Anti neoplastic drugs flashcards

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Anti neoplastic drugs flashcards

  1. 1. Anti-Neoplastics
  2. 2.  Antimetabolites ◦ ◦ ◦ ◦  Methotrexate 5-FU Mercaptopurine Azathioprine Alkylating Agents ◦ ◦ ◦ ◦  Cyclophosphamide Cisplatin Chlorambucil Carmustine Cytotoxic Antibiotics ◦ ◦ ◦ ◦  Doxorubicin Dactinomycin Daunorubicin Bleomycin Natural Products ◦ ◦ ◦ ◦ Vincristine Vinblastine Etoposide Paclitaxel
  3. 3.  Hormones  ◦ Tamoxifen ◦ Anastrazole ◦ Prednisone  ◦ Azathioprine ◦ Prednisolone ◦ Cyclosporine Monoclonal Ab ◦ Trastuzumab ◦ Rituximab Immunosuppressant s  Others ◦ Asparaginase ◦ Imatinib Mesylate ◦ Hydroxyurea
  4. 4.  S phase ◦ Methotrexate  blocks dihydrofolate reductase ◦ 5 – FU  inhibits thymidylate synthase ◦ Mercaptopurine  inhibits purine nucleotide interconversions ◦ Hydroxyurea  inhibits ribonucleotide reductase ◦ Pentostatin  inhibits adenosine deaminase Drugs acting at Cell Cycle phases
  5. 5.  G2 phase  M phase  G1 phase  Between S and G2 ◦ Bleomycin  fragments DNA ◦ Vincristine & Vinblastine binds tubulin & blocks MT polymerization ◦ Paclitaxel  prevents MT depolymerization; promotes polymerization ◦ Dactinomycin  binds DNA & inhibits DNA-dependent RNA synthesis ◦ Etoposide  interferes with topo II ◦ Dactinomycin Drugs acting at Cell Cycle phases
  6. 6.  High dose of tx for a short period of time to reduce burden on cells What is an induction regime?
  7. 7.      Used for cancers with low percentage of mitotic cells Cyclophosphamide, busulphan, chlorambucil Doxorubicin, daunorubicin, dactinomycin Cisplatin Recruitment: initial use of CCNS drugs achieves a significant log kill which causes more cells in Go to go into G1; then CCS drugs are given CCNS – Cell cycle nonspecific drugs
  8. 8. Drug/irradiation kills a constant proportion of cells in population, not fixed number of cancer cells  One log kill = 90% decrease in cell pop  3 log kill = 99.9% decrease  Smaller tumor will have greater portion of cells killed than larger tumor but they regrow quicker between cycles of therapy  Log – Kill concept
  9. 9. Cyclophosphamide  Methotrexate  5-FU  Breast Cancer Combo
  10. 10. Doxorubicin  Methotrexate  5-FU  Pancreatic Cancer Combo
  11. 11. Cisplatin  Paclitaxel  Ovarian Cancer Combo
  12. 12. Cisplatin  Vinblastine  Bleomycin  Testicular Cancer Combo
  13. 13.      Cyclophosphamide Doxorubicin Vincristine Prednisone Rituximab Non Hodgkin’s Lymphoma Combo
  14. 14.     Mechlorethamine Vincristine Prednisone Procarbazine     Doxorubicin Bleomycin Vinblastine Dacarbazine Hodgkin’s Disease Combo
  15. 15.         Cytarabine Capecitabine Carmustine Etoposide Topotecan Fulvestrant Flutamide & Finasteride Leuprolide    Rituximab Hydroxyurea Imatinib Mesylate Drugs w/ features you must know
  16. 16. Antimetabolite  DOC for AML  MoA: blocks DNA strand elongation  Neurotoxic  Cytarabine
  17. 17. Stabilizes the topo II – DNA complex causing dsDNA breaks during DNA replication  Dose limiting leukopenia  Treat first time and metastatic testicular cancer  may cause AML!!  Etoposide
  18. 18. Oral prodrug  converted to 5-FU  MoA: inhibits thymidylate synthase  Useful for paclitaxel and doxorubicin – resistant pts with colorectal or metastatic breast cancers  Capecitabine
