GI Pharmacology - Resit Flashcards

1
Q

H2 histamine receptor antagonist mechanism

A
  • competitive antagonists of H2 receptors, which are activated by histamine
  • when activated, it increased activity of the proton pump by increased cAMP via PKA
  • by blocking this, there is reduced acid production
  • reduce secretion evoked by gastrin and ACh
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2
Q

NSAIDs mechanism

A
  • COX is formed from arachidonic acid

- reduce prostaglandin formation, via COX 1 inhibition

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3
Q

PPIs mechanism

A
  • inhibit membrane inserted H+/K+ dependent ATPase

- pumps in the tubulovesicles are not inhibited

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4
Q

NSAIDs side effects

A
  • gastric ulceration

- bleeding

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5
Q

what drug can be used to prevent gastric damage, due to long term NSAID use? what does it do?

A

PGE1 analogue (e.g misoprostol)

  • inhibits basal and food stimulated gastric acid formation
  • maintains/increases secretion of mucus and bicarbonate
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6
Q

what 3 things promote peptic ulcer healing?

A
  • reduced acid secretion
  • increased mucosal resistance
  • eradicating H.pylori
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7
Q

why must PPIs make it to the canaliculus of the stomach?

A

so they can be activated here, due to the acidic pH (they are prodrugs)

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8
Q

why must PPIs make it to the canaliculus of the stomach?

A

so they can be activated here, due to the acidic pH

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9
Q

example of a PPI?

A

omeprazole

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10
Q

what gastric acid production are H2 histamine receptor antagonist effective against?

A

basal and stimulated

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11
Q

examples of H2 histamine receptor antagonist

A

ranitidine and cimetidine

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12
Q

sucralfate (mucosal strengtheners) mechanism

A
  • activated in an acidic environment
  • releases aluminium to acquire a strong negative charge
  • blinds to ulcer base, forming a complex gel with mucus
  • barrier against acid and pepsin
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13
Q

what does sucralfate do?

A

increases

  • mucosal blood flow
  • mucus
  • bicarbonate
  • prostaglandin
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14
Q

bismuth chealate (mucosal strengthener) is used for?

A
  • H.pylori, as it promotes eradication
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15
Q

what are laxatives?

A

agents that are used to treat constipation

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16
Q

what are purgatives?

A

agents that cause purging (cleansing) of the bowels, by promoting evacuation

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17
Q

when should laxatives/purgatives NOT be used?

A

when there is a physical obstruction to the bowel

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18
Q

3 uses of laxatives/purgatives?

A
  1. when straining is damaging to health or defecation is painful
  2. clearing the bowel before a procedure
  3. to treat drug induced constipation or constipated bedridden/elderly patients
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19
Q

what are bulk laxatives? examples?

A

indigestible polysaccharide polymers e.g methylcellulose, ispagula husk

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20
Q

what is slow and fast acting, out of bulk and osmotic laxatives?

A

bulk is slow, osmotic is fast

21
Q

what are osmotic laxatives? examples?

A

poorly absorbed solutes

e.g magnesium sulphate/hydroxide, sodium citrate (rectally), lactulose

22
Q

what do bulk and osmotic laxatives do to the body?

A

retain H20, increase bulk, increase peristalsis

23
Q

what are stimulant purgatives? examples?

A

increase water and electrolyte secretion from colonic mucosa and increase peristalsis

e.g senna, bisocodyl,

24
Q

examples of faecal softners?

A
docusate sodium (orally) 
arachis oil (enema)
25
Q

what drug is used for acute attacks in IBD?

A

glucocorticoids (e.g prednisolone, budesonide)

26
Q

what drugs are used in UC? examples?

A

aminosalicylates e.g sulfasalazine, mesalazine, olsalazine, balsalazide

27
Q

what do aminosalicylates all have present?

A

5-ASA (aminosalicylic acid)

28
Q

what transporter does rehydration therapy exploit?

A

SGLT1

29
Q

what is the mechanism of rehydration therapy?

A
  • 2 Na+ bind, so affinity for glucose increases and it binds
  • Na+ and glucose move from out of the cell to inside, via SGLT1
  • Na+ dissociate and affinity for glucose falls, it dissociates
  • this causes accompanying absorption oh H20
30
Q

what type of drugs are used as anti motility/diarrhoeal drugs?

A

opiates (morphine like)

31
Q

5 actions of opiates on the ailmentary tract?

A
  • inhibition of enteric neurones
  • decreases peristalsis, increased segmentation
  • increased fluid absoroption
  • constriction of pylorid, ileocaecal and anal sphincters
  • increased tone of LI
32
Q

what can be used to dissolve non calcified cholesterol gallstones?

A

Ursodeoxycholic acid

33
Q

two treatments for biliary spasm?

A

atropine and GTN

34
Q

5-HT3 receptor antagonist mechanism?

A

block peripheral and central 5-HT3 receptors

35
Q

5-HT3 receptor antagonist uses and examples?

A
  • used to suppress chemo and radiation induced emesis
  • also used for post op
  • e.g onsansetron, palonosetron
36
Q

Muscarinic acetylcholine receptor antagonists use?

A

used for motion sickness

37
Q

Muscarinic acetylcholine receptor antagonists mechanism?

A
  • block muscarinic acetyl choline receptors at multiple sites
  • causing inhibition of movements and relaxation of the GI tract
38
Q

side effects of Muscarinic acetylcholine receptor antagonists ?

A

blurred vision, urinary retention, dry mouth, drowsiness

39
Q

Histamine H1 receptor antagonists use?

A

motion sickness, acute labyrinthitis (inner ear inflam), stomach irritants that cause vomiting

40
Q

Muscarinic acetylcholine receptor antagonists examples?

A

e.g hyosine, scopolamine

41
Q

Histamine H1 receptor antagonists mechanism?

A

blockade of H1 receptors in vestibular nuclei and NTS

42
Q

mechanism of Dopamine receptor antagonists?

A

block dopamine receptors in CTS, exert a prokinetic action on the oesophagus, stomach and intestine

43
Q

examples of Dopamine receptor antagonists ?

A

domperidone and metaclopramide

44
Q

what is Dopamine receptor antagonists used for?

A

drug induced vomiting and vomiting in GI disorders

45
Q

what is an NK1 receptor antagonists used with?

A

used in combo with a 5-HT3 receptor antagonist and dexamethasone

46
Q

when is NK1 receptor antagonists used?

A

in chemo that makes you very sick

47
Q

example of an NK1 receptor antagonist?

A

aprepitant

48
Q

Cannabinoid (CB1) receptor agonists used for?

A

treatment of cytotoxic chemo that is unresponsive to other anti emetics