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Endocrine > Pharmacology > Flashcards

Pharmacology Flashcards

(57 cards)

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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

Study These Flashcards
A

sulphonylureas

24
Q

which class of drug has an increased weight risk

Study These Flashcards
A

sulphonylureas

25
clinical disadvantages
increase weight hypoglycaemic risk increased CDV risk
26
examples of sulphonylureas
gliclazide- pancreatic specific so doesn’t bind to cardiac , glipizide, glimepiride, glibenclamide
27
which type of sulphonylureas is pancreatic specific
gliclazide
28
where do sulphonylureas act
kATP channels
29
MOA of sulphonylureas
Bind to extracellular s1 sulfonylureas receptor Cause closure of ATP sensitive potassium channels Rise in membrane potential calcium influx- insulin secretion
30
do sulphonyljureas act to close or open kATP channels
close
31
clinical benefits of sulphonylureas
potent glucose lowering lowers Hb1Ac
32
clinical benefits of TZDs
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
side effects of TZDs
weight gain fluid retention fracture risk
34
what drugs are not used in over 65s and why
TZDs due to fracture risk - osteoporosis
35
MOA of TZDs
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
site of main effect of TZDs
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
example of TZD
pioglitazone
38
example of SGLT2I
empagliflozin (Jardiance®) dapagliflozin (Forxiga®) canagliflozin (lnvokana®)
39
what is metformin contraindicated in
renal impairment, cardiac failure and hepatic failure because of the risk of lactic acidosis
40
when are sulphonylureas indicated
when cost is a mjaor issue - developing countries
41
when should SGLT2I be given with metformin
Diabetic patients with heart failure or chronic kidney disease
42
main indications of DPP4s
- 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
which drug is most effective in early stages of type 2 when insulin is preserved
DPP4s
44
what are incretins
group of metabolic hormones that are released after eating and play a crucial role in regulating blood glucose levels
45
what are incretins produced by and what is their role
the gut and stimulate the release of insulin from the pancreas in response to food intake, even before blood glucose levels rise.
46
what are the two main incretins
GIP (Glucose-dependent insulinotropic polypeptide) and GLP-1 - glucose like peptide
47
where are the two mian incretins produced
small intestine
48
function of DPP4
breaks down incretins so reduces their ability to stimulate the release of insulin
49
MOA of DPP4 inhibitors
- Inhibit DPP4 , which usually inactivate GLP-1 (incretin effect) - This in turn increases insulin secretion and reduces glucagon secretion
50
what drug class has a possible increased risk of pancreatitis
DPP4Is
51
Examples of DPP4is
sitagliptin, alogliptin, saxagliptin
52
examples of GLP-1 receptor antagonists
liraglutide, semaglutide
53
main indications of GLP-1 receptor antagonists
- 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
administration of GLP-1 recpetor antagonists
injection once a week
55
avderse effects of GLP-1 receptor antagonist
- 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
contraindications of GLP-1 receptor antagonists
Contraindicated in patients with a history of pancreatitis due to a risk of acute pancreatitis
57

Endocrine (48 decks)

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