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Pharm > Immunosuppressives > Flashcards

Immunosuppressives Flashcards

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
Q

FK506, Tacrolimus Admin

A
  • IV
  • Oral
  • Topical
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26
Q

FK506, Tacrolimus SE (8)

A
  • Nephrotoxic
  • HTN
  • HYPERGLYCEMIA
  • Tremor, HA, insomnia
  • GI (empty stomach, avoid grapefruit)
  • Increased infections (skin CA)
  • Narrow therapeutic range
  • Drug interactions
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27
Q

Sirolimus MOA

A
  • Inhibits proliferation of T and B-cells
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28
Q

Sirolimus SE (2)

A
  • Increases cholesterol/triglycerides

- NO RENAL TOXICITY

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29
Q

Pimecrolimus Admin

A
  • Topical for atopic dermatitis

- Does not thin/atrophy skin, but may irritate or burn

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30
Q

Mycophenolate-Mofetil MOA (2)

A
  • Decreases DNA synthesis by inhibiting monophosphate dehydrogenase
  • T and B-cells need this for PURINE synthesis
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31
Q

Mycophenolate-Mofetil Tx

A
  • Prevent rejection after transplants (often combined with Tacrolimus)
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32
Q

Mycophenolate-Mofetil SE (3)

A
  • Rash
  • GI
  • Infections
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33
Q

Thalidomide MOA

A
  • Blocks TNFa
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34
Q

Thalidomide SE (3)

A
  • TERATOGENIC!
  • Drowsiness
  • Neutropenia
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35
Q

Thalidomide Tx

A
  • Prevents graft vs host rxn
36
Q

Azathioprine MOA (2)

A
  • Converted in vivo to 6-mercaptopurine

- INHIBITS PURINE SYNTHESIS

37
Q

Azathioprine Tx (4)

A
  • Prevents rejection in transplant pts
  • Glomerulonephritis in lupus
  • Severe RA
  • In dental practice for random stuff
38
Q

Azathioprine SE (7)

A
  • Bone marrow suppression
  • TERATOGENIC
  • Increased infections
  • Liver toxicity
  • N/V/D
  • Metabolized by Xanthine oxidase –> reduce dose if used w/ Allopurinol
39
Q

Cyclophosphamide MOA (3)

A
  • Direct effect on T and B cells
  • Blocks response to new antigens
  • Can inhibit established immune response
  • Alkalating agent
40
Q

Cyclophosphamide Tx (3)

A
  • Organ transplant RESCUE
  • Bone marrow transplant
  • Severe autoimmune dz
41
Q

Cyclophosphamide SE (6)

A
  • Hemorrhagic cystitis
  • N/V
  • Bone marrow suppression
  • Aspermia, infertility
  • Bladder fibrosis, CA
  • Alopecia
42
Q

Methotrexate MOA

A
  • Human dihydrofolate reductase inhibitor
43
Q

Methotrexate Tx (5)

A
  • Organ transplants
  • Psoriasis
  • Antineoplastic
  • RA
  • Severe asthma
44
Q

Methotrexate SE (3)

A
  • FETAL TOXICITY
  • Alopecia
  • Hepatotoxicity with chronic use
45
Q

Antibody Immunosuppressives MOA

A
  • Form antibodies against specific cells
46
Q

Antibody Immunosuppressives SE

A
  • Allergic rxn (chimeric or humanized mabs decrease SE)
47
Q

Lymphocyte Immune Globulin, Antithymocyte, Globulin, Muromonab CD3 MOA (2)

A
  • Antibodies to T cells or CD3 receptor on T cells

- Bind/inactivate circulating T cells

48
Q

Lymphocyte Immune Globulin, Antithymocyte, Globulin, Muromonab CD3 SE (3)

A
  • Allergic Rxn, rash (give with corticosteroids to decrease rxn)
  • Chills, fever
  • Hypotension
49
Q

Daclizumab/Basiliximab MOA

A
  • Bind to IL-2 receptor on activated T cells, inhibit IL-2 activation
50
Q

Daclizumab/Basiliximab SE

A
  • Humanized/chimeric reduce adv SE

- NO general immunosuppression

51
Q

Daclizumab/Basiliximab Tx

A
  • Used right after transplant - induction
52
Q

Efalizumba MOA (3)

