B29-31 Flashcards
Alkylating agent used as immunosuppressive?
Cyclophosphamide
in organ transplantation and rheumatic diseases
what about cyclophosphamide?
- nitrogen mustard
- CCNS
Antimetabolite that is used in immunosupressive agent?
methotrexate
what about methotrexate?
antagonists of folic acid
methotrexate MOA?
- inhibitor of dihydrofolate reductase
- interferes with nucleic acid and protein metabolism
methotrexate pharmacoKinetix?
- Oral and I.V.
- good tissue distribution (except CNS)
- not metabolized,
- clearance is dependent on renal function
- Adequate hydration is needed to prevent crystallization in renal tubules
Clinical uses of methotrexate as immunosupressive agent?
- rheumatoid arthritis
- psoriasis
drug used in Kidney, Liver and heart transplantation?
Mycophenolate Mofetil
Mycophenolate Mofetil MOA
- converted into mycophenolic acid –> inhibits inosine monophosphate dehydrogenase –> blocks GTP synthesis –> supresses both B and T lymphocyte activation
Mycophenolate Mofetil Clinical use?
kidney
Liver
heart transplantations
Mycophenolate Mofetil Toxicity?
G.I disturbances
neutropenia
cytotoxic drug used in IBD, rheumatic diseases and organ transplantation?
Azathioprine
Azathioprine MOA?
interferes with purine nucleic acid metabolism of immune cells
give example of disease modifying antirheumatoc drug?
leflunomide
Leflunomide MOA?
Inhibitor of dihydroorotate dehydrogenase –> inhibits pyrimidine synthesis –> interfere with the activity of T lymphocytes
Leflunomide administration?
orally
Leflunomide clinical uses?
rheumatoid arthritis
Inhibitors of cytokine gene expression, 5-ASA derivatives?
cyclosporin A tacrolimus sirolimus tofacitinib sulfasalazine
Calcineurin and mTOR Inhibitors?
Cyclosporine
tacrolimus
sirolimus
Cyclosporine A MOA?
binds to cyclophilin –> inhibits calcineurin –> inhibits the production of IL-2,3 IFN-g
Tacrolimus MOA?
binds to FKBP –> inhibit calcineurin –> inhibits the production of IL-2,3 IFN-g