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Questions and Answers
What is the main effect of methotrexate on nucleotide and amino acid synthesis?
What is the main effect of methotrexate on nucleotide and amino acid synthesis?
- It has no effect on their synthesis.
- It decreases their synthesis. (correct)
- It converts them into non-functional forms.
- It increases their synthesis significantly.
Which of the following cancers is not effectively treated with methotrexate?
Which of the following cancers is not effectively treated with methotrexate?
- Choriocarcinoma
- Breast cancer
- Wilms' tumor (correct)
- Acute lymphocytic leukemia
What is a significant adverse effect associated with long-term use of methotrexate?
What is a significant adverse effect associated with long-term use of methotrexate?
- Hemolytic anemia
- Pulmonary infiltrates and fibrosis (correct)
- Severe myelosuppression
- Neurotoxicity
What is the primary mechanism of action for vincristine?
What is the primary mechanism of action for vincristine?
Which of the following is an adverse effect of vincristine?
Which of the following is an adverse effect of vincristine?
How does bleomycin primarily damage DNA?
How does bleomycin primarily damage DNA?
In which phase of the cell cycle does bleomycin act?
In which phase of the cell cycle does bleomycin act?
What potential benefit does leucovorin provide during methotrexate treatment?
What potential benefit does leucovorin provide during methotrexate treatment?
Which phase of the cell cycle do chemotherapeutic agents like 5-Fluorouracil primarily target?
Which phase of the cell cycle do chemotherapeutic agents like 5-Fluorouracil primarily target?
What is the primary mechanism of action for 5-Fluorouracil?
What is the primary mechanism of action for 5-Fluorouracil?
For which type of cancer is 5-Fluorouracil most widely used?
For which type of cancer is 5-Fluorouracil most widely used?
Which of the following is NOT a common adverse effect of 5-Fluorouracil?
Which of the following is NOT a common adverse effect of 5-Fluorouracil?
Methotrexate primarily inhibits which enzyme?
Methotrexate primarily inhibits which enzyme?
What category does Methotrexate fall under in cancer treatment?
What category does Methotrexate fall under in cancer treatment?
Which of the following is a characteristic of cell cycle-specific (CCS) drugs?
Which of the following is a characteristic of cell cycle-specific (CCS) drugs?
Which drug is primarily used for the treatment of lymphomas?
Which drug is primarily used for the treatment of lymphomas?
Which of the following drugs is a pyrimidine analogue used in cancer treatment?
Which of the following drugs is a pyrimidine analogue used in cancer treatment?
What is a common adverse effect associated with Bleomycin?
What is a common adverse effect associated with Bleomycin?
Which mechanism describes how 5-Fluorouracil exerts its effects?
Which mechanism describes how 5-Fluorouracil exerts its effects?
Which drug is classified as an alkylating agent?
Which drug is classified as an alkylating agent?
What adverse effect is specifically linked to Cyclophosphamide?
What adverse effect is specifically linked to Cyclophosphamide?
Which of the following is true about Imatinib?
Which of the following is true about Imatinib?
Which cancer is NOT a clinical use for Methotrexate?
Which cancer is NOT a clinical use for Methotrexate?
Which statement best describes the action of Vincristine?
Which statement best describes the action of Vincristine?
Which mechanism best explains the resistance to fluorouracil in recurrent colon cancer?
Which mechanism best explains the resistance to fluorouracil in recurrent colon cancer?
Which drug should be administered to counteract the toxicity of high-dose methotrexate in a patient?
Which drug should be administered to counteract the toxicity of high-dose methotrexate in a patient?
What is the primary molecular action that mediates the therapeutic effect of doxorubicin?
What is the primary molecular action that mediates the therapeutic effect of doxorubicin?
Which of the following is NOT a common side effect associated with fluorouracil chemotherapy?
Which of the following is NOT a common side effect associated with fluorouracil chemotherapy?
In what scenario is decreased activity of the cell efflux pump primarily relevant?
In what scenario is decreased activity of the cell efflux pump primarily relevant?
What is the primary clinical use of trastuzumab?
What is the primary clinical use of trastuzumab?
Which of the following is a severe side effect of trastuzumab?
Which of the following is a severe side effect of trastuzumab?
What mechanism of action does doxorubicin employ to exert its effects?
What mechanism of action does doxorubicin employ to exert its effects?
Tamoxifen is primarily used to treat which condition?
Tamoxifen is primarily used to treat which condition?
Which of the following side effects is commonly associated with doxorubicin?
Which of the following side effects is commonly associated with doxorubicin?
What is the mechanism of action of trastuzumab?
What is the mechanism of action of trastuzumab?
What type of cancer is NOT primarily treated with doxorubicin?
What type of cancer is NOT primarily treated with doxorubicin?
What are common side effects associated with tamoxifen?
What are common side effects associated with tamoxifen?
