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Immunosuppressives Flashcards

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1
Q

Which immune response is more easily suppressive?

A

Primary

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2
Q

Inhibition is more likely if therapy begins ______ exposure

A

before

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3
Q

Broad based, low affinity, no priming, early response

A

Innate

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4
Q

Antigen specific, primed, high affinity, later response, T and B cells

A

Adaptive

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5
Q

Broad spectrum

A

Glucocorticoids

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6
Q

Inhibit B and T cell proliferation

A

Mycophenolate mofetil, antiproliferative agents

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7
Q

Bind to and deplete T cells

A

Monoclonal antibodies

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8
Q

Inhibit T cell activation and cytokine production

A

Tacrolimus and cyclosporine

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9
Q

Uses of immunosuppressives (4)

A
  • Prevent/Tx rejection after organ transplant
  • Autoimmune dz
  • Allergies and asthma
  • Macular degeneration
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10
Q

SE Immunosuppressants (2)

A
  • Infections

- Increased risk of lymphomas and other malignancies

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11
Q

Corticosteroids MOA (3)

A
  • Inhibits T cell proliferation and response to cytokines (IL-2)
  • Decreases size and lymphoid content of spleen
  • Decrease response to antibodies
  • Depress macrophage fxn
  • Modify T helper cells
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12
Q

Corticosteroid Tx (4)

A
  • Organ transplant
  • Long term immunosuppress
  • Prevention of rxn to other drugs
  • Topical: dermatitis, psoriasis
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13
Q

Corticosteroid SE (6)

A
  • Cushing’s like syndrome
  • Suppressed immune system
  • Suppress pituitary-hypothalamic axis
  • Osteoporosis
  • PUD
  • Menstrual/reproductive
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14
Q

T- Cell Suppressants (3)

A
  • Calcineurin Inhibitors (Cyclosporine, Tacrolimus)
  • Sirolimus
  • Pimecrolimus
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15
Q

Calcineurin Inhibitors (2)

A
  • Cyclosporine

- Tacrolimus

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16
Q

Cyclosporine MOA (6)

A
  • SELECTIVE inhibition of T lymphocytes
  • Binds to specific receptor
  • INHIBITS CALCINEURIN/T-CELL ACTIVATION
  • Decrease formation of IL-1/IL-2
  • Increases TGF-B
  • Suppresses immune response
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17
Q

Does cyclosporine suppress bone marrow?

A

NO! thus it is better tolerated

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18
Q

Cyclosporine Drug Interactions

A
  • CYP3A4 metabolism
  • Narrow therapeutic range
  • NO GRAPEFRUIT JUICE
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19
Q

Drugs that decrease concentration of Cyclosporine

A
  • Phenobarbital
  • Phenytoin
  • Rifampin
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20
Q

Drugs that increase concentration of Cyclosporine

A
  • Erythromycin
  • Ketoconazole
  • Verapamil
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21
Q

Cyclosporine Tx (4)

A
  • Prevent rejection in organ transplant
  • Maintenance after organ transplant
  • Bone marrow transplant
  • Autoimmune dz
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22
Q

Cyclosporine SE (6)

A
  • RENAL TOXICITY!!!
  • HTN
  • GINGIVAL HYPERPLASIA
  • Tremor, hirsutism
  • Hyperlipid, hyperglycemia
  • N/V/D, anorexia
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23
Q

FK506, Tacrolimus MOA (3)

A
  • Inhibits T cell activation
  • Decrease IL-2 and IL-4
  • Similar to Cyclosporine (Less toxic)
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24
Q

