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19 Cards in this Set

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Prednisone, Prednisolone, Methylprednisolone, Dexamethasone
-Glucocorticoid receptor agonist: immunosuppressant
-Mechanism: Inhibit COX-2 expression, induce lipocotins, active endogenous anti-inflammatory pathways
-Use: Negatively regulates cytokine transcription (among other things)
-Side: Impaired healing, hypertension, fluid retention, hyperglycemia, muscle atrophy, immunosuppression
-Contra: systemic fungal infection
Aziathioprine/Methotrexate
-Inhibitor of purine metabolism and immunosuppression in transplant and autoimmune diseases/cancer
-Mechanism: Inhibits IMDPH and DHFR, stops AMP/GMP synthesis
-Side: Pancreatitis, myelosuppression, hepatotoxicity, infection, gastritis
Contra: Pregnancy
Cyclophosphamide
-Covalent modifier of DNA, crosslinker, indicated for autoimmunity/cancer
-Mech: Alkylates DNA, prevent transcription and synthesis
-Side: myelosuppression, cardiomyopathy, hemm. cystitis, interstitial pneumonia, alopecia, GI upset, leukopenia, amennorhea
Toxic: Acrolein, causes hemm. cystitis, treated with mesna
Contra: Depressed bone marrow fxn
Cyclosporine
-Lymphocyte-signaling inhibitor, for Sjorgen syndrome (k. sicca)
-Mech: Binds cyclophilin, binds to calcineurin and stops phosphatase activity. NFAT keeps P and cannot translocate: stops IL-2
-Side: Nephro/neuro/hepatotox, infxn, HTN, hyperlipidemia, GI upset, hirsutism
Contra: Ocular infxn
Inter: Androgens incr. serum level, Rifampin/St. John's Wort decrease
Mycophenolic acid/Mycophenolate mofetil
-Cytotoxic agent use for transplant, RA, pemphigus
-Mech: Inhibitor of IMPDH, x guanosine
-Side: HTN, peripheral edema, GI hemm., leukopenia, myelosuppression, neutropenia, lymphoma, GI upset, headache
-Contra: Hypersensitivity to drug
-Inter: Iron reduces bioavailability
Leflunomide
-Cytotoxic agent/Immunosuppression of rheum. arthritis
-Mech: Inhibits dihydroororate reductase, x pyrimidine synthesis
-Side: HTN, hepatotox, interstitial lung disease, alopecia, diarrhea, rash
-Contra: Pregnancy
Tacrolimus
-Lymphocyte signal inhibitor for transplant and atopic dermatitis
-Mech: Binds to FKBP and complex inhibits calcineurin; stops IL-3/4. TNF and IFN-G
-Side: GI upset, alopecia, anemia, headache, insomnia, parethesia, tremor, thrombocytopenia
-Contra: Hypersensitive to castor oil in IV formula
-Route: IV/Topical
-Inter: St. John's Wort reduces serum levels
Sirolimus (rapamycin)
-Lymphocyte-signaling inhibitor for transplant and CAD stents
-Mech: Complexes with mTOR to stop IL-2 receptor protein synthesis
-Side: HTN, edema, thromboembolic disorder, hyperlipidemia, hepatotox, anemia, thrombocytopenia, headache
-Contra: Hypersensitivity to drug
-Inter: Coadmin with voriconazole incr. serum level
Etanercept
TNF inhibitor--TNF receptor dimer for RA, psoriasis, ankylosing spondylitis
-Mech: Binds to both TNF a and b
-Side: Myelosuppression, HF, infxn risk, URI, abdominal pain, vomiting
-Contra: Sepsis, HF, latent TB
Infliximab/Adalimumab
TNF antibodies for RA, Crohn's, ulcerative colitis, ank. spondy, psoriatic arthritis
-Mech: Antibody
-Side: Myelosuppression, HF, infxn risk, URI, abdominal pain, vomiting
-Contra: Sepsis, HF
Anakinra
IL-1 Inhibitor, treatment of rheumatoid arthritis via reducing bony erosions
Mech: Recombinant IL-1 receptor antagonist
Side: Neutropenia, infxn risk
Contra: Hypersensitivity to E coli derived proteins
Antithymocyte globulin
Immunosuppression in organ transplant
-Mech: Polyclonal antibodies against human T-cell epitopes
-Side: Increased infxn risk, cytokine release syndrome, HTN, anemia, penia
-Contra: acute viral illness, allergy to rabbit proteins
**Very broad immunosuppression
OKT3
Immunosuppressant for transplant
-Mech: Mouse monoclonal Ab against CD3
-Side: Increased infxn risk, cytokine release syndrome, HTN, anemia, penia
-Contra: HF, seizures, pregnancy, HTN
Daclizumab/Basiliximab
Immunosuppression in organ transplantation
-Mech: Ab to CD-25
-Side: Increased infxn risk, cytokine release syndrome, HTN, anemia, penia
-Contra: Hypersensitivity
Alemtuzumab
Immunosuppression in B-cell leukemia
-Mech: Ab to CD52
-Side: Increased infxn risk, cytokine release syndrome, HTN, anemia, penia
-Contra: Systemic Infxn, immunodeficiency
Alefacept
Immunosuppression to treat psoriasis
Mech: Binds to CD2, interrupts CD2/LFA-3 signaling, inhibits T cell activation
Side: Increased infxn risk, cytokine release syndrome, HTN, anemia, penia
Contra: HIV, low CD4
Abatacept
Inhibition of costimulation in refractory RA.
Mech: CTLA-4 fused to IgG1 binds to B7, preventing costimlation of T cells and anergy results
Side: COPD exacerbation, infxn risk, nausea, HA, UTI
Contra: Hypersensitivity
Inter: No concurrent with TNF inhibitors or anakinra -- increased infxn risk
Efalizumab
Blocks cell adhesion in treatment of chronic plaque psoriasis
-Mech: Mono Ab against LFA-1 inhibits LFA-1/ICAM-1 interaction, limiting T cell adhesion, migration, etc.
-Side: Lymphocytosis, alkaline phosphotase elevation, Ab formation
-Contra: Hypersensitivity
Natalizumab
Blocks cell adhesion in treatment of MS
-Mech: Monoclonal Ab against alpha-4 integrin inhibits immune cell interaction with VCAM-1
-Side: Rash, arthralgia, HA, fatigue, UTI, LRI, pneumonia
-Contra: PML