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    Antineoplastic Drugs

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    theintrov
    The document discusses cancer and antineoplastic drugs that target different phases of the cell cycle. It describes how cancer results from a shift in mechanisms controlling cell proliferation and differentiation. There are two main classes of genes involved: oncogenes and tumor suppressor genes like p53. The cell cycle consists of phases like G1, S, G2, and mitosis. Some drugs target specific phases while others are non-specific. Alkylating agents are a major class of antineoplastic drugs that exert cytotoxic effects by transferring alkyl groups to cellular components like DNA. They can cause side effects like nausea and damage bone marrow, the GI tract, and gonads. Resistance can develop through DNA repair, reduced drug permeability

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    Antineoplastic Drugs

    Uploaded by

    theintrov
    169 views16 pages
    The document discusses cancer and antineoplastic drugs that target different phases of the cell cycle. It describes how cancer results from a shift in mechanisms controlling cell proliferation and differentiation. There are two main classes of genes involved: oncogenes and tumor suppressor genes like p53. The cell cycle consists of phases like G1, S, G2, and mitosis. Some drugs target specific phases while others are non-specific. Alkylating agents are a major class of antineoplastic drugs that exert cytotoxic effects by transferring alkyl groups to cellular components like DNA. They can cause side effects like nausea and damage bone marrow, the GI tract, and gonads. Resistance can develop through DNA repair, reduced drug permeability

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    The document discusses cancer and antineoplastic drugs that target different phases of the cell cycle. It describes how cancer results from a shift in mechanisms controlling cell proliferation and differentiation. There are two main classes of genes involved: oncogenes and tumor suppressor genes like p53. The cell cycle consists of phases like G1, S, G2, and mitosis. Some drugs target specific phases while others are non-specific. Alkylating agents are a major class of antineoplastic drugs that exert cytotoxic effects by transferring alkyl groups to cellular components like DNA. They can cause side effects like nausea and damage bone marrow, the GI tract, and gonads. Resistance can develop through DNA repair, reduced drug permeability

    Copyright:

    Attribution Non-Commercial (BY-NC)
    Download as PPT, PDF, TXT or read online from Scribd
    Download as ppt, pdf, or txt
    169 views16 pages

    Antineoplastic Drugs

    Uploaded by

    theintrov
    The document discusses cancer and antineoplastic drugs that target different phases of the cell cycle. It describes how cancer results from a shift in mechanisms controlling cell proliferation and differentiation. There are two main classes of genes involved: oncogenes and tumor suppressor genes like p53. The cell cycle consists of phases like G1, S, G2, and mitosis. Some drugs target specific phases while others are non-specific. Alkylating agents are a major class of antineoplastic drugs that exert cytotoxic effects by transferring alkyl groups to cellular components like DNA. They can cause side effects like nausea and damage bone marrow, the GI tract, and gonads. Resistance can develop through DNA repair, reduced drug permeability

    Copyright:

    Attribution Non-Commercial (BY-NC)
    Download as PPT, PDF, TXT or read online from Scribd
    Download as ppt, pdf, or txt
    of 16

    DR. F. O.

    WANGO

    CANCER
    Cancer is a disease characterized by a shift in the

    control mechanism that governs cell proliferation and differentiation. Two important groups of genes involved in cancer physiology are oncogenes and Tumuor Suppressor Genes(p53).

    CELL-CYCLE KINETICS.
    Cell cycle has different phases and it is some of these

    phases which are targeted by antineoplastic drugs. There are differences in the duration of cell cycles of different tissues. There are drugs which are cell cycle specific.

    PHASES OF CELL CYCLE.


    G1: Precedes the DNA synthesis. G0 : Resting phase.
    S: DNA synthesis G2: An interval following the termination of DNA

    synthesis-premitotic interval. MITOTIC PHASE.

    CELL CYCLE-SPECIFIC AGENTS.


    ANTIMETABOLITES.
    BLEOMYCIN PEPTIDE ANTIBIOTICS. PODOPHYLIN ALKALOIDS PLANT ALKALOIDS.

    CELL CYCLE-NONSPECIFIC AGENTS.


    ALKYLATING AGENTS.
    ANTIBIOTICS CISPLATIN NITROSOUREAS

    CLASSES OF ANTINEOPLASTIC AGENTS


    AKYLATING AGENTS.
    ANTIMETABOLITES NATURAL PRODUCTS (1) Vinca Alkaloids (2) Taxanes

    (3) Epipodophylotoxins (4) Antibiotics ENZYMES SUBSTITUTED UREA PROTEIN KINASE INHIBITORS HORMONE AND ANTAGONISTS

    ALKYLATING AGENTS
    Exert cytotoxic effects via transfer of their alkyl groups

    to various cellular constituents. Alkylating DNA within the nucleus probably represents the major interaction that lead to cell death. They also react with sulphydryl , amino , hydroxyl, carboxyl and phosphate groups.

    The mechanism involves intramolecular cyclization to

    form an ethyleneimonium ion that may directly or through formation of a carbonium ion transfer an alkyl group to a cellular constituent. The major site of alkylation within DNA is the N7 position of guanine and this reults in miscoding through abnormal base pairing.

    Cross-linking of DNA appears to be of major

    importance to the cytotoxic action of alkylating agents. Though alkylating agents are not cell cycle-specific, cells are most susceptible in late G1 and S phases.

    ADVERSE EFFECTS.
    Vesicant effects.
    Nausea and vomitting. Toxities on Bone marrow, GIT and Gonads. Cyclophosphamide does not have a direct vesicant

    effects unless activated

    ALKYLATING AGENTS.
    Cyclophosphamide, Mechlorethemine, melphalan,

    Chlorumbicil, thiotepa Busulphan. Carmustine, lomustine and semustine are nitrosoureas.

    NITROSOUREAS
    Require biotransformation to derivatives with both

    alkylating and carbamoylating activities. They are highly lipid-soluble and can cross bloodbrain barrier. Initial halflife is 6hrs and second half life is 1-2 days. Urinary excretion appears to be the major route of elimanation from the body.

    DRUG RESISTANCE
    Capability to repair DNA lesions
    Decreased permeability of the cell to the alkylating

    drug. Increased production of glutathione which inactivates the alkylating agent.

    RELATED DRUGS ACTING AS ALKYLATING AGENTS.


    PROCARBAZINE: Inhibits the synthesis of DNA, RNA

    and protein and produces chromosome breaks. Chemotherapeutic activity is most active in Hodgkins disease. It is also leukomonogenic, teratogenic and mutogenic.

    Dacarbazine: Used mostly in melanoma, hodgkins

    disease and soft tissue sarcoma. Cisplatin and Carboplatin: Kills cells in all stages. Has relatively little effect on the bone marrow. Major antitumuor activity in genitourinary cancers.

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