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Spring 2018 Pharm Exam 3 > Lecture 2 Part 1: Immunosuppressants for Organ Transplants > Flashcards

Lecture 2 Part 1: Immunosuppressants for Organ Transplants Flashcards

1
Q

Immunosuppressants for Organ Transplantation:

  • 3 classes of drugs for maintenance therapy
A

Immunosuppressants for Organ Transplantation:

  1. GCCs
  2. Cytotoxic Anti-metabolites
  3. Calcineurin & mTOR inhibitors
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2
Q

1 GCCs:

  1. what 2 major types of proinflammatory mediators do they inhibit
  2. what other pathway do they inhibit?
  3. what other two cellds do they inhibit that are involved in immunity
A

1 GCCs:

  1. inhibit proinflammatory mediators –> TNF-a’s and IL’s
    (IL-2!!)
  2. inhibit AA pathway
  3. inhibit B + T cells (immunity)
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3
Q

1 GCCs & AA pathway

  1. what is the result of them inhibiting mobilization of AA (2 steps)
  2. what is the result of them inhibiting COX-2?

what is the overall result of both of these 2 things (what types of cells involved)

A

1 GCCs & AA pathway

  1. inhibit mobilization of AA –> incr in liprotein –> blocks PLA2
  2. inhibit COX-2 –> decr PG production

both play role in inflam –> blocking these –> decr inflam

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4
Q

What is the major drug in the GCC drug class used for immunosuppression of organ transplantation

A

Cortisol

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5
Q

1 GCCs

What is the major toxicity a/w this class when combined w/calcineurin inhibitors

A

1 GCCs

GCCs (Cortisol) + Calcineurin inhbitor –> Hyperglycemia (Diabetogenic)

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6
Q
  1. Growth suppression
  2. Osteopenia
  3. Risk of inf
  4. Cataracts
  5. Inhibit wound healing
  6. HTN

what drug class/drug causes these AEs?

A

GCCs (Cortisol)

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7
Q

What is the major use of GCCs

A

prevent tissue rejection (allograft rejection)

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8
Q

1 GCCs use:

blocks 1st dose of cytokine storm when using what drug in which type of patients?

A

Muromonab-CD3 in transplant recipients

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9
Q

1 GCCs use:

blocks 1st dose of cytokine storm when using what drug in which type of patients?

A

Muromonab-CD3 in transplant recipients

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10
Q

2 Cytotoxic anti-mtebolites

  • what 2 drugs in this class
A

2 Cytotoxic anti-mtebolites

  1. Azathioprine
  2. Mycophenolate Mofetil
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11
Q

What are the two active metabolites of Azathioprine?

  • which incorp into DNA? RNA?
  • overall what is their MOA
A

active metabolites of Azathioprine

  1. 6-thio-dGTP (DNA)
  2. 6 thio-GTP (RNA)

MOA = inhibit lymphocyte proliferation & fxn (B/T cells)

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12
Q

What two things cause inactivation of Azathioprine?

  • for both drugs
A

inactivation of Azathioprine by:

  1. XO
  2. TPMT (thiopurine methyltransferase)
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13
Q

inactivation of Azathioprine by XO & TPMT

  1. what is the major AE that these drug interactions cause?
  2. how to prevent?
A

inactivation of Azathioprine by XO & TPMT

  1. Major AE –> bone marrow supp (myelosupp)
  2. prevent by decr dose of Azathioprine
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14
Q

inactivation of Azathioprine by XO & TPMT

  1. XO: what drug is XO inhibitor that causes AE w/ Azathioprine
  2. TPMT - what form of this allele causes AE w/Azathioprine
A

inactivation of Azathioprine by XO & TPMT

  1. XO inhib = allopurinol (gout Tx)
  2. TPMT - inactive allele

both cause AE of myelosuppression

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15
Q

What doses of Azathioprine must be used to prevent transplant rejection

  • what is the problem w/this drug
A

high doses

causes immunosupp but also affects ALL rapidly dividing cells –> toxicity

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16
Q

What 2 drugs when given w/Azathioprine cause exacerbated bone marrow supp?

