Cancer drugs

Question 1

Alkylating agents

Answer 1

mechlorethamine (mustargen), Cyclophosphamide (cytoxan), Cisplatin (platinol), Carmustine (BCNU) and Lomustine (CCNU).

Question 2

Alkylating agents characteristics

Answer 2

Alkylate the DNA (bind it) and cause miscoding, breakage or crosslinking. Vesicants (caustic)

Question 3

Mechlorethamine (mustargen) Characteristics

Answer 3

Alkylating agent

Question 4

Mechlorethamine (mustargen) toxicity

Answer 4

Hyperuricema which can be treated by alkalizing the urine and trapping it.

Question 5

Cyclophosphamide (cytoxan) characteristics

Answer 5

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.

Question 6

Cyclophosphamide (cytoxan) toxicity

Answer 6

Hemmorrhagic cystitis (treated with MESNA to bind the by product acrolene and hydration), inappropriate ADH secretion (water toxicity).

Question 7

Cisplatin (platinol) Characteristics

Answer 7

Alkylating agent. crosslinks the DNA and makes cells more sensitive to radiation.

Question 8

Testicular cancer DOC

Answer 8

Cisplatin (platinol)

Question 9

Cisplatin (platinol) toxicity

Answer 9

acoustic nerve damage and anaphylaxis.

Question 10

Carmustine (BCNU), Lomustine (CCNU) characteristics

Answer 10

Alkylating agents. Nitrosoureas. Highly lipid soluble. Effective for brain cancer (crosses the BBB) and GI cancers.

Question 11

Carmustine (BCNU), Lomustine (CCNU) toxicity

Answer 11

PROFOUND myelosuppression.

Question 12

Antimetabolites

Answer 12

Methotrexate, 6-mercaptopurine (purinethol), 5-flourouracil (5-FU).

Question 13

Methotrexate MOA

Answer 13

antimetabolite. inhibits dihydrofolate reductase to reduce the amount of folic acid and thymidylate to block DNA/RNA/protein synthesis.

Question 14

Methotrexate characteristics

Answer 14

Give a large dose to “slam” the tumor then rescue the other cells by giving leucovorin which bypasses the blockade.

Question 15

Methotrexate toxicity

Answer 15

hepatotoxic (chronic use), pulmonary damage.

Question 16

6-mercaptopurine (purinethol) MOA

Answer 16

antimetabolite. guanine analogue

Question 17

6-mercaptopurine (purinethol) characteristics

Answer 17

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.

Question 18

6-mercaptopurine (purinethol) toxicity

Answer 18

Jaundice, interacts with allopurinol.

Question 19

5-fluorouracil (5-FU) MOA

Answer 19

Antimetabolite. inhibits thymidylate synthase and blocks DNA synthesis directly. Cell cycle specific to G1 and S phases.

Question 20

5-fluorouracil (5-FU) characterisitics

Answer 20

Leucovorin increases it’s response because FH4 is needed to form thymidylate synthase complex.

Question 21

5-fluorouracil (5-FU) uses

Answer 21

broad spectrum. solid tumors and BCC

Question 22

Antibiotics used with cancer

Answer 22

Doxorubicin (adriamycin), Bleomycin (blenoxane).

Question 23

Doxorubicin (adriamycin) MOA

Answer 23

Antibiotic. Bulky compound that intercalates into DNA and physically blocks replication and repair.

Question 24

Doxorubicin (adriamycin) Characteristics

Answer 24

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.

Question 25

Doxorubicin (adriamycin) toxicity

Answer 25

Cardiac toxicity (iron)

Question 26

DOC for thyroid cancer

Answer 26

Doxorubicin (adriamycin)

Question 27

Bleomycin (blenoxane) MOA

Answer 27

Antibiotic. Binds directly to DNA. Cell cycle specific to G2 and M phases. Used orally or injected into the bladder.

Question 28

Bleomycin (blenoxane) uses

Answer 28

testicular and ovarian cancers

Question 29

Bleomycin (blenoxane) toxicity

Answer 29

Pulmonary fibrosis, anaphylactoid symptoms but little bone marrow suppression.

Question 30

Plant alkaloids MOA

Answer 30

block mitosis by interacting with microtubules so the cell can't divide.

Question 31

Plant alkaloids

Answer 31

Vincristine, vinblastine, paclitaxel (taxol).

Question 32

Vincristine/vinblastine MOA

Answer 32

Bind tubulin and inhibit microtubule formation

Question 33

Plant alkaloids common toxicity

Answer 33

Axonal transport also uses microtubules so causes peripheral neuropathy.

Question 34

Vincristine

Answer 34

Plant alkaloid. Low myelosuppression but causes peripheral neuropathy. "crisps the neurons"

Question 35

Vinblastine

Answer 35

plant alkaloid. More myelosuppression with less peripheral neuropathy. "blasts the bone"

Question 36

Paclitaxel (taxol) MOA

Answer 36

Plant alkaloid. Binds the tubulin/microtubulin and inhibits disassembly which arrests mitosis. Very active but very toxic.

Question 37

Paclitaxel (taxol) toxicity

Answer 37

peripheral neuropathy, myalgias, arthralgias and hypersensitivity.

Question 38

Tyrosine Kinase Inhibitors

Answer 38

Imantinib (gleevac), and Erlotinib (tarceva)

Question 39

Imantinib (gleevac) MOA

Answer 39

TKR inhibitor. inhibits the BCR-Abl fusion protein which is a mutation mainly seen in CML and GI stromal tumors.

Question 40

Imantinib (gleevac) toxicity

Answer 40

fluid retention and myalgias.

Question 41

Erlotinib (larceva) MOA

Answer 41

blocks ATP binding to the HER1/EGFR tyrosine kinase.

Question 42

Erlotinib (larceva) toxicity

Answer 42

severe diarrhea

Question 43

Cetuximab (erbitux) MOA

Answer 43

Monoclonal antibody that blocks the EGF receptor and cell growth.

Question 44

Cetuximab (erbitux) toxicity

Answer 44

diarrhea and anaphylaxis

Question 45

Bevacizumab (avastin) MOA

Answer 45

Monoclonal antibody for VEGF which is needed for angiogenesis and is over expressed in tumor cells. Decreases tumor blood supply and slows growth.

Question 46

Bevacizumab (avastin) uses

Answer 46

solid tumors and macular degeneration.

Question 47

Dabrafenib/tramentinib uses

Answer 47

treats malignant melanoma

Question 48

Dabrafenib/tramentinib MOA

Answer 48

inhibit mutant BRAF kinases that lead to unregulated cell proliferation.

Question 49

Dabrafenib/tramentinib toxicity

Answer 49

severe skin toxicity

Question 50

Nivolumab/ipilimumab MOA

Answer 50

activate cytotoxic T cells (leads to really bad side effects).

Question 51

Nivolumab/ipilimumab uses

Answer 51

malignant melanoma

Question 52

Prednisone MOA

Answer 52

antiproliferative.

Question 53

Tamoxifen MOA

Answer 53

estrogen receptor blocker in breast tissue

Question 54

Tamoxifen toxicity

Answer 54

estrogen agonist in the uterus, hot flashes, uterine hyperplasia.

Question 55

Trastuzumab MOA

Answer 55

Antibody to HER2 receptor

Question 56

Trastuzumab toxicity

Answer 56

cardiac toxicity (don't use with doxorubicin)

Question 57

Flutamide MOA

Answer 57

anti-androgen used with prostate cancer.