Card Set Information
Lecture Notes Pharm4
What is azathioprine?
High toxicities prevent long-term use
What is Cyclosporine?
--> CD4 & CD8 T-cells
High affinity to cyclophilin
What's the metabolism of Cyclosporine?
Hepatic CYP3A4 metabolism
What's the therapeutic uses/toxicity of Cyclosporine?
: transplants, autoimmune disorders
, neuro, Acute Tubular Necrosis, Lymphomas
What is Calcineurin?
Dephosphorylation of NFAT --> IL-2 activation
What's the difference between acute/chronic toxicities of cyclosporin A?
Acute - reversable
Chronic - irreversible
What's the absorption of Cyclosporin A?
Oral; different for various people (measure!!)
NARROW THERAPEUTIC RANGE
Potent Calcineurin Inhibitor
What's the MoA of tacrolimus?
Binding to FKBP-12 --> calcineurin inhibition
What are metabolisl considerations of tacrolimus?
Shorter half-life than cyclosporine; 2x daily
What's the clinical use of tacrolimus?
Prophylaxis after transplans
Graft rejection Tx
What is sirolimus?
Cell Proliferation Inhibitor
What's the MoA of sirolimus?
Bind to FKBP-12 --> inhibit mTOR
Lack of response to growth stimulator signals
What are uses for sirolimus?
Prevent acute regection
prevent neointimal proliferation following stent placement in coronary arteries
What's mycophenolate mofetil?
Inhibitor of inosine monophosphate dehydrogenase
Prevent de novo purine biosynthesis
What are clinical uses for mycophenolate mofetil?
Renal & heart transplants
What are daclizumab & basiliximab
Bind to a-chain at IL-2 receptor
What toxicity is associated with basiliximab?
Block ε chain of T cell CD3
What's the use of Muromonab?
Reverse rejection of heart, liver, kidney rejection
What's MoA of abatacept?
Bind to CD80 & CD86
Prevent CD28 T-Cell activation
What's the MoA of leflunomide?
Inhibition of dihydroorotate -> pyrimidine biosynthesis
What's the clinical use of leflunomide?
What are toxicities of leflunomide?
Diarrhea, nausea, hepatotoxicity
What's the clinical use of Thalidomide?
erythema nodosum leprosum
What are toxicities of thalidomide?
What's the MoA of infliximab?
Ab against TNFa
Chron's, UC, RA, Psoriasis
What are toxicities of infliximab?
Increased infection (TB, HBV reactivation)
What's the MoA of etanercept?
Recombinant TNF receptor to soak up free TNF
What are uses of etanercept?
RA, ankylosing spondylitis, psoriasis
What are toxicities of etanercept?
What's the MoA of natalizumab?
Ab against antibody against α4β1-integrin
Inhibit lymphocyte migration
What's the use of natalizumab?
What's an associated risk from Natalizumab?
JC virus induced PML
What's the MoA of Azathiprine?
Purine analog used to interupt de novo purine synthesis
Combination therapy of RA --> leukopenia
What's the MOA of Fingolimod?
Block migration of lymphocytes from LN
What's the MoA of glatiramer?
Mix of AAs similar to myelin basic protein
What's the MoA of Lymphocyte Immune Globulin?
Ab to T-cell surface antigens
Block cell surface receptors
What's the MoA of Immune globulin?
Human IgG to replace Abs in immune deficiencies
What's the MoA of Anakinura?
IL-1 receptor antagonist
: bacterial infection
What's the Use of IFN-b?
What's epoetin alfa?
Stimulate RBC synthesis in anemic pts
What's darbepoetin alfa?
EPO analogue with longer half life
What's the risk with EPO analogues?
Cancer - stimulate tumor cell proliferation
Renal Failure - CVA