ANTICANCER. 99 good questions, nicely answered!

Hemorrhagic cystitis is a side effect of which drug?

Hemorrhagic cystitis is a side effect of:

a. Carmustine
b. Doxorubicine
c. Cyclophosphomide
d. Paclitaxel

Which of the following is used to prevent hemorrhagic cystitis?

The following is used to prevent hemorrhagic cystitis:

a. Acrolein
b. Mesna
c. Allupurinal
d. None of the above

What is the role of cytoprotectants in relation to cytotoxic drugs?

Cytoprotectants reduce severe adverse effects of cytotoxic drugs. They include agents like Amifostine, Dexrazoxane, and Colony-stimulating factors such as erythropoietin, filgrastim, oprelvekin, and sargamostim.

Which of the following drugs are cell cycle specific?

Vincristine and Doxorubicine are cell cycle specific. Options include:

a. Vincristine
b. Doxorubicine
c. Cyclophosphomide
d. Cisplatin

What are the effects of bone marrow depression caused by cytotoxic drugs?

Anemia
Leucopenia
Thrombocytopenia
Pancytopenia

What does Amifostine ameliorate?

Amifostine ameliorates cisplatin-induced renal damage. It is one of the cytoprotectant agents used to reduce adverse effects of cytotoxic drugs.

What are the consequences of immunosuppression and myelosuppression due to cytotoxic drugs?

Increased liability to infection
Delayed healing of wounds

What is the rationale behind combination therapy in cancer chemotherapy?

The rationale includes:

Each drug attacks cancerous cells at different phases of cell cycle.
Combination effect yields better efficacy than used alone.
Decreases incidence of resistance.
Decreases incidence of adverse effects and dose-dependent toxicities (lower effective doses used for each drug in combination).
Optimizes doses of anticancer drugs.

How does Dexrazoxane help in chemotherapy?

Dexrazoxane decreases cardiac toxicity of doxorubicin. It acts as a cytoprotectant to reduce severe adverse effects of cytotoxic drugs.

What gastrointestinal disturbances are associated with cytotoxic drugs?

Typhlitis
Nausea
Vomiting
GIT ulcers

What is the function of colony-stimulating factors in chemotherapy?

Colony-stimulating factors, such as erythropoietin, filgrastim, oprelvekin, and sargamostim, stimulate bone marrow erythropoiesis and help in managing neutropenia.

How do cytotoxic drugs affect the immune system and myelosuppression?

Increase liability to infection
Delayed healing of wounds

What reproductive issues can cytotoxic drugs cause?

Infertility
Sterility
Amenorrhea
Azoospermia

When is Leucovorin used in chemotherapy?

Leucovorin (folinic acid) is used with Methotrexate when administered in high doses. It acts as a cytoprotectant to mitigate adverse effects.

What are the potential organ damages from cytotoxic drugs?

Hepatotoxicity
Nephrotoxicity
Cardiotoxicity
Ototoxicity
Due to toxic free radicals

What are Adrenal Corticosteroids used for in hormone-dependent tumor growth suppression?

Adrenal Corticosteroids, such as (Dexamethasone), are used in acute lymphocytic leukemia and lymphomas to suppress hormone-dependent tumor growth.

How does Hydroxyurea function and in what conditions is it used?

Hydroxyurea acts in S phase to impair DNA synthesis. It is used in leukemia, melanoma, and advanced ovarian cancer.

What adverse effect does Mesna decrease?

Mesna decreases cyclophosphamide-induced cystitis. It is used as a cytoprotectant to reduce severe adverse effects of cytotoxic drugs.

What is Tumor Lysis Syndrome and its effects?

Hyperuricemia
Electrolyte elevation
Renal failure
Cardiac arrhythmia

How do monoclonal antibodies inhibit tumor growth?

They inhibit tumor growth by binding to growth factor receptors on the cell surface of the malignant. Used in conjunction with other agents.

What is the mechanism and use of Procarbazine?

Procarbazine inhibits DNA, RNA & protein synthesis. It is also a MAOI and used in Hodgkin’s disease.

What are the effects of cytotoxic drugs on hair and gonadal function?

Alopecia (Hair loss)
Infertility
Sterility
Amenorrhea
Azospermia

What are the potential genetic and cancer-related side effects of cytotoxic drugs?

Teratogenicity
Mutagenicity
Secondary malignancy (secondary neoplasia)

What is Trastuzumab used for in clinical applications?

Trastuzumab is used in breast cancer and targets HER2 receptors.

What is the mechanism of action for Camptothecins (Topotecan)?

The mechanism of action for Camptothecins (Topotecan) is to inhibit topoisomerase enzyme required for DNA replication and repair. It is used for several types of cancers, e.g., colorectal, lung, ovarian cancers, etc. Side effect includes myelosuppression.