A
  • CD-11a monoclonal
  • Prevents binding to intercellular adhesion molecule (increased in psoriasis)
  • PREVENTS T CELL ACTIVATION, but doesn’t destroy them
53
Q

Alefacept MOA

A
  • Binds to CD-2 receptor on cell surface, blocks T-cell activation
54
Q

Alefacept and Efalizumab Tx

A
  • Psoriasis
55
Q

Drugs for Macular Degeneration (4)

A
  • Bevacizumab, Ranibizumab

- Pegaptanib, Aflibercept

56
Q

Pegaptanib, Aflibercept MOA

A
  • Bind to VEGF-A
57
Q

Drugs for Macular Degeneration MOA

A
  • Decrease formation of new blood vessels
58
Q

Drugs for Macular Degeneration Admin

A
  • Intra-vitreous
59
Q

Drugs for Macular Degeneration SE

A
  • Thromboembolism

- Stroke, MI

60
Q

Interleukin-2 MOA (2)

A
  • Proliferation/differentiation of helper T and cytotoxic T cell
  • Proliferation of B cells/macrophages
61
Q

Interleukin-2 Tx (2)

A
  • Renal cell carcinoma

- Malignant melanoma

62
Q

Interleukin-2 SE (3)

A
  • Pulmonary edema
  • SEVERE HYPOTENSION
  • Hematologic
63
Q

Granulocyte Colony Stimulating Factor; Filgrastim MOA

A
  • Human recombinant
64
Q

Granulocyte Colony Stimulating Factor; Filgrastim Tx

A
  • Severe neutropenia induced by stem cell transplant or chemo
65
Q

Granulocyte Colony Stimulating Factor; Filgrastim Admin

A
  • SC
66
Q

Granulocyte Colony Stimulating Factor; Filgrastim SE (2)

A
  • Bone pain

- Injection site rxn

67
Q

Epoetin-alfa MOA

A
  • Human recombinant form of erythropoetin
68
Q

Epoetin-alfa Tx

A
  • severe anemia induced by Zidovudine, interferon chemo or pts with kidney dz
69
Q

Epoetin-alfa Admin

A
  • SC
70
Q

Epoetin-alfa SE (2)

A
  • HTN

- Risk thrombosis/stroke

71
Q

Interferons MOA (2)

A
  • a/b response to viruses
  • g increase T lymphocytes and NK cells (activates macrophages, increase expression of major histocompatibility antigens)
72
Q

Interferon Tx (3)

A
  • Hep C (a2b)
  • Severe uveitis (a2b)
  • MS (b1b)
73
Q

Multiple Sclerosis

A
  • Immune system attacks myelin around nerves –> weakness, difficulty walking
74
Q

Multiple Sclerosis Drugs (4)

A
  • Interferon b1b
  • Glatiramer
  • Fingolimod
  • Dimethyl fumarate
75
Q

Interferon b1b MS (2)

A
  • Injected

- Decrease relapses

76
Q

Glatiramer MS

A
  • Antibodies bind to drug instead of nerve (decoy)
77
Q

Corticosteroid (1)

A

Prednisone

78
Q

Proliferation Signal Inhibitors (4)

A
  • Sirolimus
  • Pimecrolimus
  • Mycophenolate Mofetil
  • Thalidamide
79
Q

Cytotoxic Agents (3)

A
  • Azathioprine
  • Cyclophosphamide
  • Methotrexate
80
Q

Immunomodulators (7)

A
  • Interferone a2b
  • Interferon b1b
  • Interleukin-2
  • G-CSF
  • Erythropoetin
  • Glatiramer
  • Dimethyl fumarate
81
Q

Immunosuppressives

A
  • Corticosteroids
  • T cell Suppressants
  • Proliferation Signal Inhibitors
  • Cytotoxic Agents
  • Antibodies
82
Q

Two drugs that inhibit S phase?

A

Doxorubicin, Cisplatin

83
Q

What drug affects G2 and M phase?

A

Bleomycin and Paclitaxel

84
Q

What two drugs affect M phase?

A

Vinblastine, Vincistine

85
Q

What drug affects G1 and M phase?

A

Mechlorethamine

86
Q

What drug affects G and S phase?

A

5 FU

Pharm (10 decks)

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