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GI Exam 3 > IBD Treatment > Flashcards

IBD Treatment Flashcards

1
Q

Most important drug for the continuous treatment of IBD

A

5-ASA (mesalamine)

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2
Q

Sulfasalazine =

A

Sulfapyrazine + 5-ASA (active part

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3
Q

Mesalamine MOA

A
  • Alters eicosanoid metabolism via inhibition of 5-lipoxygenase and suppression of leukotriene formation (anti-inflammatory)
  • Immunomodulatory: suppresses chemotaxis of neutrophils and macrophages and inhibits release of cytokines
  • Scavenger of free radicals
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4
Q

Mesalamine Dosing

A

High doses (3 grams QD)
Unmodified 5-ASA is ineffective and only 25% is absorbed in the colon
Can be given by enema if disease is limited to rectum and right colon

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5
Q

Enema Pros and Cons

A

Reduces systemic load
Difficult to hold the enema in place for long enough time for efficacy
Don’t go beyond the splenic flexure

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6
Q

Pentasa General

A

Pure 5-ASA but coated with a membrane which dissovles in the stomach and duodenum
60% is released in the upper small intestine and the rest in the colon

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7
Q

Asacol and Claversal General

A

Mesalamine coated with Eudragit-S or L which dissolves at a pH greater than 6-7 so most of the drug is released in the small intestine and colon

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8
Q

5-ASA PK and ADR

A

Unclear which metabolite and body compartment

Headache, skin rash and GI complications (watery diarrhea, exacerbation of colitis)

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9
Q

Sulfasalazine (Azulfidine)

A 
Sulfonamide + 5-ASA
GI Symptoms
Hematological symptoms (neutropenia) 
Skin rxns
Impaired folic acid absorption and male infertility
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10
Q

White people have more

A

NAT2 vs N-acetyltransferase-1

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11
Q

Steroids + IBD

A

Anti-inflammatory (suppress symptoms)
Lots of side effects (immunosuppresion, osteoporosis, etc)
Local applications are preferred for colitis

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12
Q

Steroids used in IBD

A

Prednisone or Prednisolone or Hydrocortisone

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13
Q

Budesonide (Entocort) + IBD

A

Topical GLUCOCORTICOID

Less systemic side effects

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14
Q

Metronidazole + IBD

A

Effective in killing anaerobic

Long-term = peripheral neuropathy

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15
Q

Ciprofloxacin + IBD

A

Best alternative to metronidazole if not tolerated

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16
Q

Azathioprine + CD

A

Cytostatic agent
Pro-drug of 6-mercaptopurine
Suppresses DNA replication and proliferation of lymphocytes
- Not acute due to taking several months to start working
SUPPRESS BONE MARROW
Mutagenic and TERATOGENIC

17
Q

Monitoring with Azathioprine

A

Thiopurine methyl-transferase (TPMT deficiency increase the risk of toxicity

18
Q

Methotrexate + CD

A

Alternative to Azathioprine

19
Q

Tacrolimus + UC

A

Suppress IL-2

20
Q

Cytostatic or Immunosuppressant drugs

A 
Risk of infection!!!
Azathioprine
Methotrexate
Tacrolimus
Cyclosporine
21
Q

Cyclosporine MOA

A

Blocks calcineurin from getting activated
- Ca + Calmodulin → activates calcineurin → dephosphorylate NFAT (activated T cells) → NFAT is activated and goes to the nucleus and it causes IL-2 transcription

22
Q

Supportive therapies for IBD

A

Antidiarrheal agents and Nutrition

23
Q

Antidiarrheal Use

A 
CAUSE toxic megacolon
Loperamide
Diphenoxylate/atropine
Anticholinergic
Cholestyramine
24
Q

Nutrition Therapies for IBD

A

Iron, folate, B12
Corrects consequences (malabsorption, etc)
TPN for severe pts

25
Q

TNF Targeted therapies in IBD

A

Treatment-resistant cases

i.e. infliximab, adalimumab (humira), etancercept

26
Q

Infliximab (Remicade)

A

Bind TNF-alpha
Moderate to sever CD
IV drug
More likely to suffer from infections like TB

27
Q

Etanercept (Enbrel)

A

Human TNF receptor with antibody portion
Works as a decoy and bind circulating TNF alpha for 5 days!
AE: Infection

28
Q

Natalizumab (Antegren)

A

Antibody against integrin alpha 4 (allows leukocyte infiltration into the intestine normally) - reduces the attachment of inflammatory immune cells
Recalled due to risk of progressive multifocal leukoencephalopathy but benefits outweigh risk so it was put back out

29
Q

TNF alpha as a drug target

A

TNF can induce apoptosis or inflammatory process so if you can prevent the formation of TNF alpha that better than just blocking it

30
Q

5-ASA True Statements

A

Inhibits leukotriene production
Sulfosalazine is a prodrug of 5-ASA
Olsalazine is activated by diazo reduction carried out by colonic bacteria

31
Q

Characteristics of Infliximab (remicade)?

A

TNF alpha antibody
Inhibits TNF alpha activity
Must be given IV
Makes the patient more susceptible to bacterial infections

GI Exam 3 (9 decks)

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