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Exam 4 lecture 1 Flashcards

1
Q

What is IBD? What are the two types?

A

IBD: Is an inflammatory condition with chronic or recurring immune response and inflammation of the GI tract.

Two types
1) Ulcerative colitis (UC): Mucosal inflammation (superficial) confined to rectum and colon. Smoking is protective.

2) Crohn’s disease (CD): Transmural (deeper and thicker) inflammation of GI tract that can affect any part from mouth to anus. You see fistulas. Smoking is a risk factor.

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2
Q

What signs and symptoms are consistent with IBD

A

Frequent bowel movements.
Include blood and mucous.
FInd out if they smoke? Gluten allergy?
Nsaids cause IBD aswell.

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3
Q

What is an imprtant goal of therapy for IBD

A

Inducing and maintaining remission , Mucosal healing associated with better long term outcomes.

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4
Q

Nutrition support for IBD

A

No specific diet shown to be beneficial
Nutritional support to address nutritional deficiencies, impaire absorption (supplement vitamin/mineral deficiencies like calcium/vit D, folate), EN/PN

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5
Q

Pharmacologic therapy for IBD

A

None of them are curative. They get patients into remission.

  1. ASAs (aminosalicylates)
    - SUlfasazine, Mesalamine (5-ASA)
  2. Corticosteroids
  3. Immunomodulators (immunosuppressives)
    - Azathropine, mercaptopurine, cyclosporine, methotrexate
  4. Biologics
    - anti TNF agents (infliximab, adalimumab, certolizumab, golimumab)
    - Other- Natalizumab, vedolizumab, ustekinumab, risankizumab
  5. Tofactinib, upadactinib, ozanimod, estrasimod
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6
Q

Name ASA agents

A

Sulfasazine, Meslamine

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7
Q

What is sulfasazine made of? WHat happens to it in the body? What is associated with ADRs? WHat is the inactive component? active component?

A

Made up of sulfapyridine + 5- ASA (mesalamine)

cleaved by colonic bacteria to release sulfapyridine (absorbed and renally excreted) and 5- ASA (mainly remains in lumen, excreted in stool)

Sulfapyridine is inactive, but is associated with ADRs

5-ASA is active component

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8
Q

Can we administer mesalamine alone ( to prevent ADRs?) Explain

A

Yes we can. It is rapidly and completely absorbed in small intestine, but not colon. It is important to deliver to affected area.

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8
Q

How can we get Mesalamine to colon (past small instestine)

A

Suppository (for patients with Proctitis
Enema (for patients with left sided disease)

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9
Q

Is topical or oral mesalamine more effective? Can we use both together?

A

Topical is more effective

We can give both

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10
Q

ASA agents ADRs? how to avoid?

A

Sulfasalazine-> Sulfapyridine is associated with ADRs

  • > 10% nausea, vomiting, headache, anorexia, rash

-Initiate with low dose and titrate up slowly
-<10% anemia, hepatotoxicity, thrombocytopenia

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11
Q

What in sulfasalazine causes ADRs? What to monitor? Drug interactions of sulfasalazines

A

May be associated with hypersensitivity rxns in sulfonamide allergy

MOnitor CBC and LFTs at baseline, every other week for first 3 months, monthly for second three months and perioically there after

Monitor BUN/Scr periodically

Drug i/a with antiplatelets/anticoags/NSAIDs-> increase bleeding risks

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12
Q

If sulfasalazine is not tolerated, what drug is used? Side effects?

A

Mesalamine (much better tolerated)

N/V, headaches
olsalazine has diarrhea (up to 25%)

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13
Q

Drug i/a of mesalamine

A

Antiplatelets/anticoags/NSAIDs may increase bleeding risk

Agents affecting gastric PH (PPIs, H2RAs, antacids) could influence release of drug in PH dependent dosage forms

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14
Q

MOA of coticosteroids? ROA? use?

A

Antiinflammatory (systemic or local)

Can be used parenterally (severe exacerbation, orally or rectally)

systemic corticosteroids may be used for induction of remission, but not for maintenance

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15
Q

tOPICAL FORMULATIONS FOR IBD

A

RECTAL HYDROCORTISONE (Suppositories, foam, enema)

Budesonide (can be inhaled), systemic absorption is lower than other steroids, can be used for 16 weeks

Prednisone/prednisolone

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16
Q

What are the two types of budesonide

A

Entocort- Pill
Uceris- foam

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17
Q

Budesonide drug i/a

A

CYP3A4 inhibitors (ketoconazole, grapefruit juice), may increase systemic exposure

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18
Q

What are IV steroids used in IBD

A

Methylprednisolone\Hydrocortisone

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19
Q

ADRs for corticosteroids

A

Short term- hyperglycemia, gastritis, mood changes, elevated BP

Long term- aseptic necrosis, cataracts, obesity, growth failure, HPA suppression, Osteoporosis

