GI

Question 1

What is usually used as “salvage” therapy?

Answer 1

Prednisone - trying to keep people off more intense steroids. Also used for acute flaires

Question 2

Budesonide/Entocort EC (Glucocorticoid): what receptor is it highly receptive for?

Answer 2

Mineralcorticoid receptor (immunosuprresant effects of steroids)

Question 3

True or False: Budesonide/Entocort EC (Glucocorticoid) is extensively metabolized during first pass

Answer 3

True. 90%.
This is good, because we want it to act locally/as a topical agent - so it’s an advantage (where its not for a lot of other drugs). This also means it has low systemic availability.

Question 4

Mesalamine (an Aminosalicylate) MOA

Answer 4

Modulates local chemical mediators of the inflammatory response (anti-inflammatory), particularly leukotrienes, and acts as a free radical scavenger or an inhibitor of tumor necrosis factor (TNF)

Question 5

Mesalamine: where is it working?

Answer 5

Want it to act topically: enteric coated, delayed release, etc.

Question 6

Sulfasalazine (Aminosalicylate): when does it start to work?

Answer 6

Prodrug of Mesalamine. The Azo (N=N) bond is cleaved by colonic bacteria. That’s when it starts to work.

Question 7

Sulfasalazine (Aminosalicylate): what vitamin deficiency is associated?

Answer 7

Folate: if someone is supplementing, have them take it at a different time of day.

(*Sulfasalazine inhibits the absorption of dietary folate (e.g. pteroylmonoglutamates) via inhibition of intestinal transport and inhibits various folate-dependent enzymes. Pts should supplement folic acid (1 mg/day) during treatment and take the medication between meals (to limit absorption competition).

Question 8

Azathioprine MOA

Answer 8

Inhibits purine synthesis and DNA replication, resulting in an anti-proliferative effect & induction of apoptosis of T-cells (IMMUNOSUPPRESSION)

Question 9

Side fx of Azathioprine

Answer 9

Leukopenia, thrombocytopenia, hepatotoxicity, infection, malignancy, malaise, n/v (not in our notes)

Question 10

MOA of monoclonal Abs?

Answer 10

Make things more visible to immune system: its like tagging things for destruction

Question 11

Corticosteroid/Prednisone MOA

Answer 11

Modulates protein synthesis –> reduced migration of polymorphonuclear leukocytes & fibroblasts. Reverses capillary permeability and lysosomal stabilization at the cellular level to prevent or control inflammation. Immunosuppression.

Question 12

Corticosteroid/Prednisone Duration

Answer 12

12-18 hours

Question 13

Corticosteroid/Prednisone Onset

Answer 13

Days - Weeks

Question 14

When are corticosteroids used?

Answer 14

Acute flare or salvage therapy

Question 15

When are corticosteroids used?

Answer 15

Acute flare or salvage therapy

Question 16

Major interactions for Budesonide/Entocort EC (Glucocorticoid)

Answer 16

Grapefruit (CYP3A4 inhibitor) and St. John’s wort (CYP3A4 inducer)

Question 17

Mesalamine onset

Answer 17

3-4 weeks

Question 18

What causes urine, tears, and sweat to develop a yellow/orange tinge?

Answer 18

Sulfasalazine