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PHAR2200 > insulin and other hypoglycaemic agents > Flashcards

insulin and other hypoglycaemic agents Flashcards

1
Q

Why is it necessary to have rigid blood glucose control?

A
  • obligatory energy source for the brain

- tightly regulated to keep blood glucose levels within normal range

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2
Q

What are the main glucose regulating hormones?

A

Insulin - β / B cells
Glucagon - α / A cells
Somatostatin - D cells

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3
Q

What are some supplementary hormones that regulate glucose?

A

adrenalin - adrenal medulla
glucocorticoids - adrenal cortex
growth hormone - pituitary

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4
Q

How is insulin formed?

A

Proteolytically cleaved –> mature insulin and C-peptide

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5
Q

What stimulates insulin release?

A

increase glucose - hyperglycaemia
amino acid and fatty acids
peptide gut hormones - incretins - GLP1

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6
Q

What are the main areas that insulin targets?

A

liver, muscle and adipose tissue

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7
Q

What are the metabolic targets of insulin?

A
  1. CHO
  2. Fat
  3. Protein
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8
Q

What is the insulin receptor (Ins-R)?

A

receptor tyrosine kinase (RTK)

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9
Q

What happens when insulin binds to Ins-R?

A

dimerisation and auto-phosphorylation

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10
Q

What substrate does Ins-R phosphorylates?

A

IRS-1

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11
Q

what does phosphorylated IRS-1 activate?

A

PI3K and Ras-MAPK pathway

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12
Q

What does the PI3K and AKT pathway activate?

A
  1. GLUT4 transporter –> glucose into cells
  2. glycogen synthase
  3. cell growth
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13
Q

What is Diabetes Mellitus?

A

metabolic disorders characterised by HYPERGLYCAEMIA

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14
Q

What is chronic metabolic disorders caused by?

A

relative or absolute insulin deficiency

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15
Q

What is type 1 diabetes?

A

ABSOLUTE insulin deficiency

auto-immune destruction of β cells

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16
Q

What is type 2 diabetes?

A

RELATIVE insulin deficiency
peripheral resistance to ‘normal’ insulin levels
subsequent progressive decrease in β cell function/mass

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17
Q

What are some complications of diabetes?

A

acute

chronic

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18
Q

What are some acute complications of diabetes?

A 
diabetic ketoacidosis (DKA)
insufficient/absent insulin in IDDM
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19
Q

What does insufficient/absent insulin in IDDM cause?

A

fats used for energy = ketones (strong acids)
decrease pH
dehydration

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20
Q

What are the chronic complications of diabetes?

A

macrovascular –> cardiovascular risk

microvascular –> huge burden/costs

21
Q

What are ways of treating type 1 diabetes?

A

recapitulate normal pattern of pancreatic insulin secretion - insulin, lifestyle and monitoring

22
Q

How is insulin administered?

A

subcutaneously

injection sites must be rotated

23
Q

What is the pharmacokinetics of insulin?

A

absorption affected by formulation, blood flow, scars
short-lived effects
enzymatically inactivated in cells after uptake

24
Q

What are ways to mimic normal insulin levels?

A

ideal
basal-bolus regimen
insulin pump

25
Q

What is ideal mimicking technique?

A

constant basal insulin production

+ post-prandial insulin surges

26
Q

What is the basal-bolus regimen?

A

long acting insulin at bedtime = basal
prandial rapid-acting insulin = bolus
4 or more injections/day

27
Q

What is the insulin pump technique?

A

basal infusion + patient-activated boluses

improved glycaemic control

28
Q

What are some side-effects of insulin therapy for diabetes type 1?

A

hypoglycaemia
weight gain
injection site

29
Q

What is the main goal of treatment of type 2 diabetes?

A

lower blood glucose levels –> prevents microvascular complications
individualised treatments

30
Q

What are the treatments for type 2 diabetes?

A

lifestyle
oral hypoglycaemic agents
insulin

31
Q

What are some hypoglycaemic drugs?

A 
metformin
sulfonylureas
incretin-based therapies
dapagliflozin (SGLT2 inhibitor)
acarbose (intestinal α-glucosidase inhibitor)
pioglitazone (thiazolidinediones)
32
Q

What is the mechanism of metformin?

A

mainly decrease hepatic gluconeogenesis

may cause GLP1 release

33
Q

What are the effects/benefits of metformin?

A

no hypoglycaemia
improved lipid profile
probable anti-cancer properties

34
Q

What is the pharmacokinetics of metformin?

A

40-60% orally bioavailable excreted unchanged in urine

decrease drug clearance with other renally excreted drugs

35
Q

What are some side-effects/caution of metformin?

A

GI - transient anorexia + diarrhoea
vitamin B12 deficiency
lactic acidosis
C/I in severe renal failure + severe hepatic impairment

36
Q

What is the mechanism of sulfonylureas?

A

insulin secretagogues

37
Q

What is the mechanism of insulin secretagogues?

A

block SU receptor (SUR1) / K+ channel on β cells –> Ca2+ influx activates insulin secretion

38
Q

What is the pharmacokinetics of sulfonylureas?

A

albumin binding, hepatic metabolism, renal excretion

drug interactions –> increase hypoglycaemic effect

39
Q

What is the benefits of sulfonylureas?

A

robust glucose decrease in early stages of type 2 diabetes

cheap and effective

40
Q

What are some side-effects/cautions of sulfonylureas?

A

hypoglycaemia
weight gain
C/I in liver failure - hepatic metabolism

41
Q

What is the incretin effect?

A

oral glucose induces a much greater insulin response than an equivalent IV glucose dose

42
Q

What are incretins?

A

gut peptides that increase insulin release after food

43
Q

What are some incretin-based therapies?

A

GLP1 receptor agonists
DDP-4 inhibitors
GIP receptor agonist

44
Q

Why is DDP-4 inhibitors used?

A

blocks DDP-4 enzyme which inactivates GLP-1

45
Q

What is GLP1 used for?

A

stimulates insulin release

inhibits glucagon release

46
Q

What does SGLT2 inhibitors use?

A

inhibit sodium glucose co-transporter 2
block glucose reabsorption in proximal tubule –> lost in urine
S/E = urinary tract infections

47
Q

What is the use of intestinal α-Glucosidase inhibitors?

A

competitive inhibition of maltose –> glucose

S/E = bloating, flatuelence, diarrhoea

48
Q

What is the use of Thiazolidinediones?

A

PPARγ agonist - activate gene transcription

increase insulin sensitivity

PHAR2200 (9 decks)

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