immunosuppressants/anti-neoplastic agents Flashcards
methotrexate
MOA: folic acid analog, inhibits dihydrofolate reductase
USE: cancer, RA, IBD, psoriasis, abortion
ADR: myelosuppression (leucovorin), teratogen, macrovesicular fatty change in liver
5-FU
MOA: pyrimidine analog that binds folic acid, inhibits thymidylate synthase
USE: cancer
ADR: myelosuppression (leucovorin), photosensitivity
cytarabine
MOA: pyrimidine analog, inhibits DNA polymerase
USE: leukemia, lymphoma
ADR: panCYTopenia
6-MP, azathioprine
MOA: purine analogs, activated by HGPRT
USE: RA, SLE, preventing organ rejection, IBD, leukemia
ADR: myelosuppression
dactinomycin
MOA: intercalates in DNA
USE: childhood tumors
ADR: myelosuppression
doxorubicin
MOA: generates free radicals, intercalates in DNA and breaks it
USE: cancer
ADR: dilated cardiomyopathy (use dexrazoxane to prevent), myelosuppression
bleomycin
MOA: free radicals break DNA strains
USE: cancer
ADR: pulmonary fibrosis, skin changes
cyclophosphamide
MOA: alkylating agent
USE: cancer
ADR: myelosuppression, hemorrhagic cystitis (mesna)
busulfan
MOA: cross-links DNA
USE: CML, bone marrow ablation before transplantation
ADR: severe myelosuppression, pulmonary fibrosis
cisplatin, carboplatin
MOA: cross-links DNA
USE: cancer
ADR: nephrotoxicity, acoustic nerve damage (prevent with amifostine and chloride diuresis)
etoposide, teniposide
MOA: inhibits TOPOisomerase II
USE: cancer
ADR: myelosuppression, alopeica
tamoxifen, raloxifene
MOA: SERM antagonist in breast, agonist in bone
USE: breast cancer, osteoporosis
ADR: hot flashes, risk of endometrial cancer (only tamoxifen)
trastuzumab
herceptin
MOA: HER-2 antibody
USE: HER-2 breast cancer, gastric cancer
ADR: cardiotoxicity, “HEARTceptin”
rituximab
MOA: CD20 antibody
USE: cancer, RA, ITP
ADR: risk of PML
vemurafenib
MOA: inhibits BRaf kinase
USE: metastatic melanoma
bevacizumab
MOA: VEGF antibody
USE: cancer
ADR: hemorrhage, impaired would healing
cyclosporine
MOA: calcineurin inhibitor, binds cyclophilin, prevents IL-2, blocks T-cell activation
USE: transplant rejection prophylaxis, psoriasis, RA
ADR: nephrotoxicity, gingival hyperplasia, hirsutism, others
tacrolimus
MOA: calcineurin inhibitor, binds FKBP
USE: transplant rejection prophylaxis
ADR: nephrotoxicity, risk of DM
rapamycin
sirolimus
MOA: mTOR inhibitor, binds FKBP, blocks IL-2….
MOA: kidney transplant rejection prophylaxis
ADR: non-nephrotoxic
basiliximab
MOA: IL-2 antibody
USE: kidney transplant rejection prophylaxis
ADR: edema, HTN, tremor
azathioprine
MOA: precursor of 6-MP, inhibits lymphocyte proliferation by blocking nucleotide synthesis
USE: transplant rejection, RA, Crohn, other autoimmune
glucocorticoids
MOA: inhibit NF-kB to suppress B and T cell function by decreasing transcription of cytokines
use of IFN-alpha
HBV, HCV, kaposi, hairy cell leukemia, condyloma acuminatum, renal cell carcinoma, malignant melanoma
use of IFN-beta
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