pharmacology for diabetes and obesity and hormonal control of weight Flashcards

1
Q

what is the drug of choice if you want to treat a relative lack of insulin in T2DM

A

sulfonylureas

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2
Q

action of sulfonylureas and mechanism of action

A

increases insulin secretion from B cells (specifically the initial phase 1 spike)
does this by inhibiting K(ATP) channels –> allows Ca entry and therefore insulin fusion with the cell membrane

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3
Q

adverse effects of sulfonylureas

A

hypoglycaemia

weight gain

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4
Q

what is the 1st drug of choice when treating T2DM

A

metformin

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5
Q

actions of metformin

A
  • increases insulin-mediated peripheral glucose uptake
  • reduces the hepatic glucose production
  • decreases carbohydrate absorption in the gut
  • reduces LDL cholesterol level and TGs
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6
Q

mechanism of action of metformin

A

activates AMP kinase

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7
Q

adverse effects of metformin

A
  • GI disturbances
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8
Q

when is prescription of metformin contraindicated

A

in patients with renal disease –> would lead to increase dosage and side effects

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9
Q

what type of drug is metformin

A

biguanides

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10
Q

what drug would you use if you wanted to decrease the absorption of carbohydrates from the gut in a patient with T2DM

A

alpha-glucosidase inhibitors - acarbose

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11
Q

mechanism of action of alpha-glucosidase inhibitors

A

blocks the enzymes that digest and promote absorption of starches in the small intestin

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12
Q

adverse effects of alpha-glucosidase inhibitors

A
  • flatulence or abdominal discomfort

- loose stools

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13
Q

when is the prescription of alpha-glucosidase inhibitors cotraindicated

A

in patients with IBD or cirrhosis

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14
Q

2 drug types that act through the incretin pathway

A

GLP-1 receptor agonists

DPP-4 inhibitors

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15
Q

action of DPP-4 inhibitors

A

prevents the inactivation of endogenous GLP-1 –> increases insulin and decreases glucagon

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16
Q

what is a name of a drug that is a DPP-4 inhibitor

A

sitagliptin

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17
Q

adverse effects of DPP-4 inhibitors

A
  • URT infection
  • headache
  • hypoglycaemia when combined with insulin
  • allergy
  • pancreatitis
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18
Q

actions of GLP-1 agonists

A
  • potentiates glucose-mediated insulin secretion
  • suppresses glucagon release
  • slow gastric emptying
  • loss of appetite
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19
Q

drug name that is a GLP-1 agonist

A

exenatide

20
Q

adverse effects of GLP-1 agonists

A
  • nausea, vomiting, diarrhoea
  • weight loss
  • antibody formation - immune reactions, pancreatitis
21
Q

with hormones/peptides increase hunger

A
  • ghrelin
  • melanin concentrating hormone
  • agouti-related peptide
  • orexin A and B
  • endocannabinoids
22
Q

which hormones/peptides decrease hunger

A
  • alpha-MSH
  • urocortin
  • CRH
  • serotonin
  • NA
  • leptin
  • insulin
  • CCK
23
Q

where are the receptors for leptin

A

in the hypothalamus

24
Q

what is the drug action of phentermine

A

sympathomimetic amine - increases the NA in the brain predominantly (also dopamine and serotonin) –> decreases food intake

25
Q

when can phentermine be used?

A
  • patient has BMI >30

- only in the short term

26
Q

adverse effects of phentermine

A
  • increased BP and HR
  • insomnia
  • nervousness
  • headache
  • dry mouth
27
Q

which drug has been approved to be prescribed in conjunction with phentermine

A

topiramate

28
Q

action of topiramate

A

increases energy expenditure and suppresses apetite

29
Q

adverse effects of topiramate

A

dizziness
taste alterations
teratogenic

30
Q

action of orlistat

A

inhibits gastric and pancreatic lipases to decrease dietary far absorption

31
Q

orlistat has been shown to reduce what

A
  • body weight
  • waist circumference
  • blood glucose
  • dyslipidaemia
  • blood pressure
32
Q

ghrelin antagonizes which hormone

A

leptin

33
Q

how does ghrelin act

A

it acts through the neuropeptide Y neurons in the arcuate nucleus of the hypothalamus to stimulate hunger (stimulates both release and synthesis of NPY)

34
Q

where is ILP-5 released

A

predominantly in the colon

35
Q

actin of ILP-5

A

stimulates hunger

36
Q

where is CCK secreted from

A

the I cells of the small intestine

37
Q

what is the action of CCK

A
  • satiety

- stimulates emptying of the gall bladder and release of digestive enzymes when fat is in the small intestine

38
Q

mechanism of how CCK release results in satiety

A

acts mainly via the CCK1R on the vagus nerve

39
Q

where is PYY made

A

by the L cells of the distal GI tract

40
Q

what is the action of DPP-4 on PYY

A

cleaves it to the active form

41
Q

action of PYY

A

reduces food intake

42
Q

where is oxyntomodulin released from

A

the L cells of the intestine (like PYY) in the GIT

43
Q

action of oxyntomodulin

A

reduces food intake and increases energy expenditure

44
Q

what is the main reason that most people who loose weight regain it againa

A

the gut hormones produce more hunger hormones if you loose weight as a way of defending against weight loss

45
Q

what is the general result on weight by having microbiota

A

increases weight

46
Q

action of microbiota in the gut

A
  • increases the activity of lipoprotein lipase
  • processing of dietary polysaccharides –> increased hepatic lipogenesis
    results in increased TG storage in adipocytes