Drugs For Inflammatory Bowel Disease

Question 1

Pathogenesis of IBD

Answer 1

More pathogenic vs beneficial microbes Is present. Also inappropriate immune responses are present as well.

TH1/TH17 pathways predominant in CD
- TNFa is the most present cytokine

TH2/TH17 pathways predominant in UC
- IL-4 is the most present cytokine

Question 2

Goals of IBD therapy

Answer 2

Induction of clincial remission and maintain remission

Avoid surgery unless needed

Treatment choices = depends on disease severity

Question 3

What are special formulations of 5-aminosalycilates that can be used for IBD?

Answer 3

Depositories

Enemas

PH dependent release capsules

Delayed released capsules

these are used since the bioavailability is 20% off normal oral doses

Question 4

Azo compounds of 5-ASA

Answer 4

Decrease absorption of the drug within the small intestine

However, normal terminal ileum and colon flora have high levels of azoreductase enzymes which cleave the 5-ASA off this drug and activate function
- is more active in colon regions of the bowel

Sulfasalazine = 5-ASA + sulfapyridine

Olsalazine = 2 5-ASA bound together

Balsalazide = 5-ASA bound to 4-aminobenzoyl-B-alanine

Question 5

What is the purpose of using corticoids with high glucocorticoid potency vs mineralcorticoid potency?

Answer 5

Glucocorticoid = actual anti inflammatory actions

Mineralcorticoid = salt/water imbalances

• *goal is to have high glucocorticoid potency vs mineralcorticoid potency**
• this is why hydrocortisone can be used for treatment of IBD, but is almost never really used

Question 6

What enzyme breaks down 6-mercaptopurine into its active form (6-methyl-mercaptopurine)

Answer 6

TPMT