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Y1 GI > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

Examples of PPI

A

Omeprazole
esomeprazole
lansoprazole

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2
Q

Examples of antacids

A

Gaviscon
Calcium carbonate
Magnesium hydroxide

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3
Q

Mechanism of action of histamine receptor antagonists (H2 blockers)

A

Prevents histamine from binding to the H2 blockers on parietal cells -> adenylyl cyclase not activated -> cAMP not produced -> PKA not produced -> proton pump not activated

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4
Q

What activates PKG

A

cGMP

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5
Q

What is the effect of cGMP on smooth muscle

A

smooth muscle relaxation

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6
Q

Examples of H2 receptor antagonists

A

ranitidine
cimetidine
nizatidine
famotidine

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7
Q

NSAID mechanism of action

A

Inhibits COX1 , COX2 and prostaglandin E2

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8
Q

What type of NSAID is aspirin

A

Non-selective NSAID, but weakly more selective for COX1

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9
Q

Function of COX1 and COX2

A

Produce prostaglandin E2 to protect the GI lining

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10
Q

How does PGE2 protect the lining of GI mucosa

A

It stimulates the production of mucus and inhibits gastric acid and pepsin production

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11
Q

How does NSAID cause peptic ulcers

A

NSAID inhibits the production of prostaglandin E2, COX1 and COX2 hence decreases the production of protective mucous and inhibition of gastric acid secretion and pepsin. This leads to overproduction of acid and damage of the lining

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12
Q

Use of aminosalicylates

A

In ulcerative colitis

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13
Q

How is mesalazine metabolised in the liver

A

By adding acetyl group to mesalazine, forming mesalamine to be excreted in urine

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14
Q

Side effects of PPI

A 
Headache
Diarrhea
Constipation
Dizziness
Nausea 
Increases pH reducing defense against bacteria
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15
Q

Contraindications for PPI

A
  • for those that will be testing for H. pylori

- for those that have red flag symptoms and will be undergoing endoscopy

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16
Q

Why shouldn’t PPI be used in patients with red flag symptoms before their endoscopy

A

PPI might mask malignancy

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17
Q

Use of H2 receptor antagonists

A

second line treatment for GORD

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18
Q

Use of PPI

A 
first line for GORD
first line PUD
H.pylori infection (antibiotics + PPI)
Bleeding PUD
Functional dyspepsia
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19
Q

Long term use of PPI can increase the patient’s susceptibility for which infections

A

C. difficile infection

pneumonia

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20
Q

How does PPI cause pneumonia

A

PPI increases pH which decreases the ability to kill pathogen hence the pathogen may then be aspirated and cause pneumonia

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21
Q

What are the drugs used for Crohn’s disease to induce remission

A

Glucocorticoids - prednisolone / IV hydrocortisone

azathioprine / methotextrate / mercaptopurine

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22
Q

When should azathioprine / methotrexate / mercaptopurine be used in inducing remission for Crohn’s disease

A

If glucocorticoids are not tolerated or are ineffective

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23
Q

What drugs are used to maintain remission in Crohn’s disease

A

azathioprine / mercaptopurine

methotrexate

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24
Q

When should methotrexate be used in Crohn’s

A

If azathioprine / mercaptopurine is not tolerated or is ineffective

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25
Q

What are the drugs used to induce remission in mild ulcerative colitis

A

topical or oral aminosalicylate (5-ASA)

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26
Q

Examples of aminosalicylates

A

Mesalazine
sulfasalazine
Olsalazine

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27
Q

What is the second line treatment for mild ulcerative colitis

A

aminosalicylate + oral prednisolone

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28
Q

What is the third line of treatment for mild ulcerative colitis

A

aminosalicylate + oral prednisolone + oral tacrolimus

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29
Q

What drug is used to treat acute severe ulcerative colitis

A

IV corticosteroids

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30
Q

What is the second line treatment for acute severe ulcerative colitis

A

IV corticosteroid + IV ciclosporin

or surgery

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31
Q

Why isn’t morphine used for biliary colic

A

Because morphine worsens biliary colic; it causes constriction of sphincter of Oddi

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32
Q

Which analgesia is used for biliary colic

A

NSAID
buprenophrine

AVOID MORPHINE

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33
Q

Biliary spasm is relieved by

A

atropine

GTN

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34
Q

Loperamide type of drug

A

Opioids (opiates)

u-opioid agonist

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35
Q

Examples of anti-diarrheal drugs

A

Loperamide

Diphenoxylate

36
Q

Mechanism of action of opioids

A

acts on the μ-opioid receptors, decrease activity of myenteric plexus hence decreases tone of contraction of longitudinal and circular muscles = decreases peristalsis

Increases fluid reabsoprtion

Increases constriction of sphincters

37
Q

Side effects for opiates

A

Sedation
Respiratory depression
Constipation

38
Q

Types of laxatives

A

Bulk forming laxative

Osmotic laxative

39
Q

Example of bulk forming laxative

A

Isphagula husk

40
Q

Bulk forming laxative mechanism of action

A

Absorb water from the lumen of intestines, forming soft bulky stool. The presence of bulky mass stimulates peristaltic contraction

41
Q

Osmotic laxative mechanism of action

A

Pulls water from surrounding tissue into the lumen by osmosis, softening the stool

