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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)
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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)
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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)
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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)
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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
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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)
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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)
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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)
-
Thymoglobulin (Antithymocyte Globulin)
- Polyclonal Ab: against many TC Ag (^complement/cell-mediated attack)
- Tx: Acute Renal Rejection
- Sides: Fever, HAMA devel
-
Rhogam (Rho (D) Immune Globulin)
- Polyclonal Ag: against Rho
- Tx: Rh incompatibility
-
Muromonab-CD3 (OKT3)
- mAb to CD3:
- Tx: Acute Allograft Reject, Steroid-resistant reject.
- Sides: Cytokine Release Syndrome (mild storm), HAMA devel
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Alefacept (Amevive)
mAb for CD2:
-
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)
-
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)
-
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)
-
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)
-
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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