IBD Pharm Flashcards
What are the main classes of drugs used to threat IBD?
- 5-ASA (aminosalicylates)
- TNF-α inhibitors
- α-4 integrin inhibitors
- IL-12/23 inhibitors
- JAK inhibitors
- steroids/immune modulators and abx as well
What is the mechanism of action for 5-ASA?
inhibits both COX and LIPOX
-inhibit arachadonic acid -> prostaglandin and leukotriene -> decreased inflammation
What are the inidcations for 5-ASA drugs?
Active and maintenance of UC only (mild/moderate -> first line)
What suffix is associated with 5-ASA drugs?
“-sala-“
What is sulfasalazine?
(anything special?)
5-ASA drug (IBD -> UC only)
sulfapyridine carrier:
- generates side effects
- contraindicated in sulfa alergies
What is mesalamine?
(anything special?)
5-ASA (IBD -> UC only)
- single 5-ASA, no carrier
- multiple routes of administration (oral, rectal enema, suppositories)
What is olsalazine?
(anything special?)
5-ASA drug (IBD -> UC only)
-two 5-ASA
What is balsalazide?
(anything special?)
5-ASA drug (IBD -> UC only)
inert carrier
What side effects are associated with 5-ASA drugs?
- mild CNS
- mild GI
What are contrainidications for 5-ASA drugs?
- ASA allergies
- sulfa allergies (sulfasalazine only)
What is the mechanism of action for TNF-α inhibitors?
Binds TNF-α, inhibiting its pro-inflammatory effects and upregulation of surface adhesion molecules
What is the general indications for TNF-α inhibitors?
moderate to severe UC and/or CD (which one varies per drug)
used after inadequate response to other drugs
What is adalimumab?
(indications)
TNF-α inhibitor
indicated for:
-active/maintenance of UC and CD (moderate to severe -> doesn’t respond to others)
What is infliximab?
(indications)
TNF-α inhibitor
indicated for:
- active/maintenance CD (moderate to severe)
- active/maintenance UC (severe only)
- only with inadequate response to other treatment
What is golimumab?
(indications)
TNF-α inhibitor
indicated for:
- active/maintenance UC only (moderate to severe)
- only with inadequate response to other treatment
What is certolizumab?
(indications)
TNF-α inhibitor
indicated for:
- active/maintenance CD (moderate to severe)
- only with inadequate response to other treatment
<strong>C</strong>erto… and <strong>C</strong>rohns both start with <strong>C</strong>
What are side effects of TNF-α inhibitors?
- TB reactivation
- elevated LFTs
- EM/TEN/SJS (rare)
What is the mechanism of α-4 integrin inhibitors?
-bind and block α-4 integrins, inhibiting leukocytes migration
What is natalizumab?
(inidcations)
α-4 integrin inhibitor
- active/maintenance for CD only (moderate-to-severe)
- inadequate response to other treatements
What is vedolizumab?
(indications)
α-4 integrin inhibitor
- active/maintenance for CD and UC (moderate-to-severe)
- inadequate response to other treatements
make the letter ‘V’ with your finger, you are holding up the number two and this treats both UC/CD
What black box warning is associated with α-4 integrin inhibitors?
PML (progressive multifocal leukoencephalopathy) from JCV virus reactivation
-specific monitoring and education is required to prescirbe/take (TOUCH program)
What side effects are associated with α-4 integrin inhibitors?
- infusion reactions
- anti-medication Ab formation
- increased risk for malignancy (rare)
What is the mechanism of action for IL-12/23 inhibitors?
bind p-40 subunit that is common to IL-12 and IL-23 receptors, inhibiting their function
- inhibits Th17 and NK differentiation
- inhibits proinflammatory cytokine release
What is ustekinumab?
(indications)
IL-12/23 inhibitor
- active/maintenance of CD and UC (moderate-to-severe)
- only with inadequate response to other treatment
What are the side effects of IL-12/23 inhibitors?
- TB reactivation
- injection site reaction
- increased risk of malignancy (rare)
What is the mechanism of action for JAK inhibitors?
bind and inhibit intracellular JAKs (1 and 3) which are involved in cytokine signaling
-strong effect on JAK 3 which is involved in IL-4 signaling, particularly inhibiting Th2 differentiation (-> UC only)
What is tofacitinib?
(indications)
JAK inhibitor
- active and maintenance of UC only (moderate-to-severe)
- only with inadequate response to other treatment
What are side effects of JAK inhibitors?
- lymphopenia/lymphocytosis
- neutropenia/anemia
- increased LDL and HDL
- increased risk of malignancy (rare)
What drugs should be avoided while taking biologics?
other biologic medications
What is the order that drugs should be used with progressively treatment resistant IBD?
First line:
- 5-ASA (UC only)
- abx
- steroids/immune modulators
Second line:
-TNF-α inhibtors
Third line:
- JAK inhibitors (UC only)
- IL-12/23 inhibitors (both)
- α-4 integrin inhibitors (both)
