INMUNOSUPRESSANTS Flashcards
What are immunosuppressants
Medications that block LYMPHOCYTE ACTIVATION/PROLIFERATION
What are immunosuppressants used for
- Acute rejection prevention
- Treatment of Autoinmune disorders
Chronic use of immunosuppressants is associated to
- Increased risk of cancer
- Increased risk of infections
Glucocorticoids mechanism of action
- Inhibition of T-cell activations
- Inhibition of Transcription of Inflammatory Cytokines
Cytostatic Agents mechanism of action
Inhibition of replication of Inmune cells
Monoclonal Antibodies mechanism of action
Inhibition of cell function by:
- Inhibition of required protein
- Stimulation of cell death
Inmunophilins acting drugs mechanism of action
Inhibition of calcineurin during T-Cell activation (IL-2)
Which protein do glucocorticoids inhibit?
NF-KB
When NF-KB is inhibited, what process is impaired?
Activation of Transcription Factor for:
- Cytokines
- Receptors
Chronic use of glucocorticoids
- CUSHING DISEASE
- Diabetes
OSTEOPOROSIS - Avascular necrosis of the femur
Cyclosporin mechanism of action
Inhibition of calcineurin
Tacrolimus mechanism of action
Inhibition of calcineurin
How do Cyclosporin and Tacrolimus inhibit calcineurin
Binding to Cyclophilin A
Inhibition of Calcineurin by Tacrolimus and Cyclosporin produce decrease in production of __________
IL-2
Cyclosporin is associated with which adverse effects?
- NEPHROTOXICITY
- Also Hypertension, Hyperlipidemia and Gingival Hyperplasia
Sirolimus mechanism of action
mTOR inhibitor = inhibition of signal transduction cascade of IL2
Sirolimus is associated with
PANCYTOPENIA
Diabetes and Hyperlipidemia
Sirolimus is mainly used in
Kidney transplanted patients and Drug eluding stent
Sirolimus, Tacrolimus and Cyclosporine are
Inmunophilins acting drugs
Azathriopine mechanism of action
Antimetabolite (6-mercaptopurine) = INHIBITION OF PURINE SYNTHESIS (DNA SYNTHESIS)
Azathriopine is an example of
Cytostatic agent
Azathriopine’s impaired DNA Synthesis leads to
DECREASED Lymphocyte proliferation
Azathioprine’s adverse effects
PANCYTOPENIA
ANEMIA
Which Immunosuppressant should not be coadministered with allopurinol
Azathioprine
Mycophenolate mofetil mechanism of action
Inhibition of IMPDH (Required for purine’s synthesis)
Mycophenolate mofetil’s adverse effects
PANCYTOPENIA
INCREASED RISK OF CMV infections