Anti Neoplastic Drugs-1.pptx000ee0ehjdjsjsjs

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1. Anti Neoplastic Drugs BSN 3 rd Semester (Pharmacology)

2. What is Cancer? Cancer is a disorder of cell division (leading cause of death). Cancer is a disease caused when cells divide uncontrollably and spread into surrounding tissues. Cancer is caused by changes to DNA. Most cancer-causing DNA changes occur in sections of DNA called genes. These changes are also called genetic changes. Some terms to know Benign Refers to a tumor that is not cancerous. The tumor does not usually invade nearby tissue or spread to other parts of the body. Malignant A mass formed when normal cells begin to change and grow uncontrollably. A tumor can be benign (noncancerous) or malignant (cancerous, meaning it can spread to other parts of the body). Also called a nodule or mass.

3. Metastasis The spread of cancer from the place where the cancer began to another part of the body. Cancer cells can break away from the primary tumor and travel through the blood or the lymphatic system to the lymph nodes, brain, lungs, bones, liver, or other organs. Cancers Nomenclature Carcinoma: Cancer that starts in skin or tissues that line the inside or cover the outside of internal organs. Sarcomas: A cancer that develops in the tissues that support and connect the body, such as fat and muscle. Leukemia: A cancer of the blood. Leukemia begins when normal white blood cells change and grow uncontrollably.

4. Lymphomas: A cancer of the lymphatic system. Lymphoma begins when cells in the lymph system change and grow uncontrollably. Sometimes a tumor is formed. Adenomas: Adenomas are noncancerous tumors. They may grow along your adrenal, parathyroid or pituitary glands (glandular tissues). Treatment Modalities The most common treatments are surgery, chemotherapy, and radiation. Other options include targeted therapy, immunotherapy, laser, hormonal therapy, and others. Surgery: The removal of cancerous tissue from the body through an operation. Chemotherapy: Chemotherapy is the use of drugs to destroy cancer cells. This type of cancer treatment works by keeping cancer cells from growing, dividing, and making more cells. Chemotherapy is a systemic medication. This means it travels through the bloodstream and reaches all parts of the body.

5. Radiation therapy: The use of high-energy x-rays or other particles to destroy cancer cells. The most common type of radiation treatment is called external-beam radiation therapy, which is radiation given from a machine outside the body. When radiation treatment is given using implants (radioactive material is placed) near the cancer cells, it is called internal radiation therapy or brachytherapy. Cancer Staging Stage 0: Precancerous Stage 1: Small localized cancer Stage 2: Large cancer, probably lymph nodes involvement Stage 3: Large cancer, evident lymph nodes involvement Stage 4: Metastasis

6. Normal Cell Cycle Normal cell cycle consists of series of activities through which cell passes from the time it is formed until it reproduces. It is the process of growth and division of a single cell into daughter cells. It comprises of five phases i.e. four active and one resting phase. G1 (Presynthesis phase): Cell prepares to duplicate, synthesizes proteins and RNA which will be needed in the next phases. S (Synthesis phase): DNA replication, each of the 46 chromosomes (23 pairs) is replicated by the cell. G2 (Post-synthetic phase): Pre-mitotic phase in which cell grows more, organelles and proteins develop in preparation for cell division. M (Mitosis Phase): Cell division phase, in which there is formation of two identical daughter cells.

7. G0 (Resting phase): Cells in this phase do not replicate. The cells conduct their routine activities such as metabolism, impulse conduction, contraction or secretion. When the cell receives the signal to divide, it leaves the resting phase and enters the G1 phase. G0 is a permanent state for some cells, while others may re-start division if they get the right signals. Chemotherapy The use of chemical agents to destroy cancer cells is known as chemotherapy. It is usually given along with surgical and radiation therapy. This is the treatment of choice when cancer cannot be surgically removes or when tumor fails to respond to radiation therapy. Anticancer drug sensitivity or toxicity is directly related to the tissue growth fraction (number of cells undergoing mitosis in a tissue); chemotherapy drugs are much more toxic to tissues with high growth fractions.

8. Principles of Chemotherapy More effective against small tumors because they usually have an efficient blood supply; therefore drug delivery to the cancer site is increased. The removal of large localized tumor by surgery reduces the tumor cells burden. Combination cancer therapeutic agents have higher potency to kill cancer cells than treatment with a single drug agent, as they may affect different phases of cell cycle.

