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Questions and Answers
What is the primary goal of cancer chemotherapy?
What is the primary goal of cancer chemotherapy?
What is the target of most anticancer drugs?
What is the target of most anticancer drugs?
Why do antitumor agents have a steep dose–response curve for both therapeutic and toxic effects?
Why do antitumor agents have a steep dose–response curve for both therapeutic and toxic effects?
What is the mechanism of newer anticancer agents?
What is the mechanism of newer anticancer agents?
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What is an example of a non-cancer disease where methotrexate is used?
What is an example of a non-cancer disease where methotrexate is used?
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What is the role of chemotherapy in cancer treatment?
What is the role of chemotherapy in cancer treatment?
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What is a potential side effect of using the drug mentioned in the text?
What is a potential side effect of using the drug mentioned in the text?
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What is the category of drugs that includes 6-mercaptopurine and fludarabine?
What is the category of drugs that includes 6-mercaptopurine and fludarabine?
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What is the primary use of 6-mercaptopurine in cancer treatment?
What is the primary use of 6-mercaptopurine in cancer treatment?
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What is the mechanism of action of fludarabine in cells?
What is the mechanism of action of fludarabine in cells?
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What is the relationship between azathioprine and 6-mercaptopurine?
What is the relationship between azathioprine and 6-mercaptopurine?
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What is the additional benefit of 6-mercaptopurine and its analog, azathioprine?
What is the additional benefit of 6-mercaptopurine and its analog, azathioprine?
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What is the primary mechanism of cytotoxicity of alkylating agents?
What is the primary mechanism of cytotoxicity of alkylating agents?
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Which type of cells are alkylating agents most toxic to?
Which type of cells are alkylating agents most toxic to?
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What is a common side effect of alkylating agents?
What is a common side effect of alkylating agents?
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What is the primary mechanism of action of antitumor antibiotics?
What is the primary mechanism of action of antitumor antibiotics?
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What is the primary site of biotransformation of cyclophosphamide and ifosfamide?
What is the primary site of biotransformation of cyclophosphamide and ifosfamide?
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Which of the following is a cell cycle specific antitumor antibiotic?
Which of the following is a cell cycle specific antitumor antibiotic?
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What is the active compound formed from the metabolism of cyclophosphamide and ifosfamide?
What is the active compound formed from the metabolism of cyclophosphamide and ifosfamide?
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What is the result of gemcitabine being deaminated?
What is the result of gemcitabine being deaminated?
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What is the formulation of ifosfamide available for administration?
What is the formulation of ifosfamide available for administration?
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What is the purpose of gemcitabine administration via IV infusion?
What is the purpose of gemcitabine administration via IV infusion?
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Which of the following is used to treat prostate cancer?
Which of the following is used to treat prostate cancer?
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What is the relationship between doxorubicin and daunorubicin?
What is the relationship between doxorubicin and daunorubicin?
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What is the primary route of excretion for ifosfamide?
What is the primary route of excretion for ifosfamide?
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Which enzyme is responsible for metabolizing ifosfamide?
Which enzyme is responsible for metabolizing ifosfamide?
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What is the main cause of bladder toxicity in patients taking cyclophosphamide?
What is the main cause of bladder toxicity in patients taking cyclophosphamide?
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What is the effect of nitrosoureas on non-dividing cells?
What is the effect of nitrosoureas on non-dividing cells?
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What is the mechanism of action of nitrosoureas?
What is the mechanism of action of nitrosoureas?
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What is the primary use of nitrosoureas in cancer treatment?
What is the primary use of nitrosoureas in cancer treatment?
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Study Notes
Principles of Cancer Chemotherapy
- Cancer chemotherapy aims to cause a lethal cytotoxic event or apoptosis in cancer cells to arrest tumor progression.
- The attack is generally directed toward DNA or against metabolic sites essential to cell replication.
- Ideally, anticancer drugs should interfere only with cellular processes unique to malignant cells, but they often affect all kinds of proliferating cells, including normal cells.
Chemotherapeutic Agents
- Chemotherapeutic agents can also be used in non-cancer diseases, such as methotrexate in rheumatoid arthritis and psoriasis, azathioprine in organ transplantation, and hydroxyurea in sickle cell anemia.
- Examples of chemotherapeutic agents affecting RNA and DNA include purine analogs, alkylating agents, and antibiotics.
Treatment Strategies
- Goals of treatment include reducing neoplastic cell burden to maintain a "normal" existence of the disease with the patient as a chronic disease.
- Treatment strategies depend on the type and stage of cancer, with three main goals: cure, control, and palliation.
Purine Analogs
- Purine analogs include guanine analogs (6-mercaptopurine, 6-thioguanine) and adenosine analogs (fludarabine, cladribine).
- 6-Mercaptopurine is used in the maintenance of remission in acute lymphoblastic leukemia and also beneficial in the treatment of Crohn's disease.
- Adenosine analogs, such as fludarabine and cladribine, are used in leukemia and lymphomas.
Alkylating Agents
- Alkylating agents exert their cytotoxic effects by covalently binding to nucleophilic groups on various cell constituents.
- Alkylation of DNA is probably the crucial cytotoxic reaction that is lethal to tumor cells.
- Alkylating agents do not discriminate between cycling and resting cells, and are used in combination with other agents to treat a wide variety of lymphatic and solid cancers.
- Examples of alkylating agents include cyclophosphamide and ifosfamide, which are used in the treatment of non-Hodgkin lymphoma, sarcoma, and breast cancer.
Antibiotics (Antitumor)
- Antitumor antibiotics owe their cytotoxic action primarily to their interactions with DNA, leading to disruption of DNA function.
- They are cell cycle nonspecific, with bleomycin as an exception.
- Examples of antitumor antibiotics include anthracyclines (doxorubicin, daunorubicin, idarubicin, epirubicin, and mitoxantrone), which are used in the treatment of sarcomas, carcinomas, acute lymphocytic leukemia, and lymphomas.
Nitrosoureas
- Nitrosoureas, such as carmustine and lomustine, are primarily employed in the treatment of brain tumors due to their ability to penetrate the CNS.
- They exert cytotoxic effects by an alkylation that inhibits replication and eventually RNA and protein synthesis.
- Although they alkylate DNA in resting cells, cytotoxicity is expressed primarily in cells that are actively dividing.
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Description
This quiz covers the fundamental principles of cancer chemotherapy, including the mechanisms of action and targets of anticancer drugs. Learn how cancer chemotherapy works to arrest tumor progression and the challenges of developing effective treatments. Test your understanding of the principles of cancer chemotherapy and its applications.