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Management of GI and Endocrine Conditions > Lecture 18 - Medicines for Type 2 Diabetes > Flashcards

Lecture 18 - Medicines for Type 2 Diabetes Flashcards

1
Q

What type of medicine is metformin?

A

a biguanide

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2
Q

What is metformin?

A

first line oral glucose lowering agent for type 2 diabetes

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3
Q

How many people is metformin prescribed to?

A

83.6% of patients in the UK with type 2 diabetes (2013)

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4
Q

What are the advantages of metformin?

A

it doesn’t cause weight gain or hypoglycaemia

can be used in overweight patients

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5
Q

When was metformin first used?

A

1953

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6
Q

What is the most important effect of metformin?

A

to reduce hepatic glucose production

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7
Q

Mechanism of action of metformin?

A

still unknown

can affect multiple cellular processes and the most widely accepted is linked to inhibition of mitochondrial respiratory chain-complex 1

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8
Q

How does metformin enter hepatocytes?

A

through the organic cation transporter 1

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9
Q

What does inhibiton of the complex 1 of the respiratory chain cause?

A

inhibition of ATP synthesis

increase in AMP

activation of AMPK

phosphorylation and inhibition of CRTC2

inhibition of gluconeogenic gene expression

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10
Q

What is CRTC2?

A

a transcription factor that normally plays a role in transcription of genes involved in gluconeogenesis so when blocked it leads to decreased synthesis of genes and reduction in glucose production

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11
Q

Side effects of metformin?

A

GI effects such as diarrhoea, nausea, vomiting, abdominal bloating, reduced appetite

vit B12 deficiency

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12
Q

What % of patients on metformin have a reduced appetite?

A

20%

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13
Q

What % of patients discontinue metformin use from GI side effects?

A

5%

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14
Q

How does metformin cause B12 deficiency?

A

it reduces intestinal absorption of vit B12 in up to 30% of patients and lower serum levels in a dose-dependent manner in 5-10% of patients

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15
Q

What symptoms does B12 deficiency cause?

A

tiredness and tingling in hands and feet

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16
Q

What is a rare side effect of metformin?

A

lactic acidosis

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17
Q

Brands of metformin?

A 
bolamyn
diagment
glucient 
glucophage
metabet
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18
Q

What do sulfonylureas do?

A

stimulate insulin secretion from pancreatic beta cells

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19
Q

How to sulfonylureas work?

A

they bind to ATP-gated K+ channels, causing channel closure and membrane depolarisation, which causes calcium to enter the cell and stimulate insulin secretion

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20
Q

Daonil?

A

glibenclamide

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21
Q

Diamicron, Diamicron MR?

A

gliclazide

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22
Q

Glibenese, Minodiab?

A

Glipizide

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23
Q

Amaryl?

A

glimepiride

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24
Q

Tolbutamide?

A

tolbutamide

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25
Q

Names of sulfonylureas?

A

glibenclamide, gliclazide, glipizide, glimepiride, tolbutamide

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26
Q

Side effects of sulfonylureas?

A

Hypoglycaemia, can also cause weight gain

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27
Q

What are meglitinides?

A

prandial glucose regulators

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28
Q

Mechanism of action of meglitinides?

A

similar mechanism to sulfonylureas but rapid onset and short duration

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29
Q

When are meglitinides taken?

A

before meals

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30
Q

Examples of meglitinides?

A

repaglinide, nateglinide

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31
Q

Prandin?

A

repaglinide

32
Q

Starlix?

A

Nateglinide

33
Q

What are thiazolidinediones?

A

Glitazones

34
Q

What is the only tablet in the thiazolidinediones?

A

pioglitazone

35
Q

How do glitazones work?

A

increase insulin sensitivity by stimulating the expression of insulin sensitising genes

they are insulin sensitisers

36
Q

What do thiazolidinediones bind to?

A

the nuclear receptor PPAR gamma

37
Q

What does PPAR gamma do?

