Pharmacology

Question 1

Which transporter transports glutamate?

Answer 1

GLUT2

Question 2

What does the KATP channel look like?

Answer 2

4 K+ inward rectifiers

4 sulfonylurea receptor subuntis (arrange on the outside)

Question 3

What closes the KATP channel?

Answer 3

When ATP binds to the kir6.2 subunits

Question 4

What opens the channel?

Answer 4

When ADP-Mg2+ binds to the SUR1 subunits

Question 5

Side effects of sulfonylureas?

Answer 5

Hypoglycemia and weight gain

Question 6

Mg2+ from the SUR1 subunit (thus closing the KATP channel and stimulating insulin release)

Answer 6

Sulfonylureas

Question 7

bind to SUR1 (at a distinct benzamido site) to close the KATP channel and trigger insulin release

Answer 7

Glinides (Meglitinides)

Question 8

When and how would you take glinides?

Answer 8

Orally, before a meal

Question 9

These molecules enhance insulin release from pancreatic beta cells and delay gastric empyting

Answer 9

GLP-1 and GIP

= enhanced glucose uptake and utilization

Question 10

This molecule decreaes glucagon release from pancreatic alpha cells

Answer 10

GLP-1

= decreased glucose production

Question 11

Increase insulin secretion
Decrease glucagon secretion
Slow gastric emptying
Decrease appetitie

Answer 11

Incretin analogues e.g. extenatide

Question 12

Good effects of incretin analogues

Answer 12

Cause modest weight loss

Reduce hepatic fat accumulation

Question 13

How do you administer incretin analogues?

Answer 13

SC injection twice daily

Question 14

Side effects of incretin analgoues

Answer 14

Nausea, hypoglycemia, pancreatitis (rare)

Question 15

Liraglutide

Answer 15

Long acting incretin analogue (suitable for once daily administration)

Question 16

DPP-4 inhibitors

Answer 16

Gliptins

Question 17

Do gliptins cause hypoglycemia or weight gain?

Answer 17

No hypoglycemia

Weight neutral

Question 18

Acarbose

Answer 18

alpha glucosidase inhibitor

Question 19

How do alpha glucosidase inhibitors work?

Answer 19

Delay absorption of glucose and thus reduce prostprandial rise in blood glucose

Question 20

Adverse effects of alpha-glucosidase inhibitors

Answer 20

GI effects:

Flatulence, loose stools, diarhorrea, abdominal pain., bloating

Question 21

Risk of hypoglycemia with acarbose?

Answer 21

No

Question 22

Biguanide

Answer 22

Metformin

Question 23

Reduces hepatic gluoconeogenesis

(by stimulating AMP-activated protein kinase (AMPK) )

Reduces carbohydrate absorption

Increase fatty acid oxidation

Answer 23

Metformin

Question 24

Increase insulin secretion

Answer 24

Sulfonylureas

Glinides

Question 25

Inhibit DPP4

Answer 25

Gliptins

Question 26

GLP-1 mimickers

Answer 26

Incretin analogues

Question 27

Delay absorption of glucose and reduce post-prandial rise in blood glucose

Answer 27

Alpha glucosidase inhibitors

Question 28

Enhance action of insulin at target tissues

Answer 28

Thiazolidinediones

Question 29

Selectively block reabsorption of glucose by SGLT2 in proximal tubule Cause decrease in blood glucose

Answer 29

SGLT2 inhibitors | cause decrease in blood glucose but little risk of hypoglycemia

Question 30

Adverse effects of metformin

Answer 30

``` GI side effects Lactic acidosis (rare) ```

Question 31

Where would you find PPARy?

Answer 31

Adipocytes

Question 32

PPARy binds to DNA and promotes expression of genes encoding which proteins

Answer 32

Lipoprotein lipase Fatty acid transport protein GLUT 4

Question 33

Promote fatty acid uptake and storage in adipocytes, rather than skeletal muscle and liver Reduced hepatic glucose output

Answer 33

Thiazolidinediones

Question 34

Adverse effects of TZD's (glitazones)

Answer 34

Weight gain Fluid retention Bone fractures