Diabetes Medications

Question 1

Metformin is the most common used drug in what class?

Answer 1

biguanides

Question 2

WHat is metformin derived from?

Answer 2

french lilac

Question 3

What does metformin do?

Answer 3

1. inhibits the enzymes used for gluconeogenesis
2. inhibits hepatic uptake of gluconeogenic substrates
3. suppresses the mitochondrial repsiratory chain, increases insulin receptor tyrosine kinase activity and stimualtes GLUT4 transporters —– all increasing insulin sensitivity

Question 4

What are the side effects of metformin?

Answer 4

about 50% complain of diarrhea with the initial dose

lactic acidosis is the most serious side effect

Question 5

Why does the lactic acidosis happen?

Answer 5

the circulating lactate isn’t used as a substrate for gluconeogenesis, but those enzymes are inhibited

this means the lactate just builds up in the blood causing an acidosis

Question 6

What are sufonylureas in general?

Answer 6

insulin secretagogues (meaning they promote insulin secretion)

Question 7

What is the most commonly used sulfonylurea?

Answer 7

Glimepiride

Question 8

How does Glimepiride work?

Answer 8

by binding to the SUR1 subunit of the ATP=sensitive potassium channel

it makes the channel close (essentially acting like glucose does)

This activates the Ca channels increasing intracellular Ca and thus triggering insulin release

Question 9

What are the primary side effects of glimepiride?

Answer 9

hypoglyecmia

weight gain

Question 10

Glimepiride is the most common, but what are some otherse?

Answer 10

First gen: tolbutamide, chlorporpamide

second gen: Glimepiride, glyburide, Glipizide

Question 11

What made the second generations better than the first generations?

Answer 11

the first generations has half lives that were too long

Question 12

How do they alter the pharmacokinetics of synthetic insulin preparations?

Answer 12

they use different amino acid substitutions in the alpha and beta chains

Question 13

What insulin preparations are rapid acting?

Answer 13

Lispro
Aspart
Glulisine

Question 14

What is the time of onset for the rapid acting? Peak effect? Duration?

Answer 14

15 minute to onset
max at .5-1.5 hours
Duration about 3-4 hours

Question 15

What is the short acting insulin?

Answer 15

regular insulin!

Question 16

What is the time of onset for insulin? Maximum effect? Duration?

Answer 16

30 minutes to onset
max at 2-3 hours
4-8 hr duration

Question 17

What is the intermediate acting insulin?

Answer 17

NPH insulin

Question 18

How long to onset? Maximum? Duration?

Answer 18

2-4 hours to onset
4-12 hours maximum effect
10-20 hour duration

Question 19

What are the two long acting insulins?

Answer 19

Glargine

Detemir

Question 20

How long does it take for the long acting to start having effect? WHen’s their max effect? Duration?

Answer 20

1-2 hours to onset
there’s no peak!!!
duration of 18-24 hours

Question 21

What are the main side effects of insulin?

Answer 21

hypoglycemia (duh)
weight gain
allergic reaction to the preparation
atrophy or hypertrophy of subcutaneous fat at injection site
insulin resistance

Question 22

Which incretin do we make analogs of to promote insulin secretion and inhbit glucagon secretion?

Answer 22

GLP-1 analogs

Question 23

What is the main example of a GLP-1 analog?

Answer 23

Exenatide

Question 24

How is exenatide administered?

Answer 24

administered subq before a meal

Question 25

What are the side effects of exenatide?

Answer 25

nausea, vomiting and pancreatitis

Question 26

What’s another way we can use the action of GLP-1 in our favor?

Answer 26

We can use a DDP-IV enzyme inhibitor to prevent it’s degradation and increase it’s activity

Question 27

Name the DDP-IV inhibitor we learned.

Answer 27

Sitagliptin (Januvia)

Question 28

How do Meglitinides work?

Answer 28

they’re insulin secretagogues –block the K channel

Question 29

What are the two examples of Meglitinides?

Answer 29

Repaglinide

Nateglinide

Question 30

What are the main side effects of the melitinides?

Answer 30

hypoglycemia, weight gain, tremor, nausea, vomiting, dizziness

Question 31

How are the meglitinides administered?

Answer 31

orally, take with meal, duration of action 5-8 hours

Question 32

So…the meglitinides work sort of like what other class of drug?

Answer 32

sulfonylureas like glipizide

Question 33

What class of drugs will slow intestinal digestion and absorption of carbohydrates?

Answer 33

alpha-glucosidase inhibitors

the glucosidases hydrolyze carbs to monosaccharides

Question 34

What are the two alpha-glucosidase inhibitors we know?

Answer 34

acarbose

miglitol

Question 35

What would an amylin analog do?

Answer 35

delay gastric emptying and inhibit glucagon secretion
inhibit gluconeogenesis
increase satiety

Question 36

What’s the amylin analog we know?

Answer 36

PrAMLIntide

Question 37

How is Pramlintide administered?

Answer 37

SC administration before meals with peak concentration in 30 minutes

Question 38

Why would you probably not gives pramlintide in combo with insulin?

Answer 38

it can induce severe hypoglycemia

Question 39

What do the Thiazolidinediones do?

Answer 39

they are PPAR receptor agonists that increase glucose uptake and utilization by increasing synthesis and transport of GLUT transporter in muscle, adipose and liver

Question 40

What are the two thiazolidinediones we know?

Answer 40

Rosiglitazone

Pioglitazone

Question 41

So what do you need if the thiazolidinediones are going to work?

Answer 41

some level of insulin

Question 42

Why did a lot of doctors stop prescribing the thiazolidinediones?

Answer 42

there was maybe an increased risk of heart failure and cardiovascular events, but probably not now

Question 43

What group of people should you not use pioglitazone in?

Answer 43

those with previous or current bladder cancer - it’s been found to increase the risk