A

works with retinoid X receptor to drive the expression of insulin sensitising genes

38
Q

What are examples of insulin sensitising genes?

A

GLUT4, PI3 kinase, IRS proteins

39
Q

Medicines in the thiazolidinedione group?

A

pioglitazone, and pioglitazone in combination with metformin

40
Q

Actos?

A

pioglitazone

41
Q

Competact?

A

pioglitazone & metformin

42
Q

Side effects of thiazolidinediodes?

A

water retention (oedema) and weight gain

43
Q

What are GLP-1 analogues?

A

incretin mimetics

glucagon like peptide 1 analogues that increase insulin release

44
Q

What is GLP1

A

glucagon like peptide 1

45
Q

What happens when GLP1 is released?

A

following food intake released with GIP, they activate or stimulate insulin release from pancreatic beta cells

46
Q

GLP and GIP are degraded by?

A

they have short have lives and are degraded by protease DPP4

47
Q

Examples of GLP-1 analogues

A

exenatide, liraglutide, lixisenatide, dulaglutide, semaglutaide

48
Q

Byetta?

A

exenatide (twice daily injection)

49
Q

Bydureon?

A

exenatide (once weekly injection)

50
Q

Victoza?

A

liraglutide (once daily injection)

51
Q

Lixumia?

A

lixisenatide (once daily injection)

52
Q

Trulicity?

A

dulaglutide (once weekly injection)

53
Q

Ozempic?

A

semaglutide (once weekly injection)

54
Q

What are DPP4 inhibitors?

A

gliptins

they bind to DPP4 and inhibit its activity, which allows endogenously produced GLP-1 and GIP to accumulate to higher levels and stimulate more secretion of insulin

55
Q

DPP4 medicines?

A

sitagliptin, vildagliptin, saxagliptin, alogliptin, linagliptin

56
Q

Januvia and janumet?

A

sitagliptin

sitaglipin & metformin

57
Q

galvus and eucreas?

A

Vildagliptin

vildagliptin & metformin

58
Q

Onglyza & Kombolyze?

A

saxagliptin

saxagliptin & metformin

59
Q

Vipidia & vipdomet?

A

alogliptin

alogliptin & metformin

60
Q

Trajenta & Jentadueto?

A

linagliptin

linagliptin & metformin

61
Q

What do alpha glucosidase inhibitor (Acarbose) do?

A

slow down the absorption of starchy foods by intestine - slows the rise in blood glucose after a meal

62
Q

What do SGLT2 inhibits do?

A

act by inhibiting glucose transporter SGLT2, which functions in the kidney to mediate glucose reabsorption, excess glucose is lost in urine

63
Q

Examples of SGLT2 inhibitors?

A

dapagliflozin, empagliflozin, canagliflozin

64
Q

Forxiga?

A

dapagliflozin

65
Q

Invokana?

A

canagliflozin

66
Q

Jardiance?

A

empagliflozin

67
Q

What else is important to control symptoms of type 2 diabetes?

A

eating a healthy diet and regular exercise

68
Q

What else may be prescribed if glucose control is not adequate in type 2 diabetes?

A

Insulin

69
Q

What has type 2 been discovered as?

A

A reversible disease

70
Q

What happens if monotherapy does not work for someone with type 2 diabetes?

A

an additional oral antidiabetic might be added, can also move to triple therapy if this is not enough

71
Q

Surgery for diabetes?

A

~65% of patients with type 2 diabetes were no longer on any diabetic medication 2 years after bariatric surgery

72
Q

What have NICE recommended with surgery?

A

all patients in the UK with BMI>35 with recent onset type 2 diabetes should be assessed for surgery

73
Q

What is the initial cost of surgery?

A

~£6,000

74
Q

What else has been shown to put type 2 diabetes into remission?

A

a very low calorie diet of about 600-700 calories per day

can put diabetes into remission after 4-6 weeks

75
Q

What is the success of the low calorie diet correlated with?

A

weight loss - fat loss from pancreas and the liver

Management of GI and Endocrine Conditions (24 decks)

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