9. Classification of Anti-Neoplastic Drugs There are two main classifications of these drugs: Agents that are most effective in one specific phase are referred to as Cell cycle specific agents (CCS) or Cell cycle dependent. Example, antimetabolites, vinca alkaloids, bleomycin, taxanes Agents that are effective against cells in different phases cells in different phases (proliferative & resting phases) are called Cell cycle non specific agents (CCNS) or Cell cycle independent. Example, alkylating agents, antibiotics Antimetabolites Antitumor Antibiotics Alkylating Agents Mitotic Inhibitors Steroid hormones and their antagonists

10. Antimetabolites Antimetabolites are group of anticancer agents that exert their cytotoxic effects by interfering with the DNA synthesis. Some of the important drugs from this class are 5-fluorouracil (5-FU), 6-mercaptopurine, methotrexate, capecitabine, floxuridine, cytarabine, gemcitabine, decitabine Interfere with various metabolic functions of cells, disrupting normal cell functions. Inactivating enzymes Alter the structure of DNA, thus changing its ability to replicate. Most effective for rapidly dividing neoplastic cells. Major side effect is bone marrow depression.

11. Antitumor Antibiotics Antitumor antibiotics treat cancer by affecting the genetic material within cancerous cells. This prevents cancer cells from growing and spreading. Antitumor antibiotics, also known as antineoplastic antibiotics, are the product of soil microbes, Streptomyces bacteria. The commonly used types of antitumor antibiotics— bleomycin, dactinomycin, and anthracyclines —have a wide spectrum of activity against hematologic malignancies and solid tumors. Some of the common side effects include: nausea, vomiting, mild rash, diarrhea, abdominal pain, headache, tiredness/weakness, mouth sores, loss of appetite.

12. Alkylating agents Alkylating agents are a class of antineoplastic or anticancer drugs which act by inhibiting the transcription of DNA into RNA and thereby stopping the protein synthesis. Alkylating agents prevent cells from dividing and replicating by damaging the DNA. The most common alkylating agents are Nitrogen mustard derivatives (cyclophosphamide, ifosfamide), Nitrosoureas (carmustine, lomustine), Triazenes (dacarbazine, temozolomide), other alkylating agents (busulfan, procarbazine)

13. Alkylating antineoplastics are a class of drugs used to treat various types of cancers such as multiple myeloma (a type of cancer of the bone marrow), ovarian cancer (cancer that begins in the female reproductive organs), brain tumors, Hodgkin's disease (a malignant though often curable disease of lymphatic tissues, typically causing painless enlargement of the lymph nodes, liver, and spleen), non-Hodgkin's lymphoma (cancer that begins in the cells of the immune system), certain types of leukemia (cancer of the white blood cells) including chronic lymphocytic leukemia and chronic myelogenous leukemia, and lung cancer. Common adverse effects of alkylating agents include, nausea, vomiting, dry mouth, sores in mouth and throat, bone marrow depression, pulmonary fibrosis and hyperuricemia, hives, infertility.

14. Mitotic Inhibitors Mitotic inhibitors are also called plant alkaloids. They are compounds derived from natural products, such as plants. They work by stopping cells from dividing to form new cells, but can damage cells in all phases by keeping enzymes from making proteins needed for cell reproduction. They include Vinca alkaloids (vincristine, vinblastine), Podophyllotoxins (etoposide, teniposide), Taxanes (paclitaxel, docetaxel) They are used to treat many different types of cancer including breast, lung, myelomas, lymphomas, and leukemias. These drugs may cause nerve damage, which can limit the amount that can be given. The major toxicities of these groups are bone marrow depression, nausea and vomiting, mucositis, and diarrhea.

15. Steroid Hormones and their Antagonists Corticosteroids, often simply called steroids, are natural hormones and hormone-like drugs that are useful in the treatment of many types of cancer, as well as other illnesses. When these drugs are used as part of cancer treatment, they are considered chemotherapy drugs. Use in cancers that are sensitive to estrogen stimulation. These include estrogens, antiestrogens, androgens, antiandrogens, aromatase inhibitors, adrenal corticosteroids.