Anticancer Drugs Flashcards
Name common side effects of Anticancer drugs
• Bone marrow toxicity with
decreased leucocyte production and thus
decreased resistance to infection
• Impaired wound healing
• Loss of hair (alopecia)
• Damage to the gastrointestinal epithelium
• Depression of growth in children
• Sterility
• Teratogenicity
• Cardiotoxicity with some drugs like doxorubicin
Hodgkin’s lymphoma TTT
Adriamycin, doxorubicin, bleomycin, vinblastine, dacarbazine ± rituximab
• Radiation Therapy
Non Hodgkin’s lymphoma TTT
cyclophosphamide, doxorubicin, vincristine, prednisone ± rituximab
• Radiation Therapy
Two classifications of drugs
Cell cycle-specific agents
Cell cycle-Non specific agents
Cell cycle-specific agents, name them
Antimetabolites
Topoisomerase inhivitors
Vinca alkolids
Antimicrotubular inhibitors
Cell cycle- Non specific agents, name them
Alkylating agents
Antitumor antibiotics
Platinum analogues
Anthracyclins
Alkylating agents include?
chlorambucil, cyclophosphamide, and dacarbazine
Drug that act in part as alkylating agents is?
Cisplatin
alkylating agents Mechanism of action? And what’s The major site of action within DNA?
- Combine w DNA —> Damage malignant and dividing normal cells
- Guanine
alkylating agents clinical use and adverse effects?
• Clinical Uses: Non-Hodgkin’s lymphoma, leukemia, and other cancers like breast cance
• Adverse effects: myelosuppression, gastrointestinal tract-like diarrhea, reproductive system toxicity, and secondary malignancies
Antimetabolites includes?
Methotrexate
mercaptopurine
Fluorouracil
In addition to their cytotoxic effects on neoplastic cells the antimetabolites also have?
immunosuppressant actions
Methotrexate mechanism of action?
Binds with DHFR results in inhibition of the synthesis of tetrahydrofolate THF so all Thymidylate, purine nucleotides, the amino acid series are inhibitid
This interferes w the formation of DNA, RNA and key cellular proteins
Methotrexate is used to Treat?
lymphomas
Methotrexate adverse effects?
Mucositis, diarrhea, myelosuppression with
neutropenia and thrombocytopenia
Natural product anticancer drugs includes?
Vincristine and Vinblastine
Vincristine and Vinblastine Mechanism of action and uses?
Inhibits mitosis, useful lymphoma, leukemia, and breast cancer
Vincristine and Vinblastine side effects?
Nausea and vomiting, Myelosuppression,
mucositis, alopecia, inappropriate secretion of antidiuretic hormone,etc.
Antitumor antibiotics includes?
Bleomycin
Doxorubicin
Bleomycin mechanism of action and uses?
M. Of Action: Oxygen free radicals bind to DNA causing DNA breaks
Uses: Hodgkin’s and non-Hodgkin’s lymphoma, germ cell cancer, head, and neck cancer
Bleomycin Side effects
Allergic reactions, fever, hypotension, Skin
toxicity,pulmonaryfibrosis,mucositis,alopecia
O
Doxorubicin
Doxorubicin mechanism of action
Oxygen free radicals bind to DNA causing strand
DNA breaks Inhibiting topoisomerase II and intercalating into DNA
Doxorubicin uses and side effects?
Uses: Breast cancer, Hodgkin’s and non-Hodgkin’s lymphoma, soft tissue sarcoma, ovarian cancer, non-small cell and small cell lung cancer, thyroid cancer, Wilms’ tumor, neuroblastoma
Side effects: Nausea, red urine (not hematuria) Cardiotoxicity, alopecia, myelosuppression, stomatitis
Imatinib mechanism of action/Uses/Side effects?
• Mechanism of action includes Inhibition of Bcr-Abl
tyrosinekinase and other receptor tyrosinekinases
• Uses:Leukemia and gastrointestinal stromal tumor
• Side effects: Nausea and vomiting, Fluid retention with edema, diarrhea, myalgias, congestive heart failure
Rituximab is a? What its mechanism?
monoclonal antibody
Mechanism: Rituximab binds to CD20 protein which is present on the B cells and induces cell lysis, direct cytotoxicity, and
inductionofapoptosis.
Rituximab Uses and side effects?
Uses: It is currently used with conventional anticancer drugs in lymphomas. Sideeffects:Hypersensitivity reactions and myelosuppression
Prednisone is a? What’s it’s mechanism?
• When glucocorticoids enter the cell after passive
diffusion and bind to the GR in the cytoplasm, a
(GR/GC)complex is formed.
• Subsequently, GR/GC complex binds to the DNA and initiates theanticanceractivity
Prednisone needs what to be sufficient?
Needs conversion to prednisolone via metabolism process