Flashcards
Cancer
Cancer
Uncontrolled cell growth and division, invading surrounding tissues and potentially spreading to other parts of the body
Cell Cycle-Specific (CCS) Drugs
Cell Cycle-Specific (CCS) Drugs
Anticancer drugs that target cells actively dividing in a specific stage of the cell cycle.
Cell Cycle-Nonspecific (CCNS) Drugs
Cell Cycle-Nonspecific (CCNS) Drugs
Anticancer drugs that target both dividing and resting tumor cells.
Antimetabolites (Antineoplastic Agents)
Antimetabolites (Antineoplastic Agents)
A class of anticancer drugs that interfere with the synthesis of essential molecules required for DNA replication and metabolic function within cells.
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5-Fluorouracil (5-FU)
5-Fluorouracil (5-FU)
An antimetabolite drug that inhibits thymidylate synthase, blocking DNA synthesis, primarily acting in S phase.
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Methotrexate
Methotrexate
An antifolate drug that inhibits dihydrofolate reductase, an enzyme crucial for DNA synthesis.
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S phase of cell cycle
S phase of cell cycle
The part of the cell cycle where DNA replication occurs.
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Clinical Use of 5-FU
Clinical Use of 5-FU
Commonly used in treating colorectal, GI, breast, and neck cancers.
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Methotrexate clinical indication
Methotrexate clinical indication
Effective against some cancers like acute lymphocytic leukemia, choriocarcinoma, breast cancer, and head and neck carcinomas, and certain inflammatory diseases like psoriasis and rheumatoid arthritis. Also abortive in ectopic pregnancy.
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Methotrexate adverse effects
Methotrexate adverse effects
Common side effects include bone marrow suppression and toxic effects on skin and gastrointestinal mucosa (mucositis). Long-term use may cause hepatotoxicity and pulmonary problems.
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Vinca Alkaloids
Vinca Alkaloids
Plant-derived cancer chemotherapy drugs targeting specific phases of the cell cycle.
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Vincristine mode of action
Vincristine mode of action
Blocks mitotic spindle formation by halting tubulin dimer assembly into microtubules, disrupting mitosis, leading to cell death.
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Vincristine clinical uses
Vincristine clinical uses
Used in acute lymphocytic leukemia, Hodgkin's and non-Hodgkin's lymphoma, Wilms' tumor, and neuroblastoma.
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Vincristine adverse effects
Vincristine adverse effects
Usually does not cause severe bone marrow suppression, but can lead to neurotoxicity, potentially causing areflexia, peripheral neuritis, and paralytic ileus.
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Bleomycin mode of action
Bleomycin mode of action
Causes DNA scission through oxidative processes; a DNA-bleomycin-iron complex undergoes oxidation, leading to DNA damage.
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Bleomycin clinical uses
Bleomycin clinical uses
Part of treatment regimens for Hodgkin's lymphoma and testicular cancer.
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Fluorouracil resistance mechanism
Fluorouracil resistance mechanism
Cancer cells may be resistant to fluorouracil because they have a decreased ability to phosphorylate pyrimidines, leading to reduced drug effectiveness.
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Methotrexate antidote
Methotrexate antidote
Leucovorin is given to counteract methotrexate toxicity by providing a substitute for the folate needed.
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Doxorubicin's mechanism of action
Doxorubicin's mechanism of action
Doxorubicin intercalates between DNA strands, hindering topoisomerase II, thus disrupting DNA function, and causing cell death.
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Recurrent colon cancer
Recurrent colon cancer
Colon cancer that returns after treatment. It might be due to resistance to fluorouracil.
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Acute lymphoblastic leukemia
Acute lymphoblastic leukemia
A type of blood cancer, where abnormal white blood cells grow uncontrollably.
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Bleomycin's use
Bleomycin's use
Bleomycin is used to treat lymphomas and squamous cell carcinomas.
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Bleomycin adverse effects
Bleomycin adverse effects
Bleomycin can cause pulmonary problems (pneumonitis, fibrosis), hypersensitivity reactions (chills, fever), and mucocutaneous reactions (hair loss, blisters).
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Cell cycle-specific drugs (CCS)
Cell cycle-specific drugs (CCS)
Drugs that target cells actively dividing (cycling).
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Cell cycle-nonspecific drugs (CCNS)
Cell cycle-nonspecific drugs (CCNS)
Drugs targeting both dividing and resting cells.
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5-Fluorouracil mechanism
5-Fluorouracil mechanism
5-Fluorouracil blocks thymidylate synthase, affecting DNA and RNA synthesis.
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Methotrexate mechanism
Methotrexate mechanism
Methotrexate stops the creation of purine nucleotides by inhibiting DHFR.
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Vincristine mechanism
Vincristine mechanism
Vincristine disrupts microtubule formation, hindering cell division.
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Antimetabolite example
Antimetabolite example
Methotrexate is an example of an antimetabolite drug.
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Trastuzumab's target
Trastuzumab's target
Trastuzumab targets the extracellular domain of HER2, a protein involved in cell growth.
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Trastuzumab's action
Trastuzumab's action
Trastuzumab triggers an immune response to internalize and reduce HER2, slowing cell growth.