  19. 19. Alkylating agent; nitrosoureas  Most alkylating agents taken up by active transport but nitrosoureas taken up by passive transport  Liphopilic & passes BBB  CNS Toxicity  Used for CNS cancers that are metastatic  malignant astrocytoma  Carmustine
  20. 20. Unique topo I inhibitor, preventing religation of bits of helices  accumulation of single stranded breaks in DNA  Dose limiting neutropenia  Topotecan
  21. 21. Antiestrogen for hormone-sensitive tumors  Give to post-menopausal women who are resistant to tamoxifen  Fulvestrant
  22. 22. Flutamide is a nonsteroidal androgen antagonist which inhibits the translocation of steroid receptors to the nucleus  Finasteride is a 5-alpha reductase inhibitor which inhibits synthesis of dihydrotestosterone  Both used to treat prostate cancer  Flutamide & Finestiride
  23. 23. GnRH analog which acts as a partial agonist at GnRH receptors  When administered in constant doses to maintain stable blood levels, it inhibits the release of LH and FSH  Used in tx of prostate cancer  Leuprolide
  24. 24.  This is an unconjugated chimeric (murine/human) antiCD20 monoclonal antibody which binds to the CD20 antigen on follicular B cells in Non Hodgkins lymphoma Rituximab
  25. 25. Inhibits ribonucleotide reductase  ribonucleotides to deoxyribonucleotides  Used for myeloproliferative disorders  Hydroxyurea
  26. 26.  Inhibits bcr-abl tyrosine kinase found in chronic myelocytic leukemia (CML) Imatinib Mesylate
  27. 27. Methotrexate (CCS  works during S phase)  Uses  ◦ ◦ ◦ ◦ ◦  Solid tumors such as choriocarcinoma Osteogenic sarcoma Acute Lymphoblastic Leukemia (ALL) Psoriasis Abortifacient Looks like folate  take up by cells readily Antimetabolites
  28. 28. Inhibits dihydrofolate Reductase  This enzyme reduces folate to tetrahydrofolate which is a one carbon unit carrier used in synthesis of purines and pyrimidines which are part of DNA and RNA  cell replication  ANTIDOTE: Leucovorin  folinic acid rescue  ◦ Host cells are rescued while cancer cells die MoA of Methotrexate
  29. 29. Nephrotoxicity  Myelosuppression  ◦ Neutropenia, thrombocytopenia, mucositis, diarrhea, and GI ulceration (oral) ◦ G-CSF can counteract leukopenia  Pulmonary toxicity and hepatotoxicity (long term) Methotrexate Toxicity
  30. 30.  Pyrimidine analogs ◦ 5 – FU ◦ Capecitabine  5-FU ◦ Cytarabine  5 – FU ◦ MoA: inihibit thymidylate synthase ◦ Uses: colon, breast, rectal, gastric, pancreatic cancer ◦ Capecitabine is same but one of the newest drugs for pancreatic cancer Other Antimetabolites
  31. 31.      Anorexia, nausea Alopecia Stomatitis and diarrhea Myelosuppression (less for capecitaine) Maculopapular rash  Resistance develops when thymidylate synthase becomes less sensitive to the drug Toxicity of 5-FU and Antimetabolites
  32. 32.      Azathioprine, Mercaptopurine MoA: as nucleotides they inhibit phosphoribosylpyrophosphate (PRPP) synthetase  reduction in PRPP They also inhibit PRPP amidotransferase  reduction in phosphoribosylamine Block de novo PURINE synthesis and salvage pathways Toxicity: ◦ ◦ ◦ ◦ Bone marrow suppression Leukopenia Hyperuricemia (Mercaptopurine) Hepatotoxicity Purine Analogs
  33. 33.  Pentostatin ◦ Uses: Hairy Cell Leukemia ◦ MoA: blocks adenosine deaminase  impairment of DNA replication and cell division ◦ Toxicity: Myelosuppression Purine analogs
