pharmacology for diabetes and obesity and hormonal control of weight

Question 1

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

Answer 1

sulfonylureas

Question 2

action of sulfonylureas and mechanism of action

Answer 2

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

Question 3

adverse effects of sulfonylureas

Answer 3

hypoglycaemia

weight gain

Question 4

what is the 1st drug of choice when treating T2DM

Answer 4

metformin

Question 5

actions of metformin

Answer 5

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

Question 6

mechanism of action of metformin

Answer 6

activates AMP kinase

Question 7

adverse effects of metformin

Answer 7

• GI disturbances

Question 8

when is prescription of metformin contraindicated

Answer 8

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

Question 9

what type of drug is metformin

Answer 9

biguanides

Question 10

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

Answer 10

alpha-glucosidase inhibitors - acarbose

Question 11

mechanism of action of alpha-glucosidase inhibitors

Answer 11

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

Question 12

adverse effects of alpha-glucosidase inhibitors

Answer 12

• flatulence or abdominal discomfort

- loose stools

Question 13

when is the prescription of alpha-glucosidase inhibitors cotraindicated

Answer 13

in patients with IBD or cirrhosis

Question 14

2 drug types that act through the incretin pathway

Answer 14

GLP-1 receptor agonists

DPP-4 inhibitors

Question 15

action of DPP-4 inhibitors

Answer 15

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

Question 16

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

Answer 16

sitagliptin

Question 17

adverse effects of DPP-4 inhibitors

Answer 17

• URT infection
• headache
• hypoglycaemia when combined with insulin
• allergy
• pancreatitis

Question 18

actions of GLP-1 agonists

Answer 18

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

Question 19

drug name that is a GLP-1 agonist

Answer 19

exenatide

Question 20

adverse effects of GLP-1 agonists

Answer 20

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

Question 21

with hormones/peptides increase hunger

Answer 21

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

Question 22

which hormones/peptides decrease hunger

Answer 22

• alpha-MSH
• urocortin
• CRH
• serotonin
• NA
• leptin
• insulin
• CCK

Question 23

where are the receptors for leptin

Answer 23

in the hypothalamus

Question 24

what is the drug action of phentermine

Answer 24

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

Question 25

when can phentermine be used?

Answer 25

- patient has BMI >30 | - only in the short term

Question 26

adverse effects of phentermine

Answer 26

- increased BP and HR - insomnia - nervousness - headache - dry mouth

Question 27

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

Answer 27

topiramate

Question 28

action of topiramate

Answer 28

increases energy expenditure and suppresses apetite

Question 29

adverse effects of topiramate

Answer 29

dizziness taste alterations teratogenic

Question 30

action of orlistat

Answer 30

inhibits gastric and pancreatic lipases to decrease dietary far absorption

Question 31

orlistat has been shown to reduce what

Answer 31

- body weight - waist circumference - blood glucose - dyslipidaemia - blood pressure

Question 32

ghrelin antagonizes which hormone

Answer 32

leptin

Question 33

how does ghrelin act

Answer 33

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

Question 34

where is ILP-5 released

Answer 34

predominantly in the colon

Question 35

actin of ILP-5

Answer 35

stimulates hunger

Question 36

where is CCK secreted from

Answer 36

the I cells of the small intestine

Question 37

what is the action of CCK

Answer 37

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

Question 38

mechanism of how CCK release results in satiety

Answer 38

acts mainly via the CCK1R on the vagus nerve

Question 39

where is PYY made

Answer 39

by the L cells of the distal GI tract

Question 40

what is the action of DPP-4 on PYY

Answer 40

cleaves it to the active form

Question 41

action of PYY

Answer 41

reduces food intake

Question 42

where is oxyntomodulin released from

Answer 42

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

Question 43

action of oxyntomodulin

Answer 43

reduces food intake and increases energy expenditure

Question 44

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

Answer 44

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

Question 45

what is the general result on weight by having microbiota

Answer 45

increases weight

Question 46

action of microbiota in the gut

Answer 46

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