Oral anti-diabetic Drugs

Question 0

A DM Type 2 patient that is pregnant or undergoing surgery should switch to what for treatment?

Answer 0

Insulin instead of relying on the oral agents.

Question 1

In DM type 2, patients can take an oral anti-diabetic agent.
True/False:
1) These agents require injection.
2) Used only in Type 2 DM.

Answer 1

1) False- do not require injection

2) True

Question 2

The first oral agents for DM Type 2. The MOA is to stimulate insulin secretion by beta cells by blocking the same ATP-sensitive K+ channels that are blocked by ATP when endogenous glucose is high, causing physiological insulin secretion. What is it?

Answer 2

Sulfonylureas- Glimepiride

Question 3

T/F: Glimepiride also

1) Increase glucagon production?
2) Increase tissue sensitivity to insulin?

Answer 3

1) False- decrease

2) True

Question 4

Concerns with Glimepiride (Sulfonylureas) are what? When should you avoid use of this drug?

Answer 4

• Hypoglycemia (only hypoglycemic agents). Weight gain. Risky in elderly.
• Avoid in Liver and kidney disease.

Question 5

Glimepiride is metabolized by the ______, excreted by the ________ and in bile.

Answer 5

Liver, kidneys

Question 6

What class of drugs acts similar to sulfonylureas (binding to ATP-sensitive potassium channels). What are they?

Answer 6

Meglitinides (Repaglinide, Nateglinide- not required drugs!)

Question 7

What drug targets AMP kinase, which is a regulator of glucose metabolism primarily in the liver, to decrease glucose production, increase glucose uptake?

Answer 7

Biguanides- METFORMIN

Question 8

T/F: Metformin

1) Increases insulin excretion.
2) increase insulin effectiveness.
3) Can be used together with insulin and together with SUs.

Answer 8

1) False- Does not increase insulin-no hypoglycemia.
2) True
3) True- b/c different mechanisms

Question 9

How is metformin excreted?

Answer 9

Renal excretion without metabolism. Dangerous in pts with kidney disease.

Question 10

Concerns with metformin

Answer 10

Lactic acidosis- inhibits lactate metabolism.

-GI distress- Metallic tastes, diarrhea, vomiting, anorexia (no weight gain)

Question 11

Drug that decreases glucose formation in the gut?

Answer 11

Acarbose.

Question 12

An alpha-glucosidase inhibitor, Microbial sugars that inhibit amylase. Block disaccharide hydrolysis, prevent glucose uptake. What drug?

Answer 12

Acarbose

Question 13

When should acarbose be taken?

Answer 13

Before meals

Question 14

What is poorly absorbed, and thus remains in the gut, its site of action.

Answer 14

Acarbose

Question 15

Side effects/ concerns with acarbose

Answer 15

• GI distress (flatulance, cramps, diarrhea).
• Do not use with metformin due to additive GI SE.
• No hypoglycemia on their own- increase risk with insulin- glucose required to treat.

Question 16

Activate peroxisome proliferator-activated receptor-y(PPAR-y), a nuclear transcription factor receptor. Increases insulin response. What is it?

Answer 16

Thiazolidinediones (Pioglitazone)

Question 17

T/F: Multiple beneficial effects of Pioglitazone include:

1) decrease gluconeogenesis, glucose output and triglyceride synthesis in liver.
2) Increase glucose uptake and utilization in muscle.
3) Increase glucose uptake and decreases fatty acid production in adipocytes.
4) Can be used alone or together with insulin, SU or metformin.

Answer 17

All true

Question 18

How is pioglitazone metabolized and excreted?

Answer 18

By the liver and in the feces.

Question 19

Concerns with pioglitazone?

Answer 19

• Liver toxicity!!
• Cardiovascular toxicity!!
• May increase bladder cancer risk.
• Can increase fracture risk.

Question 20

What is an analog of gut peptide glucagon-like peptide-1, an “incretin” released in response to food?

Answer 20

Exenatide- potentiate insulin secretion, decrease glucagon, slow gastric emptying , promote satiety.

Question 21

Exenitide is now approved for use alone or with what type of insulin?

Answer 21

Insulin glargine

Question 22

Exenatide cause weight gain/loss?

Answer 22

Often weight loss

Question 23

Concerns with exenatide

Answer 23

• Hypoglycemia

- Decreased absorption of contraceptives and antibiotics.

Question 24

How is exenitide given?

Answer 24

Injected SC before morning and evening meals.

Question 25

What inhibits dipeptidyl-peptidase IV, the enzyme that degrades endogenous incretins. Increases endogenous incretins rather than providing exogenous incretin?

Answer 25

Sitagliptin

Question 26

Administration of Sitagliptin

Answer 26

Oral, once/day

Question 27

Weight effects of sitagliptin?

Answer 27

Neither gain nor loss

Question 28

Effects of sitagliptin

Answer 28

Increase insulin secretion, decrease glucagon secretion, lower glucose and increase satiety.

Question 29

Name an amylin-based anti diabetic agent?

Answer 29

Pramlintide- used in type 1, but more extensive in type 2 DM.