  34. 34. Cyclophosphamide (ifosphamide also)  Busulphan  Carmustine (nitrosoureas)  Alkylating Agents
  35. 35.  MoA: prodrug converted in liver to active nitrogen mustard (nephrotoxic) and acrolein (causes cystitis)  interferes with transcription and translation and causes increased ADH secretion (water reabsorption leading to hyponatremia results) ◦ Drug is given with high water load   ANTIDOTE: Mesna ADH antidote: Demeclocycline Cyclophosphamide
  36. 36.  Uses  Toxicity ◦ ◦ ◦ ◦ Hodgkin’s disease Lymphomas, myeloma Leukemia Ovarian & breast tumors ◦ Myelosuppression ◦ Permanent amenorrhea and azoospermia ◦ Renal and bladder toxicity (hemorrhagic cystitis & hematuria) ◦ Alopecia ◦ Cardiotoxic at high doses Cyclophosphamide Use and Toxicity
  37. 37. MoA: cross-links DNA strands by covalently bonding guanine residues  prevents DNA replication & transcription  Use: CML  Toxicity:  ◦ Busulphan Lung - pulmonary fibrosis ◦ Busulphan tan – hyper pigmentation Busulphan
  38. 38.  Some success in treating malignant gliomas (multiforme glioblastoma  thought to be incurable) Temozolamide
  39. 39. Doxorubicin  Daunorubicin  Dactinomycin  Bleomycin   All CCNS mostly Cytotoxic Antibiotics
  40. 40.  MoA: ◦ Intercalates DNA and is topo II block/poison ◦ Increases radicals ◦ Causes extravasation  ulcers and inflammation  USES: ◦ Breast, ovarian, bladder tumors – Solid tumors ◦ Bronchogenic carcinoma ◦ Lymphoma and leukemia Doxorubicin
  41. 41.        Cardiomyopathy Colors urine red Stomatitis Alopecia Anemia, leukemia ANTIDOTE for radicals: Dimethyl Sulphoxide ANTIDOTE for cardiomyopathy: Dexrazoxane Doxorubicin Toxicity
  42. 42. Similar to doxorubicin  Use: LEUKEMIA  Daunorubicin
  43. 43. MoA: binds DNA Helix  prevents transcription of DNA by RNA polymerase  USES  ◦ ◦ ◦ ◦  Rhabdomyosarcoma Wilm’s tumor in children Ewing’s Tumor Kaposi’s sarcoma Toxicity: Pancytopenia Dactinomycin
  44. 44. MoA: fragments DNA via free radicals  cells accumulate in G2 phase  USES  ◦ ◦ ◦ ◦  Lymphomas SCC Testicular carcinoma Choriocarcinoma Toxicity: Pulmonary Fibrosis, hyperpigmentation Bleomycin
  45. 45. Vinca alkaloids: Vincristine and Vinblastine  Epidophyllotoxins: Etoposide  Camptothecins: Topotecan  Taxanes: Paclitaxel  Natural Products
  46. 46. MoA: bind tubulin and prevent MT assembly; act in M phase  Vincristine (Neurotoxic—peripheral neuropathy, loss of deep tendon reflexes)  ◦ Use: Hodgkin’s disease, rhabdomyosarcoma, lymphomas, leukemia, neuroblastoma  Vinblastine (reversibly myelotoxic) ◦ Use: Hodgkin’s, testicular carcinoma  Resistance assoc/ MDR gene mutation Vinca Alkaloids
  47. 47. MoA: stabilizes topo II-DNA complex  dsDNA breaks  Specific for late S and early G2 phases  Uses: testicular carcinoma (less toxic than other natural products), Hodgkin’s disease  Toxicity:  ◦ Leukopenia; hepatic and renal toxicity at high dose ◦ May cause AML!!! Epidophyllotoxins - ETOPOSIDE
  48. 48. MoA: inhibit MT disassembly  abnormal/dysfunctional spindles  Uses  ◦ Advanced ovarian cancer w/ cisplatin ◦ Metastatic ovarian or breast cancer  Toxicity ◦ Hypersensitivity reactions ◦ Neutropenia ◦ Peripheral neuropathy & muscle pain Taxane - Paclitaxel
  49. 49. Estrogens  Antiestrogens  ◦ Tamoxifen ◦ Fulvestrant ◦ Anastrazole Androgens  Antiandrogens  ◦ Flutamide ◦ Finasteride Hormonal Chemotherapy
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