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Pharmacology > Cancer drugs > Flashcards

Cancer drugs Flashcards

1
Q

Alkylating agents

A

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

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2
Q

Alkylating agents characteristics

A

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

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3
Q

Mechlorethamine (mustargen) Characteristics

A

Alkylating agent

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4
Q

Mechlorethamine (mustargen) toxicity

A

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

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5
Q

Cyclophosphamide (cytoxan) characteristics

A

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.

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6
Q

Cyclophosphamide (cytoxan) toxicity

A

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

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7
Q

Cisplatin (platinol) Characteristics

A

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

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8
Q

Testicular cancer DOC

A

Cisplatin (platinol)

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9
Q

Cisplatin (platinol) toxicity

A

acoustic nerve damage and anaphylaxis.

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10
Q

Carmustine (BCNU), Lomustine (CCNU) characteristics

A

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

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11
Q

Carmustine (BCNU), Lomustine (CCNU) toxicity

A

PROFOUND myelosuppression.

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12
Q

Antimetabolites

A

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

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13
Q

Methotrexate MOA

A

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

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14
Q

Methotrexate characteristics

A

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

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15
Q

Methotrexate toxicity

A

hepatotoxic (chronic use), pulmonary damage.

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16
Q

6-mercaptopurine (purinethol) MOA

A

antimetabolite. guanine analogue

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17
Q

6-mercaptopurine (purinethol) characteristics

A

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.

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18
Q

6-mercaptopurine (purinethol) toxicity

A

Jaundice, interacts with allopurinol.

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19
Q

5-fluorouracil (5-FU) MOA

A

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

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20
Q

5-fluorouracil (5-FU) characterisitics

A

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

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21
Q

5-fluorouracil (5-FU) uses

A

broad spectrum. solid tumors and BCC

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22
Q

Antibiotics used with cancer

A

Doxorubicin (adriamycin), Bleomycin (blenoxane).

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23
Q

Doxorubicin (adriamycin) MOA

A

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

24
Q

Doxorubicin (adriamycin) Characteristics

A

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
Q

Doxorubicin (adriamycin) toxicity

A

Cardiac toxicity (iron)

26
Q

DOC for thyroid cancer

A

Doxorubicin (adriamycin)

27
Q

Bleomycin (blenoxane) MOA

A

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

28
Q

Bleomycin (blenoxane) uses

A

testicular and ovarian cancers

29
Q

Bleomycin (blenoxane) toxicity

A

Pulmonary fibrosis, anaphylactoid symptoms but little bone marrow suppression.

30
Q

Plant alkaloids MOA

A

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

31
Q

Plant alkaloids

A

Vincristine, vinblastine, paclitaxel (taxol).

32
Q

Vincristine/vinblastine MOA

A

Bind tubulin and inhibit microtubule formation

33
Q

Plant alkaloids common toxicity

A

Axonal transport also uses microtubules so causes peripheral neuropathy.

34
Q

Vincristine

A

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

35
Q

Vinblastine

A

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

36
Q

Paclitaxel (taxol) MOA

A

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

37
Q

Paclitaxel (taxol) toxicity

A

peripheral neuropathy, myalgias, arthralgias and hypersensitivity.

38
Q

Tyrosine Kinase Inhibitors

A

Imantinib (gleevac), and Erlotinib (tarceva)

39
Q

Imantinib (gleevac) MOA

A

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

40
Q

Imantinib (gleevac) toxicity

A

fluid retention and myalgias.

41
Q

Erlotinib (larceva) MOA

A

blocks ATP binding to the HER1/EGFR tyrosine kinase.

42
Q

Erlotinib (larceva) toxicity

A

severe diarrhea

43
Q

Cetuximab (erbitux) MOA

A

Monoclonal antibody that blocks the EGF receptor and cell growth.

44
Q

Cetuximab (erbitux) toxicity

A

diarrhea and anaphylaxis

45
Q

Bevacizumab (avastin) MOA

A

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

46
Q

Bevacizumab (avastin) uses

A

solid tumors and macular degeneration.

47
Q

Dabrafenib/tramentinib uses

A

treats malignant melanoma

48
Q

Dabrafenib/tramentinib MOA

A

inhibit mutant BRAF kinases that lead to unregulated cell proliferation.

49
Q

Dabrafenib/tramentinib toxicity

A

severe skin toxicity

50
Q

Nivolumab/ipilimumab MOA

A

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

51
Q

Nivolumab/ipilimumab uses

A

malignant melanoma

52
Q

Prednisone MOA

A

antiproliferative.

53
Q

Tamoxifen MOA

A

estrogen receptor blocker in breast tissue

54
Q

Tamoxifen toxicity

A

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

55
Q

Trastuzumab MOA

A

Antibody to HER2 receptor

56
Q

Trastuzumab toxicity

A

cardiac toxicity (don’t use with doxorubicin)

57
Q

Flutamide MOA

A

anti-androgen used with prostate cancer.

Pharmacology (24 decks)

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