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  • Antineoplastic Drugs

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    Irene Zae Mwandoto
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    This document discusses various classes of antineoplastic agents used to treat cancer. It describes the cell cycle and its phases that certain agents target. Alkylating agents are covered in depth, with mechanisms involving alkylation of DNA to cause cell death. Specific alkylating agents mentioned include cyclophosphamide, mechlorethemine, and nitrosoureas. Resistance to these drugs can develop through DNA repair, decreased permeability, or glutathione inactivation of the alkylating agent. Adverse effects include bone marrow suppression, nausea/vomiting, and damage to organs like the gastrointestinal tract.

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    This document discusses various classes of antineoplastic agents used to treat cancer. It describes the cell cycle and its phases that certain agents target. Alkylating agents are covered in depth, with mechanisms involving alkylation of DNA to cause cell death. Specific alkylating agents mentioned include cyclophosphamide, mechlorethemine, and nitrosoureas. Resistance to these drugs can develop through DNA repair, decreased permeability, or glutathione inactivation of the alkylating agent. Adverse effects include bone marrow suppression, nausea/vomiting, and damage to organs like the gastrointestinal tract.

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    25 views16 pages

    Antineoplastic Drugs

    Uploaded by

    Irene Zae Mwandoto
    This document discusses various classes of antineoplastic agents used to treat cancer. It describes the cell cycle and its phases that certain agents target. Alkylating agents are covered in depth, with mechanisms involving alkylation of DNA to cause cell death. Specific alkylating agents mentioned include cyclophosphamide, mechlorethemine, and nitrosoureas. Resistance to these drugs can develop through DNA repair, decreased permeability, or glutathione inactivation of the alkylating agent. Adverse effects include bone marrow suppression, nausea/vomiting, and damage to organs like the gastrointestinal tract.

    Copyright:

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

    DR. F. O.

    WANGO

    CANCER
    cell proliferation and differentiation.
    oncogenes and Tumuor Suppressor Genes(p53).

    CELL-CYCLE KINETICS.
    targeted specific phases.

    PHASES OF CELL CYCLE.


    . G0 : Resting
    G1: Precedes S: DNA synthesis G2: 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
    . Alkylating DNA cell death.
    react sulphydryl , amino , hydroxyl, carboxyl and

    phosphate groups.

    mechanism
    Through ethyleneimonium ion directly /carbonium

    transfer an alkyl to cellular . @N7 Cross-linking of DNA.

    ADVERSE EFFECTS.
    Vesicant expt activated directCyclophosphamide
    Nausea and vomitting. Bone marrow, GIT and Gonads.

    ALKYLATING AGENTS.
    Cyclophosphamide, Mechlorethemine, melphalan,

    Chlorumbicil, thiotepa Busulphan. .

    NITROSOUREAS
    Carmustine, lomustine and semustine are

    nitrosoureas highly lipid-soluble cross blood-brain barrier.

    DRUG RESISTANCE
    repair DNA
    Decreased alkyl permeability. Increased glutathione inactivates the alkylating

    agent.

    DRUGS ACTING AS ALKYLATING


    PROCARBAZINE: Inhibits synthesis of NA a
    Hodgkins disease. leukomonogenic, teratogenic and mutogenic.

    Dacarbazine: melanoma, hodgkins disease and soft

    tissue sarcoma. Cisplatin and Carboplatin: genitourinary cancers & little effect bone marrow. .

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