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Heme-Onc Pharm

Antineoplastic drugs and antibodies

QuestionAnswer
When do you use a cell-cycle nonspecific drug? Low fixed growth
What drug is used to rescue from MTX? Leucovorin
MTX MoA Folic acid analog that inhibits dihydrofolate reductase (S phase)
MoA of 5-FU Pyrimidine analog in S phase
5-FU clinical use solid tumors and basal cell carcinoma (topically)
Rescue of 5-FU toxicity? thymidine
Doxorubicin side effect Cardiotoxicity
Clinical use of doxorubicin? Hodgkin's lymphoma
MoA doxorubicin Intercalates bet. DNA strands at C-G bonds; stops topoisomerase II
Bleomycin MoA G2-phase specific breakage of DNA strands with free radicals
Clinical use of bleomycin Testicular cancer and Hodgkin's
Side effect of bleomycin pulmonary fibrosis
Major side effect of cyclophosphamide hemorrhagic cystitis (prevented by coadmin of mesna and aggressive hydration)
Nitrosourea clinical use brain tumor (glioblastoma multiforme)
Side effect of vinblastine Myelosuppression (*Blasts* bone marrow)
What is side effect of vincristine? neurotoxicity, ototoxicity
MoA paclitaxel M phase: hyperstabilizes microtubules so mitotic spindles can't break down
MoA vincristine/vinblastine Blocks M phase by blocking polymerization of microtubules
Major side effect of Cisplastin Nephrotoxicity and acoustic nerve damage
What part of the cell do drugs work on if they act in M-phase? microtubules
MoA of tomoxifen ER antagonist in breast, blocking the binding of estrogen receptor ligands
What drug also has same MoA as tamoxifen? raloxifene
When is Imatinib used? CML with Philadelphia chromosome
Trastuzumab clinical uses monoclonal antibody agains HER-2; aka herceptin
Folic acid analog that inhibits dihydrofolate reductase Methotrexate
Pyrimidine analog that inhibits thymidylate synthase 5-fluorouracil
Inhibitor of de novo purine synthesis 6-mercaptopurine
Inhibits DNA polymerase cytarabine
Alkylating agents used to treat Non-Hodgkin lymphoma, breast and ovarian carcinoma. Notable side effect of hemorrhagic cystitis Cyclophosphamide, ifosfamide
Alkylating agent capable of crossing blood brain barrier Nitrosoureas (carmustine, lomustine)
Similar to alkylating agents; notable toxicities include nephrotoxicity and acoustic nerve damage Cisplatin, carboplatin
Alkylating agent used to treat CML Busulfan
Free radical generator; intercalates DNA to form strand breaks ("A" in ABVD treatment for Hodgkins) Doxorubicin, daunorubicin
Used to treat childhood tumors (Wilm's tumor, rhabdomyosarcoma, and Ewing's sarcoma) Dactinomycin (Actinomycin D; Children ACT out)
DNA-cleaving free radical generator which can cause life-threatening pulmonary fibrosis Bleomycin
Topoisomerase II inhibitor Etoposide
Steroid that triggers apoptosis Prednisone
Estrogen receptor antagonist Tamoxifen
Monoclonal antibody against HER-2 Trastuzumab
Philadelphia chromosome (bcr-abl) tyrosine kinase inhibitor Imatinib (Gleevec)
Binds tubulin, blocking polymerization of microtubules and mitotic spindle formation Vincristine, vinblastine
Binds tubulin, hyperstabilizing microtubules and blocking mitotic spindle formation Paclitaxel
Toxicity includes Cushing-like symptoms Prednisone
Used for "metastatic" breast cancer Trastuzumab
Increased risk of endometrial carcinoma Tamoxifen
Do not use with allopurinol 6-mercaptopurine (activated by xanthine oxidase; allopurinol is a xanthine oxidase inhibitor used to treat gout)
CNS toxicity Nitrosoureas (carmustine, lomustine)
Reversible myelosuppression with leucovorin rescue of healthy cells Methotrexate
SE: Neurotoxicity (areflexia, peripheral neuritis) paralytic ileus Vincristine (Vinblastine is notable for bone marrow suppression)
Antineoplastic used for therapeutic abortion Methotrexate
Androgen receptor antagonist Flutamide
Recombinantly produced cytokine used to treat hairy cell leukemia Interferon alpha
GnRH agonist used for the treatment of metastatic prostate carcinoma Leuprolide, Goserelin, Nafarelin
Monoclonal antibody used for treatment of low grade non-Hodgkin lymphoma Rituximab
Forms a complex between topoisomerase II & DNA Etoposide (Inhibits topoisomerase II)
Alkylates DNA, toxicity = pulmonary fibrosis, hyperpigmentation Busulfan
Fragments DNA, toxicity = pulmonary fibrosis, skin changes Bleomycin (MOA: induces free radicals- breaks DNA strands)
Blocks purine synthesis, metabolized by xanthine oxidase 6-mercaptopurine
Cross-links DNA, nephrotoxic, ototoxic Cisplatin & carboplatin
Nitrogen mustard, alkylates DNA Cyclophosphamide
Folic acid analog that inhibits dihydrofolate reductase Methotrexate
Prevents microtubule disassembly (stabilizes) Paclitaxel
Intercalates DNA, produces oxygen free radicals, cardiotoxic Doxorubicin & daunorubicin
DNA alkylating agents used in brain cancer nitrosoureas (carmustine, lomustinem, semustine, streptozocin)
Prevents microtubule assembly Vincristine & Vinblastine
Inhibits thymidylate synthase--> decreased nucleotide synthesis 5-fluorouacil
SERM—blocks estrogen binding on ER (+) cells tamoxifen, raloxifene
MOA similar to antiviral acyclovir & foscarnet cytarabine (MOA: inhibits DNA polymerase)
MOA similar to fluoroquinolones Etoposide (MOA: inhibits tomoisomerase II)
MOA similar to trimethoprim Methotrexate - folic acid analog that inhibits dihydrofolate reductase
Monoclonal antibody against HER-2 (ER-B2) Trastuzumab
MOA: free-radical induced DNA strand breakage Bleomycin
Reversible with leucovorin Methotrexate (reverses myelosuppression)
Treatment for choriocarcinoma Methotrexate
Treatment for testicular cancer Etoposide-teniposide, bleomycin, cisplatin ("Eradicate ball cancer")
Inhibits ribonucleotide reductase Hydroxyurea
SE: Hemorrhagic cystitis Cyclophosphamide
Antibody against philadelphia chromosome Imatinib
Side effects of prednisone Cushing-like symptoms, immunosuppression, psychosis
Created by: srebeiro
 

 



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