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IHO 5 > Immunosuppressive Drugs > Flashcards

Immunosuppressive Drugs Flashcards

1
Q

Immunosuppressive therapy

A
  • Drugs that will affect multiple mediator pathways to affect inflammation and/or specific immunity.
  • Used in organ transplants, autoimmune disease and hypersensitivity
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2
Q

Gen. principles of immunosuppression

A
  • Primary immune responses more effectively suppressed than secondary immune responses.
  • Effect of drugs not the same on all immune responses
  • Immune response more likely to be INHIBITED if therapy begun before immunogen
  • Suppress the immune response to prevent immune mediated tissue damage
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3
Q

Limitations of immunosuppressive therapy

A
  • Increased risk of all types of infections

- Increased risk of lymphomas and related malignancies

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4
Q

Major classes of immunosuppressive drugs

A
  • Glucocorticoids
  • Calcineurin inhibitors
  • Antiproliferative/antimetabolic drugs
  • Antibodies
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5
Q

Primary uses of immunosuppression

A

Autoimmune diseae

  • Transplants
  • Hemolytic anemia in newborns
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6
Q

Drug of choice for autoimmune diseases, idopathic thrombocytopenic purpura, autoimmune hemolytic anemia, acute glomerulonephritis, acquired factor XIII antibodies, autoreactive tissue disorders

A

Prednisone. Response is usually good

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7
Q

Drugs of choice for organ transplant (renal and heart)

A
  • Cyclosporine
  • Prednisone
  • ALG
  • OKT3
  • monoclonal antibody
  • Tacrolimus
  • Basiliximab
  • Daclizumab
  • Sirolimus
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8
Q

Best drugs for liver transplant

A
  • Cyclosporine
  • Prednisone
  • Tacrolimus
  • Sirolimus
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9
Q

Best drugs for bone marrow suppression

A
  • Cyclosporine
  • Prednisone
  • ALC
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10
Q

What 2 classes of steroids does the adrenal cortex synthesize?

A

Corticosteroids (glucocorticoids and mineralcorticoids) (21 carbons)
Androgens (19 carbons)

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11
Q

Glucocorticoid activity

A

Carbohydrate metabolism regulating activity

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12
Q

Mineralcorticoid activity

A

Electrolyte balancing activity

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13
Q

Main glucocorticoid

A

Hydrocortisone (cortisol)

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14
Q

Main mineralcorticoid

A

Aldosterone

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15
Q

What are corticosteroids secreted in response to?

A

ACTH (Adrenocorticotropic hormone)

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16
Q

Endogenous corticosteroids

A

Varying degrees of both mineralcorticoid and glucocorticoid activity.

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17
Q

Physiologic effects of corticosteroids

A

Regulation of intermediary metabolism, CV function, growth and immunity

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18
Q

Do mineralcorticoids or glucocorticoids cause sodium retention?

A

Mineralcorticoids

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19
Q

Do mineralcorticoids or glucocorticoids cause liver glycogen deposition?

A

Glucocorticoids

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20
Q

Are mineralcorticoids and glucocorticoids cause anti-inflammatory?

A

Glucocorticoids

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21
Q

Sodium retention

A

Ability of steroid to reduce Na+ excretion by kidney in an adrenalectomized animals

22
Q

Liver glycogen deposition

A

Ability of steroid to cause hepatic deposition of glycogen in fasted adrenalectomized animal.

23
Q

Liver glycogen deposition, anti-inflammatory activity, and involution of lymhoid tissue activity do what?

