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Pharmacology
Immunosuppressants
64
Pharmacology
Graduate
08/01/2014

Additional Pharmacology Flashcards

 


 

Cards

Term
What was wrong with early immunosuppressants?
Definition

were nonselective w/ general suppression of the entire immune system leading to death from infection

(opportunistic infection)

Term
T Cell inhibitor (non-specific)
Definition
adrenocorticoids (prednisone)
Term
Antigen receptor blocker
Definition
muronomab-CD3
Term
T-cell activation blockers
Definition

cyclosporine 

tacrolimus

Term
IL-2 receptor blockers
Definition

basiliximab

daclizumab

Term
IL-2 response blocker
Definition

sirolimus

everolimus

Term
Cell cycle inhibitors
Definition

azathioprine

mycophenolate mofetil

Term

What were the early anti-cancer drugs targeted at inhibiting cell proliferation of inflammatory/immunological cells?

very non-specific

Definition

methotraxate

cyclophosphamide

azathioprine

prednisone

Term
Adverse effects of prednisone
Definition

diabetogenic (hyperglycemia)

cataracts 

osteoporosis

hypertension

hypercholesterolemia

Term

???MOA-  T-cells most affect probably by lysis

suppression of DNA translation of genes involved w/ inflmmatory process

Definition

Adrenocorticoids/glucocorticoids

prednisone

Term
Mainstay for preventing rejection in transplantation and auto-immune disorders (RA, SLE, arthritis, asthma)
Definition

prednisone

adrenocorticoids/glucocorticoids

Term
Antithymocyte antibodys, what are the types mentioned?
Definition

antilymphocyte globulin

antithymocyte globulin (thymoglobulin)

Term
Binds to surface of circulating T lymphocytes, phagocytized --> lymphopenia & impaired T-cell responses
Definition
Antithymocyte globulin (thymoglobulin)
Term
Which antibody has an acute phase of allograft rejection
Definition

antithymocyte antibody

antithymocyte globulin

Term
What is the half-life of antithymocyte globulin?
Definition
3-9 days
Term
Antibodies against these can be formed
Definition
antithymocyte globulin
Term
What are the adverse effects of antithymocyte antibodies
Definition

chills/fever

decreased WBC

decreased platelets

skin rashes

Term
Murine monoclonal antibody against glycoprotein CD3 antigen on human T cells
Definition
Muromonab-CD3
Term
Muromonab - CD3 uses
Definition

acute allograft rejection- renal, cardiac, & hepatic transplants

deplete T cells from donor bone marrow prior to transplant

 

Term
Initial treatment cytokine storm therefore pre-medicate with prenisolone, diphenhydramine, and acetaminophen
Definition
Muromonab-CD3
Term
Adverse effects - mild flu to anaphylactic rxn due to cytokine release, headache, fever, encephalopathy
Definition
Muronomab-CD3
Term
What are the contraindications of Muronomab-CD3?
Definition

pregnant

seizure

CHF patient

Term
____ is on human T-cells and it is the antibody that links to antigen presented to it. First step in inflammatory process
Definition
CD3
Term

Humanized monoclonal antibody against CD 52

Depletes T cells

Definition
Alemtuzumab
Term
Alemtuzumab uses
Definition
experimental in replacement of steriod
Term

Adverse effects: initial treatment "cytokine storm" therefore premedicate with prenisolone, diphenhydramine, and acetaminophen

(other one)

Definition
Alemtuzumab
Term
Adverse effects : anemia, neutropenia, pancytopenia
Definition
alemtuzumab
Term
Caution: increased B cell rejection/autoimmune disorders
Definition
Alemtuzumab
Term
Cyclosporine info
Definition

peptide isolated from fungus

inhibits cell mediated immune rxns

humoral immunity less effected

Term
MOA of cyclosporine
Definition

prevents de-phosphorylation of NFATc (cytoplasmic nuclear factor of activated T cells)

Thus inhibits production & subsequent release of IL-2 & induces activation of resting T cells

