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41 Cards in this Set
- Front
- Back
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Types of Cancer Chemotherapy:
... - These are the drugs most associated with cancer treatment. ... - These drugs are especially important in the treatment of breast and prostate cancer. ... - These are drugs with more specific molecular and enzymatic targets on or in cancer cells. ... - These drugs include copies of human cytokines that stimulate the immune system. |
Classic Chemotherapy (Cytotoxic Drugs)
Hormone Therapy Targeted Therapy Immune Therapy |
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Classic Chemotherapy: ...
Form covalent bonds to nucleic acids which cause cross-linking of DNA strands and inhibition of DNA replication. Non-phase-specific. |
Alkylating agents
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Classic Chemotherapy: alkylating agents
... -originally known as nitrogen mustard. -birth of modern cancer chemo in 1946 -uncommonly used today -myelosuppression, N/V, amenorrhea, azoospermia, increased risk of AML |
Mechlorethamine (Mustargen)
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Alkylating agents:
... and ... -cause hemorrhagic cystitis (which is prevented with hydration and ...) -pro-drugs, converted in liver to active forms. -commonly used in lymphoma, breast cancer, autoimmune disorders (...); testicular cancer, lymphoma, sarcoma (...) -N/V, hemorrhagic cystitis, myelosuppression, nephrotoxicity |
Cyclophosphamide (Cytoxan) and Ifosfamide (Ifex)
mesna Cytoxan Ifex |
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Classic Chemotherapy: ...
Act by interfering in nucleic acid synthesis, thus, interfering with DNA synthesis. Phase specific, most active in ...-phase. |
Antimetabolites
S |
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Classic Chemotherapy: Antimetabolites
... - First used in acute lymphoblastic leukemia -First chemotherapy cure of a metastatic solid neoplasm, GTD -Inhibits dihydrofolate reductase, an enzyme that acts on folic acid to produce reduced folate products needed in DNA synthesis. (... Rescue) - Used in acute lymphocytic leukemia, GTD, lymphoma, osteosarcoma, rheumatoid arthritis. - N/V, mucositis, myelosuppression, nephrotoxicity (in high doses). |
Methotrexate (Rheumatrex®) (MTX)
Leucovorin |
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Antimetabolites:
... - First chemotherapy drug shown to affect survival in metastatic and operable colorectal cancer. -Inhibits thymidylate synthase, thus blocking thymidine synthesis, an important component of DNA synthesis (by CIVI). Also, inhibits RNA synthesis (by IV bolus). - Used in colorectal cancer, breast cancer, esophageal cancer, head and neck cancer. - Mucositis, hand-foot syndrome, N/V, diarrhea, myelosuppression. |
Fluorouracil (Adrucil®) (5-FU)
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Antimetabolites:
... - Part of 7 + 3 regimen for AML induction -Damages DNA by multiple mechanisms. - Used in AML, ALL, and NHL. -Myelosuppression, mucositis, N/V, cerebellar toxicity (high doses), conjunctivitis (high doses). |
Cytarabine (Cytosar-U®) (cytosine arabinoside) (ARA-C)
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Antimetabolites:
... -increased survival rate in slow growing cancer - Revitalized interest in treating CLL and indolent NHL. - Damages DNA by multiple mechanisms. -Used in CLL, indolent NHL, and relapsed AML. - Myelosuppression, lymphopenia, opportunistic infections (give ... with this drug), autoimmune hemolytic anemia. |
Fludarabine (Fludara®)
Septra |
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Classic Chemotherapy:
Antitumor Antibiotics: ... Act by intercalation of adjoining nucleic acid pairs in DNA, causing DNA strand breakage. Also, inhibit topoisomerase II, the DNA repair enzyme. Non-phase-specific. Is notorious for causing ... |
Anthracyclines
heart failure |
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Anthracyclines:
... -Made from several streptomyces bacterial species. - Part of original 7+3 regimen for AML in 1973. - Myelosuppression, N/V, cardiac toxicity (including CHF) that is cumulative dose-related (> 600 mg/m2). |
Daunorubicin (Cerubidine®, DaunoXome®)
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Anthracyclines:
... -Made from several streptomyces bacterial species. -Used in breast cancer, NHL, ALL, sarcoma, Hodgkin’s lymphoma. -Myelosuppression, N/V, cardiac toxicity (including CHF) that is cumulative dose-related (> 550 mg/m2), secondary leukemia. |
Doxorubicin (Adriamycin®, Doxil®)
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Classic chemotherapy: ...