A

Parallel each other

24
Q

Synthetic steroids that are used as anti-inflammatory drugs

A
  • Betamethasone
  • Dexamethasone
  • Methylprednisolone
  • Prednisone
25
Duration of cortisol (hydrocortisone)
Short half-life (8-12 hrs)
26
Betamethasone and dexamethasone half-life
Long (36-72 hrs)
27
Methylprednisolone and prednisone half-life
Intermediate (12-36 hrs)
28
Inhaled glucocorticoids distribution and elimination
- Enhanced uptake and prolonged tissue binding in airway - Nearly complete hepatic first pass inactivation - Some systemic absorption - Metabolized in liver and excreted by kidney
29
Glucocorticoid administration, distribution, elimination
- Oral, Parenternal, Topical - Some systemic absorption - Metabolized in liver and excreted by kidney
30
What protein products are responsible for the immunosuppressive effects of steroids?
Many different protein products
31
Glucocorticoids/Anti-inflammatory steroid neutrophil action effects
- more neutrophils circulating - accelerated release from bone marrow - 1/2 time in circulation increased - decrease in adherence capabilities (blockage of neutrophil migration into inflammatory sites
32
Glucocorticoids/Anti-inflammatory steroid lymphocyte action effects
- profound transient lymphopenia | - cells not lysed--move to extravascular compartments like spleen, thoracic duct, lymph nodes, bone marow
33
Glucocorticoids/Anti-inflammatory steroid monocyte/eosinophil action effects
-decreased in peripheral blood
34
Glucocorticoids/Anti-inflammatory steroid effects on synthesis and/or release of inflammatory mediators
- reduce COX2 expression - inhibit arachidonic acid release from phospholipids-->affectin prostaglandin and leukotriene formation - inhibit mast cell and basophil degranulation - inhibit snthesis and release of TNF (cachectin), IL-1, IL-2, IFN
35
Use of glucocorticoids in anti-inflammatory therapy
- prevent or supress: redness, swelling, heat and pain. | - inflammation suppressed, but underlying cause of disease remains
36
What can occur with systemic administration of glucocorticoids?
- side effects more common--can be life-threatening | - host resistance to microbial and fungal infections lowered
37
Therapeutic principles of glucocorticoids?
1. Doses must be determined by trial and error and be re-evaluated. 2. Single dose virtually w/o harmful effects 3. Few days likely harmless, unless extreme doses 4. Prolonged therapy increases risk of potentially lethal side effects. 5. Treating only the symptoms 6. Adrenal insufficiency may occur w/abrupt cessation of prolonged high-dose therapy.
38
Glucocorticoid toxicity (from continued use of large doses)
- Primarily associated w/systemic administration - Increased susceptibility to infection (immune suppression) - peptic ulceration - behavioral disturbances - cataracts - osteoporosis and vertebral compression fractures - inhibition of growth
39
Glucocorticoid toxicity (from withdrawal or discontinuation of long-term use)
- reflect symptoms of acute adrenal insufficiency - fever - myalgia - arthralgia - malaise - death can occur with hypotension and shock
40
Calcineurin inhibitors
Cyclosporine | Tacrolimus (FK 506)
41
Cyclosporine
- Binds cyclophilin-->inhibits calcineurin activity - Blocks dephosphorylation events needed for cytokine gene expression and T cell activation - metabolized in liver - potential for drug interactions - long term therapy for transplants - major adverse effect: renal toxicity (must be distinguished from graft rejection in kidney transplants!) Nephrotoxicity can occur in up to 75% of patients
42
Tacrolimus
- Binds FKBP (FK506 binding protein)-->inhibits calcineurin activity - Blocks dephosphorylation events needed for cytokine gene expression and T cell activation - 100x more potent than cyclosporine - nephrotoxicity (similar adverse effects to cyclosporine)
43
Function of antiproliferative/antimetabolic drugs
Prevent clonal expansion of both B and T lymphocytes
44
Antiproliferative/antimetabolic drugs
Sirolimus | Mycophenolate mofetil
45
Sirolumus
- used in combo therapy for organ transplant rejection - Binds FKBP to inhibit mTOR. Blocks cell cycle progression from G1 to S phase - Dose dependent increase in cholesterol and triglycerides. Nephrotoxicity when in combination with cyclosporine. Increased lymphoma and infection risk. - Potential for drug interactions (substrate for cyp3A4)
46
Mycophenolate mofetil
- used in organ transplants - Metabolite is an inhibitor of IMPDH (needed for guanine nucleotide synthesis). B cells and T cells highly dependent on this pathway. - Toxicity: hematologic and GI. Leukopenia, diarrhea, vomiting.
47
Relationship between immunosuppressive therapy and cancer chemo
Overlap occurs between drugs for immunosuppression and cancer treatment drugs
48
Antibodies
Anti-thymocyte globulin (ATG) Muromonab-CD3 Daclizumab Basiliximab
49
Anti-thymocyte globulin (ATG)
- Prepared from hyperimmune syrum following immunization with human thymocytes - IG binds thymocytes in circulation-->causes lymphopenia and impaired T cell immune response - Toxicty: primarily ue to Ig being recognized as foreign resulting in serum sickness and nephritis. Anaphylaxis rare
50
Muromonab-CD3
- Used to prevent acute rejection of transplants - Mouse Ab binds to CD3 glycoprotein--> T cell receptor complex internalized and prevents further antigen recognition - Initial interaction with T cells leads to cytokine release by activating T cells (Cytokine release syndrome)--administration of glucocorticoids before admin reduces symptoms - Repeated use contraindicated (immune response occure to mouse Ab)
51
Daclizumab or basiliximab
- Anti-IL2 receptor (Anti-CD25) Ab, humanized in part - Used in organ transplants - Bind IL-2 receptor present on activatied, not resting T cells and block IL-2 mediated T cell activation events. - Toxicity: NO cytokine release syndrome. Lower incidence of lymphoproliferative disorders and opportunistic infections than many other immunosuppressive drugs. Anaphylactic reactions can occur.

IHO 5 (5 decks)

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