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2MB Endocrinology > Diabetes Pharmacology > Flashcards

Diabetes Pharmacology Flashcards

1
Q

List drug classes that increase secretion of insulin through insulin-independent action

A

Sulphonylureas
Incretin analogues
DPP-4 inhibitors

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2
Q

List drug classes that decrease insulin resistance and reduced hepatic glucose output through insulin-dependent action

A

Biguanides

Thiazolidinediones (TZD’s)

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3
Q

List a drug class that slows glucose absorption from the GI tract through insulin-independent action

A

Alpha-glucosidase inhibitors

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4
Q

List a drug class that blocks reabsorption of glucose in the kidneys through insulin-independent action

A

SGLT2 inhibitors

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5
Q

Through which transporter does glucose enter the beta-cell in the pancreas?

A

GLUT2

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6
Q

What effect does ATP in the beta-cell of the pancreas have on K channels?

A

Closes them, causing depolarisation of the membrane

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7
Q

How is insulin released following depolarisation of the membrane of the beta-cell?

A

Depolarisation causes opening of Ca channels, causing insulin-containing vesicles to exocytose

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8
Q

List the components of the Katp channel

A

4x Kir6.2 units

4x SUR1 units

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9
Q

Which part of the Katp channel does ATP bind to?

A

Kir6.2 unit

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10
Q

What binds to the SUR1 part of the Katp channel? What does this cause?

A

ADP-Mg

Repolarisation to inhibit insulin secretion

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11
Q

How do sulphonylurea drugs work?

A

Displace ADP-Mg from SUR1 on Katp channel to cause depolarisation to promote insulin release

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12
Q

The effect of sulphonylurea drugs is independent of glucose conc. True/False?

A

True

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13
Q

Give examples of sulphonylureas

A

Tolbutamide
Glibenclamide
Glipizide

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14
Q

What is the main difference between tolbutamide and glibenclamide?

A

Glibenclamide is more potent and longer acting

Only need to take glibenclamide 1x/day

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15
Q

Can sulphonylureas cause hypoglycaemia?

A

Yes

Greater risk with long-acting agents

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16
Q

How do glinides differ from sulphonylureas?

A

Bind to specific part of SUR1

Rapid action - less likely to cause hypoglycaemia

17
Q

Incretin hormones stimulate production of insulin. What are the two main endogenous incretin hormones?

A

GLP-1

GIP

18
Q

GLP-1 and GIP enhance insulin production. What effect does GLP-1 have on glucagon?

A

Decreases glucagon release from alpha-cells

19
Q

Give an example of an incretin analogue

A

Extenatide

20
Q

Which enzyme rapidly inhibits the action of incretin hormones?

A

DPP-4

21
Q

How do DPP-4 antagonists (gliptins) work?

A

Inhibit DPP-4 to prolong actions of GLP-1 and GIP

22
Q

Give an example of a DPP-4 inhibitor

A

Sitagliptin

23
Q

What is the function of alpha-glucosidase in the intestine?

A

Breaks down carbohydrate into absorbable glucose

24
Q

How do alpha-glucosidase inhibitors work?

A

Inhibit alpha-glucosidase to delay absorption of glucose, thus reducing post-prandial increase in blood glucose

25
Q

Give an example of an alpha-glucosidase inhibitor

A

Acarbose

26
Q

Acarbose has great risk of hypoglycaemia. True/False?

A

False

No risk whatsoever

27
Q

What is the 1st line therapy for type 2 diabetes?

A

Biguanides (metformin)

28
Q

What is the proposed action of metformin?

A

Reduces hepatic gluconeogenesis by stimulating AMPK

Enhances glucose uptake by muscle

29
Q

Does metformin cause hypoglycaemia?

A

No

30
Q

Metformin causes weight gain. True/False?

A

False

Weight loss

31
Q

List a significant adverse effect of metformin

A

Lactic acidosis (as a result of less gluconeogenesis)

32
Q

How do TZDs work?

A

Agonist of PPAR-alpha which associated with RXR to enhance transcription of genes encoding insulin signalling
(ultimately enhancing insulin action at tissues)

33
Q

Which transporter moves glucose into skeletal muscle?

A

GLUT4

34
Q

TZDs can cause weight gain. True/False?

A

True

35
Q

How do SGLT2 inhibitors work?

A

Block reabsorption of glucose in convoluted tube of nephron to cause glycosuria

36
Q

Name a SGLT2 inhibitor

A

Dapagliflozin

37
Q

What is the main adverse effect/risk of SGLT2 inhibitors?

A

Increased risk of UTI

Thrush

38
Q

Give an example of a TZD

A

Pioglitazone

2MB Endocrinology (19 decks)

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