FK506, Tacrolimus Tx

A
  • Prevent rejection in transplantation, particularly in liver, kidney, and heart
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25
FK506, Tacrolimus Admin
- IV - Oral - Topical
26
FK506, Tacrolimus SE (8)
- Nephrotoxic - HTN - HYPERGLYCEMIA - Tremor, HA, insomnia - GI (empty stomach, avoid grapefruit) - Increased infections (skin CA) - Narrow therapeutic range - Drug interactions
27
Sirolimus MOA
- Inhibits proliferation of T and B-cells
28
Sirolimus SE (2)
- Increases cholesterol/triglycerides | - NO RENAL TOXICITY
29
Pimecrolimus Admin
- Topical for atopic dermatitis | - Does not thin/atrophy skin, but may irritate or burn
30
Mycophenolate-Mofetil MOA (2)
- Decreases DNA synthesis by inhibiting monophosphate dehydrogenase - T and B-cells need this for PURINE synthesis
31
Mycophenolate-Mofetil Tx
- Prevent rejection after transplants (often combined with Tacrolimus)
32
Mycophenolate-Mofetil SE (3)
- Rash - GI - Infections
33
Thalidomide MOA
- Blocks TNFa
34
Thalidomide SE (3)
- TERATOGENIC! - Drowsiness - Neutropenia
35
Thalidomide Tx
- Prevents graft vs host rxn
36
Azathioprine MOA (2)
- Converted in vivo to 6-mercaptopurine | - INHIBITS PURINE SYNTHESIS
37
Azathioprine Tx (4)
- Prevents rejection in transplant pts - Glomerulonephritis in lupus - Severe RA - In dental practice for random stuff
38
Azathioprine SE (7)
- Bone marrow suppression - TERATOGENIC - Increased infections - Liver toxicity - N/V/D - Metabolized by Xanthine oxidase --> reduce dose if used w/ Allopurinol
39
Cyclophosphamide MOA (3)
- Direct effect on T and B cells - Blocks response to new antigens - Can inhibit established immune response - Alkalating agent
40
Cyclophosphamide Tx (3)
- Organ transplant RESCUE - Bone marrow transplant - Severe autoimmune dz
41
Cyclophosphamide SE (6)
- Hemorrhagic cystitis - N/V - Bone marrow suppression - Aspermia, infertility - Bladder fibrosis, CA - Alopecia
42
Methotrexate MOA
- Human dihydrofolate reductase inhibitor
43
Methotrexate Tx (5)
- Organ transplants - Psoriasis - Antineoplastic - RA - Severe asthma
44
Methotrexate SE (3)
- FETAL TOXICITY - Alopecia - Hepatotoxicity with chronic use
45
Antibody Immunosuppressives MOA
- Form antibodies against specific cells
46
Antibody Immunosuppressives SE
- Allergic rxn (chimeric or humanized mabs decrease SE)
47
Lymphocyte Immune Globulin, Antithymocyte, Globulin, Muromonab CD3 MOA (2)
- Antibodies to T cells or CD3 receptor on T cells | - Bind/inactivate circulating T cells
48
Lymphocyte Immune Globulin, Antithymocyte, Globulin, Muromonab CD3 SE (3)
- Allergic Rxn, rash (give with corticosteroids to decrease rxn) - Chills, fever - Hypotension
49
Daclizumab/Basiliximab MOA
- Bind to IL-2 receptor on activated T cells, inhibit IL-2 activation
50
Daclizumab/Basiliximab SE
- Humanized/chimeric reduce adv SE | - NO general immunosuppression
51
Daclizumab/Basiliximab Tx
- Used right after transplant - induction
52
Efalizumba MOA (3)
- CD-11a monoclonal - Prevents binding to intercellular adhesion molecule (increased in psoriasis) - PREVENTS T CELL ACTIVATION, but doesn't destroy them
53
Alefacept MOA
- Binds to CD-2 receptor on cell surface, blocks T-cell activation
54
Alefacept and Efalizumab Tx
- Psoriasis
55
Drugs for Macular Degeneration (4)
- Bevacizumab, Ranibizumab | - Pegaptanib, Aflibercept
56
Pegaptanib, Aflibercept MOA
- Bind to VEGF-A
57
Drugs for Macular Degeneration MOA
- Decrease formation of new blood vessels
58
Drugs for Macular Degeneration Admin
- Intra-vitreous
59
Drugs for Macular Degeneration SE
- Thromboembolism | - Stroke, MI
60
Interleukin-2 MOA (2)
- Proliferation/differentiation of helper T and cytotoxic T cell - Proliferation of B cells/macrophages
61
Interleukin-2 Tx (2)
- Renal cell carcinoma | - Malignant melanoma
62
Interleukin-2 SE (3)
- Pulmonary edema - SEVERE HYPOTENSION - Hematologic
63
Granulocyte Colony Stimulating Factor; Filgrastim MOA
- Human recombinant
64
Granulocyte Colony Stimulating Factor; Filgrastim Tx
- Severe neutropenia induced by stem cell transplant or chemo
65
Granulocyte Colony Stimulating Factor; Filgrastim Admin
- SC
66
Granulocyte Colony Stimulating Factor; Filgrastim SE (2)
- Bone pain | - Injection site rxn
67
Epoetin-alfa MOA
- Human recombinant form of erythropoetin
68
Epoetin-alfa Tx
- severe anemia induced by Zidovudine, interferon chemo or pts with kidney dz
69
Epoetin-alfa Admin
- SC
70
Epoetin-alfa SE (2)
- HTN | - Risk thrombosis/stroke
71
Interferons MOA (2)
- a/b response to viruses - g increase T lymphocytes and NK cells (activates macrophages, increase expression of major histocompatibility antigens)
72
Interferon Tx (3)
- Hep C (a2b) - Severe uveitis (a2b) - MS (b1b)
73
Multiple Sclerosis
- Immune system attacks myelin around nerves --> weakness, difficulty walking
74
Multiple Sclerosis Drugs (4)
- Interferon b1b - Glatiramer - Fingolimod - Dimethyl fumarate
75
Interferon b1b MS (2)
- Injected | - Decrease relapses
76
Glatiramer MS
- Antibodies bind to drug instead of nerve (decoy)
77
Corticosteroid (1)
Prednisone
78
Proliferation Signal Inhibitors (4)
- Sirolimus - Pimecrolimus - Mycophenolate Mofetil - Thalidamide
79
Cytotoxic Agents (3)
- Azathioprine - Cyclophosphamide - Methotrexate
80
Immunomodulators (7)
- Interferone a2b - Interferon b1b - Interleukin-2 - G-CSF - Erythropoetin - Glatiramer - Dimethyl fumarate
81
Immunosuppressives
- Corticosteroids - T cell Suppressants - Proliferation Signal Inhibitors - Cytotoxic Agents - Antibodies
82
Two drugs that inhibit S phase?
Doxorubicin, Cisplatin
83
What drug affects G2 and M phase?
Bleomycin and Paclitaxel
84
What two drugs affect M phase?
Vinblastine, Vincistine
85
What drug affects G1 and M phase?
Mechlorethamine
86
What drug affects G and S phase?
5 FU

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