aspirate
glulisine

2

Name short-acting insulin (meal related).

regular
lisper
aspirate
glulisine

3

Name short-acting insulin (meal related).

regular
lisper
aspirate
glulisine

4

List intermediate/long acting basal insulin.

NPH
glargine
detemir

5

What are the advantages and disadvantages of insulin analogs.

disadvantages: hypoglycemia, local reactions, weight gain
advantages: no dose limit, rapidly effective

6

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)

7

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

8

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

9

Contrast sulfonylurea and meglitinides.

meglitinides have a similar MOA but shorter acting, dosed at meal times (A1c 0.5-1.5%- less potent)

10

What are the adverse effects of meglitinides?

hypoglycemia, weight gain, use with caution in those with renal or liver failure, can be cost limited

11

In what ways does metformin (broad mechanisms) reduce blood sugar?

.

12

In what ways does metformin (broad mechanisms) reduce blood sugar?

increases insulin sensitivity and decreases hepatic glucose production

13

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

14

When is use of metformin contraindicated?

renal insufficiency
liver disease or alcohol abuse
heart failure
serious acute illness
age >80yo

15

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%)

16

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

17

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

18

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

19

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%)

20

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

21

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%)

22

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%)

23

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

24

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

25

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 orthostatic hypertension, contraindicated in liver or renal insufficiency

26

What is the mechanism by which glucagon addresses hypoglycemia?

glucagon stimulates adenylate cyclase to increase cyclic AMP, promoting hepatic gluconeogenesis and glycogenolysis (increasing BG)

27

Give an example of the type and amount of insulin in treatment of a newly diagnosed DM1 patient.

basal + bolus regimen, starting daily dose is 0.2-0.4 units/kg/d with 50% basal insulin and 50% bolus insulin (based on fixed dose or carb content of meal)

28

Describe the type of insulin pumps use and how it is delivered.

continuous insulin infusion of rapid acting insulin is delivered via a subcutaneous catheter connected to the insulin pump, additionally boluses can be administered with meals based on the carbohydrate content of the meal

29

Describe the type of insulin pumps use and how it is delivered.

continuous insulin infusion of rapid acting insulin is delivered via a subcutaneous catheter connected to the insulin pump, additionally boluses can be administered with meals based on the carbohydrate content of the meal

30

What are the advantages and disadvantages of a insulin pump?

advantages: convenience, more consistent insulin absorption, may improve glycemic control if used properly

disadvantages: cost, pump failures, having to wear a device

31

What are the keys in pharmacological management of DM2?

-lifestyle modifications are the most important intervention
-Metformin is the preferred first line treatment of DM2
-if A1c >7% after 3mo, add a second agent
-if A1c >7% after 6mo or beyond, add a third agent

32

When is insulin used in treatment of DM2?

1. start basal insulin at bed time, starting dose is 0.2 units/kg/d
2. dose adjusted to target fasting morning BG of 80-130mg/dL
3. if BG at meals or bedtime is elevated, add NPH in the morning, start mealtime insulin

33

What are the advantages and disavantages of using insulin the the treatment of DM2?

advantages: more cost effective, will improve glycemic control if used properly

disadvantages: may require multiple daily injections, requires frequent BG monitoring and includes the risk of hypoglycemia