Agents for Inflammatory Bowel Disease (IBD) Flashcards
what are the 5 family classes of agents used for ulcerative colitis?
5-ASA, Janus Kinase (JAK) Inhibitors, IL-12/23 Inhibitors, TNF-alpha inhibitors, and alpha-4 integrin inhibitors
what are the four drugs in the 5-ASA drug class?
Sulfasalazine, Mesalamine, Olsalazine, and Balsalazide
what is the drug in the Janus Kinase (JAK) Inhibitors class?
Tofacitinib
what is the drug in the IL-12/23 Inhibitors class for Ulcerative Colitis?
Ustekinumab
what are the 3 drugs in the TNF-alpha inhibitors class for ulcerative colitis?
Adalimumab, Golimumab, and Infliximab
what is the drug in the alpha-4 integrin inhibitor class for ulcerative colitis?
Vedolizumab
what are the 3 family classes of drugs used for crohn disease?
IL-12/23 inhibitors, TNF-alpha inhibitors, and alpha-4 integrin inhibitors
what is the IL-12/23 inhibitor used for crohn disease?
Ustekinumab
what are the 3 TNF-alpha inhibitors used for Crohn Disease?
Adalimumab, Certolizumab, and Infliximab
what are the 2 alpha-4 integrin inhibitors used for crohn disease?
Natalizumab and Vedolizumab
what is the MOA of the 5-ASA agents?
inhibition of PG (prostaglandin) and LT (leukotriene) production via arachidonic acid pathway–> COX and LIPOX; reduction in PMN and macrophage chemotaxis
what are the different routes of administration of 5-ASA?
oral, rectal enemas, and rectal suppositories
where do the oral 5-ASA agents reach?
varies by agent; may be released in the distal/terminal ileum, colon, or throughout the GI tract
where do the rectal enemas 5-ASA agents reach?
may reach the splenic flexure; do not frequently concentrate in the rectum
where do the rectal suppositories 5-ASA agents reach?
reach the upper rectum (15-20 cm beyond the anal verge)
what are the common side effects associated with the 5-ASA agents?
primarily GI related and some CNS related; there are fewer systemic side effects with pure 5-ASA products and topical formulations
what are the absolute contraindications of all 5-ASA compounds?
in ASA-allergic patients
when is sulfasalazine contraindicated?
in sulfonamide-allergic patients
when is the use of 5-ASA agents indicated?
with cases of mild to moderate UC (except olsalazine and Balsalazide)
when should Olsalazine be used?
only for maintenance of remission of UC
when should Balsalazide be used?
only for active disease of UC
what is the role of TNF-alpha?
binding to the TNF receptors and mediating upregulation of surface adhesion molecules (VCAM-1, E-selectin, MAdCAM-1 for leukocyte adhesion)
what is the mechanism of action of TNF-alpha inhibitors?
binds to and neutralizes membrane-associated and soluble human TNF-alpha-mediated pro-inflammatory cell signaling, ultimately blocking leukocyte migration to site of inflammation
what is the TNF-alpha inhibitor that is IV injection only?
Infliximab
what are the side effects of TNF-alpha inhibitors?
infections (TB testing pre-therapy needed); liver toxicity (increased AST/ALT enzymes)
what are the rare but severe side effects associated with TNF-alpha inhibitors?
dermatologic-related (EM,SJS, TEN) and malignancies (various)
