Exam 3: Immunopharmacology Flashcards

1
Q

What are the side effects of all immunosuppressants?

A

-Infections and increased risk of lymphoma and other malignancies

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2
Q

What are the two classes of T-cell inhibitors?

A

Calcineurin inhibitors and proliferation signal inhibitors

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3
Q

What kind of drug is prednisone?

A

Glucocorticoids- General suppression

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4
Q

What are the two types of Calcineurin inhibitors?

A

Cyclosporine and tacrolimus

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5
Q

What kind of drug is Sirolimus?

A

Proliferation signal inhibitor

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6
Q

What are the 3 drugs that are cytotoxic agents?

A

Azathioprine, cyclophosphamide, and methotrexate

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7
Q

What are the 4 drugs that are antibody immunosuppressives?

A

Basiliximab, adalimumab, abatacept, and etanercept

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8
Q

What are the adverse effects of corticosteroids?

A
  • Hyperglycemia
  • Cushing like syndrome
  • Weight gain
  • Suppression of PHA axis
  • Osteoporosis
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9
Q

What kind of drugs are used to prevent Organ rejection?

A

T-cell suppressants

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10
Q

What is the MOA of cyclosporine?

A

Binds to specific receptor and inhibits calcineurin and T cell activation. Produces selective inhibition of T lymphocytes

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11
Q

What are the toxicities associated with cyclosporine?

A
  • Renal toxicity
  • gingival hyperplasia
  • HTN
  • CNS: tremors, hallucinations, seizures
  • hyperglycemia
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12
Q

What is the MOA of Tacrolimus?

A

-Binds to specific receptor and inhibits calcineurin/T cell activation and produces selective inhibition of T lymphocytes

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13
Q

What drug can be used as a ‘rescue” for a rejection episodes?

A

Tacrolimus

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14
Q

What are the toxicities associated with Tacrolimus?

A
  • Nephrotoxicity and HTN
  • Hyperglycemia
  • Tremor, headache, insomnia
  • Less toxic than cyclosporine
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15
Q

What is the MOA of Sirolimus?

A

Inhibits Proliferation of T cells by binding to mTOR which results in T cell cycle arrest and inhibition of B cell differentiation

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16
Q

What is the main adverse effect of Sirolimus?

A

Increased cholesterol and triglycerides

17
Q

What is the MOA of mycophenolate-Mofetil?

A

Antiproliferative drug that inhibits monophosphate dehydrogenase needed for de novo purine synthesis in T and B lymphocytes as well as antibody formation by B cells.

18
Q

What are the contraindications of mycophenolate-Mofetil?

A

Pregnancy

19
Q

What is the used of mycophenolate-Mofetil?

A

Used in combo with tacrolimus and corticosteroids to prevent rejection after transplants

20
Q

What is the MOA of Azathioprine?

A

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

21
Q

What is the use of Azathioprine?

A

-Prevents rejection in transplant patients, used in combo with corticosteroids and other cytotoxic agents

22
Q

What are the main side effects of Azathioprine?

A
  • Bone marrow suppression
  • Liver toxicity
  • teratogenic
23
Q

What is the important relationship between Azathioprine and allopurinol?

A

Azathioprine is metabolized by xanthine oxidase and Allopurinol inhibits xanthine oxidase. In patients treated with allopurinol, the dose of azathioprine must be reduced significantly for potentially fatal blood dyscrasias can occur

24
Q

What is the MOA of methotrexate?

A

-Dihydrofolate reductase inhibitor, induces apoptosis of activated lymphocytes

25
Q

What are the side effects of methotrexate?

A
  • bone marrow suppression
  • stomatitis
  • hepatotoxicity
  • can produce fetal death
26
Q

What is the MOA of cyclophosphamide?

A
  • Direct effect on T and B lymphocytes causes lymphopenia and selective suppression of B lymphocyte activity.
  • Blocks response to new antigens and can inhibit established immune response
27
Q

What are the clinical uses of Cyclophosphamide?

A

-Organ transplant rescue, bone marrow transplants, and severe autoimmune disease

28
Q

What are the side effects associated with cyclophosphamide?

A
  • Hemorrhagic cystitis (prevented in hydration and MESNA and discontinue drug if it does occur)
  • Bone marrow suppression
  • Infertility
29
Q

What is the MOA of Basiliximab?

A
  • Binds to IL-2 receptor (CD25) on activated T cells, inhibiting IL-2 activation.
  • Reduces renal rejection by 50%
30
Q

What is the used of Basiliximab?

A

-Used at time of transplant for induction of immunosuppression

31
Q

What are the biologic drugs that can treat psoriasis and RA?

A

Abatacept, etanercept, and adalimumab

32
Q

What is the MOA of Abatacept?

A

-Fully recombinant fusion protein that competes with CD28 and for CD80, which prevents the delivery of the costimulatory signal that is required for T cell activation

33
Q

What is neupogen used to treat?

A

Severe neutropenia