Pharmacology of Diabetes Flashcards

1
Q

What are 4 drugs used in the treatment of diabets?

A
  1. Metformin
  2. DPP-4 inhibitors
  3. Sulphonylureas
  4. SGLT-2 inhibitors
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2
Q

What is the principle drug target for Metformin?

A

AMP activated protein kinase

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3
Q

What is the principle drug target for DPP-4 inhibitors?

A

Dipeptidyl peptidase-4 (DPP-4)

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4
Q

What is the principle drug target for Sulphonylureas?

A

ATP-sensitive K+ channels

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5
Q

What is the principle drug target for SGLT-2 inhibitors?

A

Sodium-glucose co-transporter-2

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6
Q

What is the drug target type for Metformin?

A

Enzyme

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7
Q

What is the drug target type for DPP-4 inhibitors?

A

Enzyme

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8
Q

What is the drug target type for Sulphonylureas?

A

Ion channels

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9
Q

What is the drug target type for SGLT-2 inhibitors?

A

Transport protein

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10
Q

What is the location for the actions of Metformin?

A

Hepatocyte mitochondria

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11
Q

What is the location for the actions of DPP-4 inhibitors?

A

Vascular endothelium

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12
Q

What is the location for the actions of Sulphonylureas?

A

Pancreatic beta cells

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13
Q

What is the location for the actions of SGLT-2 inhibitors?

A

Proximal convoluted tubule

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14
Q

What is the action of Metformin?

A

Decreased gluconeogenesis

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15
Q

What is the action of DPP-4 inhibitors?

A

Increased plasma incretin levels

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16
Q

What is the action of Sulphonylureas?

A

Insulin secretion

17
Q

What is the action of SGLT-2 inhibitors?

A

Decreased glucose reabsorption

18
Q

What are the 3 key steps to pharmacology?

A
  1. Identify the patient’s problem
  2. Specify the therapeutic objective
  3. Select a drug on the basis of comparative efficacy, safety, cost and sustainability
19
Q

What does it mean if a drug is ionized?

A

Ionized = less lipid soluble

Less absorption, into blood
Good distribution, once in blood

20
Q

What are the main side effects of Metformin?

A

GI effects

21
Q

When is Metformin most effective?

A

In the presence of endogenous insulin, so with some residual functioning pancreatic islet cells.

22
Q

What are the main side effects of DPP-4 inhibitors?

A

Upper respiratory tract infections

23
Q

When are DPP-4 inhibitors only effective?

A

When some residual pancreatic beta-cell activity is present

24
Q

What are the main side effects of Sulphonylurea?

A
  1. Weight gain

2. Hypoglycaemia

25
Q

When is Sulphonylurea only effective?

A

When some residual pancreatic beta-cell activity is present

26
Q

How can weight gain associated with sulphonylurea be mitigated?

A

The concurrent administration with Metformin

27
Q

What is an example of a Sulphonylurea?

A

Gliclazide

28
Q

What is an example of a DPP-4 inhibitor?

A

Sitagliptin

29
Q

What is an example of a SGLT-2 inhibitor?

A

Dapaglifozin

30
Q

What is gliclazide an example of?

A

Sulphonylurea

31
Q

What is sitagliptin an example of?

A

DPP-4 inhibitor

32
Q

What is dapaglifozin an example of?

A

SGLT-2 inhibitor

33
Q

What are the main side effects of SGLT2 inhibitors?

A
  1. Uro-genital infections
  2. Slight decrease in bone density
  3. Can worsen beta-ketoacidosis (stop immediately)1
34
Q

What can SGLT2 inhibitors cause?

A
  1. Weight loss

2. Reduction in BP

35
Q

When is SGLT2 less effective?

A

Patients with renal impairment