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The Endocrine System > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

Meformin: What class of drug?

A

Biguanide

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2
Q

Meformin: Originates from where?

A

French Lilac

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3
Q

Meformin: Structure

A

Two guanidine stuck together with two methyl groups

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4
Q

Meformin: Mechanism of Action

A

Inhibits Complex I of the Mitochondrial Respiratory Chain to cause a fall in cellular ATP which reduces gluconeogenesis via activating AMPK

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5
Q

Meformin: Impact on hepatic glucose production

A

Decreased

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6
Q

Meformin: Impact on gut glucose mobilisation and metabolism

A

Increased

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7
Q

Meformin: Impact on GLP-1 secretion

A

Increased

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8
Q

Meformin: Alters what in the GIT?

A

Microbiome

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9
Q

Meformin: Impact on lipogenesis

A

Decreased

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10
Q

Meformin: Why is it not readily uptaken by the cell?

A

Hydrophilic

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11
Q

Meformin: Mechanism of transport into cells?

A

Organic Cation Transporters

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12
Q

Meformin: Transporters are present in what organs? (3)

A

Intestines
Liver
Kidney

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13
Q

Meformin: Excretion route

A

Urine

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14
Q

Meformin: Mechanism of metabolism

A

Not metabolised - excreted as metformin in urine

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15
Q

Meformin: How does this impact weight?

A

Promotes weight loss

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16
Q

Meformin: Dose

A

500mg-1g twice per day

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17
Q

Meformin: Side Effects - Gastrointestinal (5)

A

Diarrhoea
Bloating
Abdominal Pain
Dyspepsia
Metallic taste in mouth

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18
Q

Meformin: Side Effects - How to reduce GI side effects?

A

Initiate dose slowly - 500mg once daily for 1 week then increase per week or use a modified release formulation

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19
Q

Meformin: Side Effects - MALA

A

Metformin Associated Lactic Acidosis

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20
Q

Meformin: Side Effects - Metformin increases the production of what in the liver and gut?

A

Lactate

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21
Q

Meformin: Side Effects - Metforming is associated with a greater risk of Lactic Acidosis during what? (2)

A

Sepsis
Impaired liver clearance

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22
Q

Meformin: Side Effects - If renal function becomes reduced what should happen to dose?

A

eGFR <45 ml/min - Reduce to a maximum dose of 1g daily
eGFR <30ml/min - Contraindicated

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23
Q

Sulphonylureas: 1st generation examples (2)

A

Tolbutamide
Chlorpropamide

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24
Q

Sulphonylureas: 2nd generation examples (4)

A

Gliclazide
Glipizide
Glimepiride
Gilbenclamide

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25
Q

Sulphonylureas: Derived from what?

A

Sulphonamides

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26
Q

Sulphonylureas: These are insulin …

A

Secretagogues

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27
Q

Sulphonylureas: Mechanism of Action - Binds to what?

A

Extracellular SUR1 subunits

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28
Q

Sulphonylureas: Mechanism of Action - On binding what happens to the SUR1 subunits?

A

ATP Sensitive K channel close

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29
Q

Sulphonylureas: Mechanism of Action - Closure of the ATP sensitive K channel causes what to occur to the cell?

A

Exocytosis of Insulin due to activation of calcium channels (calcium influx)

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30
Q

Sulphonylureas: Mechanism of Action - Enables what process to occur even when glucose is not increased?

A

Glucose-independent insulin secretion

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31
Q

Sulphonylureas: Impact on weight

A

Increased by 1-2 kg

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32
Q

Sulphonylureas: Major risk of what?

A

Hypoglycaemia

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33
Q

Sulphonylureas: Gliclazide dose - Start and Maximum

A

Start - 40-80 mg once daily
Maximum - 160mg twice daily

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34
Q

Sulphonylureas: Side Effects - Why may they cause hypoglycaemia?

A

As they are not glucose dependent

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35
Q

Sulphonylureas: Side Effects - Increased risk of Hypoglycaemia (4)

A

Increased age
Increased diabetic diagnosis time
Creatinine
Lower HbA1c - <50 mmol/mol

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36
Q

Sulphonylureas: Side Effects - Why may weight increase?

A

Insulin is anabolic meaning carbohydrate stores increase and increases appetite

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37
Q

TZDs

A

Thiazolidinediones

38
Q

Thiazolidinediones: Mechanism of Action

A

PPAR-gamma ligands to increase the transcription of target genes

39
Q

Thiazolidinediones: Impact on adipocytes

A

Increase differentiation from pre-adipocytes to adipocytes to increase fat mass storage

40
Q

Thiazolidinediones: How do they reduce lipotoxicity?

A

Increase subcutaneous fat mass to increase the uptake of FFA to remove it from the viscera

41
Q

Thiazolidinediones: Lipid Steal Mechanism

A

FFA uptake removes fat from the liver, pancreas and muscle to reduce lipotoxicity

42
Q

Thiazolidinediones: Impact on adiponectin

A

Increased adiponectin to increase insulin sensitivity in the liver

43
Q

Thiazolidinediones: Reduces what inflammatory cytokines? (2)

A

TNF-alpha and IL-6 from macrophages

44
Q

Thiazolidinediones: Characteristics - Impact on weight

A

Increase in weight

45
Q

Thiazolidinediones: Characteristics - Which is the only available TZD?

A

Pioglitazone

46
Q

Thiazolidinediones: Characteristics - Pioglitazone dose

A

15-30mg once daily

47
Q

Thiazolidinediones: Side Effects - (3)

A

Weight gain
Peripheral oedema
Fracture risk

48
Q

Thiazolidinediones: Side Effects - Why is fracture risk increased?

A

Fat accumulation in bone marrow and reduced bone density

49
Q

Incretin Drugs: What is produced from K cells?

