Antidiabetic Agents

Question 1

What are the functions of all the Key cell types of the endocrine pancreas?
Alpha
Beta
Delta
G
F

Answer 1

Alpha: Glucagon
Beta: Insulin
Delta: Somatostatin
G: Gastrin
F: Pancretic Polypeptide

Question 2

What positively regulates Insulin release?

Answer 2

GLucose (subs)
Amino Acids (subs)
Incretins (horm)
Epi/B2- Adrenergic Stim (horm)
Vagus Stim (neuro)

Question 3

What negatively regulates Insulin release?

Answer 3

NE/alpha 2 Adrenergic stim (neuro)

Amylin (horm)

Question 4

What are the receptors on the Beta Cell that stimulate Insulin release?

Answer 4

Glucose dn reg.
ATP Sensitive K+ Channel
leads to voltage dependant Ca++ Channel opening

Question 5

How does insulin work on the adipose and skeletal muscle cells?

Answer 5

GLUT 4 translocation

Question 6

What actions does insulin have on metabolic pathways?

Answer 6

(+)FA, glycogen, Protein synth

(-) Beta Ox, Glycogenolysis, Glycolysis, Protein catabolism

Question 7

What is the main mediatior of T1DM onset?

Answer 7

Autoimmune destruction of Beta Cells

Genetic Predisposition

Question 8

What are the precursors of Full blown T2DM?

Answer 8

Insulin resistance and insulin secretory defect
Genetic Pre-disposition
Obesity
Nutrition
Physical Activity

Question 9

What are the Signs and Symptoms of T1DM?

Answer 9

Polyuria
Thirst
Blurred Vision
Weight Loss/Polyphagia
Weakness/Dizziness
Paresthesia
Dec. LOC can be rapid or gradual onset

Question 10

How do we diagnose diabetes clinically?

Answer 10

Glucose Challenge

High Blood Glucose after a meal.

Question 11

What is the most common type of administration of Insulin?

Answer 11

Sub Cutaneous Injection

Question 12

What is the theraputic goal of Insulin therapy?

Answer 12

Maintain blood glucose concentrations between 90 and 120 mg/dL.

Question 13

Waht are the kinetic considerations of Insulin administration?

Answer 13

Diffusion into peripheral tissues is greater than with intrinsically derived insulin.

Question 14

How is insulin kinetics altered?

Answer 14

Changing the AA sequence to make it stick together for a longer or shorter amount of time.

Question 15

What are key features of Rapid acting insulin?

Answer 15

AA alteration in C terminal of B peptide Prevents insulin complex formation Duration of 3-5 hrs

Question 16

What are key features of Short acting insulin?

Answer 16

Identical to human insulin 4-12 hrs

Question 17

What are key features of Intermediate acting insulin?

Answer 17

Protaimine Insulin complex

10-20 hrs

Question 18

What are key features of Long acting insulin?

Answer 18

AA changes make it precipitate at a more neutral pH
12-20 hrs
Myristic acid added to inc duration to 22-24 hrs

Question 19

What are examples of Rapid acting Insulin?

Answer 19

Lispro
Aspart
Glulisine
Inhaled insulin

Question 20

When do you want to use short acting insulin?

Answer 20

In response to a meal.

Question 21

What are examples of Intermediate acting Insulin?

Answer 21

NPH

Question 22

What are examples of Long acting Insulin?

Answer 22

Glargine

Detemir

Question 23

What is the most common adverse effect to insulin?

Answer 23

Hypoglycemia is most common. 
Hypersensitivity(rare)
Resistance (rare)
Lipohypertrophy
Lipoatrophy

Question 24

How is Lipohypertrophy avoided?

Answer 24

Inject insulin at a different place each time.

Question 25

When is glucagon therapy used?

Answer 25

Use if pt can't take in glucose by mouth(unconcious)

Question 26

What are the key points of Metformin use?

Answer 26

1st line agent Doesn't prduce hypoglycemia Not dependant on B cell function

Question 27

What is the MOA of Metformin?

Answer 27

Dec. Hepatic Glucose output Increase peripheral glucose utilization Activation of hepatic enzyme AMP-activated protein kinase

Question 28

What are the Adverse effects of Metformin?

Answer 28

GI disturbances | Vit B12 deficiency

Question 29

What is the MOA of Sulfonylureas and Meglitinides?

Answer 29

Inhibition of ATP-sensitive potassium channel of B cell, insulin release

Question 30

What are the Contraindications of the Glucosidase inhibitors?

Answer 30

Those with GI diseases bc: Inhibits brush border glucosidase enzyme and subsequent absorption of glucose

Question 31

What is the MOA of Thiazolidinediones?

Answer 31

Dec peripheral resistance by activating peroxisome proliferator-activated receptor Effect on glucagon metabolism/insulin signaling

Question 32

What are the AA of Thiazolidinediones?

Answer 32

Peripheral edema, weight gain, hepato tox, Bone Fractures Hypoglycemia

Question 33

What is the MOA of Amylinomimetics?

Answer 33

Inhibits glucagon release Inhibits gastric emptying Anoretic effect.

Question 34

What is the MOA of Incretins?

Answer 34

Insulin secretion | otherwise the same as the amylinomimetics

Question 35

What is the MOA of DPP inhibitors?

Answer 35

inhibit incretin degradation.