Cancer drugs Flashcards
Give examples of DNA mutation due to inheritance.
Defective BRCA1/2 gene in breast cancer.
Give examples of DNA mutation that has been acquired.
Viruses Carcinogens (abestos, smoking, radiation) Alcohol Drugs Sun exposure.
List examples of how cell growth is regulated.
Growth Factors
Cell Cycle transducers
Apoptoic genes
Telomeres- cap chromosomes.
What are the objectives of cancer therapy
Curing patient- eliminating tumour.
Prolonging life- shrinking tumour.
Palliative care.
What are the toxic effects of chemotherapy
Bone marrow supression Impaired wound healing Loss of hair. Damage to GI epithelial. Stunted growth Sterility Teratogenicity.
What are the different classes of cancer drugs and what are their targets?
Cytotoxic drugs- inhibit DNA synthesis preventing cell division.
Hormones and hormone antagonists- suppress opposing hormone secretion.
Monoclonal antibodies- target specific cancer cells.
Protein kinase inhibitors-block signal cell pathways in rapidly dividing cells.
What are alkylating agents?
Target the S phase of cell division.
Form covalent bonds that prevent DNA uncoiling.
This therefore prevents replication.
What are the prolonged effects of alkylating agents.
Sterility in men. Increased risk of non-lymphotic leukemia. This is because too much WBC are produced that can cannot mature.
What are nitrogen mustard?
A form of alkylating agents.
Mechlorethamine- first anti-cancer drug.
Administered intravenously.
Explain cyclophosphamide?
Nitrogen mustard- a form of alkylating agent.
Forms covalent bonds on DNA therefore preventing uncoiling.
Prodrug. Administered orally.
Activated in the liver to form phosphamide nitrate.
Causes acrolein- haemorhagic cystitis.
What is melphalan
Nitrogen mustard.
Used to treat multiple myeloma, childhood neoblastoma and sarcoma of the extremities.
What are nitrosoureas?
A form of alkylating agent- inhibits DNA.
Highly lipophilic- used to treat CNS tumours.
Lomustine (CCNU)- a type of nitrosoureas that is administered orally and is used to treat hodkins disease and malignant melanomas.
Carmustine (BCNU)- administered intravenously. Used to non-hodkins lymphoma, multiple myeloma and brain tumours.
What are platinum compounds?
Potent alkylators.
Bind to purine bases in RNA.
However resistance may occur.
Drug is administered intravenously, very slowly (up to 8 hours).
Used to treat testicular, ovarian and cervical cancer.
Explain cisplatin
Platinum compound so a potent alkyating agent.
Used to treat testicular and cervical cancer.
Administered slowly.
Very nephrotoxic- requires hydration.
Causes severe nausea and vomiting. Risk of tinitus, peripheral neuropathy, hyperuricaemia and analphalyxsis.
Explain carbosplatin.
Platinum compound- potent alkylating agent.
Derivative of cisplating. Much fewer side effects so can be used as outpatients.
However is myelotoxic so can lead to bone marrow supression.
Used to treat ovarian and lung cancer.
Explain oxaliplatin
Platinum compound. Potent alkylating agent.
Used to treat colorectal cancer.
Explain busulfan.
Alkylating agent that is selective for bone marrow. Used to treat leukaemia.
Explain Procarbazine
An alkylating agent that is used to treat hodgkins disease.
Causes hypersensitivity rash and inhibits MAOs.
Explain Trabectedin
An alkylating agent that is used to treat soft tissue sarcoma and advanced breast cancer.
However is hepatotoxic.
Explain methotrexate.
An antimetaboline Folate antagonist. Low lipid solubility- excreted in urine virtually unchanged. Used to treat RA. Used on people with renal impairments.
Explain fluorouracil
Antimetabolite
Pyrimidine analogues.
Inhibits C T bases.
Explain Capecitabine
Antimetabolite.
Pyramidine analouge.
Inhibits C T bases.
Explain mercaptopurine
Antimetabolite.
Purine analouge.
Inhibits A G bases
Used to treat leukemia.
Explain fludarabine.
Antimetabolite
Purine analogue
Inhibits A G baes
Explain dioxorubicin?
Cytotoxic antibiotic
Binds to DNA, inhibits topII.
Local necrosis can occur at site of injection so nurses must wear gloves.
Used to treat leukaemia.
What is bleomycin?
Cytotoxic antibody.
Degrades preformed DNA.
Effective at targeting non-dividing cells.
Other cytotoxic drugs are only effective at non-dividing cells.
Causes pulmonary fibrosis,
mucotaneous reactions and hyperpyrexia.
Explain plant derivatives
Otherwise known as vinca alkaloids.
Prevent polymerisation of tubin- prevent spindle formation.
Only effective against mitosis.
Relatively non-toxic
Explain include vincristine, vinblastine.
What are taxanes?
A plant derivative.
Prevent spindle forming- only effective in mitosis.
Used to treat advanced breast and ovarian cancer.
Paclitaxel and docetaxel.
Explain etoposide?
A plant derivative- prevents spindles forming, only effective in mitosis.
Used to treat testicular cancer and lymphonmas.
Avoid skin contact.
Can causes a rapid fall in BP during IV infusion.
How do hormones treat cancer?
Used to treat cancer in hormone sensitive tissues- breast, ovaries and prostate.
Block secretion of opposing hormones and prevent the secretion of endogenous hormones.
Rarely cure but are used to treat symptoms.
Explain oestrogens
Hormone treatment- antagonists to androgen-dependent prostate cancer.
Causes resting mammary cells to proliferate, making them easier to treat.
Side effects, nausea, fluid retention, thrombosis, gynaecomastia.
Eg Ethinyloestradiol and diethylstilbesterol
Explain progesterones
Hormone treatment used to treat endometrial cancer.
e.g Megestrol, medroxyprogesterone, norethisterone
What are GnRH analogues?
A hormone treatment that inhibits the release of GnRH. This therefore reduces levels of LH/FSh which lowers testosterone levels.
Used to treat prostate cancer and advanced breast cancer in premenopausal women.
e.g Goserelin, buserelin, leuprorelin
What are somatostatin analouges
Hormone therapy that inhibits the release of CCK/gastrin.
Some tumours are reliant on stomatostatin to grow.
Octrotide lanreotide.
What is tamoxifen?
Antioestrogen.
Used in breast cancer treatment.
However causes menopausal effects, may cause endometrial cancer and blood clots.
What is letrozole?
Antioestrogen aromatase inhibitor.
Blocks conversion of androgen to oestrogen.
Not to be used in premenopausal women.
What is flutamide
Androgen antagonist used to treat prostate cancer.
How do glucocorticoids treat cancer?
Inhibit lymphocyte proliferation. Used to treat lymphomas and leukemias.
Can counteract the side effects- e.g nausea and vomiting.
Predinsolone and dexamethasone
What are monoclonal antibodies?
Cultured from hybridoma cells.
Work on specific target proteins causing lysis and apoptosis.
Advantage- targeted therapy so few unwanted side effects.
Explain teastuzumab
Monoclonal antibody- targeted protein
Targets breast cancer.
Explain ofatumumab
Monoclonal anti-body- targeted protein.
Used to treat lymphocytic leukemia.
What is rituximab?
Monoclonal antibody
Used to treat non-hodkins disease.
Binds to CD20 protein.
Causes hypertension and hypersensitivity.
What are protein kinase inhibitors?
Used to block tyrosine kinase.
Used to treat chronic meyloid leukemia. (CML)
matinib, dasatinib and nilotinib
What is lenograstim?
Myelosuppressant. Used in stem cell transplant.
Used to speed up recovery of immune system,