Imunosuppressants

Question 1

What are the uses of Immunosupressant drugs?

Answer 1

Transplantation
-prophylactic
-acute rejection
Autoimmune diseases
-lupus or RA
Inflamatory diseases
-UC or CD

Question 2

What are the major classes of immunosupressive agents?

Answer 2

GLucocorticoids
Calcineurinn inh.
Anti-proliferative/Anti Metabolic
Biologicals (Ab)

Question 3

Steroids

Answer 3

A common multiple ring structure

Question 4

Why is Corticosteroid an incorrect term for Immunosupressive drugs

Answer 4

Adrenal cortex secretes Glucocorticoids and mineralocorticoids

Question 5

How do glucocorticoids cause Genomic effects?

Answer 5

Bind to cytosolic receptors > Nucleus > Bind to DNA

Question 6

How do glucocorticoids cause Non-Genomic effects?

Answer 6

Can influence cell signaling pathways and intercalate into the cell membraneto alter ion transport. RAPID immunosupression

Question 7

What are the effects of Glucocorticoids?

Answer 7

Dec. in peripheral blood lymphocytes
DR key pro-inflammatory cytokines
Inhibit IL-2 production by T cells
Reduce Neutrophil chemotaxis

Question 8

What are the Theraputic uses of Glucocorticoids?

Answer 8

Prevent and Treat transplant rejection
Treat GVHD
Block first dose Cytokine storm
Treat AI disorders such as RA, SLE, etc

Question 9

WHat are the Adverse effects of Glucocorticoids

Answer 9

Potential Disabling and LT effects including growth retardation in children
poor wound healing
HTN
Avascular Necrosis
Cataracts
Hyperglycemia
Adrenal Crisis upon rapid discontinuation

Question 10

What is the Standard prototype Glucocoirticoid?

Answer 10

Prednisone

Question 11

What is the Standard Low dose GLC?

Question 12

What is the Standard Med dose GLC?

Answer 12

> 7.5mg but

Question 13

What is the Standard High dose GLC?

Answer 13

> 30mg but

Question 14

What is the Standard Very High dose GLC?

Answer 14

> 100 mg prednisone eq/day

Question 15

What is the Standard Pulse Therapy dose GLC?

Answer 15

> 250 mg prednisone eq/day

Question 16

What is the best drug for Preventing transplant rejection?

Answer 16

Cyclosporine

Question 17

What is the MOA of Cyclosporine?

Answer 17

Suppresses T-Cell mediated immunity

Prevents IL-2 Production

Question 18

What is the utilization for cyclosporines?

Answer 18

Prophylaxis for Organ transplant
RA
Psoriasis
Combined with other agents, esp glucocorticoids
Not usually given to renal transplant Pts bc of nephrotox

Question 19

What are the adverse rxns of Cyclosporine?

Answer 19

Renal Dysfunction, Htn…

CSN can be increased with Grapefruit juice ingestion

Question 20

What is the prefered Calcineurin inhibitor for transplantation?

Answer 20

Tacrolimus. Easier to monitor blood levels

Question 21

What type of rejection is treatable by immunosupressants?

Answer 21

Acute Rejection!

Question 22

What type of Immunosupressant is Azathioprine?

Answer 22

Anti-proliferative and anti-metabolic agent

Question 23

What is the MOA of Azathioprene?

Answer 23

Inhibits lymphocyte proliferation and blocks the de novo pathway of purine synth is blocked

Question 24

What is the theraputic use of Azathioprene?

Answer 24

Prevent Organ transplant rejection

Crohns, RA, MS, TPurpura, Hemolytic anemia

Question 25

What is the MOA of Mycophenolate Mofetil?

Answer 25

Inhibits inosine monophosphate dehydrogenase(inhibits lymphocytes

Question 26

Whao should not take Mycophenolate Mofetil?

Answer 26

Pregnant women!

Question 27

What is the MOA of Sirolimus?

Answer 27

Inhibits T lymphocyte Proliferation via inhibition of mTOR. In. of G1-S phase

Question 28

What is the Theraputic use of Sirolimus

Answer 28

Prevents Organ transpplant rejection w/ GCC | In renal transplant recipients that can't tolerate calcineurin

Question 29

What is the adverse effect of Sirolimus

Answer 29

``` Anemia, Leukopenia, thrombocytopenia Hypokalemia, GI Delayed Wound healing Inc. Cancer risk ```

Question 30

What suface marker do all T cells have?

Answer 30

CD3

Question 31

What is the MOA of anti-thymocyte Globulin?

Answer 31

Depletes circulating lymphocytes - Complement - Binding to cell and inhibiting lymph functions

Question 32

What are the theraputic uses of A-Thymocyte Globulin?

Answer 32

Induction immunosupression | Tx of acute rejection of solid organ transplants

Question 33

What are the Adverse rxns to A-thymocyte globulins

Answer 33

Serum sickness, etc...

Question 34

What is the MOA of Muromonab?

Answer 34

T cell depletion through complement or bind to CD3

Question 35

Pros/cons of Muromonab.

Answer 35

Very fast! | Can only use once bc the body can make Abs toward this Ab.

Question 36

Adverse Rxns to muromonab?

Answer 36

Cytokine Storm | Serum sickness

Question 37

What are the Anti TNF-alpha Reagents and MOA?

Answer 37

Infliximab-human constant region and murine var region Adalimumab-recombinant human IgG1 monoclonal Etancercept-ligand binding portion of TNF-alpha receptor fused to the Fc portion of human IgG1

Question 38

What are the Theraputic uses of Anti TNF-alpha Reagents?

Answer 38

RA, Crohns, UC, Ankylosing Spondylitis, plaque psoriasis, psoriatic arthritis

Question 39

What are the Adverse Rxns to Anti TNF-alpha Reagents?

Answer 39

Risk for serious infections | Risk for lymphomas and other malignancies