Cancer drugs Flashcards Preview

Pharmacology > Cancer drugs > Flashcards

Flashcards in Cancer drugs Deck (57):
1

Alkylating agents

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

2

Alkylating agents characteristics

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

3

Mechlorethamine (mustargen) Characteristics

Alkylating agent

4

Mechlorethamine (mustargen) toxicity

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

5

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.

6

Cyclophosphamide (cytoxan) toxicity

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

7

Cisplatin (platinol) Characteristics

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

8

Testicular cancer DOC

Cisplatin (platinol)

9

Cisplatin (platinol) toxicity

acoustic nerve damage and anaphylaxis.

10

Carmustine (BCNU), Lomustine (CCNU) characteristics

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

11

Carmustine (BCNU), Lomustine (CCNU) toxicity

PROFOUND myelosuppression.

12

Antimetabolites

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

13

Methotrexate MOA

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

14

Methotrexate characteristics

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

15

Methotrexate toxicity

hepatotoxic (chronic use), pulmonary damage.

16

6-mercaptopurine (purinethol) MOA

antimetabolite. guanine analogue

17

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.

18

6-mercaptopurine (purinethol) toxicity

Jaundice, interacts with allopurinol.

19

5-fluorouracil (5-FU) MOA

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

20

5-fluorouracil (5-FU) characterisitics

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

21

5-fluorouracil (5-FU) uses

broad spectrum. solid tumors and BCC

22

Antibiotics used with cancer

Doxorubicin (adriamycin), Bleomycin (blenoxane).

23

Doxorubicin (adriamycin) MOA

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

24

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.

25

Doxorubicin (adriamycin) toxicity

Cardiac toxicity (iron)

26

DOC for thyroid cancer

Doxorubicin (adriamycin)

27

Bleomycin (blenoxane) MOA

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

28

Bleomycin (blenoxane) uses

testicular and ovarian cancers

29

Bleomycin (blenoxane) toxicity

Pulmonary fibrosis, anaphylactoid symptoms but little bone marrow suppression.

30

Plant alkaloids MOA

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

31

Plant alkaloids

Vincristine, vinblastine, paclitaxel (taxol).

32

Vincristine/vinblastine MOA

Bind tubulin and inhibit microtubule formation

33

Plant alkaloids common toxicity

Axonal transport also uses microtubules so causes peripheral neuropathy.

34

Vincristine

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

35

Vinblastine

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

36

Paclitaxel (taxol) MOA

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

37

Paclitaxel (taxol) toxicity

peripheral neuropathy, myalgias, arthralgias and hypersensitivity.

38

Tyrosine Kinase Inhibitors

Imantinib (gleevac), and Erlotinib (tarceva)

39

Imantinib (gleevac) MOA

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

40

Imantinib (gleevac) toxicity

fluid retention and myalgias.

41

Erlotinib (larceva) MOA

blocks ATP binding to the HER1/EGFR tyrosine kinase.

42

Erlotinib (larceva) toxicity

severe diarrhea

43

Cetuximab (erbitux) MOA

Monoclonal antibody that blocks the EGF receptor and cell growth.

44

Cetuximab (erbitux) toxicity

diarrhea and anaphylaxis

45

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.

46

Bevacizumab (avastin) uses

solid tumors and macular degeneration.

47

Dabrafenib/tramentinib uses

treats malignant melanoma

48

Dabrafenib/tramentinib MOA

inhibit mutant BRAF kinases that lead to unregulated cell proliferation.

49

Dabrafenib/tramentinib toxicity

severe skin toxicity

50

Nivolumab/ipilimumab MOA

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

51

Nivolumab/ipilimumab uses

malignant melanoma

52

Prednisone MOA

antiproliferative.

53

Tamoxifen MOA

estrogen receptor blocker in breast tissue

54

Tamoxifen toxicity

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

55

Trastuzumab MOA

Antibody to HER2 receptor

56

Trastuzumab toxicity

cardiac toxicity (don't use with doxorubicin)

57

Flutamide MOA

anti-androgen used with prostate cancer.