DM Drugs

Question 1

Metformin

Glycemia? Weight? Other effects?

Answer 1

Euglycemic, weight loss, decreases macrovascular events (stroke, #1 DM killer), decreases TG.

Question 2

Metformin S/E

Answer 2

Common: GI (diarrhea)

Serious: Lactic acidosis (esp in ESRD, also in hepatic dz, alcoholism, diseases that predispose to hypoxia: CHF, COPD, being super sick in the hospital, etc). Take pts off 2 days before contrast and when in hospital sick.

Question 3

Metformin–does it have a black box?

Answer 3

Yes, Lactic acidosis

Question 4

Metformin–when to take off

Answer 4

2 days before getting contrast
If sick in the hospital
If kidneys are failing
If pt can’t tolerate the diarrhea

Question 5

Which drugs are second line after Metformin?

Answer 5

Incretins:

incretin mimetics {“-tide”, exenatide (Byetta), Liraglutide (Victoza), Dulaglutide (Trulicity)}

DPP-IV inhibitors {“-gliptin”, sitagliptin (Januvia), saxagliptin (Ongyliza), Linagliptin (Tradjenta), Alogliptin (Nesina)}

Question 6

How is Metformin given?

Answer 6

Orally–

850-1000mg PO bid, start low and move up. Give w meals, stop for contrast

Extended release: 1000-2000 PO qpm

Question 7

Metformin MOA

Answer 7

Increases insulin sensitivity–> increased glucose uptake.

Decreases hepatic glucose production (gluconeogenesis)

decreases GI glucose absorption

Decreases glucagon production

Question 8

MOA incretin mimetics

Answer 8

Activate glucagon-like-peptide-1 (GLP1) receptor–> increase insulin secretion, decrease glucagon secretion, delay gastric emptying

Question 9

MOA DPP-IV inhibitors

Answer 9

Blocks DPP-IV, which degrades incretins, thereby potentiality incretin effects. (Up insulin, dn glucagon, dn gastric emptying)

Question 10

Name the incretin mimetics

Answer 10

Exenatide (Byetta)
Liraglutide (Victoza)
Dulaglutide (Trulicity)

Question 11

Name the DPP-IV inhibitors

Answer 11

Sitagliptin (Januvia)
Saxagliptin (Ongyliza)
Linagliptin (Tradjenta)
Alogliptin (Nesina)

Question 12

How are incretin mimetics administered?

Answer 12

S.C…..either 60 min before 2 main meals, or once a week

Question 13

How are DPP-IV inhibitors administered?

Answer 13

Orally…once a day (Januvia 100mg)

Question 14

Adverse effects of Incretin mimetics

Answer 14

Common: GI disturbance. Slows GI emptying, so careful w pts w slow GI dz. careful w renal impairment.

Bad: pancreatitis, pancreatic CA.

Question 15

Adverse effects of DPP-IV inhibitors

Answer 15

Common: Less than incretin mimetics. Slow GI probs

Bad: pancreatitis, pancreatic CA (less than incretins)

Question 16

Main difference between incretin mimetics and DPP-IV inhibitors

Answer 16

Incretin mimetics cause weight loss, DPP-IV I are weight neutral.

Question 17

Do incretin mimetics have a black box?

Answer 17

Yes—Liraglutide (Victoza), for Thyroid CA. Contraindicated in pts w medullary thyroid carcinoma hx or FHx, and in pts w MEN-2

Question 18

Do DPP-IV inhibitors have a black box?

Answer 18

No

Question 19

Third line after Metformin and incretins?

Answer 19

SLGT2 Inhibitors, glitizones, alpha-glucosidase inhibitors, welchol/colesevelam

Question 20

Name the SLGT2 inhibitors

Answer 20

Canagliflozin (Invokana)

Dapagliflozin (Farxiga)

Question 21

SGLT2 inhibitors MOA

Answer 21

Inhibit SGLT2 transporters in proximal tubule, causing glucose to be peed out

Question 22

Contraindications/cautions to SGLT2-I

Answer 22

Severe renal impairment/dialysis; prone to UTIs, etc

Question 23

Adverse effects of SGLT2-I

Answer 23

Genital mycotoxins infections, UTIs etc

Osmotic diuresis (causes ortho hypo, dehydration, so careful in pts w renal impairment.)

Question 24

Incretins lower glucose when?

Answer 24

Fasting and post prandial

Question 25

SGLT2-I decrease glucose when?

Answer 25

A1c

Question 26

MOA alpha-glucosidase inhibitors

Answer 26

Inhibit alpha-glucose fade in small intestine–> decrease in absorption of glucose.

Question 27

S/E alpha-glucosidase inhibitors

Answer 27

Common: gas (VERY gassy)

Question 28

AGI caution

Answer 28

Slow GI (ileus, obstruction, IBS, hernia)
Hepatic dz
Renal impairment

Question 29

AGI decreases glucose when? Other effects?

Answer 29

Decreases post prandial glucose

No effect on weight or fasting glucose

Question 30

Thiazolindinediones names

Answer 30

-glitazones

Pioglitazone (Actos)
Rosuglitazone (Avandia)

Question 31

Do AGI have a black box?

Answer 31

No

Question 32

Do TZDs have a black box?

Answer 32

Yes–Rosiglitazone, for CHF, cause or exacerbate it (edema). MI/angina.

Question 33

MOA TZDs

Answer 33

Insulin sensitizers. Bind to nuclear PPAR-alpha receptor–> inc glucose transporters.

DO NOT increase insulin secretion

Question 34

Effects of TZDs

Answer 34

Decrease insulin resistance (can use prophylactically), TG, fasting glucose, A1c. Slight inc HDL.

Question 35

Adverse s/e, cautions

Answer 35

Appetite stimulant–> weight gain
Edema–> inc risk of HF in CHF

caution in liver dz, CHF (EF

Question 36

MOA Colesevelam

Answer 36

Bile acid binding resin…unk why it works.

Question 37

Colesevelam uses

Answer 37

Decrease fasting glucose in combo. Good in HLD but also inc TG.

Question 38

Name bile acid binding resin

Answer 38

Colesevelam (Welchol)

Question 39

Do resins have a black box?

Answer 39

No

Question 40

Adverse effects/cautions of resins

Answer 40

Generally safe/no common s/e

Caution: Slow GI dz, TG>500, GI obstruction /surgery,

Question 41

Sulfonylureas/Meglitinides

Answer 41

Stimulate beta cells to produce insulin. VERY hypoglycemic. Destroy pancreas quicker. Sulfonylureas=sulfas, contra in sulfa Ax. Also cause weight gain. Meglitinides are short acting, others are long.

Question 42

Name the Sulfonylureas

Answer 42

First gen: Tolbutamide, Chlorpropamide, Tolazamide

Second gen: Gluburide, Glipizide, Glimepiride

Question 43

Name the Meglitinides

Answer 43

-glinides
Repaglinide (Prandin)
Nateglinide (Starlix)

Question 44

What is Metformin used for?

Answer 44

DM2 and PCOS