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Doxorubicin's MOA
Doxorubicin's MOA
Doxorubicin creates oxygen free radicals that damage DNA, inhibiting an enzyme (topoisomerase 2).
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Tamoxifen's Mechanism
Tamoxifen's Mechanism
Tamoxifen blocks estrogen from binding to receptors in breast cells, thus preventing growth.
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Growth Factor Receptor Inhibitors
Growth Factor Receptor Inhibitors
Drugs targeting growth factor receptors on cells, for example, EGFR or VEGFR.
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Doxorubicin's Clinical Uses
Doxorubicin's Clinical Uses
Doxorubicin treats various cancers (lymphomas, myelomas, breast, lung, ovarian, thyroid), and some leukemias.
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Tamoxifen's Clinical Uses
Tamoxifen's Clinical Uses
Tamoxifen treats breast cancers, particularly those that have spread or early-stage cancers.
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CML Treatment Types
CML Treatment Types
Chronic myelogenous leukemia (CML) treatments are targeted at different stages of the disease.
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Cancer Overview
- Cancer involves uncontrolled cell growth and division, invading adjacent tissues and potentially spreading to distant sites.
Cell Cycle Phases
- The cell cycle has distinct phases: G1, S, G2, and M.
- G1: Cell growth and preparation for DNA replication.
- S: DNA synthesis (replication).
- G2: Cell growth and preparation for mitosis.
- M: Mitosis (cell division).
- The specific percentages of each phase are variable (G₁: 40%, S: 39%, G₂: 19%, M: 2%).
- Go phase is a quiescent state.
Learning Objectives
- Understand cancer cell cycle kinetics.
- Classify cell cycle-specific and -nonspecific anticancer drugs.
- Explain the mechanism of action of specific anticancer drugs (5-fluorouracil, methotrexate, vincristine, bleomycin).
- Identify clinical uses of these drugs.
- Understand adverse effects of these drugs.
Cancer Cell Cycle Kinetics
- Cell cycle-specific (CCS) drugs selectively target cells in specific phases of the cell cycle.
- Cell cycle-nonspecific (CCNS) drugs target cells in both cycling and resting phases.
Cell Cycle-Specific Drugs (CCS): Examples
-
Antimetabolites (S phase): 5-Fluorouracil (5-FU), Capecitabine, Cytarabine (ara-C), Gemcitabine
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Taxanes (M phase): Paclitaxel, Albumin-bound paclitaxel, Cabazitaxel
-
Vinca Alkaloids (M phase): Vinblastine, Vincristine, Vinorelbine
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Epipodophyllotoxins (G₁-S phase): Etoposide
-
Antitumor antibiotics (G₂-M phase): Bleomycin
Antimetabolites (detailed)
- Pyrimidine Analogues: 5-Fluorouracil (5-FU), Capecitabine, Cytarabine (ara-C).
- Purine Analogues: Mercaptopurine (6-MP), Thioguanine (6-TG), Azathioprine
- Anti-folates: Methotrexate, Pralatrexate.
5-Fluorouracil (5-FU)
- An antimetabolite that acts primarily during the S phase.
- It inhibits thymidylate synthase, interfering with DNA synthesis.
- Common clinical uses include colorectal cancer.
- Common adverse effects include myelosuppression, diarrhea, nausea, vomiting, and neurotoxicity.
Methotrexate
- Inhibits dihydrofolate reductase (DHFR), reducing purine nucleotide synthesis.
- Effective against acute lymphocytic leukemia, choriocarcinoma, breast cancer, and head and neck cancers.
- Common adverse effects include Bone marrow suppression, skin and gastrointestinal mucosa toxicity (mucositis).
- Leucovorin rescue can be used to reduce toxicity.
Vinca Alkaloids (Vincristine)
- Disrupts microtubule assembly during mitosis.
- Used for acute lymphocytic leukemia, Hodgkin's and non-Hodgkin's lymphoma, Wilms' tumor, and neuroblastoma.
- Adverse effects include neurotoxicity (areflexia, peripheral neuritis, paralytic ileus), lack of myelosuppression.
Bleomycin
- A cell-cycle specific (G2) anti-tumor antibiotic.
- Causes DNA damage via oxidative process.
- Used in Hodgkin's lymphoma and testicular cancer.
- Adverse effects include pulmonary dysfunction, hypersensitivity reactions, and mucocutaneous reactions.
Other Drugs and Classes
- Cyclophosphamide (CCNS): Alkylating agent used for various cancers.
- Doxorubicin: Anthracycline antibiotic, damages DNA via oxygen free radicals and inhibits topoisomerase.
- Imatinib: Tyrosine kinase inhibitor, used for chronic myelogenous leukemia (CML).
- Trastuzumab: Humanized monoclonal antibody that targets HER2, used in breast cancer.
Additional Information
- Drug classifications based on cell cycle specificity and mechanism of action.
- Specific examples of cancers typically treated with each drug.
- Potential adverse effects of each anticancer drug.
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