Endrocrine drugs 3: Anti-diabetes

Question 1

representative for insulin secretagogues

Answer 1

glipizide

Question 2

metformin class

Answer 2

biguanide

Question 3

amylin analog rep

Answer 3

pramlintide

Question 4

thiazolidinediones rep

Answer 4

pioglitazone

Question 5

incretin modulator reps

Answer 5

GLP-1 analog
-exenatide

DPP-4 inhibitor
-sitagliptin

Question 6

SGLT2 inhibitor rep

Answer 6

canagliflozin

Question 7

insulin secretagogues

Answer 7

1st GEN SUR
Chlorpropamide
Tolbutamide
Tolazamide

2nd GEN SUR
Glipizide
Glimepiride
Glyburide
Glibenclamide
Gliclazide

MEGLITINIDES
Repaglinide
-GLINIDE

Question 8

1st gen SUR

Answer 8

1st GEN SUR
Chlorpropamide
Tolbutamide
Tolazamide

Question 9

2nd gen SUR

Answer 9

2nd GEN SUR
Glipizide
Glimepiride
Glyburide
Glibenclamide
Gliclazide

Question 10

MEGLITINIDE

Answer 10

MEGLITINIDES
Repaglinide
-GLINIDE

Question 11

Insulin sensitizers

Answer 11

metformin

tzd (pioglitazone, rosi-, tro-)

Question 12

insulin secretagogue with the least incidence of hypoglycemia

Answer 12

NATEGLINIDE
(meglitinide)
-may be used in ckd patients
-used in diabetics with sulfa allergies
-s/e: URTI

Question 13

MOA OF BIGUIANIDES

Answer 13

1. activates AMP-stimulated protein kinase leading to inhibition of hepatic and renal gluconeogenesis
2. stimulates glucose uptake and glycolysis in peripheral tissues
3. slows gluocse absorption from the GI tract
4. reduces plasma glucagon levels

metformin and TZD bypass the insulin receptor. both act via gene expression to sensitize tissue receptor to insulin

Question 14

DOC for obese diabetics

Answer 14

metformin

Question 15

metformin remarks

Answer 15

no hypoglycemia
no weight gain (in fact, modest weight loss)
-caauses decrease in endogenous insulin production by increasing insulin sensitivity - “INSULIN SPARING EFFECT”

Question 16

s/e of TZD

Answer 16

weight gain
bone fractures
cardiovascular events, MI (rosiglitazone)
hepatotoxicity (troglitazone)
inc’d risk of bladder cncer by 63% -pioglitazole

Question 17

brothers of acarbose

Answer 17

miglitol

voglibose

Question 18

anti-diabetic that can cause acte pancreatitis

Answer 18

exenatide (GLP1 agonist)

Question 19

anti-diabetic that can cause nasopharyngitis

Answer 19

stiagliptin (DPP4 inh)

Question 20

anti-diabetic with possible thyroid ca risk

Answer 20

liraglutide (glp1 agonist)

Question 21

bile acid sequestrant

Answer 21

colesevelam

• lowers glucose through unknown mechanism
• used in type 2 dm
• s/e: malabsorption of fat-soluble vitamins and steatorrhea

Question 22

rimonabant

Answer 22

blocks cannabinoid-1 rceptors
reduces apetitie

uses

• obesity
• smoking cessation
• drug addiction

s/e
-suicidality, depression

Question 23

anti-obesity that’s a relative of methamphetamine

Answer 23

sibutramine

phentermine
-appetite suppressant which is an amphetamin derivative

Question 24

necrolytic migratory erythema

Answer 24

glucagonomas

Question 25

MOA of TZD

Answer 25

THIAZOLIDINEDIONES - increases target tissue sensitivity to insulin by activating PPAR-γ - increases uptake of glucose to adipocytes and skeletal muscles - inhibits hepatic gluconeogenesis

Question 26

most common toxic effects of metformin

Answer 26

GI (20%; DIARRHEA, nausea, vomiting, anorexia) other toxicities - vit B12 defi (interference with calcium-dep abs of B12-IF complex) - lactic acidosis (sometimes, esp in renal failure, radiocontrast) lower dose in elderly who may limited renal reserve and in those with eGFR 30-45 mL/min per 1.73 m^2

Question 27

anti-dm with proven CV benefit

Answer 27

liraglutide (GLP-1 agonist) | empagliflozin (SGLT2 i)

Question 28

no hypoglyceia

Answer 28

``` gliptin (dpp4) glutide (glp) gliflozin (sglt2i) glitazone (tzd) metformin (biguanide) ```

Question 29

with hypoglycemia

Answer 29

``` insulin SUR Meglitinide (least among secretagogues, esp NATEGLINIDE) Acarbose (when taken with SUR) Pramlintide (amylin analog) ```

Question 30

anti-dm with diarrhea side effects

Answer 30

acarbose metformin dulaglutide

Question 31

exenatide MOA

Answer 31

1. activates GLP-1 receptors 2. augments glucose-stimulated insulin release from pancreatic B cells 3. retards gastric emptying 4. inhibits glucagon secretion 5. produces satiety

Question 32

Repaglinide

Answer 32

Meglitinide (insulin secretagogue)

Question 33

Gliclazide

Answer 33

``` 2nd GEN SUR Glipizide Glimepiride Glyburide Glibenclamide Gliclazide ```

Question 34

Tolbutamide

Answer 34

1st GEN SUR Chlorpropamide Tolbutamide Tolazamide