Diabetes Druges

Question 1

Clear solution of insulin
Only insulin suitable for intravenous use
Human sequence

Answer 1

Regular insulin

Question 2

Cloudy suspension of insulin aggregated with protamine and zinc
Longer time to break down aggregates –> delayed, longer time course vs regular insulin

Answer 2

NPH insulin

Question 3

Mixture of NPH and regular insulin in fixed proportions (70%, 30%)

Answer 3

Pre-mixed insulins

Question 4

Synthetic insulins where one or more amino acids of human insulin have been changed to yield either very short or long acting insulins

Answer 4

Insulin analogs

Question 5

Insulin analogs that more readily form monomers in solution
Compressed time course of action relative to regular insulin
Shorter onset of action and quicker deactivation
Time course closer to that or normal meal-induced peak of pancreatic insulin

Answer 5

Lispro insulin

Insulin aspart

Question 6

Lispro insulin amino acid changes

Answer 6

Normal pro-lys dipeptide at positions B28 and B29 are reversed

Question 7

Insulin aspart amino acid changes

Answer 7

B28 proline is replaced by an aspartic acid residue

Question 8

Long acting insulin analog
Amino acid asparagine normally found at position A21 is replaced by glycine and 2 arginines are added to the C-terminus of the B-chain
Soluble at pH4 but poorly soluble at pH7
Forms a fine ppt in interstitial fluids

Answer 8

Insulin glargine

Question 9

Long acting due to self-associated at the subcutaneous injection sites and by binding albumin in the blood stream
Threonine at B30 omitted and a C14 fatty acid chain is attached to B29

Answer 9

Insulin Detemir

Question 10

Short acting insulin

Answer 10

Regular
Lispro
Insulin aspart

Question 11

Intermediate acting

Answer 11

NPH

Question 12

Long acting

Answer 12

Insulin Glargine

Insulin Detemir

Question 13

How are intermediate and long acting insulins given?

Answer 13

To mimic a 24 hour basal insulin secretion

Question 14

How are short acting insulins given?

Answer 14

Pre-prandially to mimic nutrient-stimulated insulin secretion

Question 15

What are the goal for glycemic control??

Answer 15

1. fasting and pre-prandial glucoses 70-130mg%
2. post-prandial glucoses 2 hours after a meal less than 180 mg%
3. Hemoglobin a1C less than 7%

Question 16

What are some examples of insulin regimens?

Answer 16

Split-mixed regimens
Dinner NPH moved to bedtime to move peak of action from 3am to 7am
Basal-bolus regimen ( short acting analog before each meal and once per day insulin glargine)
Continulous subcutaneous insulin (CSI) = insulin pump therapy

Question 17

What are some side effects of insulin?

Answer 17

Hypoglycemia
Insulin allergy 
Lipoatrophy 
Lipohypertorphy
Insulin edema
Weight gain 
? Atherosclerosis (high doses)
? Increased cancer (high doses)

Question 18

Simulate insulin secretion by the pancreas

Interact directly with B-cells potassium transporter causing depolarization and secondarily calcium influx

Answer 18

Sulfonylureas

Question 19

Sulfonylurea drugs

Answer 19

Glipizide
Glyburide
Glimepiride

Question 20

SE of sulfonylurea drugs

Answer 20

Hyponatremia (rare)
Disulfiram-like reaction (rare)
Rashes/GI upset
Hypoglycemia (common)

Question 21

Insulin-sensitizing drugs
Reduce insulin resistance
Making a given amount of insulin more effective at reducing hepatic glucose production and or increases peripheral glucose utilization in the presence of medications
Reduce glucose levels approximately 50mg%

Answer 21

Metformin (biguanide)

Thiazolidinediones (rosiglitazone, pioglitazone)

Question 22

Biguanide
Major effect is to make the liver more sensitive to insulin
CI in renal insufficiency

Answer 22

Metformin

Question 23

SE of Metformin

Answer 23

GI side effects
Lactic acidosis (serious)

Question 24

Make peripheral tissues (fat and muscle) more sensitive to insulin by activating PPAR (peroxisome proliferator-activated receptor)

Answer 24

Thiazolidinediones (rosiglitazone, pioglitazone)

Question 25

SE of Thiazolidinediones

Answer 25

Liver toxicity
Weight gain
Fluid retention
CI in heart failure
Rosiglitzaone may increase cardiac ischemic events
Pioglitazone has a FDA advisory for increased cancer risk

Question 26

Glucosidase inhibitors
Inhibits enteric enzymes that break down complex carbohydrates, resulting in partial malabsorption of carbs
Reduces post-prandial hyperglycemia

Answer 26

Acarbose

Question 27

Major side effects of Acarbose

Answer 27

Bloating, abdominal discomfort, diarrhea, flatulence

Question 28

GLP-1 analog 
Augments insulin secretion
Increases beta-cell mass
Inhibits glucagon secretion 
Promotes a bit of weight loss

Answer 28

Exenatide

Liraglutide

Question 29

Inhibitor of GLP-1 protease DPP-4

Prolongs the action of GLP-1 in portal circulation

Answer 29

Sitagliptin

Question 30

Inhibits the sodium-glucose transport protein (SGTP-2) that reabsorbs glucose
Leads to loss of glucose in the urine
Decreases serum glucose by 20 mg% and decreases glycated hemoglobin by 0.75%

Answer 30

Canagliflozin

Question 31

SE of Canagliflozin – SGTP-2 inhibitor

Answer 31

Genital yeast infections

Question 32

Lower HgbA1C by 1.5%

Answer 32

Sulfonylureas

Metformin

Question 33

Lower HgbA1C by 0.75%

Answer 33

Acarbose
Thiazolidinediones
DPP-4 inhibitors
SGPT-2 inhibitors

Question 34

What is a common combination treatment for type 2 diabetes?

Answer 34

Insulin or an oral sulfonylurea with an insulin sensitizing drug

Sulfonylurea/DPP-4 OR Insulin
WITH
Metformin OR Thiazolidinedione

Question 35

A rapid-acting insulin secretion-stimulating agent for the treatment of type 2 diabetes
Not recommended as mono therapy – >may be added to metformin therapy for those patients with continued postprandial hyperglycemia

Answer 35

Meglitinide