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Questions and Answers
Match the following cancer terminologies with their definitions:
Match the following cancer terminologies with their definitions:
Neoplasm = New growth Tumor = Local swelling Benign cancer = Tumor that is not life-threatening Malignant cancer = Tumor that is life-threatening
Match the types of cancer based on their tissue origin:
Match the types of cancer based on their tissue origin:
Carcinoma = Epithelial tissue Sarcoma = Connective tissue Blastoma = Immature embryonic tissues Hemopoietic cancers = Blood and lymph tissues
Match the causes of cancer with their descriptions:
Match the causes of cancer with their descriptions:
Carcinogenic chemicals = Found in smoke Viruses = Implicated in human cancer Food & environment = Potential cancer contributors Chemotherapy = Can induce secondary cancers
Match the cancer treatment methods with their applications:
Match the cancer treatment methods with their applications:
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Match the classifications of chemotherapeutics with their descriptions:
Match the classifications of chemotherapeutics with their descriptions:
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Match the drug with its mechanism of action:
Match the drug with its mechanism of action:
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Match the drug with the specific target enzyme:
Match the drug with the specific target enzyme:
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Match the drug with its primary indication:
Match the drug with its primary indication:
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Match the drug with its classification:
Match the drug with its classification:
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Match the drug with its adverse effect:
Match the drug with its adverse effect:
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Study Notes
Antineoplastic Agents
- Antineoplastic agents are used to treat cancer.
- Cancer is characterized by abnormal, rapid, and uncontrolled cell growth.
- Normal cells divide and proliferate in a controlled manner.
- Cell death (apoptosis) is a natural process of removing damaged cells.
- Neoplasm refers to a new growth.
- Tumor is a local swelling.
- Cancer is a type of fire cell.
- Benign cancer is a type of tumor that is not life-threatening.
- Malignant cancer is a tumor that is life-threatening.
- Metastasis is the separation of individual cancer cells from an established tumor, entering the blood supply and initiating new tumors elsewhere in the body.
- Cancer can arise from various tissues.
Classification
- Carcinoma arises from epithelial tissues.
- Sarcoma originates from mesodermal tissues (e.g., connective tissue, muscle, bone).
- Blastoma originates from blood and hemopoietic tissues (e.g., lymphoid, erythroid).
Causes of Cancer
- Carcinogenic chemicals in smoke.
- Viruses.
- Food and environmental factors.
- Chemotherapy or radiotherapy.
Cancer Treatment
- Surgery and radiation therapy are preferred for localized cancers.
- Chemotherapy is reserved for systemic cancers.
Classification of Chemotherapy
- Antimetabolites
- Alkylation agents
- Hormones
Antimetabolites
- Antimetabolites are false substrates that inhibit DNA nucleotide synthesis.
- They are prodrugs and require conversion to nucleotide forms.
- They are actively taken up by cells via selective nucleoside transporter proteins.
Dihydrofolate Reductase Inhibitors (DHFRIs)
- Methotrexate inhibits the enzyme DHFR, leading to decreased FH4 and thymidine levels.
- Dihydrofolic acid is converted to tetrahydrofolic acid (FH4), an important co-enzyme.
Thymidylate Synthase Inhibitors
- 5-Fluorouracil inhibits thymidylate synthase, disrupting dTMP synthesis and DNA synthesis. – 5-Fluorouracil is a suicidal inhibitor.
- The reaction requires the loss of H+.
DNA Polymerase Inhibitors
- Cytarabine is an analogue of deoxycytidine.
- It’s a competitive inhibitor of DNA polymerase, causing chain termination upon incorporation.
Purine Antagonists
- 6-Mercaptopurine is a prodrug converted to thio-dGTP.
- It inhibits purine synthesis, incorporates into DNA/RNA, and promotes apoptosis.
- Used to treat leukemias.
Drugs Acting Directly on DNA
- Alkylating agents damage DNA through alkylation or intercalation.
- They react with both DNA and proteins, causing poor selectivity.
- Alkylating agents can be mutagenic and carcinogenic.
Alkylating Agents
- Nitrogen mustards (like mechlorethamine, melphalan, chlorambucil) – Mechlorethamine and Mustine: The only aliphatic nitrogen-mustard used clinically. – Melphalan: Orally active. – Chlorambucil: The phenyl ring contributes greatly to reactivity, side effects, and bioavailability.
- Mechanism: Intra/Intermolecular cross linking.
- Assay: Hydrolysis with KOH to form KCL which can be determined using Volhard’s method.
Oxazaphosphorines
- Cyclophosphamide is a prodrug activated by cytochrome P450.
- It generates a highly reactive intermediate, acrolein, which damages tissues.
- Kidney toxicity is reduced via co-administration of mesna
- It is commonly used and has broad applications.
2-Nitrosoureas
- Carmustine is a chloroethyl-nitrosourea derivative.
- It is lipid soluble so it can cross the blood-brain-barrier and is used for brain tumor treatment.
- It decomposes spontaneously in the body.
3-Merthane Sulfonate
- Busulphan alkylates the N7 position of guanine.
- The sulfonate group acts as a good leaving group, similar to chlorine in nitrogen mustards.
- Assay to measure Busulfan: Hydrolyzed in water to liberate methane sulphonic acid.
4-Platinum Complexes
- Platinum complexes form intrastrand cross-links in DNA.
- They inhibit H-bonding between guanine and cytosine, inhibiting transcription.
5-Mitomycin C
- Mitomycin C is an alkylating agent forming interstrand cross-links in DNA.
- Bodily activation involves reduction and loss of methoxy group.
- Highly effective in anaerobic conditions, like in solid tumors, however, it has many side effects.
B - Antisense therapy
- Oblimersen is an antisense drug targeting mRNA of the Bal-2 protein.
- This approach suppresses apoptosis and increases sensitivity to chemotherapy and radiation.
C- Intercalating Agents
- Amsacrine contains a planar heteroaromatic ring.
- It disrupts DNA structure and inhibits replication and transcription.
Natural Products
- Vinca alkaloids (vinblastine, vincristine, vindesine) and acridone alkaloids (acronycine) contain natural anticancer products .
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Description
This quiz covers the fundamentals of antineoplastic agents used in cancer treatment. It explores cancer characteristics, types of tumors, classifications of cancer, and their causes. Test your knowledge on how these agents work against abnormal cell growth and cancer development.
