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Endocrine > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

first line treatment for diabetes

A

metformin

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2
Q

MOA of metformin

A

Inhibits complex 1 of mitochondrial respiratory chain
Binds to complex one, reduces efficiency of mitochondrial respiratory, resulting in a fall in cellular energy/ cellular ATP

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3
Q

consequences of metformin MOA

A
  • Rise in amp; atp, activates amp kinase;
    • Reduction in gluconeogenesis
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4
Q

is metformin hydrophobic or philic

A

hydrophilic so it is not readily taken up into cells

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5
Q

what does metformin require

A

active transport by organic cation transporters

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6
Q

where are organic cation transporters

A

intestines, liver and kidneys

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7
Q

where is metformin excreted

A

kidneys

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8
Q

main site of action of metformin

A

liver

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9
Q

how is metforminexcreted in the urine

A

unchanged, it is not metabolised in any way

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10
Q

main effect of metformin

A

to increase glucose utilisation and lower hepatic glucose production

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11
Q

metformin and gi tract

A

alters microbiome

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12
Q

side effects of metformin

A

GI side effects, diarrhoea, bloating, abdominal pain, dyspepsia, metallic taste in mouth , highly concentrated in intestine

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13
Q

how to reduce side effects of metformin

A

initiate slowly , start low and go slow

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14
Q

main concern of metformin

A

lactic acidosis as it increases lactate production

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15
Q

acute kidney failure and metformin

A

metformin may accumulate and so lactate isnt cleared

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16
Q

which drug has a sustained benefit of CDV disease

A

metformin

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17
Q

clinical benefits of metformin

A

potent
lowers HbA1c
cheap
well tolerated
weight losing

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18
Q

side effects of SGLT2 inhibitors

A

thrush
risk of ketoacidosis

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19
Q

second line drugs to metformin if have previous CVD,CKD or heart failure

A

SGLT2 inhibitors

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20
Q

role of SGLT2I

A

makes you pee out sugar which is good to remove sugar and lower caolires- plateaus after a while

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21
Q

clinical benefits of SGLT2I

A
  • Diuresis
    • Improved myocardial energetics
    • Renal protection
    • Increased renal glucose losses
    • Lowers blood pressure
    • Moderate efficacy
      Good for kidneys and heart
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22
Q

second line drug in africans

A

sulphonylureas

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23
Q

which class of drugs have an increased CDV risk

A

sulphonylureas

24
Q

which class of drug has an increased weight risk

A

sulphonylureas

25
Q

clinical disadvantages

A

increase weight
hypoglycaemic risk
increased CDV risk

26
Q

examples of sulphonylureas

A

gliclazide- pancreatic specific so doesn’t bind to cardiac , glipizide, glimepiride, glibenclamide

27
Q

which type of sulphonylureas is pancreatic specific

A

gliclazide

28
Q

where do sulphonylureas act

A

kATP channels

29
Q

MOA of sulphonylureas

A

Bind to extracellular s1 sulfonylureas receptor
Cause closure of ATP sensitive potassium channels
Rise in membrane potential calcium influx- insulin secretion

30
Q

do sulphonyljureas act to close or open kATP channels

A

close

31
Q

clinical benefits of sulphonylureas

A

potent glucose lowering
lowers Hb1Ac

32
Q

clinical benefits of TZDs

A

dont cause hypoglycaemia
reduce harmful adipose cytokines
- Reduction in liver fat
- Increase in glucose uptake in muscle
- Reduction in atherosclerotic disease
- Potent in obese women
Beneficial effect on blood pressure ; pioglitazone reduced cdv risk

33
Q

side effects of TZDs

A

weight gain
fluid retention
fracture risk

34
Q

what drugs are not used in over 65s and why

A

TZDs due to fracture risk - osteoporosis

35
Q

MOA of TZDs

A

PPARgamma is a transcription factor
TZD’s are ligands which bind to PP gamma receptors
Present in lots of diff tissues and TZDs will bind
Binding results in formation of a complex with a co factor

36
Q

site of main effect of TZDs

A

Main on adipose tissue ; cause pre adipocytes to mature into adipocytes- immature to mature; increase fat mass storage ; healthy place to store fat
Increases triglyceride storage
Increase uptake in free fatty acids; remove fat from viscera and muscle; remove lipotoxicity; fat in liver, pancreas, taking fat out is beneficial

37
Q

example of TZD

A

pioglitazone

38
Q

example of SGLT2I

A

empagliflozin (Jardiance®) dapagliflozin (Forxiga®) canagliflozin (lnvokana®)

39
Q

what is metformin contraindicated in

A

renal impairment, cardiac failure and hepatic failure because of the risk of lactic acidosis

40
Q

when are sulphonylureas indicated

A

when cost is a mjaor issue - developing countries

41
Q

when should SGLT2I be given with metformin

A

Diabetic patients with heart failure or chronic kidney disease

42
Q

main indications of DPP4s

A
  • Most effective in the early stages of type 2 diabetes, when insulin secretion is relatively preserved
  • Can be used as a monotherapy when metformin not tolerated/contraindiated, or as an addon
43
Q

which drug is most effective in early stages of type 2 when insulin is preserved

A

DPP4s

44
Q

what are incretins

A

group of metabolic hormones that are released after eating and play a crucial role in regulating blood glucose levels

45
Q

what are incretins produced by and what is their role

A

the gut and stimulate the release of insulin from the pancreas in response to food intake, even before blood glucose levels rise.

46
Q

what are the two main incretins

A

GIP (Glucose-dependent insulinotropic polypeptide) and GLP-1 - glucose like peptide

47
Q

where are the two mian incretins produced

A

small intestine

48
Q

function of DPP4

A

breaks down incretins so reduces their ability to stimulate the release of insulin

49
Q

MOA of DPP4 inhibitors

A
  • Inhibit DPP4 , which usually inactivate GLP-1 (incretin effect)
  • This in turn increases insulin secretion and reduces glucagon secretion
50
Q

what drug class has a possible increased risk of pancreatitis

A

DPP4Is

51
Q

Examples of DPP4is

A

sitagliptin, alogliptin, saxagliptin

52
Q

examples of GLP-1 receptor antagonists

A

liraglutide, semaglutide

53
Q

main indications of GLP-1 receptor antagonists

A
  • Diabetic patients with atherosclerotic CVD (e.g. previous MI) should be given metformin + GLP-1 receptor antagonist
  • Diabetic patients with heart failure or chronic kidney disease where SGLT2i are contraindicated/not tolerated should be given metformin + GLP-1 receptor antagonist
  • Valuable in diabetic patients who need to loose weight
54
Q

administration of GLP-1 recpetor antagonists

A

injection once a week

55
Q

avderse effects of GLP-1 receptor antagonist

A
  • GI - nausea, vomiting, bloating, diarrhoea
    • Often improves after ~6 weeks but can be intractable
    • May be related to early satiety with reduced gastric emptying
  • Small increase in incidence of gallstones
56
Q

contraindications of GLP-1 receptor antagonists

A

Contraindicated in patients with a history of pancreatitis due to a risk of acute pancreatitis

57
Q
A

Endocrine (19 decks)

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