Anticancer Flashcards
What are the alkylating agents?
- Mechlorethamine
- Cyclophosphamide
- Carmustine
- Cisplatin
What are the antimetabolites?
- Methotrexate
- Mercaptopurine
- Fluorouracil
- Cytarabine
What are the natural antibiotics?
- Daunorubicin
2. Doxorubicin
What are the natural vinca alkaloids, etc?
- Vinblastine
- Vincristine
- Etoposide
- Paclitaxel
What are the hormonal agents?
- prednisone
- deamethasone
- tamoxifen
What is the tyrosine kinase inhibitor?
imatinib mesylate
What is the monoclonal antibodies?
trastuzumab
What is the log-kill hypothesis?
The relationship of tumor cell number to the time of diagnosis, symptoms, treatment, and survival.
What size must a tumor be to be diagnosed?
1cm diameter
Explain the difference between CCS and CCNS,
CCS - cell cycle-specific are effective in hematologic malignancies that are proliferating and in growth.
CCNS cell cycle non-specific are effective in low-growth solid tumors.
What are all the CCS agents?
- Methotrexate (S-phase)
- Mercaptopurine (S-phase)
- Fluorouracil (S-phase)
- Cytarabine (S-phase)
- Etoposide (G2 phase)
- Paclitaxel (G2 phase)
- Vinblastine (M phase)
- Vincristine (M phase)
- Trastuzumab (G1 phase)
- imatinib mesylate (G1 phase)
- Prednisone (G1 phase)
- Tamoxifen (G1 phase)
What are all the CCNS agents?
- Daunorubicin
- Doxorubicin
- Cisplatin
- Mechlorethamine
- Carmustine
- Cyclophosphamide
What are the host determinants?
Factors that influence response to cancer chemotherapy such as overall performance status of patient, immune system, age, sex, race, organ function, other diseases
What is the drug receptor assays usefulness?
Biopsy of specimen to establish management of endocrine-responsive tumors. ER-negative numbers are not likely to respond to hormonal therapy
What is the mechanism of action for alkylating agents?
Reactive alkyl group to the DNA molecule. N7 position of guanine.
Leads to miscoding, incomplete repair, excessive crosslinking
This drug is activated in the liver.
Cyclosphamide
This drug is highly lipid soluble. What indication does it have?
Carmustine, brain tumors
This drug can cause nephrotoxicity and otoxicity.
Cisplatin
What is the mechanism of action of antimetabolites?
They are metabolized instead of normal substrate, compete with normal metabolite, effect nucleotide and nucleic acid synthesis
This drug is an inhibitor of dihydrofolate reductase. Blocks conversion of folic acid to tetrahydrofolate.
Methotrexate
This drug causes an inability to convert deoxyuridylate to thymidylate in synthesis.
Methotrexate
This drug can bypass the metabolic block of methotrexate and protect normal cells.
Leucovorin
This drug inhibits enzymes of the purine nucleotide synthesis.
Mercaptopurine
This drug binds to thymidylate synthtase, blocking ratelimiting step of DNA synthesis.
Fluorouracil
This drug is converted to cytarabine triphosphate to inhibit DNA polymerase.
Cytarabine
What is the mechanism of action for natural antibiotics?
The bind to DNA through intercalation, interfere with replication. It results in uncoiling of the DNA helix.
What side effects is seen with both the anthracyclines?
cardiotoxic
What is the mechanism of action of the vinca alkaloids?
They bind to tubulin and disrupt the mitotic spindle apparatus resulting in metaphase arrest.
What side effect is seen with vinca alkaloids?
neurological toxicity
This drug forms a complex with topoisomerase II causing inhibition and DNA breaks.
Etoposide
This drug is from the bark of the taxus brevifolia. It is an antimicrotubule that promotes microtubules assembly.
Paclitaxel
What are some mechanisms of action of adrenocorticosteroids?
Suppress mitosis in lymphocytes, inhibit COX2, PLA2, cytokines, PMN, binds cytosolic receptors.
What side effect is seen with steroid use and what are the symptoms?
iatrogenic cushing’s syndrome
puffy/moon face, acne, fat distribution, thin skin, hypercalcemia
What drug is a nonsterodial antiestrogen?
tamoxifen
What drug competes with estradiol for binding to cytoplasmatic estrogen receptors.
Tamoxifen
What are the short and long term effects associated with tamoxifen?
Short: hot flash, nausea, vomiting
Long: vision, hypercalcemia, vaginal bleeding
What is the indication of use for tamoxifen?
ER positive breast carcinoma
This drug inhibits the Bcr-Abl tyrosine kinase, preventing phosphorylation.
Imatinib mesylate
This drug inhibits cell proliferation and induces apoptosis in Bcr-Abl positive cells with CML (chronic myelopid leukemia)
Imatinib mesylate
This drug is used to treat c-Kit CD117 receptor positive gastrointestinal stromal tumor.
Imatinib mesylate
This drug does not result in bone marrow suppression.
Imatinib mesylate
This drug binds to extracellular domain of the EGF human epidermal growth factor receptor HER-2.
Trastuzumab
This drug results in the downregulation of EGF receptor tyrosine kinase signaling activity.
Trastuzumab
This drug is used as an adjuvant breast cancer in EGF2 positive tumors or
metastatic breast cancer Her-2.
Trastuzumab
