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Therapeutics 2 Exam1


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
Created by: Newby549