D. Pharm Of Insulin - Sulfonylureas

Front 1

What in general is the mechanism of action of the Sulfonylureas?

Back 1

Stimulate Insulin secretion by the Pancreas!

Front 2

How do the Sulfonylureas stimulate the pancreas to secrete insulin?

Back 2

They act like ATP; they close K channels, depolarize the cells, and allow Ca influx.

Front 3

What is a 1st generation Sulfonylurea to know?

Back 3

Tolbutamide

Front 4

What are 2 second generation Sulfonylureas to know?

Back 4

-Glipizide
-Glyburide

Front 5

What is the main advantage of the 2nd generations over Tolbutamide?

Back 5

They require much lower doses and thus cause much less toxicity

Front 6

What are 4 side effects of the sulfonylureas?

Back 6

-Hyponatremia (stim ADH secrn)
-Disulfiram-like rxn (flush)
-Drug interactions
-Hypoglycemia

Front 7

What is the mechanism of insulin Sensitizing drugs in general?

Back 7

Reduced Insulin resistance

Front 8

What does reduced insulin resistance allow for in diabetics?

Back 8

Insulin shots are better able to achieve their effects:
-Decreased glucose production
-Increased glucose utilization

Front 9

What are the 2 Insulin-Sensitizing drugs to know of?

Back 9

-Metformin
-Rosiglitazone

Front 10

What is Metformin's molecule type?

Back 10

Biguanide

Front 11

At what specific site is insulin sensitivity increased by Metformin?

Back 11

The LIVER

Front 12

So what is the principle effect of Metformin?

Back 12

Decreased gluconeogenesis during the fasting state.

Front 13

What is the major common side effects of Metformin?

Back 13

GI upset

Front 14

What is the most potentially fatal side effect of Metformin? What patients are most susceptible to it?

Back 14

Lactic acidosis - in renal insufficiency patients

Front 15

So what is the main contraindication to Metformin?

Back 15

Renal insufficiency

Front 16

What are 2 other contraindications to Metformin?

Back 16

-Home O2
-Binge drinking

Front 17

Where are the sensitizing effects of Rosiglitazone seen predominantly?

Back 17

At PERIPHERAL tissues - fat and muscle

Front 18

How does Rosiglitazone increase the sensitivity of fat and muscle to insulin?

Back 18

By activating PPAR

Front 19

What are 3 major side effects of Rosiglitazone?

Back 19

-Liver toxicity
-Weight gain
-Fluid retention

Front 20

What is Rosiglitazone contraindicated in?

Back 20

Advanced heart failure (CHF)

Front 21

What drugs for treating diabetes are not much used anymore because of major intestinal side effects?

Back 21

Alpha Glucosidase Inhibitors

Front 22

What is the main a-glucosidase inhibitor to know?

Back 22

Acarbose

Front 23

What is the Mechanism of Action of Acarbose and the a-Glucosidases?

Back 23

Inhibition of enteric enzymes that break down complex carbs so they're not even absorbed upon eating.

Front 24

What effect does Acarbose have on blood sugar levels?

Back 24

Reduced post-prandial hyperglycemia

Front 25

What are the major side effects of Acarbose?

Back 25

-Bloating
-Abdominal discomfort
-Diarrhea
-Flatulence

Front 26

How does Acarbose compare to the other 3 oral agents in terms of ability to decrease Hgb A1c?

Back 26

it's half as effective; only reduces it by .75%

Front 27

What are the 3 other oral agents for treating diabetes again?

Back 27

-Sulfonylureas
-Metformin
-Rosiglitazone

Front 28

What is the common way to treat type 2 diabetes?

Back 28

With combination therapy

Front 29

What are the 2 types of drugs that are given in combo therapy for type 2 dm?

Back 29

-Drugs that increase insulin (Sulfonylureas or Insulin)
-Drugs that improve insulin sensitivity (Metformin or Rosiglitazone)