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Pharmacology Part 2 > Immunosuppressants > Flashcards

Immunosuppressants Flashcards

1
Q

Immunosuppressants

Clinical uses

A

1) organ transplant- prevent immune mediated rejection
2) autoimmune disorders
Lupus
RA
Psoriasis
MS
Chrons disease
Myasthenia gravis

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2
Q

Immunosuppressants

Adverse effects/ considerations

A

⬆️ risk of infection: persist and become severe
Bacterial infections- risk is very high during 1st month
Viral infections
Pneumocystis carinni- high risk no matter what
* vaccines- avoid live attenuated- will get disease
-dead can be given but may not work

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3
Q
  • malignancy

Risk of causing cancer

A
  • skin cancer- use SPF

Immune system is used to find/terminate abnormally behaving cells- this is lowered when taking immunosuppressants

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4
Q

Immunosuppressants

MOA

A

Used to turn down/off the immune system

-classes differ by the degree of which they effect the immune system

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5
Q 
Glucocorticoids 
Anti IL-2 agents 
-calcineurin inhibitors 
-mTOR inhibitors 
Cytotoxic agents 
Biologic agents 
-polyclonal antibodies 
-monoclonal antibodies 
-fusion proteins 
-kinase inhibitors
A

Immunosuppressants

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6
Q

Glucocorticoids

MOA

A 
Lysis and redistribution of lymphocytes 
-altered gene transcription 
-apoptosis of activated cells
-down regulation of pro inflammatory cytokines 
Decrease T cell regulation 
Inhibition of a rift cytotoxic T cells 
Decrease chemotaxis 
* regulate immune system in many ways
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7
Q

Glucocorticoids

Adverse effects

A
  • HPA axis suppression: stopping can be life threatening
  • close monitoring
  • body regulates production of steroids
  • high risk of GI bleeding: block cox 1&2, act like NSAID
  • mood changes- acute psychosis
  • infection risk- leukocytosis, non infectious high WBC, type of WBC matters
    Dyslipidemia
    HTN
    Weight gain
    Hyperglycemia
    Cataracts
    Osteopenia
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8
Q

Steroid related “immunosupression”

A

Dose of steroid that is considered immunosuppressant: >2mg or 20 mg of prednisone admin for 2+ weeks

  • wait t least one month after stopping systemic corticosteroids before administering a live vaccine
  • for other immunosuppressants wait af least 3 months before giving a live vaccine
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9
Q 
Cortisone 
Hydrocortisone 
Prednisone 
Methylprednisone
Triamniclone
Betamethasone
Dexamethasone
A

Steroids/glucocorticoids/corticosteroids

Systemic

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10
Q

Calcineurin inhibitors

MTOR inhibitors

A

Anti L2 agents

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11
Q

Calcineurin inhibitors-3

MOA

A

Prevent IL-2 production

  • used in transplant setting
  • really effective in preventing rejection of a transplant
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12
Q

Calcineurin inhibitors

AE

A 
* nephrotoxicity (cyclosporine, tacrolimus), monitoring of renal fxn is needed 
Dyslipidemia
HTN
Neurotoxicity 
Hirsituism
Gingival hyperplasia 
* high drug inx risk
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13
Q

Cyclosporine (gengraf, neoral, sandimmune, *restasis)

Tacrolimus (prograf, astagraf XL, *protopic)

Pimerolimus (* elidel)

A

Calcineurin inhibitors
Anti IL 2 agents
* restasis: not systemic, eye drops for chronic dry eye
*protopic: topical, not systemic, can have systemic AE, *liver damage
*elidel: topical, can have systemic AE
-dermatological, psoriasis

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14
Q

mTOR Inhibitors-2
Anti IL-2 agents
MOA

A

Inhibit response to IL-2

Used in transplant setting really effective at preventing rejection after transplant

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15
Q

Sirolimus (rapamine)