Which monoclonal antibodies are used in lymphocytic leukemia and non-Hodgkin's lymphoma?

Alemtuzumab, Ibritumomab, Rituximab, and Gemtuzumab are used in lymphocytic leukemia and non-Hodgkin's lymphoma.

What are Anti-Estrogen drugs like Tamoxifen and Anastrozole used for?

Anti-Estrogen drugs, e.g., Tamoxifen and Anastrozole, are used in estrogen-dependent (pre-menopausal) breast cancer to suppress hormone-dependent tumor growth.

Describe the function and application of Imatinib.

Imatinib is a tyrosine kinase inhibitor; it inhibits cell proliferation and increases apoptosis in chronic myelogenous leukemia.

For what condition is Gemtuzumab specifically used?

Gemtuzumab is used to treat acute myeloid leukemia.

What are the uses and side effects of Podophyllotoxins?

Podophyllotoxins prevent mitosis mainly in the G2 phase of cell cycle. They are used for testicular and small cell lung cancer (Etoposide), childhood acute lymphocytic leukemia (Teniposide), and topically for localized plantar warts (Podophyllin). Side effect is myelosuppression.

What role do Anti-Androgens like Flutemide play in hormone-dependent tumor growth suppression?

Anti-Androgens, such as Flutemide, are used in prostate cancer to suppress hormone-dependent tumor growth.

What are the adverse effects of monoclonal antibodies?

Adverse effects include allergic reactions, CVS toxicity, and blood dyscrasias.

What is the mechanism of action for Vinca alkaloids?

Vinca alkaloids are CCS agents that inhibit mitotic spindle formation, stopping mitosis. They have similar structures but different antineoplastic activity and adverse effect profiles.

What is the mechanism of action and use for Taxanes (Paclitaxel)?

Taxanes (Paclitaxel) act as antimitotic agents that inhibit cell division. They are used for advanced breast and ovarian cancers. The side effect is neutropenia.

How are GnRH analogues like Leuprolide used in cancer treatment?

GnRH analogues, e.g., Leuprolide, are used in prostate cancer to suppress hormone-dependent tumor growth.

What are the clinical uses of Vincristine?

Vincristine is used for Hodgkin’s disease, Acute lymphoblastic leukemia, and non-Hodgkin’s lymphomas.

What is the use of Progestins in hormone-dependent tumor growth suppression?

Progestins are used in endometrial carcinoma to suppress hormone-dependent tumor growth.

Describe the mechanism of action and uses for Vinca alkaloids.

Vinca alkaloids inhibit mitotic spindle formation and stop mitosis. They are used for Hodgkin’s disease, lymphoblastic leukemia, non-Hodgkin’s lymphomas, choriocarcinoma, and non-lymphocytic leukemia. Side effects include tissue extravasation and bone marrow depression.

What are the clinical uses of Vinblastine?

Vinblastine is used for Hodgkin’s disease and choriocarcinoma.

What are the plant alkaloid derivatives listed under Camptothecins?

Camptothecins are derived from Camptotheca acuminate.
The derivative listed is Topotecan.

Which plant is Podophyllotoxin derived from, and what is its derivative?

Podophyllotoxin is derived from Podophyllum peltatum.
The derivative listed is Etoposide.

What are the Taxanes derived from, and what is the derivative mentioned?

Taxanes are derived from Taxus baccata.
The derivative mentioned is PACLiTAXEL.

From which plant are Vinca alkaloids derived, and what are the derivatives?

Vinca alkaloids are derived from Catharanthus roseus.
The derivatives listed are Vincristine and Vinblastine.

What is Epirubicin similar to, and what is its use in cancer treatment?

Epirubicin is similar to doxorubicin. It is used as an adjuvant in breast cancer, colorectal, and bladder cancer. Side effects include alopecia, nausea & vomiting, leukopenia, amenorrhea, anemia, mucositis. Dose: 60 – 90mg/m2.

What are the uses and side effects of Doxorubicin?

Doxorubicin is used for various cancers (breast, ovarian, prostate, thyroid, etc.), multiple myeloma, solid tumors, and childhood cancers. Side effects include bone marrow suppression, stomatitis, emesis, and local tissue damage.

What are the side effects and dosage of Bleomycin?

Bleomycin is used for squamous cell carcinoma, Hodgkin’s disease, Non-Hodgkin’s lymphoma, testicular carcinoma. Side effects include mucocutaneous toxicity, febrile reactions, mucositis, stomatitis, pulmonary fibrosis. Dose: 10 – 20unit/m2.

What conditions is Daunorubicin used to treat?

Daunorubicin is used to treat Wilms' tumour, rhabdomyosarcoma, choriocarcinoma, and Ewing’s sarcoma.

What category do cytotoxic antibiotics fall under, and from what are they isolated?