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20
Q

What supplemets should be given for patients on systemic corticosteroids

A

Give calcium and vitamin D while on steroids

May give bisphosphonates for patients with high risk for osteoporosis, patients using for more than 3 months or recurrent users

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21
Q

Monitoring for corticosteroids

A

BP, blood glucose baseline and every 3-6 months
Consider occasional bone mineral density scan (DEXA) in pts > 60 years old, at risk for osteoporosis, patients using for more than 3 months or recurrent users

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22
Q

What are immunosuppresants used in IBD

A

Thiopurines
1) Azathropine (AZA)
2) Mercaptopurine (MP, 6-MP)

AZA is a prodrug rapidly converted to 6-MP

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23
Q

What are the uses AZA and MP? WHo can use them? MOA? Can they be used in other drugs?

A

can be used n long term tx of UC and CD

Reserved for pts who fail tx with ASA or refractory to steroids.

Can maintain remission, but are not used in induction

They can be use din conjunction with ASA, steroids, TNF

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24
ADRs of AZA and 6-MP? Monitoring?
Hematologic effects :(life threatening anemia) due to bone marrow suppression GI: N/V/D, anorexia Hepatic: Hepatotoxicity Monitoring Baseline- TOMT, CBC, LFTs CBC- weekly for 1st months and every 1-2 weeks after dose change.
25
Use of cyclosporine in IBD? Can be used long term? WHo is itreserved for?
Can be effective in inducing remission in patients with refractory UC (not recommended for CD) NOt used long term Generally reserved for pts who are refractory to steroids
26
ADRs of cyclosporine? Monitoring?
nephrotoxicity (dose related) Neurotoxicity Metabolic (HTN, HLD, hyperglycemia) other: GI upset, hirsutism, gingival hyperplasia Monitoring Baseline BP, BUN/SCr, LFTs, Cya tr. concentration BP- q visit BUN/SCr- q 2 weeks until stable, then periodically LFTs- q 2 weeks until stable, then periodically
27
cyclosporine drug i/a? drugs/food that iincreases cyclosporine concentrations? Drugs that decrease cyclosporine concentrations
substrate CYP3A and p- glycoprotein Increase cyclosporone concentration - azole antifungal, macrolide antibiotics, calcium channel blockers, grapefruit decrease cyclosporine phenytoin, rifampin
28
Methotrexate use?
Can be used in tx and maintenance of CD (not UC) May have steroid sparring effects, assist in inducing remission, allow steroid tapering
29
Methotrexate ADRs
Hematologic (bone marrow suppression) (thats why we add folic acid 1 mg/day) GI: N/V/D, mucositis Hepatic: Cirrhosis, hepatitis, fibrosis Pulmonary: Pneumonitis derm: rash, urticaria, alopecia teratogenic drug (contraception)
30
CI of methotrexate? Monitoring
CI Pregnancy pleural effusions chronic liver/EtH abuse Immunodeficiency preexisting blood dyscrasias CrCl<40 leukopenia/thrombocytopenia Monitoring Baseline: Chest x ray, CBC, SCr, LFTs, pregnancy, check CBC, Scr and LFTs q 4-8 weeks
31
What are some biologic TNF-a antagonist drugs
infliximab adalimumab golimumab certolizumab
32
Which TNF-a antagonists treat CD? UC? both? are they anti TNF-a? human monoclonal or human pegylated (only know UC OR CD FOR EXAM)
infliximab (remicade) - Anti- TNF-a antibody for CD AND UC adalimumab (humira)- anti TNF-a antibody for CD AND UC golimumab- human monoclonal anti- TNF only used for UC Certolizumab pegol- human pegylated anti TNF-a Fab fragemnt. Only used in CD
33
What are anti integrin bilogics used in CD and UC? Which drug is used inwhich?
Natalizimab- CD Vedolizumab (UC and CD
34
What are some IL biologics that target CD and UC? Which ones can we use them for?
Ustekinumab- CD and UC Risankizumab (skyrizi)- CD and UC mirikizumab-mrkz- UC
35
WHat are some small molecule biologics used in IBD? Which one do they treat?
Tofactinib- UC upadacitinib- UC, UD Ozanimod- UC estrasimod- UC
36
TNF-a inhibitors ADRs
1. increased risk of infection (bacterial, viral, fungal) - avoid if active infection - tuberculin test (PPD), CXR, hepatitis prior to therapy - ensure vaccinations up to date -live vaccines contraindicated during tx and for 3 months after 2. Injection site rxn and infusion related rxns 3. Risk of malignancy (lymphoma) - hepatosplenic T cell lymphoma 4. Risk of demyelinating disease Contraindocated in pts with history of cancer, demyelinating CNS disease, optic neuritis 5. May exacerbate CHF 6. hepatotoxicity
37
Monitoring TNF inhibitors
Baseline chest x ray, PPD, s/s infection Maintenance (every 8-12 wks) s/s of infection, UA, CBC, Scr, LFTs (for LFTs q 1-2 wks for first 1-2 months)
