Immunosuppressants Flashcards
What are the T-cell inhibitors
Cyclosporine
Tacrolimus
Sirolimus
What is the Glucocorticoid
Prednisone
What are the Cytotoxic drugs
Mycophenolate mofetil
Cyclophosphamide
Azathioprine
MTX
What are the Immunosuppresive Abs
Muromonab Daclizumab Basiliximab Antithymocyte globulin RhoD Immunoglobulin
How do T-cell inhibitors work
Immunophilin ligands
Prevent activation, differentiation and cytokine release
What is Cyclosporine’s MOA
Bind cyclophilin and inhibit calcineurin
Decreased cytokine production
How does grapefruit juice increase the absorption of Cyclosporine
Inhibit P-glycoprotein
What metabolizes Cyclosporine
3A4
What does Cyclosporine interact with
Aminoglycosides (Amikacin)
Spironolactone
What are the main Cyclosporine AE
Gum hyperplasia
Hirsuitism
What are the other Cyclosporine AE
Nephrotoxicity
Hyperkalemia
Increased Lymphoma risk
Which T-cell inhibitor is a macrolide, 100x more potent than Cyclosporine
Tacrolimus
How does Tacrolimus act
Bind FK-506 inhibiting calcineurin
What does Tacrolimus absorption depend on
Bile
What is the main Tacrolimus AE
Neurologic effects
Does Tacrolimus cause gum hyperplasia and hirsutism
No
How does Sirolimus act
Inhibit mTOR and IL-2 action
What is Sirolimus used for
Prevent re-stenosis after angioplasty
What happens if you combine Sirolimus with Cyclosporine
Nephrotoxicity
What is the Sirolimus AE
Hyperlipidemia
How does Prednisone act
Inhibit cell cycle
Induce apoptosis in activated T-cells
Decrease cellular and humoral response
What are the Prednisone AE
Adrenal suppression, Cushing features
Ostoporosis
HTN, Peptic ulcer, Muscle wasting
What does Mycophenolate mofetil do
Inhibit IMP dehydrogenase
Blocks PURINE synthesis
Suppress B and T cell activation
What are the Mycophenolate mofetil AE
Diarrhea
Myelosuppression (neutropenia)
What is Azathioprine used for
Renal transplant
Autoimmune disease
What is Azathioprine converted to
6-MP
How does Allopurinol affect Azathioprine
Increases its concentration by inhibiting Xanthine oxidase
What is the Alkylating agent
Cyclophosphamide
What is Cyclophosphamide used for
Wegener’s
SLE
Autoimmune
What are the Cyclophosphamide AE
Hemorrhagic Cystitis
BM suppression
Tx for Cyclophosphamide Hemorrhagic Cystitis
Mesna
What is useful in RA
MTX
How does MTX act
Inhibit AICAR transformylase
What are the MTX AE
BM suppression
Mucositis
Hepatic fibrosis
What is the Anti-CD3 Ab
Muromonab
What is Muromonab used for
Acute graft rejection
What does Muromonab kill
T-cells
What are the Muromonab AE
HS
IL-2r antagonist used pre-op for transplantation
Daclizumab
Basiliximab
Human IgG Ab against Rh Ag
RhoD Immunoglobulin
What is RhoD Immunoglobulin used for
Prevent hemolytic disease of the newborn
