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Module 203 Reproduction & endocrinology > T1 L14 Drug treatment of T2DM > Flashcards

T1 L14 Drug treatment of T2DM Flashcards

1
Q

What are the major target tissues affected by insulin?

A

Liver
Adipose
Skeletal muscle

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2
Q

What are the effects of insulin on hepatic cells?

A

Decrease gluconeogenesis
Decrease glycogenolysis
Decrease ketogenesis
Increase glycogen synthesis

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3
Q

What are the effects of insulin on muscle cells?

A 
Increases GLUT-4 translocation to the membrane which increases glucose uptake
Increase glucose oxidation
Increase glycogen synthesis
Increase amino acid uptake
Increase amino acid release
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4
Q

What are the effects of adipocytes on muscle cells?

A

Increase glucose uptake
Increase triglyceride synthesis
Decrease free fatty acid and glycerol release

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5
Q

What is the overall effect of insulin?

A

Hypoglycaemia

Increase fuel storage in muscle, fat tissue and liver

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6
Q

What does T2DM treatment target?

A 
Insulin resistance
Renal glucose absorption
Beta-cell dysfunction 
Loss of beta-cell mass
Obesity and dyslipidaemia
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7
Q

What drugs target insulin resistance?

A

Metformin

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8
Q

What drugs target renal glucose absorption?

A

SGLT2 inhibitors

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9
Q

What drugs target beta-cell dysfunction?

A

Sulfonylureas

  • GLP-1 analogues
  • DDP-4 inhibitors
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10
Q

What drugs target the loss of B-cell mass?

A

Insulin replacement

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11
Q

Give examples of sulfonylureas

A

Gliclazide
Glipzide
Glimepride

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12
Q

Describe the mechanism of insulin secretion

A

1) Glucose is picked up by GLUT2
2) Glucose is metabolised to produce ATP
3) ATP inhibits the ATP-sensitive K+ channels
4) Closes K+ channels
5) K+ builds up inside beta cell
6) Depolarises cell
7) Calcium channels open
8) Calcium moves into beta cells
9) Insulin secretion is dependent on these calcium ions

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13
Q

What are the primary mechanisms of sulfonylureas?

A

Stimulates endogenous insulin release

Binds to site on ATP-sensitive K+ channels to inhibit the opening of the channel in a similar way to ATP

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14
Q

What are the secondary mechanisms of sulfonylureas?

A

Sensitise beta cells to glucose
Decrease lipolysis
Decrease clearance of insulin by the liver

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15
Q

What is the ideal patient to give sulfonylureas to?

A

Over 40 years old
DM duration < 10 years
Daily insulin intake ≤40 units

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16
Q

Why can’t sulfonylureas be used in type 1 diabetes?

A

In type 1 diabetes the beta cells aren’t present so insulin secretion can’t occur

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17
Q

What is the major side effect of sulfonylureas?

A

Hypoglycaemia

18
Q

How do biguanides differ from sulfonylureas and meglitinides?

A

Don’t stimulate insulin release
Don’t cause hypoglycaemia
Increase glucose uptake in muscle
Decrease glucose production in liver

19
Q

What are the mechanisms of actions of biguanides?

A

Suppresses hepatic glucose production by gluconeogenesis
AMPK increases expression of nuclear transcription factor SHP
Increases insulin sensitivity
Enhances peripheral glucose uptake
Increases fatty acid oxidation by decreasing insulin-induced suppression of fatty acid oxidation
Decrease glucose absorption from GI tract

20
Q

What are the properties of metformin?

A 
Orally active
Doesn't bind plasma proteins
Excreted unchanged in urine
Often combined in a single pill with other anti-diabetic medications
Also used for PCOS
21
Q

What are the adverse effects of biguanides?

A 
Metformin produces lactic acidaemia
Nausea
Abdominal discomfort
Diarrhoea
Metallic taste
Anorexia
Vit B12 and folate deficiency
22
Q

What are the contraindications of metformin?

A

Hepatic disease
Past history of lactic acidosis
Cardiac failure
Chronic hypoxic lung disease

23
Q

What do thiazolidinediones do?

A

Activate peroxisome proliferator-activated receptor gamma

24
Q

What is PPARy involved in?

A

Transcription of insulin-responsive genes and in regulation of adipocyte lipid metabolism

25
Q

What is the effect of glitazones in the presence of endogenous or exogenous insulin?

A

Decrease gluconeogenesis, glucose output and triglyceride production in the liver
Increase glucose uptake and utilisation in skeletal muscle
Increase glucose uptake and decrease fatty acid output in adipose tissue
Cause differentiation of adipocytes

26
Q

Describe the pharmacokinetics of glitazone

A 
Pioglitazone is taken once / twice daily, orally
Plasma levels peak after 3 hours
Plasma half life is 3-7 hours
Liver metabolism
Excreted in faeces and urine
27
Q

What are the adverse effects of glitazones?

A

Fluid retention
Dose-related weight gain
Liver damage

28
Q

Why do glitazones cause fluid retention?

A

Promote amiloride-sensitive sodium ion reabsorption in renal collecting ducts leading to oedema and mild anaemia

29
Q

Give an example of a glucagon-like peptide

A

Exenatide

30
Q

When is exenatide given?

A

Administered by S.C. injection, 30-60 minutes before last meal of the day

31
Q

How does exenatide facilitate glucose control?

A

Augmenting pancreas response
Suppress pancreatic release of glucagon to stop the liver overproducing glucose
Slows gastric emptying
Reduces appetite and promotes satiety via hypothalamic receptors
Reduces fat liver content

32
Q

What are the side effects of exenatide?

A

Acid or sour stomach
Belching
Diarrhoea
Heartburn

33
Q

What is the mechanism of DDP-4 inhibitors?

A

Increase levels of incretins GLP-1 and GIP which:

  • inhibit glucagon release
  • increase glucose induced insulin secretions
  • decrease gastric emptying
  • reduce hepatic glucose production
  • improved peripheral glucose utilisation
34
Q

What are some examples of DDP-4 inhibitors?

A

Vildagliptin (reversible)
Sitagliptin (reversible)
Saxagliptin (covalently bound)

35
Q

Where is SGLT1 found?

A

Small intestine

Proximal straight tubule of the nephron

36
Q

Where is SGLT2 found?

A

Proximal convoluted tubule

37
Q

How much glucose is reabsorbed by SGLT2?

A

90%

38
Q

Give some examples of SGLT2 inhibitors?

A

Dapagliflozin

Canagliflozin

39
Q

What is the mechanism of SGLT2 inhibitors?

A 
Inhibit renal tubular Na+ glucose transporter --> reversal of hyperglycaemia --> reversal of glucotoxicity
Increase insulin sensitivity in muscle
Increase insulin sensitivity in liver
Decrease gluconeogenesis
Improve beta cell function
40
Q

How do SGLT2 inhibitors increase insulin sensitivity in muscles?

A

Increase GLUT4 translocation

Increase insulin signalling

41
Q

What are the side effects of SGLT2 inhibitors?

A

Rapid weight loss due to glycosuria
Tiredness
Osmotic diuretic –> dehydration
Worsen UTI and thrush

Module 203 Reproduction & endocrinology (52 decks)

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