Pharm2 1 T2DM Agents pt3

Question 1

What are Alpha-glucosidase inhibitors?

Answer 1

A T2DM drug not commonly utilized

These block the digestion of carbohydrates. They just go through GI system and you don’t absorb those calories.

Question 2

Why are Alpha-glucosidase inhibitors not commonly used?

Answer 2

b/c this causes very understandable GI side effects.

Question 3

Example of an Alpha-glucosidase inhibitors

Answer 3

Acarbose

Question 4

due to MOA, Acarbose (Alpha-glucosidase inhibitors) must be taken when?

Answer 4

with first bite of each main meal

Question 5

Acarbose: Cautions, Precautions, Pregnancy info.

Answer 5

Cautions: liver disease/dysfunction, IBS (or any chronic bowel disease), predisposition to bowel obstruction
Precautions: monitor LFTs, use glucose (not sucrose) to reverse hypoglycemia
Pregnancy: Cat B; consider switch to insulin

Question 6

If Acarbose causes hypoglycemia, how would you reverse it?

Answer 6

Using glucose. (cannot use sucrose)

Question 7

Alpha-glucosidase inhibitors Efficacy of lowering HbA1C in monotherapy is

Answer 7

~0.8

0.6 – 1.3

Question 8

Meglitinides MoA

Answer 8

Lowers blood glucose by stimulating the release of insulin from the pancreas in a similar manner to sulonylureas BUT AT A SEPARATE BINDING SITE

Question 9

How to take Meglitinide

Answer 9

take within 30 minutes before meals adding/skipping a dose if meal is added/skipped

Question 10

All T2DM agents in this PPT are FDA approved for people >__years old.
EXCEPT ___, which is >_ years old

Answer 10

> 18 years old

except Metformin’s immediate release form (Glucophage, taken BID). This is >10 years old

Question 11

Meglitinide: Caution, Precaution, What to do w/ preg patient

Answer 11

Cautions: not for use concurrently with NPH insulin – serious cardiovascular events may occur; when combined with other oral agents may increase CV risk mortality
Precautions: involved in CYP3A4 pathway resulting in multiple drug-drug interactions
Pregnancy: switch to insulin

Question 12

Meglitinide is involved in ___ pathway resulting in multiple drug-drug interactions

Answer 12

CYP3A4

Question 13

Overall, Meglitinides work similar to SU’s, buuuut:

Answer 13

SU’s have less side effects, so this isn’t often prescribed.

Question 14

Dual MOA of DPP-4 inhibitors

Answer 14

slows gastric emptying
inhibit insulin degradation, glucagon release, and increase satiety (you feel full), resulting in lowering of serum glucose levels

(insulin hangs around longer, making insulin levels higher, glucose is pulled across membrane better, and there will be better glucose labs),

Question 15

What is incretin? (its lvl is increased by DPP-4 Inhibitors)

Answer 15

gastrointestinal hormones that cause an increase in the amount of insulin released from the beta cells of the islets of Langerhans after eating, even before blood glucose levels become elevated.

Question 16

When you eat the body recognizes food as it enters your gut (stomach, into duodenum). These drugs mediate the natural response (to release insulin through a cascade of responses, and insulin after about 3 minutes is degraded naturally by the body)
So what 2 types of drugs only affect us when we eat?

Answer 16

DPP-4 inhibitors and GLP-1 inhibitors

Both of these drugs work on incretin effect
Prof Herman thinks they’re cool

Question 17

Ex of a DPP-4 Inhibitor

What is it often combined with?

Answer 17

Sitagliptin. Often combined with Metformin.

Question 18

Sitagliptin: Cautions, Precautions, Pregnancy

Answer 18

Cautions: renal disease (adjust dose) or dysfunction, severe hepatic insufficiency
Precautions: confirm normal renal function prior to initiation and periodically; consider cutting dose in half when used with CYP-450 drugs
Pregnancy: Cat B; consider switch to insulin

Question 19

2 big side effects of Sitagliptin (DPP-4). Why do they happen?

Answer 19

URI, nasopharyngitis
This is a DPP 4 (receptor) drug, and there is also a DPP 1,2,3,5 as well. There is crossover into these receptors. These other receptors are what leads to the URI, nasopharyngitis.

Question 20

What is Sodium-Glucose Co-transport-2?

Answer 20

expressed naturally in the proximal renal tubules, is responsible for at least 90% of the reabsorption of filtered glucose from the tubular lumen

Question 21

SGLT-2 example:

What’s its MoA?

Answer 21

Canagliflozin
inhibits SGLT2, reducing reabsorption of filtered glucose and lowers the renal threshold for glucose (RTG), and thereby increases urinary glucose excretion

Question 22

“Piss profit” put a drop of urine on their tongue, and predicted if ppl were about to die, and did this very accurately bc:

Answer 22

these ‘patients’ had DKA

Question 23

Body normally tries to pee glucose out, but ___ reabsorbs it at levels you normally physiologically don’t.

Answer 23

SGLT-2