Cytotoxic antibiotics fall under Anthracycline antibiotics, which are natural in nature and isolated from the fungus Streptomyces.

What is one mechanism of action of cytotoxic antibiotics related to DNA?

Intercalate DNA resulting in inhibition of DNA synthesis.

What are the clinical uses of the medication mentioned?

Leukemia
Non-Hodgkin’s lymphoma
Metastatic breast and colorectal cancer
Basal cell carcinomas
Immunosuppressant therapy (e.g., in transplantation)
Other non-neoplastic conditions (Methotrexate used in Crohn's disease, Psoriasis, Rheumatoid Arthritis)

What are the side effects and dose for Daunorubicin?

Side effects of Daunorubicin include vomiting, stomatitis, diarrhoea, erythema, desquamation of skin, and alopecia. The dose is 15 μg/kg for 5 days.

What are examples of folic acid antagonists in anti-metabolite agents?

Examples of folic acid antagonists include:

Methotrexate
Pemetrexed

How do cytotoxic antibiotics generate highly reactive free radicals?

They generate highly reactive free radicals through enzyme mediated reductive process.

What are the side effects associated with the medication?

Bone marrow suppression
Leukocytosis & increased risk of infection
GIT stomatitis
Hepatotoxicity
Liver cirrhosis
Hyperuricemia
Teratogenicity (avoid in pregnancy)
Neurological toxicity

Name the purine antagonists listed as anti-metabolite agents.

Purine antagonists include:

Mercaptopurine
Thioguanine

What is the MOA of cytotoxic antibiotics regarding vital enzymes in the cell cycle?

MOA: Inhibit vital enzymes in cell cycle e.g. inhibit topoisomerase II enzyme inhibiting DNA and RNA synthesis.

What are some side effects related to bone marrow?

Bone marrow toxicity & myelosuppression
Aplastic anemia

What is the mode of action of anti-metabolites?

The mode of action involves competing with natural metabolites for enzyme systems, resulting in the inhibition of nucleic acid synthesis. They are effective in the CCS (S phase).

Identify the pyrimidine antagonists mentioned in the list of anti-metabolite agents.

Pyrimidine antagonists are:

Fluorouracil
Capecitabine (prodrug of 5-FU)

What are the effects of pharmacokinetics/pdynamics on tissues?

Can damage tissues directly.
Can produce systemic toxicity (dose-dependent).
Have more effects on rapidly growing tissues (e.g. bone marrow, reproductive organs, hair, etc.).

During which phase are anti-metabolites effective, and what do they target?

Anti-metabolites are effective during the CCS (S phase) and are particularly effective against rapidly growing neoplasms.

List the deoxynucleoside analogues included in the anti-metabolite agents.

Deoxynucleoside analogues include:

Cytarabine
Gemcitabine
Fludarabine
Nelarabine
Cladribine
Clofarabine
Pentostatin

Which agents are used for most lymphomas?

Most lymphomas are treated with Cyclophosphamide and Ifosfamide.

Which side effects involve the gastrointestinal system?

Severe nausea & vomiting
Mucosal toxicity

Which alkyl sulphonate is used in bone marrow tumors?

Busulphan (used in bone marrow tumors)

What are the clinical uses of Thiotepa, Cyclophosphamide, and Ifosfamide?

Breast cancer
Ovarian cancer
Bladder cancer

What are the side effects related to reproductive health?

Gonadal atrophy, Infertility

Which drug is used for multiple myeloma, melanoma, and sarcomas?

Melphalan is used for multiple myeloma, melanoma, and sarcomas.

What is the role of Methotrexate in anticancer drug mechanisms?

Methotrexate inhibits the conversion of Folic Acid to Tetrahydrofolic Acid. This process is crucial in the synthesis of nucleotides, affecting DNA and RNA synthesis.

Describe the mode of action of carbonium ions in alkylating agents.

Carbonium ions transfer reactive alkyl groups to cell constituents, mainly nucleophilic sites of DNA bases, RNA, proteins, and enzymes, inhibiting their function and causing cross linkage and DNA strand breakage.

How does 5-fluorouracil function in anticancer drug mechanisms?

5-fluorouracil targets Pyrimidines by interfering with the synthesis of cytosine, thymine, and uracil. This disruption affects the formation of nucleotides and subsequently DNA and RNA.

What is the effectiveness of CCNS in relation to neoplasms?

CCNS is effective against both slow and fast growing neoplasms. It inhibits cell proliferation by causing cross linkage, abnormal base pairing, and DNA strand breakage.

Which agents are available both orally and intravenously?

Some agents are available orally and intravenously (per m2).

What is the impact of Hydroxyurea on nucleotide synthesis?

