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Year 2 Endocrine > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

List the drugs which are dependent on insulin?

Increase insulin secretion

A

sulfonylureas
Incretin analogues
Glinides
DPP-4 inhibitors

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2
Q

List the drugs which are dependent on insulin?

Decrease insulin resistance

A

Biuanide

(Glitazones) Thiazolinediomes

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3
Q

List the drugs which are independent of insulin?

Slow Glucose absorption

A

alpha glucoside inhibitors

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4
Q

List the drugs which are independent of insulin?

Enhance glucose excretion

A

Sodium Glucose Transporter Type 2 Inhibitor

SGLT2 inhibitor

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5
Q

Name some sulfonylureas

A

Tolbutamide
Glibenclamide
Gliclazide
Glipizide

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6
Q

How do sulfonylureas function?

A

Bind to SUR1 subunit
Close KATP channels
Increase Ca2+ entry
Increase Insulin secretion

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7
Q

What is the issue with sulfonylureas?

A

Require functional B cells in order to work

Only type II

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8
Q

Short Acting Sulfonylureas

A

Tolbutamide ( large dosage is required)

Gliclazide

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9
Q

Long Acting sulfonylureas

A

Glibenclamide

Gliplizide

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10
Q

Positives of sulfonylureas

A

Well absorbed orally

Reduce microvascular damage

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11
Q

Negatives of sulfonylureas

A

Risk of hypoglycaemia
Unwanted weight gain
Increased appetite

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12
Q

When should sulfonyureas never be used?

A

Renal impairment
Pregnancy - crosses placenta
Breastfeeding
Elderly

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13
Q

When are sulfonylureas 1st line?

A

If intolerant to metformin

If patient has lost weight

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14
Q

Can sulfonylureas be used in combination?

A

Used with metformin second line

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15
Q

Glinides mode of action

A

Similar to sulfonylureas
Close KATP channels
Increase Ca2+ levels
Secreting insulin

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16
Q

Name some glinides

A

Repaglinide

Nateglinide

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17
Q

Benefits of glinides over sulfonylureas

A

Less likely to cause hypoglycaemia
Active orally
Safer for use in renal impairment as mainly subject to hepatic metabolism.

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18
Q

Negatives of glinide use

A

Active time is much shorter so must take more frequently

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19
Q

When should glinides not be used?

A

In hepatic impairment
Pregnancy
Breast feeding

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20
Q

What cells release GLP-1 and GIP?

A

Enteroendocrine cells in small intestine
L in ileum
K in duodenum

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21
Q

Effect of GLP-1 and GIP

A

Enhance insulin secretion and delay gastric emptying

Enhance glucose uptake by skeletal muscles

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22
Q

What does GLP-1 also do?

A

Decrease glucagon release from alpha cells

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23
Q

What triggers the release of GLP-1 and GIP?

A

Ingestion of food

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24
Q

Which molecule terminates GLP-1 and GIP?

A

DPP-4

Stops reduction in blood sugar levels

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25
Q

What is the function of DPP-4 inhibitors?

A

By inhibiting DPP-4 they maintain the incretin response and lower blood glucose levels and increase plasma insulin levels.

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26
Q

Name some DPP-4 inhibitors?

A

Sitagliptin
Saxagliptin
Alogliptin

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27
Q

Benefits of DPP-4 inhibitors

A

Can be used as a mono therapy
generally well tolerated
No hypoglycaemia
Orally active

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28
Q

What are the side effects of DPP-4 inhibitors?

A

Nausea

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29
Q

Incretin analogues

A

Mimic GLP-1 and GIP, acts as agonists at the receptors increasing intracellular cAMP

30
Q

What do incretin analogues do?

A

Suppress glucagon release
Suppress gastric emptying
Decrease appetite
Increase glucose uptake by skeletal muscle

31
Q

How are incretin analogues administered?

A

Subcutaneously

32
Q

Some side effects of incretin analogues

A

Nausea

May rarely cause pancreatitis

33
Q

Benefits of incretin analogues

A

Modest weight loss

No risk of hypoglycaemia

34
Q

When are alpha glucosidase inhibitors used?

A

When lifestyles modification isn’t adequate

Rarely used

35
Q

Function of alpha glucosidase inhibitors

A

Inhibit brush border enzyme that breaks down starch

Glucose isn’t absorbed

36
Q

Side effects of alpha glucosidase inhibitors

A

GI flatulence nausea vomiting diarrhoea

37
Q

When is metformin used?

