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Endocrine 2020 > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

what are four types of membrane-bound receptors?

A
  1. ligand-gated ion channels
  2. GPCR
  3. receptor tyrosine kinase (kinase-linked receptors)
  4. steroid hormone receptors
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2
Q

what happens to ligand-gated ion channels when neurotransmitters bind?

A

causes a conformational change allowing influx/efflux of ions

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3
Q

structure of a GPCR

A

7 transmembrane spans across membrane coupled with G-proteins

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4
Q

role of G-proteins

A

stimulate or inhibit various effectors

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5
Q

what does binding to the GPCR cause?

A

G-protein dissociation

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6
Q

can GPCR do signal amplification?

A

yes

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7
Q

what binds to receptor tyrosine kinases?

A

hormones

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8
Q

what does binding of hormones do to receptor tyrosine kinases?

A

causes dimer formation and autophosphorylation of tyrosine residues and relay proteins activate divergent response

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9
Q

what happens when there is binding to steroid hormone receptors?

A

pass through cell membrane and bind to response elements activating transcriptions

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10
Q

three types of signalling

A
  1. autocrine
  2. paracrine
  3. endocrine
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11
Q

what does endocrine signalling need that the others do not?

A

a blood supply

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12
Q

what are the three types of hormones?

A

protein/peptide
steroid
amines

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13
Q

when are steroid hormones active?

A

when they are unbound

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14
Q

what are the two types of amine hormones?

A

catecholamines

tyrosine amines

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15
Q

what does hormone binding to carrier proteins facilitate?

A

transport

increased half-life

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16
Q

specific hormone carriers

A

CBG
TBG
SSBG

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17
Q

what are the actions of insulin?

A

glucose uptake by cells
glycogenesis
lipogenesis
protein formation

this collectively reduces blood glucose

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18
Q

how is insulin secreted from the pancreatic beta cell?

A
  • elevated blood glucose causes facilitated diffusion via GLUT2 into the beta cell
  • glucose is phosphorylated by glucokinase and glycolysis yields ATP
  • ATP-sensitive K+ channels are closed causing depolarisation and Ca2+ channels open triggering insulin release
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19
Q

examples of sulfonylureas

A

tolbutamide
gliclazide
glipizide

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20
Q

what do SUs require to work?

A

functional beta cells

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21
Q

mechanism of action of SUs

A

displace ADP-Mg2+ from SUR1 closing KATP channels stimulating insulin release

22
Q

adverse of SUs

A 
hypoglycaemia
weight gain (anabolic effect of insulin increases appetite)
23
Q

when are SUs first line?

A

for those intolerant to metformin

24
Q

what decreases the action of SUs?

A

thiazides

corticosteriods

25
Q

examples of glinides

A

repaglinide

nateglinide

26
Q

action of glinides

A

bind to SUR1 to close KATP channel and trigger insulin release

27
Q

when are glinides used?

A

in conjunction with metformin and TZDs

28
Q

what is the incretin effect?

A

insulin responds greater to oral glucose than IV

29
Q

what does the ingestion of oral glucose cause?

A
  • stimulates GLP-1 and GIP to enter portal blood
  • enhance insulin release and delay gastric emptying
  • decrease glucagon

all decrease blood glucose

30
Q

what breaks down the hormones GLP-1 and GIP?

A

DPP4 enzyme

31
Q

two pharmacological options that use the incretin effect?

A
  1. DPP-4 inhibitors

2. incretin analogues

32
Q

examples of DPP-4 inhibitors

A

sitagliptin

saxagliptin

33
Q

action of DPP-4 inhibitors

A

inhibit DPP4 actions causing insulin secretion to be preserved

34
Q

adverse of DPP-4 inhibitors

A

they are weak drugs so nothing really, can cause a bit of nausea

35
Q

examples of incretin analogues

A

extenatide

liraglutide

36
Q

what do incretin analogues do?

A

mimic action of GLP-1 but resist breakdown by DPP4

cause weight loss and reduce hepatic fat accumulation

37
Q

how are incretin analogues administered?

A

SC weekly

38
Q

adverse of incretin analogues?

A

nausea

39
Q

example of a biguanide

A

metformin

40
Q

mechanism of action of metformin

A

activate AMPK increasing glucose uptake, reducing absorption and increasing fatty acid oxidation

prevents hyperglycaemia but doesn’t cause hypoglycaemia

41
Q

when is metformin first line?

A

T2DM

42
Q

adverse of metformin

A

GI upset
lactic acidosis

causes weight loss but seen as a good thing

43
Q

example of thiazolidinediones (TZDS)

A

pioglitzone

44
Q

mechanism of action of TZDs

A

agonists of PPAR-gamma receptor and activated complexes act as transcription factors promoting encoding of proteins involved in insulin signalling and lipid metabolism

shifts fat from visceral to liver

45
Q

adverse of TZDs

A

weight gain

fluid retention

46
Q

examples of sodium-glucose cotransporter-2 inhibitors (SGLT2i)

A

dapaliflozin

canagliglozin

47
Q

mechanism of action of SGLT2i

A

selectively block reabsorption of glucose by SGLT2 in proximal tubule causing glucosuria

48
Q

benefits of SGLT2i

A

weight loss

cardiovascular and renal disease benefits

49
Q

adverse of SGLT2i

A

increased risk of thrush

beware of euglycaemic DKA

50
Q

which drug class is infrequently used in the UK?

A

alpha-glucosidase inhibitors

Endocrine 2020 (35 decks)

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