Chemotherapy drugs. Flashcards
List the toxic effects of chemotherapy
bone marrow suppression impaired wound healing loss of hair damage to GI epithelium growth stunted bleeding/bruising N&V Kidney damage
What do Alkylating Agents do?
Target cells in the S phase. Form covalent bonds with DNA to prevent uncoiling which inhibits replication.
Name the 4 different classes of alkylating agents…
Nitrogen Mustards
Nitrosoureas
Platinum compounds
Others
What is Cyclophosphamide?
A nitrogen mustard. Prodrug - can be administered orally. Activated into Acrolein in the liver.
Name some other nitrogen mustard drugs…
Melphalan, chlorambucil, bendamustine, estramustine
Carmustine (IV) and Lomustine (oral) are examples of what?
Nitrosoureas. They are given for CNS tumours.
Cisplatin is a what?
A Platinum Compound.
How does Cisplatin work and what type of cancers can it treat?
Binds to RND, DNA and protein. Binds to purine bases. Testicular, Ovarian, Cervical, Lung, Bladder, Head and neck cancers
What are the side effects of Cisplatin?
V. nephrotoxic - requires hydration/infusion
Causes severe N&V
Risk of tinnitus, peripheral neuropathy, gout and anaphylaxis.
Name the 2 other platinum compounds…
Carboplatin - for advanced ovarian and lung cancer
Oxaliplatin - colorectal cancer
What do antimetabolites do?
Act as folate antagonists so DNA synthesis and cell division is inhibited.
Give an example of a folate antagonist.
Methotrexate
What does methotrexate do?
Given orally, IM or IV. Mostly excreted unchanged in urine. Tumour cells may develop resistance. Also used to suppress immune system (e.g in RA)
What are the other two types of antimetabolites?
Pyrimidine analogues - fluorouracil, capecitabine, cytarabine, gemcitabine.
Purine analogues - mercaptopurine
What do cytotoxic antibiotics do?
Bind to DNA and inhibits DNA/RNA synthesis or degrade DNA.
What are the names of some cytotoxic antibiotics?
Doxorubicin, Bleomycin, Dactinomycin, Mitomycin.
What does Bleomycin do?
Degrades pre-formed DNA> Causes little myelosuppression BUT causes pulmonary fibrosis in 10% of patients.
What are Vinca Alkaloids?
Plant derivatives. Prevent polymerisation of tubulin - prevents spindle formation.
What are the names of some vinca alkaloids?
Vincristine, Vinblastine, Vindesine.
What are taxanes?
Plant derivatives. Similar to vinca alkaloids - prevent spindle formation. E.g paclitaxel, docetaxel.
What are oestrogen’s used for?
Ethinyloestradiol - used in prostate cancer palliative care treatment.
What are the side effects of Ethinyloestradiol?
nausea, fluid retention, thrombosis, impotence
What are the drug names for Progestogens?
Megestrol, Medroxyprogesterone, Norethisterone. Used to treat endometrial cancer.
What are GnRH analogues?
Hormones used in prostate and breast cancer.
Name the GnRH analogues.
Goserelin, Buserelin, Leuprorelim
What are hormone antagonists?
E.g Tamoxifen, Letrozole, Flutamide. Inhibit transcription of oestrogen-responsive genes. Androgen antagonists.
How do prednisolone and dexamethasone help to treat cancer?
Inhibit lymphocyte proliferation - for treatment of lymphomas and leukaemia’s.
What are the actions of monoclonal antibodies?
React with specific target proteins expressed on cancer cells - this activates the immune system and causes lysis of cancer cells.
What is RituxiMAB?
A monoclonal antibody. Causes lysis of B-lymphocytes.
What is ImatiNIB?
A protein kinase inhibitor. Blocks tyrosine kniases - prevents angiogenesis. Used to treat chronic myeloid leukaemia.