drugsss
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| ATGAM | Polyclonal Antibody - Depleting Induction
These antibodies coat the T-cells in the blood; these coated T-cells are then destroyed by the complement system
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| Thymoglobulin | Polyclonal Antibody - Depleting Induction
These antibodies coat the T-cells in the blood; these coated T-cells are then destroyed by the complement system
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| Basiliximab | Simulect - antibody against CD25 (IL-2 receptor) which will prevent activated T lymphocyte proliferation
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| CAMPATH-1H | Alemtuzumab - Monoclonal antibody - depleting Induction - acts directly at CD52 on all lymphocytes, NK cells, macrophages, monocytes, and granulocytes - activates complement and antibody dependent cellular cytotoxicity and lysis
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| Azathioprine | Maintenance Immunosuppression - Antiproliferative drug -prodrug of 6-mercaptopurine - inhibition of DNA and RNA synthesis to inhibit lymphocyte proliferation - not first line!
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| Mycophenolate mofetil | Cell-Cept - maintenance immunosuppression - prodrug of mycophenolic acid - inhibits IMPDH which interferes with purine metabolism required for lymphocyte development
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| Myfortic | EC-MPS - enteric coated mycophenolic acid sodium - maintenance immunosuppression - inhibits IMPDH which interferes with purine metabolism required for lymphocyte development
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| Cyclosporin | CYA - Neoral, Gengraft, Sandimmune, Sangcya - maintenance immunosuppression - inhibits calcium dependent calcineurin
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| MOA for Calcineurin Inhibitors (CYA and TAC) | Inhibition of calcium dependent calcineurin - results in reduction of transcription of cytokine jeans needed for T-cell activation (bind calcineurin hindering the phosphatase site resoling in no activation of NFAT and inhibition of IL-2 production
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| Neoral | CYA microemulsion to improve the variable GI absorption
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| Prednisone or Methyprednisolone | General immunosuppressive with proposed action to inhibit IL-1 and IL-2 which decreases activation and proliferation of T-cells
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| Sirolimus | (Rapamycin-RAPA) - Rapamune - inhibits m-TOR -> IL-2 timulates m-TOR to activate kinase enzymes that promote cell division - used to prevent acute rejection in kidney transplant with CYA and steroids (maintenance immunosuppression) - long half life
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| Everolimus | (EVER) - mTOR inhibitor - used to prevent rejection in kedney transplant - dosed with CYA and glucocorticoids ((maintenance immunosuppression)
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| Balatacept | Nulojix - selective co-stimulation blocker (signal 2) - prevents CD80 or CD86 on APC from interacting with CD28 on T-cells - inhibits T cell activation (maintenance immunosuppression)
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| Induction Immunosuppression Regimens (High Risk Patients) | Thymoglobulin or
Alemtuzumab or
Basiliximab with MMF and glucocorticoids
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| Induction Immunosuppression Regimens (Low Risk Patients) | Basiliximab (Simulect)
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| Maintenance Immunosuppression Regimens & target troughs | TAC + MMF or EC-MPS + PRED (TAC trough 9-15 ng/mL for first 3 months)
CYA + MMF or EC-MPS + PRED (CYA trough 150-300 ng/mL for 1st 3 months)
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| Minimized Protocols (Steroid Avoidance) Maintenance Immunosuppression Regimens & Target toughs | Low dose TAC + regular dose MMF or EC-MPS (TAC tough 8-12ng/mL for first 3 months; then progress to 3-7 ng/mL)
Low dose CYA +regular dose MMF or EC-MPS (CYA tough 100-200 ng/mL for first 3 months; progress to 50-100 ng/mL)
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| Acute Cellular Rejection Medications | High Dose Methylprednisolone for 3 to 5 days
Murine Monoclonal Antibody (Orthodone OKT3)
Thymoglobulin - polyclonal AB
Alemtuzumab (Campath) - moAB
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| Humoral Rejection | Plasmapheresis: remove pathogenic immunoglobulins
IV immunoglobulin (IVIG): inhibition/suppress AB production
Rituximab - for refractory cases - humanized CD20 MoAB to deplete B cells
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| Methotrexate (MTX) | Used for RA - immunosuppressant that inhibits dihydrofolate reductace which --> inhibits lymphocyte proliferation
Must always be supplemented with folic acid
BBW: pregnancy, concomitant NSAID use, hepatotoxicity
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| Leflunomide (LEF) | Used for RA - inhibits dihydroorotate dehydrogenase which intern inhibits lymphocyte proliferation
BBW: pregnancy, hepatic disease
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| Hydroxychloroquine (HCQ) | Used for RA - inhibits migration of neutrophils and eosinophils, rheumatoid factor, acute phase reactants, and inhibits prostaglanding synthesis
BBW: ocular disease
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| Sulfasalazine (SSZ) | Used for RA
BBW: G6PD dificiency, GI obstructions, porphyria
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| Tofacitinib | Xeljanz - Used for RA - janus kinase inhibitor, prevents immune function and activation
BBW: infection, secondary malignancy
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| Adalimumab | Humira - Used for RA
inhibits TNA-a
SC every 2 weeks (every week if not on MTX)
Usually used with MTX
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| Certolizumab pegol | Cimzia - Used for RA
Inhibits TNA-a
SC every 2 weeks
Not given with MTX
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| Etanercept | Enbrel - used for RA
inhibits TNF-a
SC every week
Contraindications: Sepsis
Not used with MTX
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| Golimumab | Simponi - Used for RA
Inhibits TNF-a
SC every month
BBW: invasive fungal infections, TB
Given with MTX
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| Infliximab | Remicade - Used for RA
inhibits TNF-a
Dose every 8 weeks with MTX
Contraindications CHF Class III-V
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| Rituximab | Rituxan - Used for RA
Binds to B-lymphocyte CD-20 surface antigens
Dose IV every 16-24 weeks (commonly given with methlyprednisolone to reduce injection site reaction
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| Abatacept | Orencia - Used for RA
Selective co-stimulation modulator (inhibits Tcell activation)
Weight based IV every month
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| Anakinra | Kineret - Used for RA
Inhibits IL-1 type I receptors
Dosed SC daily
Contraindication: hypersensitivity to E. coli
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| Tocilizumab | Actermra - Used for RA
inhibits IL-6 receptors
Dose IV monthly (with or without MTX)
BBW: serious risk of infection
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| RA Triple Therapy | MTX + HCQ + SSZ
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| Gout Acute Attack | High-dose NSAID
Oral colchicine
Corticosteroids
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| Gout Long Term treatment | Allopurinol
Febuxostat
Probenecid
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| Allopurinol | Xanthine oxidase inhibitor - used for Gout
Underexcreters and overproducers
Renal dosing limits
Interaction with Warfarin, antiacids, and amoxicillin
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| Febuxostat | Xanthine oxidase inhibitors - Used for Gout
Useful in underexcreters and overproducers
Expensive
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| Probenecid | Uricosuric - used in Gout
Underexcreters only
Nephrolithiasis (must drink a lot to prevent this)
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| Off label Uricosurics | losartan, fenofibrate
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