Act by inhibiting replication of cancer cells. Phase-specific. Divided into taxanes, epipodophyllotoxins, camptothecins, vinca alkaloids, and epothilones. Taxanes, vincas, and epothilones interfere with microtubule assembly in M-phase; camptothecins and epipodophyllotoxins inhibit topoisomerase I and II, respectively, causing DNA strand breaks in G2 and S phases. |
Plant alkaloids
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Plant Alkaloids: Taxanes
... - Showed remarkable 30% response rate in refractory ovarian cancer in 1988. -Used in breast cancer, ovarian cancer, NSCLC. - Myelosuppression, N/V, neurotoxicity, hypersensitivity reactions (HSR). - HSR prophylaxis = steroid, H2 blocker, H1 blocker. |
Paclitaxel (Taxol®, Abraxane®)
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If giving the Taxol brand, MUST give ...
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hypersensitivity prophylaxis
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Plant Alkaloids: Taxanes
... - Semi-synthetic analog of paclitaxel. -Used in breast cancer, NSCLC. - Fluid retention (prevented by ...), myelosuppression, neurotoxicity, hypersensitivity, hand-foot syndrome, N/V. |
Docetaxel (Taxotere®)
dexamethasone |
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What are the 2 classic chemo agents can cause hand-foot syndrome?
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Fluorouracil and Docetaxel
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Plant Alkaloids: Vinca Alkaloids
... -has very little bone marrow suppression -NEVER give intrathecally -Used in ALL, NHL, Hodgkin’s lymphoma. - Neurotoxicity, SIADH, CONSTIPATION, little or no myelosuppression. |
Vincristine (Oncovin®) (VCR)
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Plant Alkaloids: Camptothecins
... - Used in colorectal cancer. - Acute and delayed diarrhea, myelosuppression, N/V. - Acute diarrhea treated with IV ..., delayed diarrhea treated with .... |
Irinotecan (Camptosar®) (CPT-11)
atropine loperamide |
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Plant Alkaloids: Epipodophyllotoxins
... -Used in testicular cancer, small cell lung cancer, NHL, AML. - Myelosuppression, N/V, ... (especially if given by rapid IV infusion). |
Etoposide (Vepesid®, Toposar®, Etopophos®) (VP-16)
hypotension |
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Classic Chemotherapy: ...
Inhibit DNA synthesis by forming inter- and intra-strand cross-linking of DNA molecules. Non-phase-specific. |
Platinum compounds
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Platinum Compounds:
... -90% cure rate in testicular cancer - Used in testicular cancer, lung cancer, head and neck cancer, esophageal cancer, gastric cancer, NHL, HD, GTD, cervical cancer, breast cancer. - N/V (give an anti-emetic!), nephrotoxicity (must be hydrated before and after. give saline), neurotoxicity, myelosuppression. |
Cisplatin (Platinol®)(CDDP)
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Platinum Compounds:
... - Used in lung cancer (mainly), head and neck cancer, ovarian cancer, breast cancer. - Dosed by AUC method. It’s the only chemo drug not dosed by mg/m2 - Myelosuppression, N/V, neurotoxicity. The main advantage of this drug is that it can be given to people with ... problems (as long as it’s dosed correctly) |
Carboplatin (Paraplatin®)(CBDCA)
kidney |
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Platinum Compounds:
... -Used in colorectal cancer, especially as part of the FOLFOX regimen. -Neurotoxicity (including acute cold sensitivity), myelosuppression, N/V. - Neurotoxicity can be prevented by pre- and post-dose magnesium and calcium infusions, but this is controversial. |
Oxaliplatin (Eloxatin®)
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Hormone therapy:
-Much wider therapeutic index than classic chemotherapy. -Act by inhibiting or decreasing production of the hormone that is exacerbating the cancer. -Main targets are ... and .... -Cause expected side effects of low ... and ... levels -This category was once dominated by androgens, estrogens, and progestins, but their use is now uncommon. |
estrogen and testosterone
estrogen and testosterone |
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Hormone therapy: Antiestrogens
... - FDA approved in 1977 for breast cancer (BC). - Used as adjuvant therapy in early ER+ BC, primary therapy in ER+ advanced BC, or as BC chemoprevention in high risk patients. - First selective estrogen receptor modifier (SERM). - Hot flashes, vaginal dryness, low sex drive, DVT, endometrial changes including cancer. - Positive effect on bone, lowering the incidence of osteoporosis, and on blood lipid profiles. |
Tamoxifen (Nolvadex®)
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What is the only drug that is a pure estrogen receptor blocker?
