IMMUNOLOGY- Immunosuppressants Flashcards
What are the immunosuppressants?
Agents that block lymphocyte activation and proliferation
Which is the clinical use for immunosuppressants?
Reduce acute transplant rejection by suppressing cellular immunity
Which is the recommendation to have greater efficacy with decreased toxicity for immunosuppressants use?
Frequently combined to achive them
Which is the risk of Chornic suppression with immunosuppressants?
Increased risk of infection and malignancy
These drugs are immunosuppressants
Cyclosporine Tacrolimus Sirolimus (Rapamycin) Basiliximab Azathioprine Glucocorticoids
This is the mechanism of action of Cyclosporine
Calcineurin inhibitor; binds cyclophilin
Blocks T cell activation by preventing IL-2 transcription
Which are the clinical use for Cyclosporine?
Transplant rejection, prophylaxis, psoriasis, rheumatoid arthritis
Which are the possible toxic effects of Cyclosporine?
Nephrotoxicity Hypertension Hyoerlipidemia Hyperglycemia Tremor Hirsutism Gingival hyperplasia
Which are the higher risk of Calcineurin inhibitors?
Highly nephrotoxic
Who are consider Calcineurin inhibitors?
Cyclosporine
Tacrolimus
How does Tacrolimus works?
Binds FK506 binding protein (FKBP)
Blocks T cell activation by preventing IL-2 transcription
This is the use for Tacrolimus
Transplant rejection prophylaxis
Which could be the secondary effects of Tacrolimus?
Similar to cyclosporine, ↑ risk of diabetes and neurotoxicity; no gingival hyperplasia or hirsutism
Which drugs bind to FKBP?
All -limus drugs
Who is inhibited with Sirolimus?
mTOR inhibitor
How else is Sirolimus known?
Rapamycin
This is the mechanism of Sirolimus
Binds FKBP
Blocks T cell activation and B cell diferentiation by preventing IL-2 signal transduction
When is recommended Sirolimus?
Kidney transplant rejection prophylaxis
When is consider that Rapamycin caused toxicity?
Anemia Thrombocytopenia Leukopenia Insulin resistance HyperlipidemiaIs
Is sirolimus nephrotoxic?
No
With which medicine is Sirolimus synergistic?
Ciclosporine
This is an alternative of using Sirolimus
Drug eluting stent
How does Basiliximab works?
Monoclonal antibody; blocks IL- 2R
When is recommended to use Basiliximab?
Kidney transplant rejection prophylaxis
These are secondary effects of Basiliximab
Edema, hypertension, tremor
This immunosuppressant is antimetabolite precursor of 6 mercaptopurine
Azathioprine
How does Azathioprine works?
Inhibits lymphocyte proliferation by blocking nucleotide synthesis
These are the clinical use for Azathioprine
Transplant rejection prophylaxis
Rheumatoid arthritis
Chron disease
Glomerulonephritis
Which are the possible toxic efects of Azathioprine?
Leukopenia
Anemia
Thrombocytopenia
Who degrades 6 MP?
Xanthine oxidase
Who increases 6 MP toxicity?
Allopurinol
What is inhibited by Glucocorticoids?
Inhibit NF- kB
What is suppressed by Glucocorticoids?
Both B and T cell function by ↓ transcription of many cytokines