A

exacerbated bone marrow supp when Azathioprine given w/

  1. MTX
  2. ACE inhib
17
Q

Cytotoxic Anti-metabolites:

How does Mycophenolate Mofetil differ from Azathioprine

A

Mycophenolate Mofetil = more selective in suppressing immune cells –> fewer/less severe AEs

18
Q

Cytotoxic Anti-metabolites: Mycophenolate Mofetil

  1. what does it enzyme does inhibit preferentially? which causes what to be inhibited?
  2. what 2 cells does in inhibit selectively?
A

Cytotoxic Anti-metabolites: Mycophenolate Mofetil

  1. preferentially inhib IMP Dehydrogenase II –> inhibit lymphocyte prolif
  2. inhibits B/T cells selectively

overall it inhibits: lymphs, Ab formation by B cells, cellular adhesion/migration

19
Q

Cytotoxic Anti-metabolites:

  • What is the active compound of Mycophenolate Mofetil
  • what does this compound get metab to (what type of deriative)? –> what drug impairs this?
A

Cytotoxic Anti-metabolites: Mycophenolate Mofetil

active compound = mycophenolic acid
- metab to glucoronide derivative –> impaired by Tacrolimus

20
Q

Cytotoxic Anti-metabolites: Mycophenolate Mofetil

3 major classes of toxicity

A

Cytotoxic Anti-metabolites: Mycophenolate Mofetil toxicities

  1. GI (V/D)
  2. Hematologic (leukopenia)
  3. Congenital abn/preg loss
21
Q

When is Mycophenolate Mofetil used to prevent transplant rejection

A

used as ppx for transplant rejection

22
Q

Two types of drug classes that act on T cell pathways to prevent T cell activation/proliferation

A
  1. Calcineurin inhibitors

2. mTOR inhibitors

23
Q

T cell Pathway Drugs: Calcineurin inhibitors

- what are the 2 drugs in this class

A

T cell Pathway Drugs: Calcineurin inhibitors

  1. Cyclosporine
  2. Tacrolimus
24
Q

T cell Pathway Drugs: Calcineurin inhibitors

  • what is the result of these drugs inhibiting calcineurin –> that then prevents T cell activation/prolif
A

T cell Pathway Drugs: Calcineurin inhibitors

  • inhibit calcineurin –> inhibit IL-2 –> prevent T cell activation/prolif
25
Q

T cell Pathway Drugs: Calcineurin inhibitors

  • what are these drugs metab by that –> drug interactions
A

T cell Pathway Drugs: Calcineurin inhibitors

metab by CYP34A

26
Q

T cell Pathway Drugs: Calcineurin inhibitors & drug interactions w/CYP34A

  1. what types of CYP34A drugs –> incr blood levels –> toxicity
  2. What types of CYP34A drugs –> decr blood levels –> organ transplant rejection
A

T cell Pathway Drugs: Calcineurin inhibitors & drug interactions w/CYP34A

  1. CYP34A inhibitors –> incr blood levels –> toxicity
  2. CYP34A inducers –> decr blood levels –> organ transplant rejection
27
Q

T cell Pathway Drugs: Calcineurin inhibitors & drug interactions
- what 2 drugs can aggravate renal dysfxn when given w/ Calcineurin inhib

A

T cell Pathway Drugs: Calcineurin inhibitors & drug interactions

  • NSAIDs or Sirolimus can aggravate renal dysfxn when given w/ Calcineurin inhib
28
Q

T cell Pathway Drugs: Calcineurin inhibitors

  1. major dose limiting toxicity
  2. 3 other toxicities
A

T cell Pathway Drugs: Calcineurin inhibitors

  1. major dose limiting toxicity = renal dysfxn (nephrotox)
  2. Other AEs
    - HTN
    - Diabeotgenic
    - infxn & malig
29
Q

T cell Pathway Drugs: Calcineurin inhibitors toxicity

  1. HTN: if pt on cyclosporine + azathioprine what drug class should they NOT be on for HTN & why
  2. Diabetogenic when combined w/what other drug
A

T cell Pathway Drugs: Calcineurin inhibitors toxicity

  1. pt on cyclosporine + azathioprine should NOT be given ACEI for HTN b/c risk of myelosupp
  2. Diabetogenic when combined w/GCCs
30
Q

T cell Pathway Drugs: Calcineurin inhibitors uses:

  • what 2 d/o is it used for other that transplant rejection
A

T cell Pathway Drugs: Calcineurin inhibitors uses:

  • RA and psoriasis

Spring 2018 Pharm Exam 3 (4 decks)

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