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Flashcards in Exam 7: Diabetes Deck (33):
1

Thiazolidinediones uses

Type 2 diabetes
Pioglitazone is only one commonly prescribed
Taken daily in combo with other drugs for diabetes
Effects are mediated by gene expression, so it may take 1-3 months to see benefits

2

Name 1 alpha-glucosidase inhibitor

Acarbose

3

Acarbose

Alpha-glucosidase inhibitor
Used for type 2 DM, pre diabetes
Slowly titration up to desired dose
Inhibits enzymes that break down complex carbs
Delays and spreads out absorption of glucose after meals
Minimally absorbed
If a patient on Acarbose gets hypoglycemic, they need to get glucose or dextrose, not sucrose which requires alpha-glucosidase to be broken down

4

Acarbose adverse effects

GI disturbances
Flatulence, diarrhea, abdominal pain
Side effects get less prominent over time due to up regulation of alpha-glucosidases in the distal small intestines

5

Acarbose contraindications

IBD
Renal impairment
Other GI problems

6

Which bile acid sequesterant can be used in treatment of DM?

Colesevelam

7

Pramlintide

Amylin analog, acts on receptor in hindbrain
Suppresses Glucagon release, delays gastric emptying....
Can cause nausea, weight loss, hypoglycemia.
Adjunct to insulin therapy, must be injected separately
Lowers amount of insulin need, mealtime insulin doses should be reduced by about 50%

8

Pramlintide contraindications

Gastroparesis or any other GI motility disorder

9

GLP-1 agonist

Exenatide

10

Exenatide

Synthetic exenidin 4, an incretin
Glucagon like peptide 1 receptor agonist
Therapy for type DM
Causes increased insulin synthesis and secretion in a glucose dependent manner (as opposed to sulfonureas). Less likely to cause hypoglycemia
Also causes delayed gastric emptying and decreased appetite
Also suppresses post prandial glucagon release
Rapidly absorbed after injection
GI disturbances are a common side effect

11

Liraglutide

GLP1 agonist
Like Exenatide, but is more slowly absorbed. It also binds to albumin, slowing its metabolism
Black box warning, not for use in patients with family history of medullary cancer or multiple endocrine neoplasia type 2

12

GLP1 agonist adverse effects

GI disturbances
Weight loss
Hypoglycemia maybe
Pancreatitis
Can alter pharmacokinetics of drugs that require Rapid GI absorption

13

GLP1 contraindication

Pancreatitis

14

DPP-4 inhibitors

Sitagliptin
Other gliptins

15

Sitagliptin

DPP-4 inhibitor
Increases levels of circulating incretins
Can be taken orally
Result in increased insulin, decreased glucagon release after meals

16

DPP-4 adverse effects

Increased risk of infection
Headache
Hypoglycemia when combined with a sulfonurea
Hyper sensitivities
Pancreatitis

17

Saxagliptin

DPP-4 inhibitor that is a prodrug, doses need to be adjusted with CYP inhibitors

18

SGLT2 inhibitors

Canagliflozin
Other flozins

19

Canagliflozin

SGLT2 inhibitor
Decreased glucose reabsorption in kidneys
Increase risk of genital mycotic infections, UTIs
Contraindication = severe renal impairment

20

Glucagon

Peptide produced by pancreatic alpha cells
Used for emergency treatment of severe hypoglycemia when patient is unconscious and intravenous glucose isn't feasible
Also treats beta blocker overdose
Binds to G protein receptor, increases cAMP
Raises blood glucose (glycogenolysis)
Can cause nausea, vomiting, hypertension, tachycardia

21

Contraindications for Thiazolidinediones

Pregnancy
Hepatic impairment (periodic liver function tests required)
Heart failure

22

Sulfonureas Mechanism

Increase secretion of endogenous insulin
Inhibit K ATP channels in pancreatic Beta cell membranes

23

Name 1 Sulfonurea

Glyburide

24

Glyburide

Sulfonurea

25

3 Side effects of Sulfonureas (glyburide)

Hypoglycemia, weight gain, sulfa allergy

26

Contraindications for Sulfonureas (glyburide)

Hepatic or renal impairment could compromise metabolism or excretion of the drug
Pregnant/breastfeeding women (teratogenic)
Patients especially susceptible to hypoglycemia (elderly, acute cardiovascular disease)

27

Clinical Uses of Sulfonureas

Glyburide
Used to treat DM type II.
They get less effective as pancreatic beta cells lose function
Widely used, often with metformin, thiazolidones.

28

Name one Meglitinide

Repaglinide

29

Repaglinide

Meglinitide
Like sulfonureas, increases endogenous insulin secretion by inhibiting K ATP channels
May cause hypoglycemia, weight gain
Use with caution in patents with renal/hepatic impairment
Nateglinide may be safer for those with renal/hepatic impairment

30

Meglinitide Uses/Advantages

(Repaglinide, nateglinide)
Treats DM type II
Pre-prandial delivery because they are more rapidly acting than sulfonureas.
Safe for those with sulfa allergies

31

Name two Thiazolidinedione

Pioglitazone
Rosiglitazone

32

Thiazolidinedione Mechanism

Increase insulin sensitivity in tissues by being Peroxisome proliferator-activated receptor gamma (PPARγ) agonists
These are nuclear receptors that regulate genes involved in glucose and lipid metabolism

33

What are the two most common side effects of Thiazolidinedione?

Weight gain and edema (edema may lead to CHF)
May also increase risk of osteoporosis in women.
Pioglitazone may increase risk of bladder cancer