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Pharmacology I Exam 3 > Immunosuppressants > Flashcards

Immunosuppressants Flashcards

1
Q

What is the MOA for Prednisone?

A

General suppression

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2
Q

What are the toxicities of Prednisone?

A
  • Hyperglycemia
  • Cushing’s like syndrome
  • Weight gain
  • Suppression of pituitary-hypothalamic axis
  • Osteoporosis
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3
Q

What is the MOA of Cyclosporine?

A

T-cell suppressant

Calcineurin inhibitor

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4
Q

What are the uses of Cyclosporine?

A
  • Bone marrow transplants (no bone marrow suppression)
  • Prevent rejection
  • Maintenance s/p transplant
  • Autoimmune
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5
Q

What are the toxicities of Cyclosporine?

A

Drug interactions

  • Metabolized by CYP3A4
  • Would become too concentrated with Erythromycin/Ketoconazole (inhibit CYP3A4)
  • Would be eliminated too quickly with rifampin (inducer of CYP3A4)
  • No grapefruit juice
  • Renal toxicity
  • Gingival hyperplasia
  • HTN
  • CNS
  • Hyperglycemia
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6
Q

What is the MOA for Tacrolimus?

A

T-cell suppressant

Calcineurin inhibitor

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7
Q

What are the uses of Tacrolimus?

A

DOC:
Most organ transplants to prevent rejection

“Rescue” during rejection episodes

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8
Q

What are the toxicities of Tacrolimus?

A
  • Nephrotoxicity
  • Hypertension
  • Hyperglycemia
  • Tremor, HA, insomnia
  • Drug interactions similar to cyclosporine
  • Avoid grapefruit juice
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9
Q

What is the MOA for Sirolimus?

A

T-cell suppressant

Inhibits proliferation of T cells by binding to mTOR –> prevent activation of phosphatases or kinases –> cell arrest and inhibition of B cell differentiation

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10
Q

What are the uses for Sirolimus?

A

Excellent choice for kidney transplant rejection prophylaxis as has no renal toxicity (given in combo with cyclosporine and steroids)

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11
Q

What are the toxicities of Sirolimus?

A

Increases cholesterol and triglycerides

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12
Q

What is the DOC for most organ transplants to prevent rejection and why?

A

Tacrolimus as it is more effective and less toxic than Cyclosporine

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13
Q

What is the MOA for Mycophenolate?

A

Antiproliferative

Inhibits de novo purine synthesis in T/B lymphocytes as well as antibody formation by B cells

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14
Q

What are the uses of Mycophenolate?

A

Prevent rejection after transplant

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15
Q

What are the toxicities of Mycophenolate?

A

Terotogenic!

DO NOT use in pregnancy and advise that patient uses multiple forms of birth control

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16
Q

What are special considerations for Mycophenolate?

A

Must be given in combination with Tacrolimus and steroids

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17
Q

What is the MOA for Azathioprine?

A

Cytotoxic Agent

Inhibits purine synthesis to inhibit DNA/RNA synthesis to induce apoptosis of activated T and B lymphocytes

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18
Q

What are the uses of Azathioprine?

A

Prevent rejection after transplant

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19
Q

What are the toxicities of Azathioprine?

A
  • Teratogenic!
  • Bone marrow suppression
  • Fatal blood dyscrasias if used with Allopurinol
20
Q

What are special considerations for Azathioprine?

A

Combine with steroids and other cytotoxic agents

21
Q

What is the MOA for Methotrexate?

A

Cytotoxic Agent

Inhibits DHFR, induces apoptosis of activated lymphocytes

22
Q

What are the uses of Methotrexate?

A
  • Low dose, long-term Immunosuppression in organ transplant recipient
  • Psoriasis, RA
  • Cancer (higher dose)
23
Q

What are the toxicities of Methotrexate?

A
  • Teratogenic
  • Bone marrow suppression
  • Stomatitis
24
Q

What is the MOA for Cyclophosphamide?

A

Cytotoxic Agent

Direct effect on T/B cells; phosphoramide mustard forms in DNA cross-links, inactivating DNA

25
Q

What are uses of Cyclophosphamide?

A
  • Organ transplant rescue
  • Bone marrow transplants
  • Autoimmune, cancer
26
Q

What are toxicities of Cyclophosphamide?

A
  • Hemorrhagic cystitis
  • Bone marrow suppression
  • Infertility
27
Q

What are special considerations for Cyclophosphamide?

A

MESNA/hydration to prevent HC

28
Q

What is the MOA for Basiliximab?

A

Antibody Immunosuppression

T-cell directed;
Binds to IL-2 receptor (CD25), inhibiting IL-2 activation –> inhibits T cell

29
Q

What are the uses of Basiliximab?

A

Used at time of transplant for induction of immunosuppression;

Reduces renal rejection 50%

30
Q

What is the MOA for Adalimumab?

A

Antibody Immunosuppression

Neutralizes biological activity of TNF-alpha

31
Q

What are the uses of Adalimumab?

A

Psoriasis and RA

32
Q

What is the MOA for Etanercept?

A

Antibody Immunosuppression

Neutralizes biological activity of TNF-alpha

33
Q

What are the uses for Etanercept?

A

Psoriasis and RA

34
Q

What is the MOA for Abatacept?

A

Antibody Immunosuppressent

Competes with CD28 for CD80/86 and prevents delivery of signal required for T cell activation

35
Q

What are the uses of Abatacept?

A

Psoriasis and RA

36
Q

What are the toxicities of Abatacept?

A

Infection (higher % than usual)

37
Q

What is the MOA of Neupogen?

A

Hematopoietic Stimulating Drug

38
Q

What are the uses of Neupogen?

A

Severe neutropenia (WBC) in patients taking immunosuppressants

39
Q

What is a special consideration for Neupogen?

A

Bone pain is common as bone marrow forming

40
Q

What is the MOA for Epogen?

A

Hematopoietic Stimulating Drug

41
Q

What are the uses of Epogen?

A

Severe anemia (RBC) in patients taking immunosuppressants

42
Q

What are toxicities of Epogen?

A
  • Hypertension

- Increased risk of thrombosis/stroke

43
Q

What is the DOC for most organ transplants to prevent rejection?

A

Tacrolimus

44
Q

What is the DOC for kidney transplant rejection?

A

Sirolimus

45
Q

What immunosuppressants are used for Psoriasis and RA?

A

Adalimumab (Humira)
Etanercept (Enbrel)
Abatacept (Orencia)
Methotrexate

46
Q

What can be given to combat severe neutropenia?

A

Neopogen

47
Q

What can be given to combat severe anemia?

A

Epogen

Pharmacology I Exam 3 (8 decks)

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