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GIHEP > L25: Lower GI Pharmacology > Flashcards

L25: Lower GI Pharmacology Flashcards

1
Q

What is TNF Alpha and what diseases is it present in?

A

TNF Alpha = inflammatory cytokine
- stimualtes macrophages to produce cytotoxic metabolites and increase phagocytic activity

a/w Crohn’s Disease and IBS

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2
Q

List 5 drugs that may be used in the treatment of IBD

A
  1. 5-Aminosalicylates
  2. Corticosteroids
  3. Immunosuppressive Agents
  4. Antimicrobials
  5. TNF Alpha Inhibitors (Anti-TNF Alpha Therapy)
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3
Q

What are 5-ASAs used for and what is their MOA?

A

Uses:

  • prevents relapse in UC
  • widely used in Crohn’s

MOA:

  • inhibits leukotriene/prostaglandin formation
  • blocks transcription of inflammatory cytokines
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4
Q

Give an example of a 5-ASA

A

Sulfasalazine (prodrug)
Mesalazine (active metabolite)

Sulfasalazine = Mesalazine + Sulfapyridine

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5
Q

List the adverse effects of 5-ASAs

A
  • GIT disturbance due to hypersensitivity rxns by sulfapyridine
  • thrombocytopenia
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6
Q

What GIT condition may corticosteroids be used for and what is their MOA?

A
  • used for IBD

- inhibits cytokine production (stops inflammation)

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7
Q

List 3 corticosteroids that may be used to treat IBD - which one is first line treatment?

A
  1. Prednisolone - first line
  2. Hydrocortisone
  3. Budesonide
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8
Q

What is a side effect of long term use of corticosteroids?

A

osteoporosis

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9
Q

What are immunosuppressive agents and what is their MOA in treating IBD?

A
  • purine analogues

- inhibit nucleic acid synthesis for long-term maintenance

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10
Q

Give an example of an immunosuppressive agent used in the treatment of IBD

A

Azathioprine (prodrug)
Mercaptopurine (active metabolite)

Azathioprine = Mercaptopurine

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11
Q

Why may mercaptopurine, an immunosuppressive agent used to treat IBD, NOT be used during pregnancy?

A

causes bone marrow suppression

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12
Q

Why may antimicrobials be used when treating IBD?

A
  • treats secondary complications (abscesses, fistulas)

e. g. Metronidazole

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13
Q

What antimicrobial may be used to treat complications of IBD?

A

Metronidazole

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14
Q

What are TNF Alpha Inhibitor drugs used for? (GIT)

A
  • refractory Crohn’s disease

- severe UC/Crohn’s disease

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15
Q

List 3 anti-TNF alpha therapies that may be used to treat IBD

A
  1. Infliximab
  2. Adalimumab
  3. Golimumab
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16
Q

What are the MOAs of the 3 anti-TNF alpha therapies that may be used to treat IBD

A
  1. Infliximab
    - chimeric immunoglobulin
    - binds to soluble TNF & prevents it from binding to its receptor
  2. Adalimumab
    - humanized immunoglobulin
    - binds to TNF & blocks its interaction w/ p55 and P75 TNFRs
  3. Golimumab
    - humanized anti-TNF antibody
    - lyse (all) cells involved in inflammatory process
17
Q

What are laxatives?

A
  • drugs promoting defecatin

- eliminate soft, formed stool

18
Q

List the 4 main types of laxatives

A
  1. Bulk-Forming
  2. Osmotic
  3. Contact/Stimulant
  4. Lubricants (not mentioned)
19
Q

What is the MOA of dietary fibre/bulk forming laxatives?

A
  • increases stool mass
  • insoluble + nonabsorbable carbs causes them to take up water and expand in lumen
  • e.g. bran, methycellulose, ispaghula extracts
20
Q

How long does it take for dietary fibre/bulk forming laxatives to take effect?

A

1-7 days

21
Q

Give 3 examples of dietary fibre/bulk forming laxatives

A
  • bran extracts
  • methycellulose extracts
  • ispaghula extracts
22
Q

List the adverse effects of dietary fibre/bulk forming laxatives

A
  • decreased absorption of drugs
  • intestinal impaction + obstruction [dry bulk]
  • oesophageal obstruction [dry bulk]
23
Q

What is the MOA of osmotic laxatives?

A

hold water in the lumen via osmotic properties (increased ions)
- this increases transit

24
Q

Give 4 examples of osmotic laxatives

A
  1. magenesium sulphate
  2. magnesium hydroxide
  3. sodium phosphate/biphosphate
  4. lactulose
25
Q

Which osmotic laxatives have a fast transit time of 1-3 hours?

A
  1. magenesium sulphate
  2. magnesium hydroxide
  3. sodium phosphate/biphosphate
26
Q

What is the transit time for lactulose, an osmotic laxative?

A

2-3 days

27
Q

What is an adverse effect/precaution that one should mind when administering osmotic laxatives?

A

need to take care in children + those w/ renal impairment

28
Q

What is the MOA of contact/stimulant laxatives?

A
  • direct stimulation of myenteric plexus/mucosa

- increases peristalsis/mass movements

29
Q

Contact/stimulant laxatives increase transit for how long normally?

A

increase transit over 6-8 hours

30
Q

Give 2 examples of contact/stimulant laxatives

A
  1. Senna

2. Bisacodyl

31
Q

Bisacodyl is a contact/stimulant laxative. How is it administered and what is its transit time?

A
  • suppository (usually rectally)

- increases transit over 15-30 mins

32
Q

Which laxative will most likely be administered in patients that cannot swallow or have trouble swallowing?

A

Bisacodyl - given suppository

33
Q

Give an example of a lubricant laxative

A

Docusate

34
Q

Anti-diarrheal agents are essentially…

A

constipating agents

35
Q

List the 3 types of anti-diarrheal agents/constipating agents

A
  1. Absorbent Compounds
  2. Opiates
  3. Opiate Derivatives
36
Q

How do “absorbent compound” anti-diarrheal agents/constipating agents work? Give 3 examples

A
  • absorb fluids/toxins
  • increase mass
  1. Kaolin
  2. Pectin
  3. Aluminum Hydroxide
37
Q

What is the MOA of opiates as anti-diarrheal agents? Give examples

A

MOA:

  • increase muscle tone
  • decrease propulsive movements
  • decrease sensory stimulation for defecation reflex

e.g. morphine + codeine

38
Q

Give examples of opiate derivatives that may be used as an anti-diarrheal agent

A

Diphenoxylate

Loperamide (Imodium)

39
Q

What is the benefit of using opiate derivatives as an anti-diarrheal agent over opiates?

A
  • without CNS effects

- less dependence liability

GIHEP (24 decks)

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