Immunosuppressants

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Author:
emac0408
ID:
167364
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Immunosuppressants
Updated:
2012-08-25 09:58:32
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Immunosuppressants
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Immunosuppressant Medication
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  1. Cyclosporine 
    • Calcineurin Inh:  prevents NF-AT from ^IL-2
    • Inh TC activation: 
    • Tx:  Organ Rejection, GvH, AutoI (RA)
    • Metab by CYP3A
    • Sides:  Nephrotoxic (glom vasoC, ischemic), HT
    • Interactions:  Glucocorticoids (inh CYP3A), Tacrolimus (^nephrotox)
  2. Tacrolimus
    • Calcineurin Inh:  prevents NF-AT from ^IL-2
    • Inh TC activation:  via FKBP-12
    • Tx:  Organ Rejection, GvH
    • Metab by CYP3A
    • Sides:  Nephrotoxic (glom vasoC, ischemic), Neurotoxic (tremor,HA,seizure), Hyperglycemia
    • Interactions:  Glucocorticoids (inh CYP3A), Cyclosporine (^nephrotox)
  3. Glucocorticoid
    • Inh Prolif & Act.:  inh lympho cell cycle, inh cytokine release (inflam)
    • Tx:  1st Line:  Organ Reject/GvH, RA, Crohn's
    • Sides:  Myopathy (prot catab), Hypergly, Osteoporosis/necrosis, Cushing Synd, HT (MR cross-reactive)
    • Interaction:  inh CYP3A (^cyclosporine/tacrolimus)
  4. Sirolimus (rapamycin)
    • Cytotoxic:  inh mTOR via FKBP-12 to inh IL-2R signal
    • Tx:  Organ Rejection w/ calcineurin inh or glucocort.
    • Sides:  Hyperlipidemia, BM suppression (pancytopenia)
    • ^nephrotox with cyclosporine (contraind w/ renal insuff)
  5. Mycophenolate Mofetil  (Cellcept)
    • Cytotoxic:  inh Purine Synth (inh Inosine MP-DHase
    • Tx:  Organ Rejection w/ calcineurin inh or glucocort.
    • Avoid Azathioprine
    • Sides:  BM suppression (leukopenia), GI (diarrhea/vomit)
    • Pro-Rx:  mycophenolic acid
  6. Azathiorpine (Imuran)
    • Cytotoxic:  false nucleotide (metab to 6-thio-IMP), inh DNA rep/transcr
    • Tx:  Organ Rejection, RA, Crohn's (very effective)
    • Sides:  Hepatotoxic, BM Suppression (pancytopenia)
    • Interaction:  Xanthine Oxidase Inh for gout (severe leukopenia)
  7. Methotrexate
    • Cytotoxic:  inh DHF Reductase (purine, serine, methionine:  interfere w/ DNA, RNA, and protein)
    • Tx:  Crohn's, RA, GvH, ChemoTx (high dose)
    • Sides:  Hepatotoxic, BM Depression (megaloblastic anemia)
  8. Cyclophosphamide
    • Cytotoxic:  Alkylating (cross-link DNA:  cytotox to Lymphos, can't rep/transcr)
    • Tx:  Organ Reject, chemoTx, AutoI, no affect on GvH
    • Sides:  Nausea/Vomit, toxic to rapid mitotics (BM, GI, infertility)
    • Pro-Rx (via CYP2B) 
  9. Thymoglobulin (Antithymocyte Globulin) 
    • Polyclonal Ab:  against many TC Ag (^complement/cell-mediated attack)
    • Tx:  Acute Renal Rejection
    • Sides:  Fever, HAMA devel
  10. Rhogam (Rho (D) Immune Globulin)
    • Polyclonal Ag: against Rho
    • Tx:  Rh incompatibility
  11. Muromonab-CD3 (OKT3)
    • mAb to CD3:
    • Tx:  Acute Allograft Reject, Steroid-resistant reject.
    • Sides:  Cytokine Release Syndrome (mild storm), HAMA devel
  12. Alefacept (Amevive)
    mAb for CD2:
  13. Etanercept (Enbrel)
    • mAb TNFa/B Blocker:  Suppress IL-1/6 release and adhesion mol.
    • Tx:  RA (can be used with Methotrexate)
    • Sides (not on exam):  Infusion Rxt (fever, urticaria, hypoT, dyspnea), erythema, pruritic, infection (deadly upper resp/urinary)
  14. Adalimumab (humira)
    • mAb TNFa Blocker:  suppress IL-1/6 release and adhesion mol. (same as Golimumab (simponi))
    • Tx:  RA
    • Sides (not on exam):  Infusion Rxt (fever, urticaria, hypoT, dyspnea), erythema, pruritic, infection (deadly upper resp/urinary)
  15. Golimumab (Simponi)
    • mAb TNFa Blocker:  suppress IL-1/6 release and adhesion mol.  (same as Adalimumab(humira))
    • Tx:  RA
    • Sides (not on exam):  Infusion Rxt (fever, urticaria, hypoT, dyspnea), erythema, pruritic, infection (deadly upper resp/urinary)
  16. Certolizumab (Cimzia)
    • mAb TNFa Blocker:  suppress IL-1/6 release and adhesion mol. (same as Infliximab (remicade))
    • Tx:  RA, Crohn's
    • Sides (not on exam):  Infusion Rxt (fever, urticaria, hypoT, dyspnea), erythema, pruritic, infection (deadly upper resp/urinary)
  17. Infliximab (Remicade)
    • mAb TNFa Blocker:  suppress IL-1/6 release and adhesion mol.  (same as Certolizumab (cimzia))
    • Tx:  RA, Crohn's
    • Sides (not on exam):  Infusion Rxt (fever, urticaria, hypoT, dyspnea), erythema, pruritic, infection (deadly upper resp/urinary)

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