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Year 3 - Met3a > Drugs of the GI Tract > Flashcards

Drugs of the GI Tract Flashcards

1
Q

Name examples of 5ASAa

A
  • sulphasalazine
  • mesalazine
  • osalazine
  • balsalazide
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2
Q

what does the site of release of 5ASA depend on

A
  • when given orally the site of release of 5ASA depends on formluation (coating and azo-bond)
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3
Q

what are the indications for 5ASAs

A
  • Mild/moderate UC
  • colonic crohns
  • maintenance UC - prevents recurrence of
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4
Q

What is the mechanisms of action of 5ASA

A
  • they are poorly absorbed
  • effects are largely topical
  • unknown mechanism of action
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5
Q

What do they think is the mechanism of action of 5ASAs

A
  • scavengers of ROS
  • modulates prostaglandins and leukotriene synthesis from arachidonic acid
  • modulates cytokine profile
  • PPARgamma (peroxisome proliferator activated receptor gamma) agonists
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6
Q

What are the side effects of 5ASA

A
  • nephrotoxicity
  • rash
  • worsening of colitis
  • pancreatitis
  • pericarditis
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7
Q

what are the classes of corticosteroids

A
  • Glucocorticoid

- low mineralocorticoid

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8
Q

What are the names of corticosteroids

A
  • Prednisolone
  • Hydrocortisone
  • budesonide
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9
Q

describe budesonide

A
  • topical action
  • first pass metabolism
  • fewer systemic side effects
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10
Q

What is the indication for corticosteroids in UC

A
  • induction of remission
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11
Q

What is the mechanism of action of corticosteroids

A
  • immunosuppressive
  • mediated via glucocorticoid receptor
  • regulates transcription of 100+ genes
  • reduces IL-1, TNF alpha, IL-8
  • reduces nitric oxide
  • prevents leucocyte migration
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12
Q

What is the route of administration for corticosteroids

A

Depends according to site and severity of IBD

  • oral
  • IV
  • Enema
  • suppositories
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13
Q

What are the side effects of corticosteroids

A
  • Hypertension
  • diabetes mellitus
  • central obesity
  • osteoporosis, myopathy
  • acne, bruising
  • cataracts
  • depression
  • growth failure
  • pituitary/adrenal suppression
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14
Q

what causes duodenal peptic ulcer disease

A

Helicobacter pylori

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15
Q

What causes gastric peptic ulcer disease

A
  • Helicobacter pylori

- NSAIDs and steroids

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16
Q

What are the classes of anti-secretory therapy

A
  • Proton pump inhibitors

- histamine receptor 2 antagonists

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17
Q

what are the names of proton pump inhibitors

A
  • Omeprazole
  • lanzoprazole
  • pantoprazole
  • rabeprozole
  • esomeprazole
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18
Q

Name some examples of histamine receptor 2 antagonists

A
  • Ranitidine
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19
Q

What is the indication for anti secretory therapy

A
  • PUD
  • GORD
  • prevention of ulcers in patients on NSAID
  • Zollinger ellison syndrome
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20
Q

what is zollinger ellison syndrome

A

Zollinger–Ellison syndrome (Z-E syndrome) is a disease in which tumors cause the stomach to produce too much acid, resulting in peptic ulcers

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21
Q

What is the route of admission for an anti-secretory therapy

A
  • oral

- IV

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22
Q

What are the side effects for anti-secretory therapy

A
  • Diarrhoea
  • headache
  • increase risk of C.difficile
  • weak inhibitors of cytochrome P450 (care with phenytoin, warfarin and theophyline)
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23
Q

Name the three emetic pathways

A
  • Medulla
  • afferents - labyrinth, vagus, systemic circulation
  • Efferents - oesophagus, stomach, abdominal wall
24
Q

What are the three classes of anti emetics

A
  • H1r anatognists
  • D2r antagonists, 5HT4r agonist
  • 5HT3 antagonists
25
Q

Name a H1r anatognists

A

Cyclizine

26
Q

What are the indications of use of Cyclizine (H1r anatognists)

A
  • Vertigo
  • motion sickness
  • post-op nausea and vomiting
27
Q

What are the side effects of Cyclizine (H1r anatognists)

A
  • drowsiness
  • dry mouth
  • urinary retention
28
Q

Name a D2r antagonists, 5HT4r agonist

A

Metoclopramide

29
Q

Name some indications for Metoclopramide (D2r antagonists, 5HT4r agonist)

