Question | Answer |
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 |
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 |
Basiliximab | Simulect - antibody against CD25 (IL-2 receptor) which will prevent activated T lymphocyte proliferation |
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 |
Azathioprine | Maintenance Immunosuppression - Antiproliferative drug -prodrug of 6-mercaptopurine - inhibition of DNA and RNA synthesis to inhibit lymphocyte proliferation - not first line! |
Mycophenolate mofetil | Cell-Cept - maintenance immunosuppression - prodrug of mycophenolic acid - inhibits IMPDH which interferes with purine metabolism required for lymphocyte development |
Myfortic | EC-MPS - enteric coated mycophenolic acid sodium - maintenance immunosuppression - inhibits IMPDH which interferes with purine metabolism required for lymphocyte development |
Cyclosporin | CYA - Neoral, Gengraft, Sandimmune, Sangcya - maintenance immunosuppression - inhibits calcium dependent calcineurin |
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 |
Neoral | CYA microemulsion to improve the variable GI absorption |
Prednisone or Methyprednisolone | General immunosuppressive with proposed action to inhibit IL-1 and IL-2 which decreases activation and proliferation of T-cells |
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 |
Everolimus | (EVER) - mTOR inhibitor - used to prevent rejection in kedney transplant - dosed with CYA and glucocorticoids ((maintenance immunosuppression) |
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) |
Induction Immunosuppression Regimens (High Risk Patients) | Thymoglobulin or
Alemtuzumab or
Basiliximab with MMF and glucocorticoids |
Induction Immunosuppression Regimens (Low Risk Patients) | Basiliximab (Simulect) |
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) |
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) |
Acute Cellular Rejection Medications | High Dose Methylprednisolone for 3 to 5 days
Murine Monoclonal Antibody (Orthodone OKT3)
Thymoglobulin - polyclonal AB
Alemtuzumab (Campath) - moAB |
Humoral Rejection | Plasmapheresis: remove pathogenic immunoglobulins
IV immunoglobulin (IVIG): inhibition/suppress AB production
Rituximab - for refractory cases - humanized CD20 MoAB to deplete B cells |
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 |
Leflunomide (LEF) | Used for RA - inhibits dihydroorotate dehydrogenase which intern inhibits lymphocyte proliferation
BBW: pregnancy, hepatic disease |
Hydroxychloroquine (HCQ) | Used for RA - inhibits migration of neutrophils and eosinophils, rheumatoid factor, acute phase reactants, and inhibits prostaglanding synthesis
BBW: ocular disease |
Sulfasalazine (SSZ) | Used for RA
BBW: G6PD dificiency, GI obstructions, porphyria |
Tofacitinib | Xeljanz - Used for RA - janus kinase inhibitor, prevents immune function and activation
BBW: infection, secondary malignancy |
Adalimumab | Humira - Used for RA
inhibits TNA-a
SC every 2 weeks (every week if not on MTX)
Usually used with MTX |
Certolizumab pegol | Cimzia - Used for RA
Inhibits TNA-a
SC every 2 weeks
Not given with MTX |
Etanercept | Enbrel - used for RA
inhibits TNF-a
SC every week
Contraindications: Sepsis
Not used with MTX |
Golimumab | Simponi - Used for RA
Inhibits TNF-a
SC every month
BBW: invasive fungal infections, TB
Given with MTX |
Infliximab | Remicade - Used for RA
inhibits TNF-a
Dose every 8 weeks with MTX
Contraindications CHF Class III-V |
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 |
Abatacept | Orencia - Used for RA
Selective co-stimulation modulator (inhibits Tcell activation)
Weight based IV every month |
Anakinra | Kineret - Used for RA
Inhibits IL-1 type I receptors
Dosed SC daily
Contraindication: hypersensitivity to E. coli |
Tocilizumab | Actermra - Used for RA
inhibits IL-6 receptors
Dose IV monthly (with or without MTX)
BBW: serious risk of infection |
RA Triple Therapy | MTX + HCQ + SSZ |
Gout Acute Attack | High-dose NSAID
Oral colchicine
Corticosteroids |
Gout Long Term treatment | Allopurinol
Febuxostat
Probenecid |
Allopurinol | Xanthine oxidase inhibitor - used for Gout
Underexcreters and overproducers
Renal dosing limits
Interaction with Warfarin, antiacids, and amoxicillin |
Febuxostat | Xanthine oxidase inhibitors - Used for Gout
Useful in underexcreters and overproducers
Expensive |
Probenecid | Uricosuric - used in Gout
Underexcreters only
Nephrolithiasis (must drink a lot to prevent this) |
Off label Uricosurics | losartan, fenofibrate |