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First Aid > Immunology - Immunosuppressants > Flashcards

Immunology - Immunosuppressants Flashcards

1
Q

Immunosuppressants

A
  • Agents that block lymphocyte activation and proliferation.
  • Reduce acute transplant rejection by suppressing cellular immunity.
  • Frequently combined to achieve greater efficacy with decreased toxicity.
  • Chronic suppression increases risk of infection and malignancy.
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2
Q

Cyclosporine

  • Mechanism
  • Use
  • Toxicity
  • Notes
A
  • Mechanism
    • Calcineurin inhibitor; binds cyclophilin.
    • Blocks T cell activation by preventing IL-2 transcription.
  • Use
    • Transplant rejection prophylaxis, psoriasis, rheumatoid arthritis.
  • Toxicity
    • Nephrotoxicity, hypertension, hyperlipidemia, hyperglycemia, tremor, hirsutism, gingival hyperplasia.
  • Notes
    • Both calcineurin inhibitors are highly nephrotoxic.
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3
Q

Tacrolimus

  • Mechanism
  • Use
  • Toxicity
  • Notes
A
  • Mechanism
    • Calcineurin inhibitor
    • Binds FK506 binding protein (FKBP).
    • Blocks T cell activation by preventing IL-2 transcription.
  • Use
    • Transplant rejection prophylaxis.
  • Toxicity
    • Similar to cyclosporine
      • Nephrotoxicity, hypertension, hyperlipidemia, hyperglycemia, tremor
    • Increased risk of diabetes and neurotoxicity
    • No gingival hyperplasia or hirsutism.
  • Notes
    • Both calcineurin inhibitors are highly nephrotoxic.
    • -limus drugs bind FKBP.
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4
Q

Sirolimus (Rapamycin)

  • Mechanism
  • Use
  • Toxicity
  • Notes
A
  • Mechanism
    • mTOR inhibitor
    • Binds FKBP.
    • Blocks T cell activation and B cell differentiation by preventing IL-2 signal transduction.
  • Use
    • Kidney transplant rejection prophylaxis.
  • Toxicity
    • Anemia, thrombocytopenia, leukopenia, insulin resistance, hyperlipidemia
    • Non-nephrotoxic.
  • Notes
    • Kidney “sir-vives.”
    • Synergistic with cyclosporine.
    • Also used in drug-eluting stents.
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5
Q

Basiliximab

  • Mechanism
  • Use
  • Toxicity
A
  • Mechanism
    • Monoclonal antibody
    • Blocks IL-2R.
  • Use
    • Kidney transplant rejection prophylaxis.
  • Toxicity
    • Edema, hypertension, tremor.
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6
Q

Azathioprine

  • Mechanism
  • Use
  • Toxicity
  • Notes
A
  • Mechanism
    • Antimetabolite precursor of 6-mercaptopurine.
      • Pronounce “azathiopurine.”
    • Inhibits lymphocyte proliferation by blocking nucleotide synthesis.
  • Use
    • Transplant rejection prophylaxis, rheumatoid arthritis, Crohn disease, glomerulonephritis, other autoimmune conditions.
  • Toxicity
    • Leukopenia, anemia, thrombocytopenia.
  • Notes
    • 6-MP degraded by xanthine oxidase
    • Toxicity increased by allopurinol.
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7
Q

Glucocorticoids

  • Mechanism
  • Use
  • Toxicity
  • Notes
A
  • Mechanism
    • Inhibit NF-κB.
    • Suppress both B and T cell function by decreasing transcription of many cytokines.
  • Use
    • Transplant rejection prophylaxis (immune suppression), many autoimmune disorders, inflammation.
  • Toxicity
    • Hyperglycemia, osteoporosis, central obesity, muscle breakdown, psychosis, acne, hypertension, cataracts, peptic ulcers.
  • Notes
    • Can cause iatrogenic Cushing syndrome.
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8
Q

Immunosuppression targets (216)

