Antineoplastic agents

Cancer refers to a malignant neoplasm or new growth. Cancer cells manifest uncontrolled
proliferation, loss of function due to loss of capacity to differentiate, invasiveness, and the ability
to metastasize.
Cancer arises as a result of genetic changes in the cell, the main genetic changes being;
inactivation of tumor suppressor genes and activation of oncogenes.
There are three approaches for the management of cancer:

  1. Radiotherapy
  2. Surgery
  3. Chemotherapy
    Most anticancer drugs are antiproliferative, and hence affect rapidly growing dividing normal
    cells. Anticancer drugs are broadly classified into two: cytotoxic drugs and hormones.
    Cytotoxic drugs are further classified into:
  • Alkylating agents and related compounds (e.g. cyclophosphamide, lomustine, thiotepa,
    cisplatin): These groups of drugs act by forming covalent bonds with DNA and thus
    impending DNA replication.
  • Antimetabolites (e.g. methotrexate, fluorouracil, mercaptopurine): These drugs blocks or
    destabilize pathways in DNA synthesis.
  • Cytotoxic antibiotics (e.g. Doxorubucin, bleomycin, dactinomycin): These drugs inhibit
    DNA or RNA synthesis or cause fragmentation to DNA chains or interfere with RNA
    polymerase and thus inhibit transcription.
  • Plant derivatives (e.g. vincristine): Inhibits mitosis
    Hormones and their antagonists are used in hormone sensitive tumors (eg. glucocorticoids for
    lymphomas, oestrogens for prostatic cancer, tamoxifen for breast tumors).
    General toxic effects of anticancer drugs:
  • Bone marrow toxicity.
  • Impaired wound healing.
  • Sterility.
  • Loss of hair.
  • Damage to gastrointestinal epithelium.

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