38
what is infliximab approved for? ROA? Induction/maintenance use?
mod-severe CD and UD. used as induction and maintenance therapy IV infusion
39
What is a common thing to worry about with all biologics
development of antibodies (they are foreign proteins that may cause immune response) It this immune response occur the drug becomes less efficacious These are called ADA (anti drug antibodies) or ATIs (anti treatment antibodies)
40
What does development of ADAs (antidrug antibodies) lead to? How common is it in infliximab? How to counteract?
ADAs lead to decreased response and potentially increased chance of infection. Up to 10% of pts/year need to discontinue infliximab Combining with immunosuppressives (AZA or MTX) may be of value, but will increase risk of ADRs Can escalate dose or decrease dosing interval
41
What happens if Infliximab is co administered with azathioprine?
Hepatosplenic t cell lymphoma (HSTCL) risk Infliximab could also cause infusion related rxns
42
monitoring of infliximab
Maintenance s/s of infection vitals (each dose) Infusion rxn (each dose) TDM (consider if tx failure)
43
What is adalimumab used for? Induction/maintenance? biggest difference with infliximab?
Mod- severe active CD and UC, steroid dependent can use for pts with poor response to infliximab induction and maintenance therapy Biggest d/c is that it is an SQ injection not an infusion (self injection technique is needed)
44
What is more likely to give you ADAs infliximab or adalimumab
adalimumab is less likely than infliximab
45
What is golimumab approved for? Induction/maintenance? ROA? Are ADAs likley compared to infliximab
Mod-severe UC induction and mainetnance SQ inj (self injection) ADAs possible, but less likely than infliximab
46
What is certolizumab pegol used for? ROA? Induction/maintenance?, ADAs?
Used for CD SQ injection (self administration) Induction and maintenance develops ADAs
47
What type of drug is natalizumab? What IBD is it used in? Induction/maintenance? Which patients use it? Which patients can not use it? When to discontinue?
Natalizumab is an anti integrin (prevents leukocyte adhesion/migration) Used in CD induction and maintenance Can use in pts who fail/do not tolerate TNF inhibitors Not to be used in combination with immunisuppressants or TNF inhibitors discontinue in patients with no benefits by 12 weeks and/or steroid dependent within 6 months
48
Why is natalizumab not commonly used
Associated with progressive multifocal leukoencephalopathy (PML) (rare CNS disorder related to JC virus) Test for JC antibody. Even if JC virus negative, it is not impossible to get PML
49
What is vedolizumab used for? ADRs?
UC and CD No PML risk (but still monitor for it) Can see infection, HS rxn, ADAs
50
What are IL antagonist drugs
Ustekinumab
51
What is ustekinumab used for? What kind of IL antagonist is it? Induction/maintenance?
CD and UC IL 12 and 23 antagonist induction and maintenance
52
ADRs of ustekinumab
ADAs HS rxn Possible neurotoxicity (RPLS, PRES) reports of rapidly developing cutaneous cell carcinomas
53
Monitoring Ustekinumab baseline
Baseline Check pt for TB/ hepatitis CXR (chest x ray), PPD, Hep B and C Lipids, LFTs, renal function, infection, skin
54
Monitoring Usketinumab maintenance
Lipids and LFTs- 1-2 months after start and then periodically renal function- periodically infection- monitor for s/s skin- annually
55
What kind of drug is Skyrizi? What is it used for? Induction/maintenance?
Selective IL 23 antagonist CD and UC USed for induction and maintenance
56
Adverse effects of skirizi
common- Headache, nasopharyngitis, arthralgia, abdominal pain, anemia, nausea infection/latent infection (TB) HS rxn possible ADAs possible Potential hepatotoxicity (increases LFTs) increase in lipids
57
Monitoring skyrizi
Monitor LFTs and bilirubin at baseline and by week 12
58
What kind of drug is mirikizumab? What does it treat? Induction/maintenance?
IL 23 p 19 antagonist Only used in UC induction and maintenance (infusion and then maintenance SQ)
59
ADRs of mirikizumab
COmmon- headache, arthralgia, rash, inj site rxn Infection/latent infections (TB) Upper repsiratory tract infection HS rxn ADAs Potential hepatotoxicity (increase LFTs) (monitor)
60
Monitoring Mirikizumab
Similar to other IL inhibitors Baseline CXR, PPD HEP B, C Lipids and LFTs (1-2 months after start) renal func infection (monitor for s/s)
61
WHat is TDM? Use?
Therapeutic drug monitoring Potential for determining concentrations of drugs and ADAs
62
Why consider TDMs?
Consider if loss of treatment response (check ADA concurrently) always do both together
63
