Chemotherapy Drugs Flashcards
What is cancer?
Normal cell > uncontrolled proliferation > tumour > loss of function/ability to metastasize.
What causes cancer?
DNA mutation of a normal cell.
What regulates cell growth?
Growth factors, Cell cycle, apoptotic genes, telomeres.
What do Oncogenes do?
produce large amounts of normal proteins to enhance cell survival and proliferation instead of killing.
What is Metastasis?
Primary tumour > enzymes breakdown ECM > invade tissue > angiogenesis > secondary tumour.
Objectives of cancer treatment…
cure, eliminate cancer traces, prolong life, palliative therapy.
What is Chemotherapy?
kill malignant cells in the body as immune system fails to recognise them as foreign.
Side effects of Chemotherapy?
Affects all rapidly dividing tissue, bone marrow suppression, impairs wound healing, hair loss, GI epithelium damage, stunts growth, infertility, teratogenicity, bleeding, bruising.
Mechanism of Alkylating Agents…
Target cell in S phase to form covalent bond with DNA and prevent uncoiling/inhibit replication.
Examples of Alkylating Agents…
Busulifan - bone marrow selective.
Procarbazine - Hodgkins, hypersensitivity rash.
Trabectedin - soft tissue sarcoma, advanced ovarian cancer, hepatotoxic.
Examples of Nitrogen Mustards….
Mechlorethamine - reactive IV
Cyclophosphamide - oral, leukaemia, lymphoma, melon, retino/neuroblastoma
Melphalan - multiple myeloma, child neuroblastoma
Chlorambucil/Bendamustine/Estramustine - oestrogen analogue.
Examples of Nitrosoureas…
Carmustine BCNU -, IV multiple myeloma, non-hodgkin lymphoma, brain tumours
lomustine CCNE - hodgkins, malignant melanoma.
Examples of Platinum Compounds…
Cisplatin - potent alkylator bind RNA DNA protein purine bases. testicular/ovarian cancer IV.
Carboplatin - outpatient, myelotoxic
Oxaliplatin - colorectal cancer with fluoroeracil
Side Effects of Platinum Compounds…
nephrotocix, n&v, tinnitus, peripheral neuropathy, hyperuricaema, anaphylaxis.
Use of Folate Antagonists…
Essential for DNA synthesis/cell division.
Examples of Folate Antagonists…
Methotrexate - oral IV IM, low lipid solubility. treats childhood acute lymphoblastic leukaemia, choriocarcinoma, non-hodkgins.
NSAIDS - reduce excretion, increase toxicity, tumour cells develop resistance.
Mechanism of Pyrimidine Analogues…
Compete with C and T bases and inhibit DNA synthesis.
Examples of Pyrimidine Analogues…
Flurouracil - solid tumour
Capecitabine - colon, myloblastic leukaemia.
Cytarabine - myeloblastic leukaemia
Gemcitabine - palliative, pancreatic/bladder/ovarian/breast
Mechanism of Purine Analogues…
Compete with A and G to inhibit purine metabolism
Examples of Purine Analogues…
Mercaptopurine, Tioguanine, Pentostatin, Fludarabine
Examples of Cytotoxic Antibiotics…
Doxorubicin - bind to DNA, inhibit synthesis. inhibits topoisomerase II. treats myeloblastic leukaemia 450g/m.
Bleomycin - degrades preformed DNA, active against non-dividing cells. treats metastatic germ cell cancer.
Side effects of cytotoxic antibiotics…
cardiac disarythmias, heart failure, myelosuppression, pulmonary fibrosis, mucocutaneous reactions, hyperpyrexia.
Mechanism of Plant Derivatives…
prevent polymerisation of tubular > microtubules > prevent spindle formation.
effect occurs during M phase
Examples of Plant Derivatives…
Vinca Alkaloids (Vincristine, Vinblastine, Vindesine) Texans (Paclitaxel, Docetaxel) - treat breast and ovarian cancer. Etoposide - testicular cancer/lymphomas / small cell carcinoma of bronchi
Side effects of plant derivatives…
neuromuscular effects, tingling, abode cramp, jaw pain, rapid fall in blood during IV.
Use of hormones…
tissue growth inhibited by R antagonists, hormones with opposing actions block synthesis of endogenous hormones.
Examples of hormones used…
Oestrogen (Ethinyloestradiol, Diethylstilbestrol) - androgen dependent prostate cancer. stimulate mammary cells to proliferate.
Progestogen (Megestol, Medroxyprogesterone, Norethisterone) - endometrial cancer.
GnRH Analogue (Hoserelin, Buserelin, Leuproeli, Triptorelin) - prostate/breast cancer post menopause.
Somatostatin Analogue (Octreotide, Lanreotide) -inhibit CCK gastrin secretion.
Hormone antagonists (Tamoxifen, Eulyestrant) - breast cancer. (Letrozole, Exemastine) (Flumatide, Cyproterone, Bicalutamode) - prostate cancer.
Glucocorticoids (prednisolone, dexamethasone)
Mechanism of Monoclonal Antibodies / Immunotherapy…
produced by cultured hybridoma cells, react with target protein on cancer cells to activate immune system causing lysis of cancer.
Examples of Monoclonal Antibodies…
Rituximab - B-lymphocyte.
Trastumab
Ofactumumab - resistant chronic lymphocytic leukaemia
Bevacizumab - colorectal cancer.
Mechanism of Protein Kinase Inhibitor…
Imatinib, Dasatinib, Nilotinib.
block tyrosinekinases in GF signal pathways.
treat chronic myeloid leukaemia.
Drugs that control side effects…
N&V - ondansetron, granisetron, metoclopramide.
Anxiety - Lorazepam, benzodiazepine.