Everolimus (zortress, afinitor)

A

mTOR inhibitors

Anti IL-2 agents

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16
Q

mTOR inhibitors

AE

A 
Dyslipidemia
HTN
Myelosupression 
-nephrotoxicity is less vs calcineurin inhibitors 
-high drug inx risk
17
Q

Risk with all Anti IL-2 agents

A

Atherosclerosis is high in transplanted organ blood vessels , plaque is high, lipids are off
*main cause of transplant failure

18
Q

Cytotoxic agents

2 types

A

Specific

Non specific

19
Q

Specific cytotoxic agents

A

Kills only immune cells: inhibits the enzymes needed for lymphocyte production of purines and pyrimidines

  • built to look like purines and pyrimidines
  • deprives cell of p & p which are needed to make DNA and protiens
20
Q

Mycophenolate (cellcept, myfortic): enterohepatic recycling, antibiotic inx risk
Leflunomide (arava): long half life

A

Specific cytotoxic agents

21
Q

Non specific cytotoxic agents

A

Kills only rapidly dividing cels (t cells etc)

Problem with cells that are always dividing: repro, blood etc

22
Q

Azathiopurine/6-mercaptopurine

  • methotrexate: dose dependent toxicity, anti cancer dose (>100-500) RA dose (5-30/wk)
  • first choice for TX of RA

Cyclophosphamide

A

Non specific cytotoxic agents

23
Q

Cytotoxic agents

AE

A 
Myelosuppression 
N/V 
Diarrhea
Alopecia (hair loss) 
Hepatotoxicty 
GI ulcers 
Anemia 
Thrombocytopenia 
Reproductive cells
24
Q

Polyclonal antibodies
Monoclonal antibodies
Fusion protiens
Kinase inhibitors

A

Biologic agents

25
Q

Biologic agents

MOA

A

Target one or more mediators of the immune system response

26
Q

Polyclonal antibodies

Biologic agent

A

Used to treat a variety of antigens in a patient
Anti human
Short term not a chronic approach
Used right before and right after a transplant
ATG (atgam)- horse
RATG (thymoglobulin)- rabbit
Bind to a variety of lymphocyte receptors: CD 2,34,8,25,45

27
Q

Polyclonal antibodies

Biologic agent

A 
Anaphylaxis 
⬆️⬇️ BP 
⬆️HR 
Dyspnea 
Urticaria 
Rash 
Infusion relayed reactions 
-need some premedication: anti histamine, NSAID, etc 
Used right before or right after  a transplant
28
Q

Monoclonal antibodies -“mab”

A

Specific to one antigen
Much more human vs polyclonal
* the more human- less risk of infusion related teachings
-differ by how human they are
*IV or SQ products: monthly, 1x or weekly, not daily products

29
Q

Monoclonal antibodies
Biologic agent
AE

A

Low risk of infusion related rxn
Premeditate: NSAID, steroid, antihistamine
High risk of infection
Myelosupression

30
Q

Fusion protiens

Biologic agents

A 
Etanercept (enbrel)- anti-TNF 
Belatacept (nulcjix): anti CTLA4 
Abatacept (orencia):anti CTLA4
* high risk of infection 
-postransplant lymphoprolifetative disorder
31
Q

Etanercept (enbrel)
Belatacept (nulcjix)
Abatacept (orencia)

A

Fusion proteins

Biologic agents

32
Q

Kinase inhibitors

Biologic agents

A

Tofacitinib (Xeljanz)

Ruxolitinib (jakafi)

33
Q

Tofacitinib (Xeljanz)

A

Kinase inhibitor
High risk of infection- not to be used with biologics or strong immunosupressants
PO
Many drug inx

34
Q

Ruxolitinib (Jakafi)

A

Kinase inhibitor
Similiar product used to treat myelofibosis
-dosing individualized: platelet count, renal fxn etc

Pharmacology Part 2 (16 decks)

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