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Drug Action IV > Immunosuppressants (MC) - Block 4 > Flashcards

Immunosuppressants (MC) - Block 4 Flashcards

1
Q

Indications for immunosuppressants?

A

For solid organ and bone marrow transplantation and autoimmune disorders

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2
Q

ADR of immunosuppressants?

A
  1. Increase risk of infection and malignanciess
  2. Nephrotoxicity
  3. Diabetes
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3
Q

MOA of glucocorticoids?

A

Reduce size and lymphoid content of lymph nodes and spleen -> interferes with cell cycle of activated lymphoid cells

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4
Q

Corticosteroids Examples?

A
  1. Hydrocortisone
  2. Prednisone
  3. Prednisolone
  4. Methylprednisolone
  5. Dexamethasone
  6. Betamethasone
  7. Triamcinolone
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5
Q

MOA of cyclosporine?

A

Blocks activation of T cells by binding to cyclophilin

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6
Q

Metabolism of cyclosporine?

A

CYP3A family -> requiring individual patient dosage adjustments

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7
Q

ADR of cyclosporine (calcineurin inhibitors)?

A

Nephrotoxicity (additive with NSAIDs)
HTN
Hyperglycemia
Hyperkalemia

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8
Q

How does tacrolimus binding differ from cyclosporine?

A

Binds to FK-BP instead of cyclophilin

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9
Q

What is a natural mTOR inhibitor?

A

Rapamycin

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10
Q

MOA of rapamycin?

A

Bind to FKBP12 -> complex blocks mTOR

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11
Q

What is mTOR?

A

Mammalian target of rapamycin: serine/threonin kinase
* Phosphorylated kinases result in de novo synthesis of proteins -> inhibition of T cell proliferation

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12
Q

PK properties of rapamycin?

A

Lot of hydrophobic interactions (carbon rich)
* Only 3 atoms aren’t buried in the protein - one of which is O -> can modify

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13
Q

Metabolism of sirolimus?

A

Substrate for both CYP3A family and P-gp many DDIs are possible

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14
Q

ADR of sirolimus?

A
  1. Hyperglycemia
  2. DLD (elevated cholesterol and TG)
  3. HTN
  4. Myelosuppression

Not as nephrotoxic -> good for kindey transplants

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15
Q

Describe the structural modifications of Temsirolimus/Everolimus?

A

Increased solubility - O is not in protein and ester/ether are polor -> exposed to surrounding environment (aqueous)

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16
Q

How is temsirolimus metabolized?

A

To rapamycin (active) by CYP3A4

17
Q

What mTOR Inhibitors must be pretreated with Benadryl to prevent hypersensitivity reactions?

A

Temsirolimus

18
Q

What is the drug name of rapamycin?

A

Sirolimus

19
Q

MOA of mycophenolate mofetil?

A

Prodrug for F -> inhibits T and B lymphocyte responses
* Selectively inhibits lymphocyte proliferation and function
* Inhibits de novo synthesis of purines

20
Q

What is different about the metabolism of mycophenolate mofetil?

A

Not metabolized by CYP 3As

21
Q

ADR of mycophenolate mofetil?

A

HTN, reversible myelosuppression

22
Q

What is the prodrug of mercaptopurine?

A

Azathioprine

23
Q

Additional MOA of azathioprine?

A

Antimetabolite: interferes with purine nucleic acid metabolism at steps required for lymphoid cell proliferation after antigenic stimulation

24
Q

ADR of azathioprine?

A

Myelosuppression

25
Q

MOA of Anti-thymocyte Globulin?

A

Cytotoxic to lymphocytes -> blocking lymphocyte function

26
Q

ADR of anti-thymocyte globulin?

A

Hypersensitivity

27
Q

Anti-CD-3 Monoclonal Antibody MOA?

A

CD3 = 3 glycoproteins – part of signal transduction machinery of T-cell receptor complex:
* Suppresses T cell funtion

28
Q

Type of anti-CD-3 Monoclonal antibody?

A

Muromonab

29
Q

ADR of Anti-CD-3 Monoclonal Antibody - Muromonab?

A

Cytokine release syndrome: pretreat with immune suppressants (steroids)

30
Q

MOA of Anti-IL-2-Receptor Antibodies? Example?

A

Binds to CD25 (IL-2 receptor α chain on activated lymphocytes)
Ex: Basiliximab

31
Q

ADR of Basiliximab?

A

Anaphylaxis

32
Q

MOA of daclizumab?

A

Very similar to basiliximab except IgG1 mAB

33
Q

Anti-TNF agents?

A

Infliximab
Etanercept
Adalimumab

Drug Action IV (28 decks)

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