Flashcards in Cancer drugs Deck (57)
mechlorethamine (mustargen), Cyclophosphamide (cytoxan), Cisplatin (platinol), Carmustine (BCNU) and Lomustine (CCNU).
Alkylating agents characteristics
Alkylate the DNA (bind it) and cause miscoding, breakage or crosslinking. Vesicants (caustic)
Mechlorethamine (mustargen) Characteristics
Mechlorethamine (mustargen) toxicity
Hyperuricema which can be treated by alkalizing the urine and trapping it.
Cyclophosphamide (cytoxan) characteristics
Alkylating agent. MOST important cancer drug. Broad spectrum. Needs to be activated by CYP450s so don't use with an inhibitor. Not vesicant so can be taken orally.
Cyclophosphamide (cytoxan) toxicity
Hemmorrhagic cystitis (treated with MESNA to bind the by product acrolene and hydration), inappropriate ADH secretion (water toxicity).
Cisplatin (platinol) Characteristics
Alkylating agent. crosslinks the DNA and makes cells more sensitive to radiation.
Testicular cancer DOC
Cisplatin (platinol) toxicity
acoustic nerve damage and anaphylaxis.
Carmustine (BCNU), Lomustine (CCNU) characteristics
Alkylating agents. Nitrosoureas. Highly lipid soluble. Effective for brain cancer (crosses the BBB) and GI cancers.
Carmustine (BCNU), Lomustine (CCNU) toxicity
Methotrexate, 6-mercaptopurine (purinethol), 5-flourouracil (5-FU).
antimetabolite. inhibits dihydrofolate reductase to reduce the amount of folic acid and thymidylate to block DNA/RNA/protein synthesis.
Give a large dose to "slam" the tumor then rescue the other cells by giving leucovorin which bypasses the blockade.
hepatotoxic (chronic use), pulmonary damage.
6-mercaptopurine (purinethol) MOA
antimetabolite. guanine analogue
6-mercaptopurine (purinethol) characteristics
metabolized by xanthine oxidase. If used with allopurinol to reduce hyperuricemia (xanthine oxidase inhibitor) the toxicity will increase. Have to lower the dose if given with allopurinol.
6-mercaptopurine (purinethol) toxicity
Jaundice, interacts with allopurinol.
5-fluorouracil (5-FU) MOA
Antimetabolite. inhibits thymidylate synthase and blocks DNA synthesis directly. Cell cycle specific to G1 and S phases.
5-fluorouracil (5-FU) characterisitics
Leucovorin increases it's response because FH4 is needed to form thymidylate synthase complex.
5-fluorouracil (5-FU) uses
broad spectrum. solid tumors and BCC
Antibiotics used with cancer
Doxorubicin (adriamycin), Bleomycin (blenoxane).
Doxorubicin (adriamycin) MOA
Antibiotic. Bulky compound that intercalates into DNA and physically blocks replication and repair.
Doxorubicin (adriamycin) Characteristics
Generates free radicals whose effects are worsened by iron. Can lead to cardiac toxicity. have to decrease the iron by chelating it, don't take with iron supplements.
Doxorubicin (adriamycin) toxicity
Cardiac toxicity (iron)
DOC for thyroid cancer
Bleomycin (blenoxane) MOA
Antibiotic. Binds directly to DNA. Cell cycle specific to G2 and M phases. Used orally or injected into the bladder.
Bleomycin (blenoxane) uses
testicular and ovarian cancers
Bleomycin (blenoxane) toxicity
Pulmonary fibrosis, anaphylactoid symptoms but little bone marrow suppression.
Plant alkaloids MOA
block mitosis by interacting with microtubules so the cell can't divide.
Vincristine, vinblastine, paclitaxel (taxol).
Bind tubulin and inhibit microtubule formation
Plant alkaloids common toxicity
Axonal transport also uses microtubules so causes peripheral neuropathy.
Plant alkaloid. Low myelosuppression but causes peripheral neuropathy. "crisps the neurons"
plant alkaloid. More myelosuppression with less peripheral neuropathy. "blasts the bone"
Paclitaxel (taxol) MOA
Plant alkaloid. Binds the tubulin/microtubulin and inhibits disassembly which arrests mitosis. Very active but very toxic.
Paclitaxel (taxol) toxicity
peripheral neuropathy, myalgias, arthralgias and hypersensitivity.
Tyrosine Kinase Inhibitors
Imantinib (gleevac), and Erlotinib (tarceva)
Imantinib (gleevac) MOA
TKR inhibitor. inhibits the BCR-Abl fusion protein which is a mutation mainly seen in CML and GI stromal tumors.
Imantinib (gleevac) toxicity
fluid retention and myalgias.
Erlotinib (larceva) MOA
blocks ATP binding to the HER1/EGFR tyrosine kinase.
Erlotinib (larceva) toxicity
Cetuximab (erbitux) MOA
Monoclonal antibody that blocks the EGF receptor and cell growth.
Cetuximab (erbitux) toxicity
diarrhea and anaphylaxis
Bevacizumab (avastin) MOA
Monoclonal antibody for VEGF which is needed for angiogenesis and is over expressed in tumor cells. Decreases tumor blood supply and slows growth.
Bevacizumab (avastin) uses
solid tumors and macular degeneration.
treats malignant melanoma
inhibit mutant BRAF kinases that lead to unregulated cell proliferation.
severe skin toxicity
activate cytotoxic T cells (leads to really bad side effects).
estrogen receptor blocker in breast tissue
estrogen agonist in the uterus, hot flashes, uterine hyperplasia.
Antibody to HER2 receptor
cardiac toxicity (don't use with doxorubicin)