A
  • Anti-emetic
  • gastroparesis
  • PONV
30
Q

Name the mechanism of action of metaclopramide (D2r antagonists, 5HT4r agonist)

A
  • CTZ

- increases gastric emptying

31
Q

Name the side effects of metaclopramide (D2r antagonists, 5HT4r agonist)

A
  • restlessness

- dystonic reactions

32
Q

Name an example of a 5HT3 antagonists

A

Ondansetron

33
Q

name the indications for ondansetron (5HT3 antagonists)

A
  • refractory
  • PONV
  • chemotherapy
34
Q

name the side effects for ondansetron (5HT3 antagonists)

A
  • constipation
  • headache
  • flushing
  • reduced HR
  • reduced BP
35
Q

describe how thiopurines can have different effects on the body

A

Azathiopurine can be converted into mercaptopurine (MP)
- TPMT can covert this to methyl mercaptopurine (MMP) this causes liver damage

Or

  • meracaptopurine (MP) can be converted into thioguanine this can have a therapeutic effect but also can cause bone marrow suppression
36
Q

Name some examples of thiopurines

A
  • azathioprine

- mercaptopurine

37
Q

how are thiopurines taken

A
  • oral
38
Q

What are the indications of thiopurines

A

maintenance of remission of IBD

39
Q

What are the side effects of thiopurines

A
  • bone marrow suppression
  • hepatitis, pancreatitis
  • lethargy, headache, nausea, rash
  • viral infections
  • lymphoma
40
Q

What is regularly checked when using thiopurines

A
  • blood count
  • LFTs
  • drug levels (TGN)
41
Q

What is pre checked when using thiopurines and wh y

A
  • TPMT status

this is because TMPT can convert mercaptopurine (MP) to methyl mercaptopurine (MMP) this causes liver damage

42
Q

name 4 classes of laxatives

A
    • Bulk laxative
  • stimulant laxative
  • stool softener
  • osmotic laxative
43
Q 
Name an 
- example 
- mechanism of action 
- side effect 
for a bulk laxative
A

example
- Fybogel

mechanism of action

  • increases stool mass
  • stimulates peristalsis

side effect

  • wind
  • bloating
44
Q 
Name an 
- example 
- mechanism of action 
- side effect 
for a stimulant laxative
A

example
- Senna

mechanism of action
- increases colonic motility

side effect

  • cramps
  • low potassium
45
Q 
Name an 
- example 
- mechanism of action 
- side effect 
for a stool softener
A

example
- arachis oil

mechanism of action
- lubricates stool

side effect
- peanut allergy

46
Q 
Name an 
- example 
- mechanism of action 
- side effect 
for a osmotic laxative
A

example

  • lactulose
  • movicol (macrogol)

mechanism of action

  • Lactulose = disaccarhide not absorbed, draws fluid into the gut lumen
  • Movicol = not absorbed, draws fluid into the gut lumen

side effect
- Lactulose = wind and cramps

47
Q

Name the classes of biologicals that can be used

A
  • Anti TNF
  • Anti integrin
  • Anti IL-12/23
  • JAK inhibitors
48
Q

Name some examples of Anti TNF

A
  • infliximab

- adalimumab

49
Q

Name some examples of Anti integrins

A
  • vedolizumab
50
Q

Name some examples of Anti IL-12/23

A
  • ustekinumab
51
Q

Name some examples of JAK inhibitors

A
  • Tofacitinib (oral, UC only)
52
Q

How are biological treatments in IBD given

A
  • IV or SC

- tofacitinib is given orally

53
Q

What are biologicals used in

A
  • IBD
  • rheumatoid arthritis
  • ankylosing spondylitis
  • psoriasis
54
Q

What are the side effects of biologicals

A
  • opportunistic infections
  • hypersensitivity reactions
  • loss of response due to development of antibodies
55
Q

What drugs are used in induction of remission in IBD

A

1st line

  • 5ASA (UC)
  • Corticosteroids
  • Ciclosporine (UC)

3rd line
Biologicals

56
Q

What drugs are used in. maintenance of remission in IBD

A

1st line
- 5ASA (UC)

2nd line

  • thiopurines
  • methotrexate

3rd line
- Biologicals

Year 3 - Met3a (43 decks)

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