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Fulvestrant (Faslodex)
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Hormone Therapy: ... inhibitors
-Anastrozole (Arimidex®), Letrozole (Femara®), Exemestane (Aromasin®) -Act by blocking the ... responsible for conversion of androstenedione (from the adrenal glands) to estrone in peripheral tissues, such as adipose tissue. -Used in advanced ER+ breast cancer and as adjuvant therapy in operable ER+ breast cancer. - Hot flashes, vaginal dryness, DVT (less incidence than tamoxifen). |
Aromatase
aromatase |
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Hormone Therapy: Antiandrogens
... -Testosterone receptor blocker. -FDA approved in 1995 for advanced prostate cancer as monotherapy or with LHRH agonist. -Used as primary therapy of advanced prostate cancer and adjuvant or neoadjuvant therapy of operable prostate cancer. -Hot flashes, gynecomastia, decreased sex drive. |
Bicalutamide (Casodex®)
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Hormone Therapy: ... agonists and ... antagonists
Leuprolide (Lupron®, Eligard®), Goserelin (Zoladex®), Triptorelin (Trelstar®), Abarelix (Plenaxis®) Use in a man with severe prostate cancer (slow growing) Work by reducing ovarian and testicular production of estrogen and testosterone through interference with the pituitary gland’s normal negative feedback loop. Hot flashes, reduced sex drive. |
LHRH
GNRH |
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Targeted Therapy:
Characterized by more ... targets than the “scatter gun” approach of classic chemotherapy. ... therapeutic index than classic chemotherapy. Relatively new, with marketing dating to mid-1990s. Currently a very active area of drug development. |
specific
Wider |
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Targeted Therapy: monoclonal antibodies
... - Binds to the CD20 antigen on the surface of B lymphocytes, causing antibody dependent and complement dependent cytotoxicity and apoptosis. - Used in NHL, CLL, RA, ITP. - Infusion reactions, tumor lysis syndrome. -Since CD20 is not expressed on B-cell precursors, stem cells, or plasma cells, bone marrow suppression ... a therapeutic problem. |
Rituximab (Rituxan®)
is not |
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Targeted therapy: monoclonal antibodies:
... - Binds to Her2/neu receptor, present on some breast cancer tissue, causing down-regulation of receptor and decreased proliferation of cancer cells. - Used in advanced Her2+ breast cancer and in adjuvant therapy of Her2+ breast cancer. - Cardiotoxicity (especially in combination with anthracyclines), flu-like symptoms. |
Trastuzumab (Herceptin®)
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Targeted Therapy – Tyrosine Kinase Inhibitors:
Phosphorylation of proteins by kinases is an important mechanism in signal transduction for regulation of enzyme activity, and thus, cell growth and differentiation. Tyrosine kinase inhibitors target specific tyrosine kinases that are involved in cancer, such as the ... tyrosine kinase of chronic myelogenous leukemia. |
bcr-abl
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Targeted therapy – tyrosine kinase inhibitors:
... -Inhibits the bcr-abl tyrosine kinase of chronic myelogenous leukemia (CML). -Used in CML, gastrointestinal stromal tumors. -Edema, nausea, rash, and musculoskeletal pain. |
Imatinib (Gleevec®)
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Immune therapy:
Characterized by broad stimulation of the immune system. Also known as biologic response modifiers. Wider therapeutic index than classic chemotherapy. Essentially are synthesized copies of human ..., or signaling proteins that mediate cellular communication. |
cytokines
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Immune Therapy – Interferons:
... -Binds to specific receptors on cell surface, causing, among other actions, suppression of cell proliferation, enhancement of phagocytic activity of macrophages, and augmentation of specific cytotoxicity of lymphocytes. -Used in hepatitis ..., CML, metastatic melanoma. -All side effects seem possible, psychiatric ones are most fascinating. |
Interferon alfa-2b (Intron-A®) (PegIntron®)
C |
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What are the 2 centerpiece immune therapy drugs in multiple myeloma?
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Thalidomide
Lenalidomide |
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What are the two body surface area dosing formulas that are used in clinical practice today?
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Dubois and Mosteller
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AUC dosing of ... uses the ... formula
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Carboplatin
Calvert |
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Leucovorin is RESCUE for methotrexate, but leucovorin ... the potency of 5-FU!
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INCREASES
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