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Flashcards in Pharmacology Deck (34)
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1
Q

Which transporter transports glutamate?

A

GLUT2

2
Q

What does the KATP channel look like?

A

4 K+ inward rectifiers

4 sulfonylurea receptor subuntis (arrange on the outside)

3
Q

What closes the KATP channel?

A

When ATP binds to the kir6.2 subunits

4
Q

What opens the channel?

A

When ADP-Mg2+ binds to the SUR1 subunits

5
Q

Side effects of sulfonylureas?

A

Hypoglycemia and weight gain

6
Q

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

A

Sulfonylureas

7
Q

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

A

Glinides (Meglitinides)

8
Q

When and how would you take glinides?

A

Orally, before a meal

9
Q

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

A

GLP-1 and GIP

= enhanced glucose uptake and utilization

10
Q

This molecule decreaes glucagon release from pancreatic alpha cells

A

GLP-1

= decreased glucose production

11
Q

Increase insulin secretion
Decrease glucagon secretion
Slow gastric emptying
Decrease appetitie

A

Incretin analogues e.g. extenatide

12
Q

Good effects of incretin analogues

A

Cause modest weight loss

Reduce hepatic fat accumulation

13
Q

How do you administer incretin analogues?

A

SC injection twice daily

14
Q

Side effects of incretin analgoues

A

Nausea, hypoglycemia, pancreatitis (rare)

15
Q

Liraglutide

A

Long acting incretin analogue (suitable for once daily administration)

16
Q

DPP-4 inhibitors

A

Gliptins

17
Q

Do gliptins cause hypoglycemia or weight gain?

A

No hypoglycemia

Weight neutral

18
Q

Acarbose

A

alpha glucosidase inhibitor

19
Q

How do alpha glucosidase inhibitors work?

A

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

20
Q

Adverse effects of alpha-glucosidase inhibitors

A

GI effects:

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

21
Q

Risk of hypoglycemia with acarbose?

A

No

22
Q

Biguanide

A

Metformin

23
Q

Reduces hepatic gluoconeogenesis

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

Reduces carbohydrate absorption

Increase fatty acid oxidation

A

Metformin

24
Q

Increase insulin secretion

A

Sulfonylureas

Glinides

25
Q

Inhibit DPP4

A

Gliptins

26
Q

GLP-1 mimickers

A

Incretin analogues

27
Q

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

A

Alpha glucosidase inhibitors

28
Q

Enhance action of insulin at target tissues

A

Thiazolidinediones

29
Q

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

A

SGLT2 inhibitors

cause decrease in blood glucose but little risk of hypoglycemia

30
Q

Adverse effects of metformin

A
GI side effects
Lactic acidosis (rare)
31
Q

Where would you find PPARy?

A

Adipocytes

32
Q

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

A

Lipoprotein lipase
Fatty acid transport protein
GLUT 4

33
Q

Promote fatty acid uptake and storage in adipocytes, rather than skeletal muscle and liver

Reduced hepatic glucose output

A

Thiazolidinediones

34
Q

Adverse effects of TZD’s (glitazones)

A

Weight gain
Fluid retention
Bone fractures