Immunopharmacology Flashcards

1
Q

Uses of Immunosuppressives?

A

1) Autoimmune diseases
2) Isoimmune diseases
3) Organ transplantation
4) Prevention of cell proliferation

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2
Q

Classification of Immunosuppressive Agents?

A

1) Corticosteroids
2) Calcineurin inhibitors
3) Cytotoxic agents
4) Mycophenolate mofetil
5) Proliferative signal inhibitors
6) Biologicals (antibodies)

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3
Q

Steroids are used in the treatment of?

A
RA
SLE
Psoriasis
Asthma
Inflammatory renal disease
Inflammatory opthalmic disease
Autoimmune hematological disease
MS
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4
Q

Immediate side effects of corticosteroids:

A
Cushingoid features
Weight gain (ravenous appetite)
Diabetes (transient)
Hirsutism (especially pediatrics)
Cataracts
Mood changes
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5
Q

Corticosteroids are excreted via the ___ as the metabolite ____:

A

kidneys; dihydroxyketone (17-hydroxysteroids)

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6
Q

Longest acting, most potent corticosteroids?

A

Bethamethasone

Dexamethasone

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7
Q

Least potent corticosteroid?

A

Cortisone

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8
Q

Shortest acting corticosteroid?

A

Hydrocortisone

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9
Q

Long term effects of corticosteroids:

A

Osteoporosis
Avascular necrosis
Growth retardation

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10
Q

Effects of steroids?

A

Regulates numerous gene transcription
Curtail NF-KB activation
Downregulation of IL-1 and IL-6
T-cells are inhibited from producing IL-2
CD8 activation is inhibited
Increase in neutrophils, decrease in other leukocytes
Neutrophils and monocytes display poor chemotaxis

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11
Q

The CNI Cyclosporine A is derived from?

A

Tolypocladium inflatum

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12
Q

The CNI Tacrolimus is derived from?

A

Streptomyces tsukunbaensis

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13
Q

IC mediator of CsA?

A

Cyclophilin

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14
Q

IC mediator of TAC?

A

FKBP-12

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15
Q

Adverse effects unique to CsA?

A

Hirsutism
Gum hypertrophy
Hypercholesterolemia

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16
Q

Adverse effects unique to TAC?

A

Hair loss

GI side effects

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17
Q

Adverse effects common to both TAC and CsA?

A

Nephrotoxicity
Hyperkalemia
Hypomagnesemia

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18
Q

What are the cytotoxic agents?

A
Azathioprine
Methotrexate
Cyclophosphamide
Leflunomide
Hydroxychloroquine
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19
Q

Uses of Azathioprine?

A
Transplantation
RA
Crohn's disease
Ulcerative colitis
GVHD
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20
Q

Methotrexate inhibits____ which leads to ____.

A

Dihydrofolate reductase; cessation of nucleotide synthesis

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21
Q

Uses of methotrexate?

A

GVHD
RA
SLE
Psoriasis

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22
Q

Cyclophosphamide is an ____ that forms covalent bonds with DNA and suppresses ___, which inhibits ___ production.

A

alkylating agent; cellular immunity; Ab and autoAb

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23
Q

Adverse effects of cyclophosphamide:

A
Leukopenia
Sterility
Hemorrhagic cysts (hydrate patient before infusion)
Malignancy
Cardiac toxicity
N&V
24
Q

Uses of cyclophosphamide:

A

Hematopoietic cell transplantation
SLE
Vasculitis
Wegener’s Granulomatosis

25
Q

Leflunomide is a pro-drug inhibitor of ___ synthesis and indicated in cases of __:

A

Pyrimidine; Rheumatoid arthritis

26
Q

Hydroxychlorine suppresses ___ by ____, which results in decreased ___.

A

APC processing and MHC II loading; increasing lysosomal pH; T-cell activation

27
Q

Mycophenolate mofetil reversibly inhibits ____, thereby blocking:

A

IMDPH; de novo purine synthesis

28
Q

What are the Proliferative signal inhibitors?

A

1) Sirolimus/Rapamycin/Rapammune
2) Everolimus
3) Temsirolimus

29
Q

Sirolimus is a ____ derived from __.

A

Macrocylic lactone; streptomyces hygroscopicus

30
Q

Azathiprine is metabolized to ___, which interrupts ___ and so reduces mitosis.

A

6-mercaptopurine; purine synthesis

31
Q

Adverse effects of MMF:

A

GI disturbances

Suppression of bone marrow

32
Q

Long term risks of Aza therapy:

A

Increased risk of squamous cell carcinoma
Lymphoma
Bacterial and opportunistic infections

33
Q

MOA of Sirolimus?

A

1) Binds to FKBP
2) Blocks serine threonine kinase
3) Does not block IL production but lymphocytic response to them.

34
Q

Everolimus is a ____ derived from naturally occurring ___.

A

Semi-synthetic proliferative signal inhibitor (PSI); rapamycin

35
Q

TAC is 50 -100 more potent than ___; but ___ is 27x more potent than TAC

A

CsA; Sirolimus

36
Q

Sirolimus is isolated from:

A

Streptomyces hygroscopicus

37
Q

Sirolimus arrests malignant cell growth through it’s ____ effect:

A

anti-angiogenesis

38
Q

Mechanism of the ATGs?

A

Depletion of circulating t-cells
Modulation of cell surface receptor molecule
Induction of anergy
Apoptosis of activated T-cells

39
Q

MMF is not co-administered with:

A

Azathioprine

40
Q

What is the first therapeutic monoclonal antibody? What is it’s antigen?

A

OKT3, directed against CD3 receptor on T cells

41
Q

Symptoms of cytokine release syndrome:

A

First dose effect
Fever, chills, rigors, “shake and bake”
Pulmonary edema

42
Q

This drug has a low rejection rate and minimal side effects when used in kidney transplant:

A

Alemtuzumab

43
Q

Chimeric mAb IL-2 Receptor antagonist:

A

Basiliximab

44
Q

Humanized mAb IL-2 receptor antagonist:

A

Daclizumab

45
Q

Rituximab is a ___ mAb specific for the B-cell marker ___, approved in the treatment of:

A

chimeric; CD20; refractory non-Hodgkins lymphoma

46
Q

Alemtuzumab is a ___ mAb directed against the marker ___:

A

Humanized; CD52

47
Q

Restores function of B & T lymphocytes, monocytes and macrophages:

A

Levamisole

48
Q

Indicated in erythema nodosum leprosum multiple myeloma RA:

A

Thalidomide

49
Q

Used in Ca in situ of the urinary bladder and primary recurrent papillary tumors:

A

Bacille-Calmette-Guerin

50
Q

Indications for Interferon Alpha-2b:

A

Chronic Hep B and C
Melanoma
Lymphoma follicular
Kaposi’s sarcoma

51
Q

Interferon indicated in multiple sclerosis:

A

Interferon Beta-1a

52
Q

The Recombinant cytokines:

A

Hematopoietic growth factors
Interferons
Interleukin-2 (RCC)

53
Q

The therapeutic Abs:

A
IVIG (polyclonal)
Polyclonal Ab (directed against cells)
Hyperimmune globulins (polyclonal and monoclonal)
54
Q

Used to treat Rh disease:

A

Polyclonal Ab, RhD immunoglobulin against the D blood group Ag

55
Q

The hyperimmuneglobulins:

A
Hep B Immuneglobulin
Rabies
Tetanus
Varicella
CMV
RSV
56
Q

Immunomodulator used in metastatic renal cell carcinoma?

A

IL-2