Diabetes pharmacology Flashcards

1
Q

Which drug is a first generation sulphonylurea?

A

Tolbutamide

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2
Q

Which drugs are second generation sulphonylureas?

A

Glibenclamide

Glipizide

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3
Q

How do sulphonylureas stimulate insulin release?

A

Displaces the binding of ADP-Mg2+ from the SUR1 subunit, closing the KATP channel, allowing the membrane depolarisation to occur that stimulates insulin release

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4
Q

What is the difference between first and second generation sulphonylureas?

A

Second are more potent and longer acting

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5
Q

What is the disadvantageous side effect of sulphonylureas?

A

Weight gain

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6
Q

In which patients is the risk of hypoglycaemia caused by sulphonylureas increased?

A

Elderly

Impaired hepatic/renal function

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7
Q

Which drugs are examples of glinides?

A

Repaglinide

Nateglinide

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8
Q

How do glinides work?

A

Binds to SUR1 subunit at a benzamino site, closing the KATP channel and triggering insulin release

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9
Q

Are sulphonylureas or glinides more likely to cause hypoglycaemia?

A

Sulphonylureas

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10
Q

When are glinides taken and why?

A

Before meals

Combats post-prandial rise in glucose

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11
Q

What do glucagon-like peptide 1 (GLP1) and glucose dependant insulinotropic peptide (GIP) do and when are they released?

A

Released in response to ingestion of food
GLP-1 and GIP stimulate insulin secretion from pancreatic beta cells and delay gastric emptying
GLP-1 decreases glucagon release from pancreatic alpha cells

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12
Q

Which drugs mimic the action of GLP-1?

A

Incretin analogues

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13
Q

Which drug is an incretin analogue?

A

Extenatide

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14
Q

What are the effects of incretin analogues?

A

Increases insulin secretion
Suppresses glucagon secretion
Slows gastric emptying
Decreases appetite

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15
Q

What are some of the advantages of using incretin analogues?

A

Cause modest weight loss

Reduce hepatic fat accumulation

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16
Q

How is extenatide administered?

A

Subcutaneously twice daily

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17
Q

What are some of the side effects of extenatide?

A

Nausea
Hypoglycaemia
Pancreatitis

18
Q

How do DPP-4 inhibitors/gliptins work?

A

Inhibit the actions of DPP-4 (a GLP-1 and GIP inhibitor), prolonging the effects of GLP-1 and GIP

19
Q

What are some examples of some gliptins?

A

Sitagliptin
Saxigliptin
Vildagliptin

20
Q

What are some of the advantages of using gliptins?

A

Weight neutral
Generally well tolerated
No hypoglycaemia

21
Q

How does acarbose work?

A

Inihbit alpha-glucosidase, stopping the breakdown of carbohydrates into absorbable glucose form
More carbohydrate is excreted in stools

22
Q

In which patients is acarbose used?

A

Patients whose T2DM is inadequately controlled by lifestyle changes and drugs

23
Q

What are the side effects of acarbose?

A
Flatulence
Bloating
Abdominal pain
Loose stools
Diarrhoea
24
Q

Which is the first line drug treatment for obese T2DM patients?

A

Metformin

25
Q

How does metformin work?

A

Reduces hepatic gluconeogenesis
Reduces carbohydrate absorption
Increases fatty acid oxidation
Increases glucose uptake and utilisation in skeletal muscles

26
Q

What are the advantages of using metformin?

A

Causes weight loss
Does not cause hypoglycaemia
Prevents hyperglycaemia
Can be used with other therapies

27
Q

When must use of metformin be stopped?

A

When kidney function declines

GFR <30, metformin stopped

28
Q

What are some of the adverse affects of metformin?

A
GI upsets (diarrhoea/nausea/anorexia)
(Rarely) lactic acidosis
29
Q

Which is the only thiazolidinedione licenced for use in the UK?

A

Pioglitazone

30
Q

How do thiazolidinediones work?

A
Enhance the action of insulin at target tissues
Promotes the genetic expression of:
Lipoprotein lipase
Fatty acid transport protein
GLUT4
31
Q

What are the desirable effects of thizolidinediones?

A

Promote fatty acid uptake and storage in adipocytes, rather than skeletal muscle and liver
Reduced hepatic glucose output

32
Q

What are the adverse effects of thiazolidinediones?

A

Weight gain
Fluid retention (Na+ reabsorption at kidney encouraged)
Increases incidence of bone fractures

33
Q

Which is the only Sodium-Glucose Cotransporter-2 (SGLT2) Inhibitor licesnced for use in the UK?

A

Dapagliflozin

34
Q

How do sodium-glucose cotransporter-2 (SGLT2) Inhibitors work?

A

Selectively blocks the reabsorption of glucose at the proximal tubule of the nephron to purposefully cause glucosuria
This reduces blood glucose and can cause some weight loss

35
Q

What is the required treatment for type 1 diabetes?

A

Immediate insulin therapy

36
Q

What are the aims of insulin therapy for T1DM?

A

Avoid hypoglycaemia
Reduce hyperglycaemia
Reduce chronic complications

37
Q

Which insulins are examples of rapid acting analogues?

A

Humalog* (insulin lispro)
NovoRapid
Apidra

38
Q

Which insulins are short acting?

A

Humulin S (Human insulin)
Actrapid
Insuman Rapid

39
Q

Which insulin is a long acting analogue?

A

Lantus

Levemir

40
Q

Which insulin regimen aims to mimic normal endogenous insulin production?

A

Basal bolus regimen

41
Q

What is involved in the basal bolus insulin regimen?

A

One long acting injection to maintain insulin levels

Three rapid acting injections before meals to combat post-prandial rise in glucose

42
Q

How is initial insulin requirement in basal bolus regimen calculated?

A
0.3 units/kg body weight
Divide 50% basal 50% prandial
e.g. 60kg => 18 units
9 units basal
3/3/3 units prandial