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Anti neoplastic drugs flashcards
The document provides an extensive overview of various anti-cancer drugs, including their mechanisms of action, combinations used for treatment, and associated toxicities. It categorizes drugs into classes such as antimetabolites, alkylating agents, cytotoxic antibiotics, and hormones, detailing their roles in chemotherapy regimens for different cancers. Additionally, it discusses pharmacological details and considerations for drug administration and resistance patterns.
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Anti neoplastic drugs flashcards
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- 2. Antimetabolites ◦ ◦ ◦ ◦ Methotrexate 5-FU Mercaptopurine Azathioprine Alkylating Agents ◦ ◦ ◦ ◦ Cyclophosphamide Cisplatin Chlorambucil Carmustine Cytotoxic Antibiotics ◦ ◦ ◦ ◦ Doxorubicin Dactinomycin Daunorubicin Bleomycin NaturalProducts ◦ ◦ ◦ ◦ 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 G1phase 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 oftx for a short period of time to reduce burden on cells What is an induction regime?
- 7. Used for cancerswith 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 aconstant 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 BreastCancer Combo
- 10. Doxorubicin Methotrexate 5-FU PancreaticCancer Combo
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- 12. Cisplatin Vinblastine Bleomycin TesticularCancer Combo
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- 16. Antimetabolite DOC forAML MoA: blocks DNA strand elongation Neurotoxic Cytarabine
- 17. Stabilizes the topoII – 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 Iinhibitor, 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 anonsteroidal 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 whichacts 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 anunconjugated 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 tyrosinekinase 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 anddiarrhea 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: asnucleotides 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: HairyCell 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 convertedin 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 DNAstrands by covalently bonding guanine residues prevents DNA replication & transcription Use: CML Toxicity: ◦ Busulphan Lung - pulmonary fibrosis ◦ Busulphan tan – hyper pigmentation Busulphan
- 38. Some success intreating malignant gliomas (multiforme glioblastoma thought to be incurable) Temozolamide
- 39. Doxorubicin Daunorubicin Dactinomycin Bleomycin All CCNS mostly Cytotoxic Antibiotics
- 40. MoA: ◦ Intercalates DNAand 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 DNAHelix 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 DNAvia free radicals cells accumulate in G2 phase USES ◦ ◦ ◦ ◦ Lymphomas SCC Testicular carcinoma Choriocarcinoma Toxicity: Pulmonary Fibrosis, hyperpigmentation Bleomycin
- 45. Vinca alkaloids: Vincristineand Vinblastine Epidophyllotoxins: Etoposide Camptothecins: Topotecan Taxanes: Paclitaxel Natural Products
- 46. MoA: bind tubulinand 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 topoII-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 MTdisassembly 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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