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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
What are the drugs used to induce remission in mild ulcerative colitis
topical or oral aminosalicylate (5-ASA)
26
Examples of aminosalicylates
Mesalazine sulfasalazine Olsalazine
27
What is the second line treatment for mild ulcerative colitis
aminosalicylate + oral prednisolone
28
What is the third line of treatment for mild ulcerative colitis
aminosalicylate + oral prednisolone + oral tacrolimus
29
What drug is used to treat acute severe ulcerative colitis
IV corticosteroids
30
What is the second line treatment for acute severe ulcerative colitis
IV corticosteroid + IV ciclosporin | or surgery
31
Why isn't morphine used for biliary colic
Because morphine worsens biliary colic; it causes constriction of sphincter of Oddi
32
Which analgesia is used for biliary colic
NSAID buprenophrine AVOID MORPHINE
33
Biliary spasm is relieved by
atropine | GTN
34
Loperamide type of drug
Opioids (opiates) u-opioid agonist
35
Examples of anti-diarrheal drugs
Loperamide | Diphenoxylate
36
Mechanism of action of opioids
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
Side effects for opiates
Sedation Respiratory depression Constipation
38
Types of laxatives
Bulk forming laxative | Osmotic laxative
39
Example of bulk forming laxative
Isphagula husk
40
Bulk forming laxative mechanism of action
Absorb water from the lumen of intestines, forming soft bulky stool. The presence of bulky mass stimulates peristaltic contraction
41
Osmotic laxative mechanism of action
Pulls water from surrounding tissue into the lumen by osmosis, softening the stool
42
When are laxatives used
Consatipation | IBS-C
43
Function of vomiting center
Coordinates vomiting signals from the CTZ, gut, peripheries and cortical centres
44
Where is the vomiting center located at
Brainstem
45
Where is the cortical center located at and what is its function
In the brain, senses pain / repulsive sights and smells / emotional factors
46
What are the main neurotransmitters involved in triggering nausea and vomiting
ACh, 5HT and dopamine
47
What receptors are present in chemoreceptor trigger zone
5HT3 receptors | Dopamine receptors
48
Where is CTZ located
In medulla oblongata
49
What receptor is present in the brain
Histamine 1 receptor
50
Route of emetic signals
Enterochromaffin cells in gut sense toxin -> vagal afferents to send signals from the gut -> CTZ -> vomiting center Cortical center -> vomiting center
51
Types of anti-emetic drugs
``` H1 receptor antagonist Muscarinic ACh antagonist 5HT3 receptor antagonist Dopamine receptor antagonist Neurokinin-1 receptor antagonist ```
52
Examples of H1 receptor antagonists
Cyclizine promethazine diphenhydramine
53
Use of histamine 1 receptor antagonist
Nausea/vomiting due to motion sickness
54
Side effect of H1 receptor antagonist
Sedation
55
Side effect of H1 receptor antagonist
Sedation
56
Why may H1 antagonist cause sedation
Because H1 receptors in other parts of brain are involved in sleep response
57
Where are M1 receptors found
Cerebral cortex Gastric, salivary glands Parasympathetic ganglion
58
M1 receptor antagonist example
Scopolamine
59
Use of scopolamine
Nausea / vomiting due to motion sickness
60
Side effects of M1 receptor antagonist
Tachycardia Dry mouth Constipation
61
Why may scopolamine cause constipation
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
Why can scopolamine cause tachycardia
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
Example of 5HT3 receptor antagonist
Ondansetron Granisetron Palonosetron
64
Where are 5HT3 receptors found
In chemoreceptor trigger zone and in the GI tract (enteric nervous system)
65
Effect of 5HT3 on gi tract
Regulate motility, secretion of the gut | Pain sensation
66
Side effects of 5HT3 antagonist
Constipation Diarrhea Headache
67
How does 5HT3 antagonist cause constipation
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
How does 5HT3 antagonist cause diarrhea
5HT3 in enteric nervous system regulates motility. Blocking 5HT3 = impaired motility = diarrhea
69
Examples of dopamine receptor antagonist
``` Chlorpromazine Droperidol Haloperidol Prochlorperazine Metoclopramide Domperidone ```
70
Where are dopamine 2 receptors (D2R) located
CTZ and gut
71
Side effects of Dopamine 2 receptor antagonists
``` Diarrhea extrapyramidal effects (feeling restless / muscles contract involuntarily) ```
72
Which dopamine 2 receptor antagonist does not have extra pyramidal effects
Domperidone
73
Which dopamine 2 receptor antagonist increases lower oesophageal sphincter tone
domperidone, causing food unable to enter the stomach
74
Uses of rifaximin
HE traveller’s diarrhea caused by e.coli IBS-D
75
Which laxative should be avoided in opioid-induced constipation
Bulk-forming laxative Because bulk forming laxative try to stimulate peristalsis but opioid blocks peristalsis hence this will worsen abdominal pain and constipation
76
Which laxatives should be used for chronic constipation
Bulk-forming laxative first | If ineffective, add osmotic laxative
77
Example of osmotic laxative
Macrogols | Lactulose
78
Which dopamine receptors do metoclopramide act on
Metoclopramide is more selective towards D1 receptor in CTZ
79
Which dopamine receptors do domperidone act on
Domperidone is peripherally selective towards D2 and D3
80
What are the other effects of domperidone
Increases motility in upper GI tract and increases lower oesophageal sphincter tone
81
Effect of dopamine in GI tract
Inhibits motility in upper GI | Stimulates motility in colon
82
Contraindication of metoclopramide
Intestinal obstruction Bleeding in GI tract Perforation in GI tract
83
Sulfasalazine is metabolised by
Intestinal bacteria to release 5-ASA
84
When should 5HT3 antagonist be used
In nausea and vomiting due to chemotherapy
85
Effects of 5HT3 agonists on GI tract
Increase motility | Increase secretion

Y1 GI (6 decks)

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