A
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9
Q

Clinical uses of these recombinant cytokines

  • Epoetin alfa (erythropoietin)
  • Thrombopoietin
  • Oprelvekin (interleukin-11)
  • Filgrastim (granulocyte colony-stimulating factor)
  • Sargramostim (granulocyte-macrophage colonystimulating factor)
  • Aldesleukin (interleukin-2)
  • IFN-alpha
  • IFN-beta
  • IFN-gamma
A
  • Epoetin alfa (erythropoietin)
    • Anemias (especially in renal failure)
  • Thrombopoietin
    • Thrombocytopenia
  • Oprelvekin (interleukin-11)
    • Thrombocytopenia
  • Filgrastim (granulocyte colony-stimulating factor)
    • Recovery of bone marrow
  • Sargramostim (granulocyte-macrophage colony-stimulating factor)
    • Recovery of bone marrow
  • Aldesleukin (interleukin-2)
    • Renal cell carcinoma, metastatic melanoma
  • IFN-alpha
    • Chronic hepatitis B and C, Kaposi sarcoma, hairy cell leukemia, condyloma acuminatum, renal cell carcinoma, malignant melanoma
  • IFN-beta
    • Multiple sclerosis
  • IFN-gamma
    • Chronic granulomatous disease
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10
Q

Alemtuzumab

  • Type of therapy
  • Target
  • Clinical use
  • Notes
A
  • Type of therapy
    • Cancer therapy
  • Target
    • CD52
  • Clinical use
    • CLL
  • Notes
    • “Alymtuzumab”—chronic lymphocytic leukemia
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11
Q

Bevacizumab

  • Type of therapy
  • Target
  • Clinical use
A
  • Type of therapy
    • Cancer therapy
  • Target
    • VEGF
  • Clinical use
    • Colorectal cancer
    • Renal cell carcinoma
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12
Q

Cetuximab

  • Type of therapy
  • Target
  • Clinical use
A
  • Type of therapy
    • Cancer therapy
  • Target
    • EGFR
  • Clinical use
    • Stage IV colorectal cancer
    • Head and neck cancer
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13
Q

Rituximab

  • Type of therapy
  • Target
  • Clinical use
A
  • Type of therapy
    • Cancer therapy
  • Target
    • CD20
  • Clinical use
    • B-cell non-Hodgkin lymphoma
    • Rheumatoid arthritis (with MTX)
    • ITP
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14
Q

Trastuzumab

  • Type of therapy
  • Target
  • Clinical use
  • Notes
A
  • Type of therapy
    • Cancer therapy
  • Target
    • HER2/neu
  • Clinical use
    • Breast cancer
    • Gastric cancer
  • Notes
    • HER2—“tras2zumab”
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15
Q

Infliximab, adalimumab

  • Type of therapy
  • Target
  • Clinical use
  • Notes
A
  • Type of therapy
    • Autoimmune disease therapy
  • Target
    • TNF-α
  • Clinical use
    • IBD
    • Rheumatoid arthritis
    • Ankylosing spondylitis
    • Psoriasis
  • Notes
    • Rheumatoid arthritis “inflix” pain in “_da lim_bs”
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16
Q

Natalizumab

  • Type of therapy
  • Target
  • Clinical use
  • Notes
A
  • Type of therapy
    • Autoimmune disease therapy
  • Target
    • α4-integrin
  • Clinical use
    • Multiple sclerosis
    • Crohn disease
  • Notes
    • α4-integrin: leukocyte adhesion
    • Risk of PML in patients with JC virus
17
Q

Abciximab

  • Target
  • Clinical use
  • Notes
A
  • Target
    • Glycoprotein IIb/IIIa
  • Clinical use
    • Anti-platelet agent for prevention of ischemic complications in patients undergoing percutaneous coronary intervention
  • Notes
    • IIb times IIIa equals “absiximab”
18
Q

Denosumab

  • Target
  • Clinical use
  • Notes
A
  • Target
    • RANKL
  • Clinical use
    • Osteoporosis
    • Inhibits osteoclast maturation (mimics osteoprotegrin)
  • Notes
    • Denosumab affects osteoclasts
19
Q

Digoxin immune Fab

  • Target
  • Clinical use
  • Notes
A
  • Target
    • Digoxin
  • Clinical use
    • Antidote for digoxin toxicity
20
Q

Omalizumab

  • Target
  • Clinical use
A
  • Target
    • IgE
  • Clinical use
    • Allergic asthma
    • Prevents IgE binding to FceRI
21
Q

Palivizumab

  • Target
  • Clinical use
  • Notes
A
  • Target
    • RSV F protein
  • Clinical use
    • RSV prophylaxis for high-risk infants
  • Notes
    • PaliVIzumab—VIrus

First Aid (92 decks)

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