Term
usually administed (oral or IV) in combination with glucocorticoids to increase effectiveness
Definition
cyclosporine
Term
Cyclosporine uses
Definition

prevention of rejection of allogenic transplanted (kidney, liver, heart)

severe, active RA

recalcitrant psoriasis that does not response to other therapies

Term
what does allogenic mean?
Definition
a non-cell transplant
Term
Adverse effects: reversible nephrotoxity, viral infections (CMV) hirusitism, gingival hyperplasia, anaphylaxis, lymphoma
Definition

cyclosporine

 

Term
Why does cyclosporine have an adverse effect of reversible nephrotoxicity?
Definition
if taken with NSAIDS
Term
Same MOA & uses as cyclosporine
Definition
Tacrolimus
Term
Routes of administration of tacrolimus
Definition

oral

IV

topical

Term
Why is tacrolimus favored over cyclosporine?
Definition

decreased episodes of rejection

lower doses of glucorticoids can be used, reducing likelihood of infection

Term
Adverse effects: Nephrotoxicity, neurotoxicity, insulin dependent diabetes, anaphylaxis to vehicle
Definition

tacrolimus

more severe than cyclosporine

Term

Is tacrolimus or cyclosporine?

Much better immunosuppresent but comes with much bigger toxicity

Definition
tacrolimus
Term
Which IL-2 receptor blocker is chimerized?
Definition
basiliximab
Term
Which IL-2 receptor blocker is humanized?
Definition
daclizumab
Term
IL-2 receptor blockers MOA
Definition

anti CD-25 (IL-2 receptor)

IV only, long half lives (7 and 20 days)

renal transplantation

Term
Adverse effects of IL-2 blockers
Definition

mainly GI

malignancy not a problem

Term
IL-2 response blockers are used for?
Definition
renal transplantation
Term
IL-2 response blocker MOA
Definition

prevent IL-2 induced cell proliferation

acts synergistally w/ cyclosporine

SRL coated stents

Immunosuppresent effect can persist up to 6 months after cessation of therapy

Term
Adverse effects: hyperlipidemia, nephrotoxicity, headache, nausea, diarrhea
Definition

IL-2 response blockers

sirolimus

everolimus

Term
What is the "me too" drug to sirolimus?
Definition
everolimus
Term

IL-2 response blockers

instead of inhibiting synthesis of IL-2 they inhibit..

Definition
the proliferation
Term
6 mercaptopurine, fradulent nucleotide
Definition
azathioprine
Term
Lymphocytes predominatently are affected due to their rapid proliferation and dependence on de novo synthesis of purines required for cell division
Definition
Azathioprine
Term
Little effect on chronic immune response
Definition
azathioprine
Term
Therapeutic uses for azathioprine
Definition

adjust w/ other agents in prevention of rejection of solid organ transplants

severe RA unresponsive to other agents

Other autoimmune diseases: ITP, SLE, MS, Chrohns

Term
Routes of admin for azathioprine
Definition
IV or PO
Term

Adverse effects: fever, chills, N/V, anorexia, diarrhea, pancytpenia, secondry infection

 

Definition
azathioprine
Term
Which drug has increased toxicity w/ allopurinol
Definition

azathioprine

reduce dose of azathioprine

Term
Azathioprine is contraindicated
Definition
in pregnancy
Term
Warning/Precautions of using Azathioprine for chronic immunosuppresion
Definition

increases risk of neoplasia

mutagenic potential

possible hematologic toxicities

caution in pts w/ liver disease, renal impairment

monitor hematologic fxn closely

Term
Azathioprine is not to be given with...
Definition
ACE inhibitors
Term
Potent reversible inhibitor of inosine monophosphate dehydrogenase thus blocking de novo synthesis of guanosine phosphate (GMP)
Definition
myclophenolate mofetil
Term
Deprives rapidly proliferating T and B cells of GMP
Definition
mycophenolate mofetil
Term

Mycophenolate mofetil 

mycophenolic acid

Definition

rapidly absorbed in gut

glucuronidated and excreted in urine

Term
Adverse effects: pain, diarrhea, sepsis, lymphoma
Definition
Mycophenolate mofetil
Term
Concomitant administration w/ antacids of Mg/Al or cholestyramine decrease the absorption
Definition
mycophenolate motefil
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