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PHA332 > Anti- diabetic drugs SD > Flashcards

Anti- diabetic drugs SD Flashcards

1
Q

What are the 3 fundamental strategies for anti-diabetic drugs?

A

Increase cellular sensitivity
Increase insulin release
Reduce/ delay glucose absorption

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2
Q

What class of drug is metformin?

A

Biguanide

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3
Q

What is the active ingredient in biguanides?

A

Guanidine (and galegin)

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4
Q

What do biguanides do in order to lower hyperglycaemia?

A

Improve insulin sensitivity
Stimulate tissue uptake of glucose (esp muscle)
Reduces GI uptake of carbohydrates
Antihyperglycaemic effects

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5
Q

What are the effects of metformin which make it 1st line therapy in fat people?

A

It doesn’t cause weight gain as it suppresses appetite

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6
Q

What is lactic acidosis?

A

Lactic acid build up in the blood stream

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7
Q

What is the half life of metformin?

A

1.5hrs

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8
Q

Why are biguanides useful in late stage diabetes?

A

In late stages, B cell decline has occurred so insulin can not be produced as well. Metformin does not increase insulin secretion, it sensitises patient cells to it hence why it is useful

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9
Q

What is kinase and what does it do?

A

An enzyme which adds phosphate groups

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10
Q

Why are people with impaired renal function below 45ml/min not allowed metformin?

A

Increased risk of lactic acidosis, need working kidneys to remove the lactate

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11
Q

What is glucogenesis?

A

Ability to metabolically generate new glucose

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12
Q

What are the side effects of metformin?

A

Diarrhoea
Dyspepsia
Lactic acidosis

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13
Q

What can make lactic acidosis worse/ life threatening?

A

Dehydration

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14
Q

Name another insulin sensitiser group of drugs and an example within that group (not biguanides)

A

Thiazolidinediones- pioglitazone

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15
Q

What does pioglitazone do to
a) IL-6
b) adiponectin

A

a) decreases IL-6
b) increases adiponectin

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16
Q

Name 3 adverse effects with pioglitazone

A
  1. weight gain
  2. liver dysfunction (rare)
  3. fluid retention (kidneys)
17
Q

Why should pioglitazone be avoided in patients with congestive heart failure?

A

Due to the risk of oedema (fluid retention in kidneys)

18
Q

What do secretagogues do?

A

Increase insulin production

19
Q

Name a 1st generation and a 2nd generation secretagogue

A

1st- tolbutamide
2nd- gliclazide

20
Q

What is the MOA of secretagogues?

A

They bind to the receptor, close potassium channels and open calcium channels to export insulin—> lower glucose, increase insulin

21
Q

When would sulphonylureas be used in diabetes?

A

Where metformin is contraindicated or if the patient is NOT over weight

22
Q

What is the MOA of sulphonylureas?

A

Stimulates B cells of the islet of Langerhans in the pancreas to release insulin which lowers glucose

23
Q

sulphonylureas are ineffective where there is no insulin production, why?

A

IF there is not insulin production this means there is no/ lack of B cells which means there are no B cells to drive to produce insulin.
Hence this drug is normally used in earlier stages on diabetes before a decline in B cells

24
Q

How is gliclazide metabolised and excreted? (which organs)

A

Metabolised by the liver
Excreted mainly by the kidneys

25
Q

Why is gliclazide less likely to cause hypoglycaemia compared to other sulphonylureas?

A

It only interacts with SUR1 not EPAC2 which also increases insulin levels hence decreasing glucose levels further—> hypo

26
Q

What is the new weight loss craze and how does it work?

A

GLP-1
Increases metabolism, insulin secretion and glucose break down

27
Q

Why do we use a DPP-4 enzyme inhibitor in diabetes?

A

Body naturally degrades GLP-1 though the DPP-4 enzyme, but GLP-1 lowers hyperglycaemia so we don’t want it broken down. Hence we use DPP-4 inhibitors called gliptins which are competitive inhibitors of DPP-4 which help prolong GLP-1 and GIP activity to reduce glucose

28
Q

Give a named example of DPP-4 inhibitor

A

Sinagliptin

29
Q

Name a SGLT2 inhibitor and how it works

A

‘Gliflozin’ eg. dapagliflozin
Works by inhibiting SGLT2 receptors by blocking kidney transporter so glucose is urinated out instead of recycled back into blood stream hence lowering glucose levels.

30
Q

What anti-diabetic drug alters glucose absorption?

A

SGLT2 inhibitors

PHA332 (8 decks)

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