Immuno pharm Flashcards
What is the major adverse effect of calcineurin inhibitors (Tacrolimus and Cyclosporine)
highly nephrotoxic
How do Calcineurin inhibitors (Tacrolimus F506 and Cyclosporine) function?
Shut down T cell response by inhibiting production of IL-2 by sequestering Calcineurin
Adverse effects of Cyclosporine
Nephrotoxicity, hypertension, hyperlipidemia, neurotoxicity, gingival hyperplasia, hirsuitism
Adverse effects of Tacrolimus
Nephrotoxic, neurotoxic, gingival hyperplasia, increased risk of diabetes
Which two immunosuppressants bind FKBP
Tacrolimus and Rapamycin (Sirolimus)
Mechanism of Sirolimus (Rapamycin)
binds FKBP to block T cell activaiton and B cell differentiation by preventing response to IL-2
Major uses for Cyclosporine
Transplant rejection prophylaxis, psoriasis, RA
Major uses for Tacrolimus
Transplant rejection prophylaxis
Major use for Rapamycin (Sirolimus)
Kidney transplant rejection prophylaxis
Adverse effects of Rapamycin (Sirolimus)
Pancytopenia, insulin resistance, hyperlipidemia
Side effects of Daclizumab and Basiliximab
hypertension, edema, tremore
Use and function of daclizumab, basiliximab
Monoclonal antibodies to IL-2R, kidney transplant rejection prophylaxis
Which immuno suppressant is a precursor for 6-mercaptopurine and inhibits purine synthesis by inhibiting PRPP amiodotransferase?
Azathioprine
Uses for Azathioprine
Transplant rejection prophylaxis, RA, Crohn, glomerulonephritis
Side effects of Azathioprine
Leukopenia, anemia, thrombocytopenia
Which immunosuppressant is associated with invasive CMV infection
Mycophenalate mofetil
Mechanism of Mycophenolate mofetil
reversibly inhibit IMP dehydrogenase; halt purine synthesis of B and T cells
Clinical use of Mycophenolate mofetil
Transplant rejection prophylaxis, lupus nephritis
Adverse effects of mycophenolate mofetil
GI upset, pancytopenia, hypertension, hyperglycemia. Less nephro and neurotoxic
Mechanism of corticosteroids
Inhibit NFkappaB and suppress both B and T cell function by decreasing transcription of cytokines. Induce apoptosis of T lymphocytes
Filgrastim and Sargramostim use
Bone marrow recovery
Romiplostim, eltrombopag and Oprelvekin (IL-11) use
Thrombocytopenia
Interferon-beta use
Multiple sclerosis
Use of Traztuzumab
HER2/neu Antibody; breast cancer
Rituximab use
CD20 antibody; B cell lymphomas, CLL, RA, ITP
Cetuximab use
EGFR antibody; stage IV colorectal cancer, head and neck cancer
Bevacizumab use
VEGF antibody; colorectal cancer, renal cell carcinoma
Adalimumab, Certolizumab, Infliximab use
soluble TNF-alpha; IBD, RA, ankylosing spondylitis, psoriasis
Eculizumab use
target is C5; PNH
Natalizumab use
alpha4-integrin; MS, Crohn (can cause PML–demyelination– in pts with JC)
Abciximab use
gpIIb/IIIa; antiplatelet agent
Denosumab use
RANKL antibody; Osteoporosis
Palivizumab
RSV prophylaxis for high-risk infants
Ranibizumab, bevacizumab use
VEGF antibody; neovascular age-related macular degeneration
How can high-doses of corticosteroids cause neutrophilia and induced psychosis?
Cause demargination of neutrophils from blood vessel walls, leading to an increase in circulating neutrophils
Mechanism of Bortezomib (treatment for mulitple myeloma)
Inhibit 26s proteosome, allow buildup of pro-apoptotic factors that induce apoptosis in neoplastic cells
Mycophenolate mechanism
Selectively targets B and T cell proliferation, promotes T cell apoptosis by inhibiting IMP dehydrogenase (stops purine synthesis)
Used to treat CMV retinitis
Cidofovir
Cidofovir side effect
Nephrotoxicity manifesting as proteinuria or elevated creatinine
Inhibits nonstructural protein 5B (NS5B) an RNA-dependent RNA polymerase needed for Hep C
Sofosbuvir
Used in ganciclovir-resistant CMV and associated with severe neutropenia
Valganciclovir
Aprepitant is a ___ receptor antagonist used to treat chemotherapy-induced emesis
Neurokinin-1 receptor antagonist
Fosaprepitant is a ____ receptor antagonist used to treat chemotherapy-induced emesis
Neurokinin 1
Ondansetron and Granisetron are ____ receptor antagonists used to treat chemotherapy-induced emesis
5-HT3
Scopolamine is a ____ used to to treat motion sickness
antimuscarinic
Diphenhydramine, Meclizine and Promethazine are ___ used to treat motion sickness
Antihistamines
How do calineurin inhibitors (Tacrolimus or Cyclosporine) cause renal failure?
Lead to afferent and efferent arteriolar vasoconstriction in kidneys, leading to obligerative vasculopathy and scarring