For TDM of biologics, what are 3 things we do at IBD treatment fauilure
Confirm inflammation (biomarkers) Exclude infection and non compliance to treatment Send for serum drug TLs and ADA levels
64
What TDM to do if detectable ADAs at subtherapeutic drug levels
This could be caused by "immune mediated PK failure "(insufficient bioavailability of drug as a result of induced immunogenicity resulting n increased drug clearence Change to alternate drug within the same class
65
What TDM to do for subtherapeutic drug levels with undetectable ADAs
Could be caused by non-immune mediated PK failure (insufficient availability of drug) Escalate dose
66
What to do for therapeutic drug levels with detectable ADAs? What could it be caused by?
False positive OR mechanistic failure repeat TDM levels If repeat results consistent, switch to out of class biologic agent
67
What to do for therapeutic drug levels with undetectable ADAs? What could it be caused by?
Could be caused by mechanistic failure (not effective drug), switch to out of class biol0gic
68
What type of drug is tofactinib? What is it approved for? Who can use it? ROA? WHen to discontinue
It is an oral janus kinase (JAK) inhibitor Approved for UC only Used for patients who have had an inadequate response or who are intolerant to TNF blocker Orl drug Dx after 16 weeks if repsponse is not adeqyate
69
Tofactinib should not be used in conjunction with
Immunosuppressants (AZA, CYA) or biologics
70
ADRs of tofactinib
COmmon- Diarrhea, elevated cholesterol, headache, herpes (shingles), rash, nasopharyngitis, URI, rare- malignancy (lymphoma), serious infection (TB and Hep B and C) (activation of latent TB), neutropenia, HS rxn Live vaccines CI during tx and 3 months after
71
blackbox warning of tofactinib
Increase mortality in RA patients 50 years and older with atleast one cV risk factor increase in thrombosis in same population
72
Monitoring tofactinib
baseline- CXR, PPD, HEP B, C maintenance ANC (q 3 months) , CBC (q 1-2 months then q 3 months), lipids (1-2 months after start, then periodically), LFTs (1-2 months after start) , renal fun, infection, skin exam
73
What type of drug is upadacitinib? WHat is it approved for?
oral selective JAK inhibitor (like tofactinib) UC and CD (different dosing)
74
What should upadactinib not be used in combo with? Who is it an option for?
Immunosuppressants or biologics option for pts who fail biologics
75
upadactinib Blackbox? WHne to avoid? COntraindications?
Blackbox similar to tofactinib (Increase mortality in RA patients 50 years and older with atleast one cV risk factor increase in thrombosis in same population) ADRs increase of risk of serious infection (bacterial, viral, fungal) Avoid if active infection present, pregnant or breast feeding Live vaccines contraindicated immediately prior to and during therapy (ensue=re vaccines are up to date)
76
common ADRs of upadactinib
Common upper respiratory tract infection, acne, increased creatine phosphokinase, elevated cholesterol, headache, herpes, shingles rare- malignancy (lymphoma), serioud infection, increase in LFTs, anemia, neutropenia
77
Monitoring for ipadactinib
Same as tofacitinib
78
What type of drug is ozanimod? MOA? UC or CD? How is it dosed? WHne not to use it? WHat to do if patient misses dose in first 2 weeks
S1P receptor modulators Prevents lymphocyte mobilization to inflammatory sites Only for UC 7 day dose titration, if missed dose within 2 weeks, we reinitiate the whole thing should not be used with non corticosteroid immunosuppressants or immunomodulators
79
CI of ozanimod
CVevents within last 6 months (TIA, MI< unstabe angina) sleep apnea MAO inhibitor
80
ADRs of ozanimod
increased risk of infection (PML), vaccinate with varicella prior to txm live vaccines CI bradycardia/AV conduction delays liver injuries (LFTs)
81
Drug interaction of ozanimod (exam)
Inhibition of MAO (exam) BB and CCB adrenergic and serotonergic drugs
82
Monitoring with ozanimod
CXR, PPD HEP B, C CBC LFTs Infection BP Spirometry ECG optho
83
What kind of drug is estrasimod? UC or CD? When not to be used?
Oral S1P receptor modulator Approved for UC only not used with non corticosteroid immunosuppressives or immune modulating drugs
84
CI of estrasimod
CV event in last 6 months
85
ADRs of estrasimod
Potential risk of infection (potential for PML), recommended to vaccinate against varicella prior to tx, live vaccines CI Bradycardia/AV conduction delays
86
ADRs of estrasimod
Liver injuries Moderate increase in BP edema RPLS/PRES respiratory effects
87
monitoring of estrasimod
Same as ozanimod

Therapeutics (38 decks)

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