42
Q

When are laxatives used

A

Consatipation

IBS-C

43
Q

Function of vomiting center

A

Coordinates vomiting signals from the CTZ, gut, peripheries and cortical centres

44
Q

Where is the vomiting center located at

A

Brainstem

45
Q

Where is the cortical center located at and what is its function

A

In the brain, senses pain / repulsive sights and smells / emotional factors

46
Q

What are the main neurotransmitters involved in triggering nausea and vomiting

A

ACh, 5HT and dopamine

47
Q

What receptors are present in chemoreceptor trigger zone

A

5HT3 receptors

Dopamine receptors

48
Q

Where is CTZ located

A

In medulla oblongata

49
Q

What receptor is present in the brain

A

Histamine 1 receptor

50
Q

Route of emetic signals

A

Enterochromaffin cells in gut sense toxin -> vagal afferents to send signals from the gut -> CTZ -> vomiting center

Cortical center -> vomiting center

51
Q

Types of anti-emetic drugs

A 
H1 receptor antagonist
Muscarinic ACh antagonist
5HT3 receptor antagonist
Dopamine receptor antagonist
Neurokinin-1 receptor antagonist
52
Q

Examples of H1 receptor antagonists

A

Cyclizine
promethazine
diphenhydramine

53
Q

Use of histamine 1 receptor antagonist

A

Nausea/vomiting due to motion sickness

54
Q

Side effect of H1 receptor antagonist

A

Sedation

55
Q

Side effect of H1 receptor antagonist

A

Sedation

56
Q

Why may H1 antagonist cause sedation

A

Because H1 receptors in other parts of brain are involved in sleep response

57
Q

Where are M1 receptors found

A

Cerebral cortex
Gastric, salivary glands
Parasympathetic ganglion

58
Q

M1 receptor antagonist example

A

Scopolamine

59
Q

Use of scopolamine

A

Nausea / vomiting due to motion sickness

60
Q

Side effects of M1 receptor antagonist

A

Tachycardia
Dry mouth
Constipation

61
Q

Why may scopolamine cause constipation

A

Because scopolamine is non-selective muscarinic receptor antagonist, can bind to M3 receptors on smooth muscles; peristalsis in colon can be enhanced by parasympathetic stimulation

62
Q

Why can scopolamine cause tachycardia

A

Because it is a non-selective muscarinic receptor antagonist, it can act on M2 receptors in cardiac muscle. This reduces parasympathetic tone on HR hence causes tachycardia (there is always a parasympathetic tone on HR to decrease HR to normal range)

63
Q

Example of 5HT3 receptor antagonist

A

Ondansetron
Granisetron
Palonosetron

64
Q

Where are 5HT3 receptors found

A

In chemoreceptor trigger zone and in the GI tract (enteric nervous system)

65
Q

Effect of 5HT3 on gi tract

A

Regulate motility, secretion of the gut

Pain sensation

66
Q

Side effects of 5HT3 antagonist

A

Constipation
Diarrhea
Headache

67
Q

How does 5HT3 antagonist cause constipation

A

Because 5HT3 are expressed on presynaptic efferents of parasympathetic innervation. When 5HT3 receptors are activated, ACh will be released from presynaptic neurone and ACh increases peristaltic contractions

So 5HT3 antagonist reduces peristaltic contractions = constipation

68
Q

How does 5HT3 antagonist cause diarrhea

A

5HT3 in enteric nervous system regulates motility. Blocking 5HT3 = impaired motility = diarrhea

69
Q

Examples of dopamine receptor antagonist

A 
Chlorpromazine 
Droperidol 
Haloperidol 
Prochlorperazine 
Metoclopramide
Domperidone
70
Q

Where are dopamine 2 receptors (D2R) located

A

CTZ and gut

71
Q

Side effects of Dopamine 2 receptor antagonists

A 
Diarrhea
extrapyramidal effects (feeling restless / muscles contract involuntarily)
72
Q

Which dopamine 2 receptor antagonist does not have extra pyramidal effects

A

Domperidone

73
Q

Which dopamine 2 receptor antagonist increases lower oesophageal sphincter tone

A

domperidone, causing food unable to enter the stomach

74
Q

Uses of rifaximin

A

HE
traveller’s diarrhea caused by e.coli
IBS-D

75
Q

Which laxative should be avoided in opioid-induced constipation

A

Bulk-forming laxative

Because bulk forming laxative try to stimulate peristalsis but opioid blocks peristalsis hence this will worsen abdominal pain and constipation

76
Q

Which laxatives should be used for chronic constipation

A

Bulk-forming laxative first

If ineffective, add osmotic laxative

77
Q

Example of osmotic laxative

A

Macrogols

Lactulose

78
Q

Which dopamine receptors do metoclopramide act on

A

Metoclopramide is more selective towards D1 receptor in CTZ

79
Q

Which dopamine receptors do domperidone act on

A

Domperidone is peripherally selective towards D2 and D3

80
Q

What are the other effects of domperidone

A

Increases motility in upper GI tract and increases lower oesophageal sphincter tone

81
Q

Effect of dopamine in GI tract

A

Inhibits motility in upper GI

Stimulates motility in colon

82
Q

Contraindication of metoclopramide

A

Intestinal obstruction
Bleeding in GI tract
Perforation in GI tract

83
Q

Sulfasalazine is metabolised by

A

Intestinal bacteria to release 5-ASA

84
Q

When should 5HT3 antagonist be used

A

In nausea and vomiting due to chemotherapy

85
Q

Effects of 5HT3 agonists on GI tract

A

Increase motility

Increase secretion

Y1 GI (6 decks)

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