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Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
Anti neoplastic drugs flashcards
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Anti neoplastic drugs flashcards

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Excellent study aid for medical students, pharmacology students, nursing students, and university students!

Excellent study aid for medical students, pharmacology students, nursing students, and university students!

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  • 1. Anti-Neoplastics
  • 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.  Hormones  ◦ Tamoxifen ◦ Anastrazole ◦ Prednisone  ◦ Azathioprine ◦ Prednisolone ◦ Cyclosporine Monoclonal Ab ◦ Trastuzumab ◦ Rituximab Immunosuppressant s  Others ◦ Asparaginase ◦ Imatinib Mesylate ◦ Hydroxyurea
  • 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.  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.  High dose of tx for a short period of time to reduce burden on cells What is an induction regime?
  • 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. 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. Cyclophosphamide  Methotrexate  5-FU  Breast Cancer Combo
  • 10. Doxorubicin  Methotrexate  5-FU  Pancreatic Cancer Combo
  • 11. Cisplatin  Paclitaxel  Ovarian Cancer Combo
  • 12. Cisplatin  Vinblastine  Bleomycin  Testicular Cancer Combo
  • 13.      Cyclophosphamide Doxorubicin Vincristine Prednisone Rituximab Non Hodgkin’s Lymphoma Combo
  • 14.     Mechlorethamine Vincristine Prednisone Procarbazine     Doxorubicin Bleomycin Vinblastine Dacarbazine Hodgkin’s Disease Combo
  • 15.         Cytarabine Capecitabine Carmustine Etoposide Topotecan Fulvestrant Flutamide & Finasteride Leuprolide    Rituximab Hydroxyurea Imatinib Mesylate Drugs w/ features you must know
  • 16. Antimetabolite  DOC for AML  MoA: blocks DNA strand elongation  Neurotoxic  Cytarabine
  • 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. 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. 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. Unique topo I inhibitor, preventing religation of bits of helices  accumulation of single stranded breaks in DNA  Dose limiting neutropenia  Topotecan
  • 21. Antiestrogen for hormone-sensitive tumors  Give to post-menopausal women who are resistant to tamoxifen  Fulvestrant
  • 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. 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.  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. Inhibits ribonucleotide reductase  ribonucleotides to deoxyribonucleotides  Used for myeloproliferative disorders  Hydroxyurea
  • 26.  Inhibits bcr-abl tyrosine kinase found in chronic myelocytic leukemia (CML) Imatinib Mesylate
  • 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. 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. Nephrotoxicity  Myelosuppression  ◦ Neutropenia, thrombocytopenia, mucositis, diarrhea, and GI ulceration (oral) ◦ G-CSF can counteract leukopenia  Pulmonary toxicity and hepatotoxicity (long term) Methotrexate Toxicity
  • 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.      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.      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.  Pentostatin ◦ Uses: Hairy Cell Leukemia ◦ MoA: blocks adenosine deaminase  impairment of DNA replication and cell division ◦ Toxicity: Myelosuppression Purine analogs
  • 34. Cyclophosphamide (ifosphamide also)  Busulphan  Carmustine (nitrosoureas)  Alkylating Agents
  • 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.  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. 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.  Some success in treating malignant gliomas (multiforme glioblastoma  thought to be incurable) Temozolamide
  • 39. Doxorubicin  Daunorubicin  Dactinomycin  Bleomycin   All CCNS mostly Cytotoxic Antibiotics
  • 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.        Cardiomyopathy Colors urine red Stomatitis Alopecia Anemia, leukemia ANTIDOTE for radicals: Dimethyl Sulphoxide ANTIDOTE for cardiomyopathy: Dexrazoxane Doxorubicin Toxicity
  • 42. Similar to doxorubicin  Use: LEUKEMIA  Daunorubicin
  • 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. MoA: fragments DNA via free radicals  cells accumulate in G2 phase  USES  ◦ ◦ ◦ ◦  Lymphomas SCC Testicular carcinoma Choriocarcinoma Toxicity: Pulmonary Fibrosis, hyperpigmentation Bleomycin
  • 45. Vinca alkaloids: Vincristine and Vinblastine  Epidophyllotoxins: Etoposide  Camptothecins: Topotecan  Taxanes: Paclitaxel  Natural Products
  • 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. 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. 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. Estrogens  Antiestrogens  ◦ Tamoxifen ◦ Fulvestrant ◦ Anastrazole Androgens  Antiandrogens  ◦ Flutamide ◦ Finasteride Hormonal Chemotherapy
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