A

First line irrespective of obesity

38
Q

Function of metformin

A

Reduce hepatic gluconeogenesis
Stimulate AMP activated protein kinase
-GIP-1 is secreted
Increase glucose uptake by muscle

39
Q

Benefits of metformin

A 
Reduce microvascular changes
Orally active
Prevent hypoglycaemia
Causes weight loss
Can be used in combination
40
Q

Side affects of metformin

A

GI upsets diarrhoea nausea anorexia

Can cause lactic acidosis - excessive alcohol can increase risk

41
Q

When should metformin not be used?

A

Significant renal or hepatic disease

42
Q

Glitazones (Thiazolidinediones) function

A

Promote transcription factor production which increases insulin secretion and signalling

43
Q

Glitazones (Thiazolidinediones) mode of action

A

Promote fatty acid uptake an storage
Reduce hepatic glucose output
Enhance peripheral glucose uptake

44
Q

Do Glitazones (Thiazolidinediones) increase risk of hypoglycaemia ?

A

No

45
Q

Side affects of Glitazones (Thiazolidinediones)

A

Weight gain
Fluid retention
Risk of serious hepatotoxicity
Increase bone fractures

46
Q

Sodium Glucose Cotransporter 2 inhibitor

A

Dagaglifozin

Empaglifozin

47
Q

Sodium Glucose Cotransporter 2 inhibitor mode of action

A

Selectively blocks reabsorption of glucose from proximal tubule, more glucose is excreted into the urine.

48
Q

Benefits of a Sodium Glucose Cotransporter 2 inhibitor

A

Reduced blood glucose with little hypoglycaemia risk

Calorific loss and water loss means weight loss

49
Q

Which drugs have been shown to reduce CDV death?

A

GLP-I analogues

SGLT2i

50
Q

Which GLP-I analogue has reduced CDV deaths swell as renal disease progression?

A

Liraglutide

51
Q

Which SGLT2i has reduced CDV deaths as well as renal disease progression?

A

Empagliflozin

52
Q

Which drug has been heavily criticised as it increased incidences of death on all accounts?

A

Rosiglitazon

53
Q

Glitazones (Thiazolidinediones)

A

Cause maturation of adipose cells and shift weight away to the extremities.

54
Q

SGLT2i what are 5-10% affected by?

A

Recurrent thrush and/or UTI

55
Q

If a diabetic comes in with high blood pressure what is the medication of choice?

A

ACE or ARB

56
Q

What should be given to anyone over 40 with diabetes?

A

Statin

Atorvastatin is

57
Q

issues with metformin in renal failure?

A

Metformin doesn’t damage but does accumulate.

58
Q

At what EGFR should metformin be removed?

A

30

59
Q

Is Atorvastatin or simvastatin more potent?

A

Atorvastatin

60
Q

SGLT2i in type I diabetes

A

There is no evidence to supports its use, it increases the risk of diabetic ketoacidosis so generally avoided.

61
Q

Rapid acting insulin

A

Humalog
Novarapid
Apidra

62
Q

Short acting insulin

A

Humulin B

Actrapid

63
Q

Intermediate acting insulin

A

Isophane

Insulatard

64
Q

Long acting insulin

A

Lantus Levemir

65
Q

What isa rapid acting analogue intermediate mixture?

A

Basal bolus 2x daily

Humalog Mix 25/50 or Novomix 3

66
Q

In order to use a basal bolus routine what is required?

A

A fixed routine of exercise at the same time each day and eating similar foods at similar times.

67
Q

How does an insulin pump work>

A

Continuous subcutaneous administration of short acting insulin. Basal
Manually administer a bolus when calculated carbohydrate content of food.

68
Q

What is the HbA1c of a non diabetic?

A

48mmol/ml

69
Q

What is the ideal HbA1c target range of a long term diabetic?

A

53-58 mmol/ml

7-7.5 %

70
Q

Name some factors which affect absorption of insulin

A

Temperature. Warmer = Faster
Injection site
Exercise
Adipose tissue. More = Slower

71
Q

What should you check for at the injection site?

A

Lipohypertrophy

72
Q

Why should injection sites be rotated?

A

As lipohypertrophy slows the rate of absorption down

Year 2 Endocrine (21 decks)

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