A

GIP

50
Q

Incretin Drugs: What is produced from L cells?

A

GLP-1

51
Q

Incretin Drugs: GIP and GLP-1 are broken down by what?

A

DPP-4

52
Q

Incretin Drugs: Amplifying Pathway

A

GLP-1/GIP receptor activation increases cAMP to increase insulin secretion

53
Q

Incretin Drugs: Triggering Pathway

A

Activation of Glucokinase by Glucose forms Glucose-6-Phosphate to increase ATP and thus calcium channel activation for insulin exocytosis

54
Q

Gliptins: Examples (3)

A

Sitagliptin
Alogliptin
Saxagliptin

55
Q

DPP4 Inhibitors

A

Dipeptidyl Peptidase 4 Inhibitors

56
Q

DPP4 Inhibitors: Mechanism of Action

A

Inhibit the breakdown of GLP-1 and GIP by binding and inhibiting DPP4 to increase the incretin effect

57
Q

DPP4 Inhibitors: These are insulin …

A

Secretagogues

58
Q

DPP4 Inhibitors: Why is there a reduced risk of hypoglycaemia?

A

Glucose dependent insulin secretion

59
Q

DPP4 Inhibitors: Does this impact weight?

A

No

60
Q

DPP4 Inhibitors: Sitagliptin dose

A

100mg once daily

61
Q

GLP-1 Receptor Agonists: Structure

A

Modified GLP-1 structure to prevent breakdown by DPP4 to act directly on the receptor to increase insulin secretion in a glucose-dependent manner and inhibit glucagon secretion

62
Q

GLP-1 Receptor Agonists: Example

A

Semaglutide

63
Q

GLP-1 Receptor Agonists: Semaglutide structure

A

Addition of SNAC fatty acid group increases gastric absorption

64
Q

GLP-1 Receptor Agonists: Mechanism of Action (4)

A

Promote insulin secretion in a glucose-dependent manner
Inhibit glucagon secretion
Acts on hypothalamus to reduce appetite
Acts on intestines to reduce gastric emptying

65
Q

GLP-1 Receptor Agonists: Do they impact weight?

A

Yes - reduce weight

66
Q

GLP-1 Receptor Agonists: Impact on BP

A

Reduced

67
Q

GLP-1 Receptor Agonists: Impact on HR

A

Increased

68
Q

GLP-1 Receptor Agonists: Liraglutide dose

A

1.2 mg daily

69
Q

GLP-1 Receptor Agonists: Semaglutide dose

A

0.5mg weekly

70
Q

GLP-1 Receptor Agonists: Side effects (3)

A

Nausea or Vomiting - improves after 6 weeks
Gallstones
Pancreatitis

71
Q

GLP-1 Receptor Agonists: Why is there a risk of Pancreatitis?

A

Sustained increase in pancreatic lipase and amylase

72
Q

GLP-1 Receptor Agonists: Why may nausea and vomiting occur?

A

Early satiety with reduced gastric emptying

73
Q

GLP-1 Receptor Agonists: May reduce the onset of what?

A

Macroalbuminuria

74
Q

SGLT-2 Inhibitors: Examples (3)

A

Empagliflozin
Dapagliflozin
Canagliflozin

75
Q

SGLT-2 Inhibitors: Mechanism of action

A

Inhibit the channel on the kidneys to increase uptake of sugar within the nephrons to increase urinary glucose loss

76
Q

SGLT-2 Inhibitors: Direct Effects - Glucose loss results in osmotic …

A

Diuresis

77
Q

SGLT-2 Inhibitors: Direct Effects - Inhibition of SGLT-2 reduces the reabsorption of what?

A

Sodium

78
Q

SGLT-2 Inhibitors: Direct Effects - Osmotic diuresis and reduced Na reabsorption causes what type of action?

A

Mild diuretic

79
Q

SGLT-2 Inhibitors: Direct Effects - Impact on urate excretion?

A

Increased - to reduce plasma urate concentration

80
Q

SGLT-2 Inhibitors: Direct Effects - How does it protect the kidneys? (3)

A

Increased sodium delivery to the DCT - increases uptake of Na at the macula densa
Increases adenosine secretion - reduced renal afferent vasodilation
Reduces filtration pressure

81
Q

SGLT-2 Inhibitors: Indirect Effects - Impact on glucose

A

Reduced

82
Q

SGLT-2 Inhibitors: Indirect Effects - Impact on lipolysis

A

Increased - increases FFA to the liver to increase Ketone Body production

83
Q

SGLT-2 Inhibitors: Indirect Effects - How are cardiac bioenergetics improved?

A

FFA and Ketones increase

84
Q

SGLT-2 Inhibitors: Indirect Effects - Increase the risk of what?

A

Ketosis and Ketoacidosis

85
Q

SGLT-2 Inhibitors: Glucose-lowering effects relies on what?

A

Renal glucose filtration

86
Q

SGLT-2 Inhibitors: Efficacy is reduced at an eGFR of what?

A

<90ml/min

87
Q

SGLT-2 Inhibitors: Efficacy is 0 at an eGFR of what?

A

<45ml/min

88
Q

SGLT-2 Inhibitors: Impact on blood pressure

A

Reduced

89
Q

SGLT-2 Inhibitors: Impact on cholesterol

A

Increases LDL and HDL cholesterol

90
Q

SGLT-2 Inhibitors: Dose of Empagliflozin

A

10mg once daily

91
Q

SGLT-2 Inhibitors: Side effects (5)

A

Thrush - secondary to glycosuria
Fournier Gangrene
Hypovolaemia
Hypotension
Diabetic Ketoacidosis

92
Q

SGLT-2 Inhibitors: When should these be omitted?

A

Prolonged fasting
Acute illness

The Endocrine System (5 decks)

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