Hydroxyurea inhibits the conversion of Purines and Pyrimidines into Nucleotides. This action disrupts DNA synthesis, affecting cell division and proliferation.

What are Cell Cycle Specific agents (CCS) effective against?

They are effective only against rapidly dividing (cycling) cells. Examples include:

Steroids
Anti-metabolites
Vinca-alkaloids
Taxanes

What happens in the S phase of the cell cycle?

Each of the 46 chromosomes is duplicated by the cell during the S phase. This phase is crucial for DNA synthesis and is part of interphase.

What urinary side effect is listed?

Haemorrhagic cystitis

Describe the function of Mercaptopurine in anticancer drug mechanisms.

Mercaptopurine interferes with the synthesis of Purines such as guanine and adenine. This disruption affects nucleotide formation and DNA synthesis.

Which agents are specific to the G₂ phase of the cell cycle?

Podophyllotoxins are specific to the G₂ phase of the cell cycle.

What are chemotherapeutic agents used for in cancer diseases?

Chemotherapeutic agents are used in cancer diseases to kill, damage, or retard growth of cancerous (neoplastic) cells. They are also called ‘Cytotoxic’ drugs.

What do Cell Cycle Non-specific agents (CCNS) target?

They kill whether resting or actively cycling cells. Types include:

Alkylating agents e.g. Nitrogen mustards, Cyclophosphamide
Antibiotics e.g. Adriamycin, Dactinomycin

Describe the G2 phase of the cell cycle.

The cell "double checks" the duplicated chromosomes for error, making any needed repairs during the G2 phase. It involves growth and preparation for mitosis.

What role does Thioguanine play in anticancer drug mechanisms?

Thioguanine targets the synthesis of Purines, specifically affecting guanine and adenine. This action disrupts nucleotide formation and DNA synthesis.

What are hematologic malignancies and what do they involve?

Hematologic malignancies:

Involve bone marrow & lymphoid tissues.
Include leukemias, lymphomas, and multiple myeloma.

What are the uses of chemotherapeutic agents?

Uses of chemotherapeutic agents include:

Cure and promote remission
Adjuvant chemotherapy
Palliative care

What is the role of the M phase in the cell cycle?

M phase involves mitosis, which is cell division. It follows the interphase and includes cytokinesis, leading to the formation of two daughter cells.

How do Alkylating Agents affect DNA in anticancer drug mechanisms?

Alkylating Agents directly modify DNA, leading to cross-linking and strand breaks. This action disrupts DNA replication and transcription, inhibiting cell division.

What are the two major classifications of solid neoplasms?

Solid neoplasms have two major classifications:

Carcinomas and Sarcomas.

What are the characteristics of normal cells in terms of cytoplasm, nucleus, nucleolus, and chromatin?

Normal cells have:

Large cytoplasm
Single nucleus
Single nucleolus
Fine chromatin

What is the significance of the G0 phase?

G0 phase is a state of cell cycle arrest. Cells in this phase are not actively preparing to divide and may enter this phase from G1.

What is the role of Antibiotics in anticancer drug mechanisms?

Antibiotics interfere with the synthesis of RNA from DNA. This disruption affects protein synthesis and cell division, contributing to anticancer effects.

What type of differences are more prominent between malignant and normal cells?

There is more of quantitative differences compared to qualitative between malignant and normal cells.

How do cancer cells differ from normal cells regarding cytoplasm and nuclei?

Cancer cells have:

Small cytoplasm
Multiple nuclei
Multiple and large nucleoli
Coarse chromatin

From what tissues are carcinomas derived, and how common are they?

Carcinomas are derived from epithelial tissues (skin, mucous membrane, linings and coverings of viscera) and are the most common type of malignant tumors.

How do Mitotic Disrupters function in anticancer drug mechanisms?

Mitotic Disrupters inhibit Cell Mitosis by interfering with spindle formation. This action prevents proper chromosome segregation, halting cell division.

What are chemotherapeutic agents used for in cancer disorders?

Chemotherapeutic agents used in cancer disorders include those used to:

kill
Damage
Retard growth of cancer cells
Prevent or treat adverse drug effects

List the characteristics of cancer cells.

Cancer cells have the following characteristics:

Rapid, uncontrolled rate of mitosis
Rapid turnover of nucleoproteins
High anabolic & low catabolic enzyme activity
High dephosphorylating activity
(Phosphorylation is the regulator of cellular activity)
Undifferentiated structure & function

What is cancer characterized by?

Cancer is characterized by a derangement in the control mechanisms that govern cell survival, proliferation, and differentiation. It involves abnormal cell growth and is a leading cause of morbidity and mortality.

What are the treatment modalities for cancer mentioned?

Treatment modalities for cancer include:

1. Surgery – for localised cancers
2. Radiotherapy – using radioisotopes
3. Chemotherapy – using drugs

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