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Heme-Onc Pharm
Antineoplastic drugs and antibodies
| Question | Answer |
|---|---|
| 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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