IBD Pharm Flashcards by Jordan Trager

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

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What is the mechanism of action for 5-ASA?

inhibits both COX and LIPOX

-inhibit arachadonic acid -> prostaglandin and leukotriene -> decreased inflammation

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What are the inidcations for 5-ASA drugs?

Active and maintenance of UC only (mild/moderate -> first line)

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What suffix is associated with 5-ASA drugs?

“-sala-“

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What is sulfasalazine?

(anything special?)

5-ASA drug (IBD -> UC only)

sulfapyridine carrier:

generates side effects
contraindicated in sulfa alergies

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What is mesalamine?

(anything special?)

5-ASA (IBD -> UC only)

single 5-ASA, no carrier
multiple routes of administration (oral, rectal enema, suppositories)

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What is olsalazine?

(anything special?)

5-ASA drug (IBD -> UC only)

-two 5-ASA

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What is balsalazide?

(anything special?)

5-ASA drug (IBD -> UC only)

inert carrier

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What side effects are associated with 5-ASA drugs?

mild CNS
mild GI

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What are contrainidications for 5-ASA drugs?

ASA allergies
sulfa allergies (sulfasalazine only)

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What is the mechanism of action for TNF-α inhibitors?

Binds TNF-α, inhibiting its pro-inflammatory effects and upregulation of surface adhesion molecules

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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

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What is adalimumab?

(indications)

TNF-α inhibitor

indicated for:

-active/maintenance of UC and CD (moderate to severe -> doesn’t respond to others)

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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

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What is golimumab?

(indications)

TNF-α inhibitor

indicated for:

active/maintenance UC only (moderate to severe)
only with inadequate response to other treatment

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What is certolizumab?

(indications)

TNF-α inhibitor

indicated for:

active/maintenance CD (moderate to severe)
only with inadequate response to other treatment

_{Certo… and Crohns both start with C}

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)