Diabetes Pharmacology Type I and Type II

Question 1

Earliest signs of diabetes?

Answer 1

Increased:
Postprandial chylomicrons
VLDL cholesterol
Gluconeogenesis, ketogenesis
Plasma triglycerides

Question 2

Three microvascular injuries that occur with diabetes?

Answer 2

Cataracts and retinopathy
Nephropathy
Neuropathy

Question 3

How to prevent cataracts and retinopathy?

Answer 3

Keep A1c below 9%

Question 4

How to prevent nephropathy?

Answer 4

Keep A1c below 8%

Question 5

How to prevent neuropathy?

Answer 5

Keep A1c below 7%

Question 6

What are the four goals of therapy?

Answer 6

1. ) Prevent hyperosmolar coma/ketoacidosis
2. ) Reduce microvascular injury
3. ) Reduce hypertension
4. ) Prevention of atherosclerotic disease

Question 7

Two general types of drugs that increase plasma insulin?

Answer 7

Insulin

Secretagogues

Question 8

Three general types of insulins?

Answer 8

Rapid acting and short acting
Moderate acting
Long acting

Question 9

What are the rapid acting insulin?

Answer 9

Lispro insulin (Humalog)
Insulin aspart (Novolog)

Question 10

What are the short acting insulin?

Answer 10

Regular insulin

Question 11

What are the moderate acting insulins?

Answer 11

Isophane/NPH

Question 12

What are the long acting insulins?

Answer 12

Glargine
Detemir
Degludec

Question 13

What are two types of secretagogues?

Answer 13

Sulfonylureas

Short-acting secretagogues

Question 14

What are the sulfonylureas?

Answer 14

Glyburid
Glipizide
Glimepiride

Question 15

What are the short acting secretagogues?

Answer 15

Repaglinide

Nateglinide

Question 16

What are intermediate-mixed insulins preparations?

Answer 16

Isophane + regular insulin or Lispro

Question 17

What may be used in a patient that has a high insulin dosage requirement?

Answer 17

Pramlintide

Question 18

What are two general categories of direct acting agents for increased glucose uptake?

Answer 18

Biguanides

Thiazolidinediones

Question 19

What are the Biguanides?

Answer 19

Metformin

Question 20

What are the thiazolidinediones?

Answer 20

Pioglitazone

Rosiglitazone

Question 21

What are the two general categories of GLP-1 mechanism for increased tissue glucose uptake?

Answer 21

GLP-1 Analogs

Dipeptidyl peptidase inhibitors

Question 22

What are the GLP-1 analogs?

Answer 22

Liraglutide

Exenitide

Question 23

What are the Dipeptidyl peptidase inhibitors?

Answer 23

Sitagliptin
Linagliptin
Saxigliptin

Question 24

What does metformin cause?

Answer 24

Increased insulin sensitivity

Decreased gluconeogenesis

Question 25

How does metformin mediate its affects?

Answer 25

Not well understood but increase AMP:ATP ratio activating AMP kinase

Question 26

What are contraindications of metformin?

Answer 26

Hepatic and renal insufficiency MI Uncompensated CHF

Question 27

What can metformin cause?

Answer 27

Lactic acidosis

Question 28

How do thiazolidinediones work?

Answer 28

Ligands for cytosolic and nuclear PPAR receptors

Question 29

What are the two PPAR receptors?

Answer 29

Gamma | Alpha

Question 30

What affect to thiazolidinediones have?

Answer 30

Increased fatty acid uptake Increased fatty acid oxidation Increased insulin sensitivity and glucose uptake Anti-inflammatory affects

Question 31

What are the two thiazolidinediones?

Answer 31

Pioglitazone | Rosiglitazone

Question 32

What receptors does pioglitazone work on?

Answer 32

PPAR-alpha | PPAR-gamma

Question 33

What receptors does rosiglitazone work on?

Answer 33

PPAR-gamma

Question 34

Which thiazolidinedione has better lipid metabolism effects?

Answer 34

Pioglitazone (PPAR-alpha)

Question 35

What do incretins/GLP-1 do?

Answer 35

Increase GLUT-2 expression in beta-cells of the pancreas

Question 36

When is GLP-1 released and where?

Answer 36

From small intestine and colon in response to carbohydrate, protein and fat intake

Question 37

What enzyme breaks down GLP-1 and GIP?

Answer 37

DPP4

Question 38

What do dipeptidylpeptidase inhibitors do?

Answer 38

Inhibit DPP4 increasing the life span of GLP-1 and GIP

Question 39

What releases GLP-1?

Answer 39

Distal small intestines and colon

Question 40

What releases GIP?

Answer 40

Duodenum | Jejunum

Question 41

What are the effects of GLP-1 (7-36) amide (active form)?

Answer 41

``` Increased: Insulin secretion Satiety Beta-cell survival Decreased: Glucagon secretion Gastric emptying Food intake ```

Question 42

What is are the effects of GLP-1 (9-36) amide (inactive form)?

Answer 42

Increased independent glucose clearance Cardioprotective Vasoactive

Question 43

What are the effects of GIP (1-42) active form?

Answer 43

``` Increased: Insulin secretion Lipogenesis Beta-cell survival Decreased: Lipolysis ```

Question 44

What are the effects of GIP (3-42) inactive form?

Answer 44

None

Question 45

What are the GLP-1 analogs?

Answer 45

Exenatide | Liraglutide

Question 46

Which GLP-1 analog has reduced DPP4 sensitivity?

Answer 46

Liraglutide

Question 47

What are examples of DPP4 inhibitors?

Answer 47

Sitagliptin | Linagliptin

Question 48

What are amylin analogs?

Answer 48

Pramlintide

Question 49

What are alpha-glucosidase inhibitors?

Answer 49

Acarbose | Miglitol

Question 50

What are inhibitors of sodium-glucose transport?

Answer 50

Dapagliflozin Empagliflozin Canagliflozin

Question 51

What is amylin?

Answer 51

Small peptide hormone that is released into the bloodstream by the beta cells of the pancreas along with insulin after a meal

Question 52

What is the only drug approved to lower blood sugar in Type I diabetics since insulin?

Answer 52

Pramlintide

Question 53

Mechanism of action of Pramlintide?

Answer 53

Inhibit release of glucagon

Question 54

What do alpha-glucosidase inhibitors do?

Answer 54

Inhibit intestinal alpha-glucosidase slowing post-prandial increase in plasma glucose

Question 55

What does alpha-glucosidase enzyme do?

Answer 55

Digests carbohydrates

Question 56

What is more commonly used among "skinny" Type II diabetics?

Answer 56

Alpha-glucosidase inhibitors

Question 57

Where do SGLT-2 transporters work and what do they do?

Answer 57

Co-transport sodium and glucose in the proximal convoluted tubule

Question 58

What are the SGLT-2 inhibitors?

Answer 58

Canagliflozin Empagliflozin Dapagliflozin

Question 59

What do the SLGT-2 inhibitors cause?

Answer 59

Decrease in reabsorption of glucose and sodium from the PCT allowing it to be released in the urine

Question 60

What are side effects of glucose in the urine?

Answer 60

Polyuria/dehydration Urinary tract infections (fungal) Urine loss of 200-500 Kcals/day Ketoacidosis

Question 61

What drug is acid-soluble and precipitates at body pH?

Answer 61

Glargine insulin

Question 62

What drug heavily binds to albumin?

Answer 62

Detemir insulin

Question 63

What is the standard insulin therapy for Type I diabetics?

Answer 63

``` Glargine insulin (once daily) + rapid acting insulin with meals or insulin pump with rapid-acting insulin ```