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Pharmacology Unit 1 > Cancer III > Flashcards

Cancer III Flashcards

1
Q

DNA Intercalating Agents

A
  • often called anti-tumor antibiotics
  • derived from various strains of soil microbe streotomyces
  • bind to DNA through intercalation between specific bases
  • cause DNA strand breaks
  • block synthesis of DNA, RNA or both
  • dactinomycin, antracyclines, bleomycin
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2
Q

dactinomycin

A
  • intercalating
  • actinomycin D
  • first anti cancer antibiotic derived from streptomyces
  • intercalates between G-C bp
  • interferes with DNA dependent RNA pol, causing inhibition of DNA transcription
  • also causes single strand breaks in DNA
  • wilms tumor, rhabdomyosarcoma, ewings
  • anorexia, nausea, vomiting
  • hematopoietic suppression with pancytopenia
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3
Q

anthracyclines

A

intercalating

  • daunorubucin, doxorubicin, epirubicin, idarubicin
  • reduced to intermediates that donate electrons to oxygen to make superoxide
  • superoxide reacts with itself to make h2o2, which is cleaved in presence iron to form an OH radical
  • Oh radical cleaves DNA
  • dose limiting cardiotoxicity
  • dexrazoxane needed- iron chelating that blocks free radicals
  • neutropenia
  • stomatitis, alopecia
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4
Q

doxorubicin

A
  • intercalates via OH (anthracycline)
  • adriamycin
  • broad clinical spectrum, one of most widely used
  • used for sarcomas, breast and lung carcinomas, lymphomas
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5
Q

daunorubicin and idarubicin

A
  • intercalating via OH (anthra)

- used in combo with AraC for AML

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6
Q

epirubicin

A
  • intercalating anthra (OH)

- used in FEC for treatment of metastatic breast cancer

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7
Q

bleomycin

A
  • DNA intercalating
  • mixture of two peptides from streptomyces
  • binds to DNA and induces single/double strand DNA breaks
  • acts in G2 phase
  • used as component of PEB combo regimen for trt of testicular carcinoma or as a component of AVBD for hodgkins
  • also effective agains sq cell carcinomas
  • dose related pulmonary tox (fibrosis)
  • minimally myelosuppressive
  • cutaneous tox- hyperpig, hyperkeratosis, erythema
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8
Q

MT inhibitors

A

-plant natural products
-bind to tubulin, interfere with MT function
-cause mitotic arrest
-M phase!
vinca alkaloids-vinblastine, vincristing
-taxanes- paclitaxel, docetaxel

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9
Q

vinca alkaloids

A

-MT inhib
-vinblastine
vincristine
-derived from periwinkle plant Vinca rosea
-bind to tubulin, prevent polymerization of tubulin into MT

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10
Q

taxanes

A
  • MT inhib
  • paclitaxel
  • docetaxel
  • derived from yew trees
  • paclitaxel first from slow growing pacific yew
  • docetaxel from needles of european yew
  • bind to tubuling and prevent DEpolymerization of MT
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11
Q

vinblastine

A

vinca alk-MT inhib (pol)

  • component of ABVD for hodgkins
  • myelosuppression, nausea, vomiting
  • resistance through amp of p glycoproteins and mutations in the cancer tubulins reduce binding of drugs to targets
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12
Q

vincristine

A
  • vinca alk MT inhib (pol)
  • glucocorticoids in trt of childhood ALL
  • component of MOPP
  • dose limiting neurotox-peripheral neuropathy
  • relatively low tox in bone marrow
  • amp of p glycoproteins and mutated tubulin
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13
Q

paclitaxel

A

taxane MT inhib (depol)

  • metastatic breast, ovarian, lung, head and neck
  • neutropenia, peripheral neuropathy
  • hypersensitivity reactions
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14
Q

docetaxel

A
  • taxane MT inhib (depol)
  • met breast, ovarian, lung, head and neck
  • hormone refractory prostate cancer
  • neutropenia, peripheral neuropathy
  • hypersensitivity reactions
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15
Q

topoisomerase inhibitors

A
  • normally mediate DNA strand breakage and resealing during replication or transcription of DNA
  • I breaks and reseals ss, II double strand
  • inhibitors cause permanent DNA strand breaks by preventing resealing
  • epipodophyllotoxins- etoposide, teniposide
  • camptothecin analogs- irinotecan, topotecan
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16
Q

epipodophyllotoxins

A

top II inhib

  • etoposide
  • teniposide
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17
Q

camptothecin analogs

A
  • top I inhib

- irinotecan, topotecan

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18
Q

etoposide

A
  • epipodophyllotoxin
  • topo II inhibitor
  • broad clinical spectrum
  • testicular carcinoma, lung cancer, non-hodgkins
  • dose limiting myelosuppression
  • oral mucositis
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19
Q

teniposide

A
  • -epipodophyllotoxin
  • top II inhib
  • ALL
  • dose limiting myelosuppression
  • oral mucositis
20
Q

irinotecan

A
  • camptothecin analog, top I inhib
  • advanced colorectal cancer, lung, ovarian, cervical, brain
  • severe neutropenia and diarrhea
21
Q

topotecan

A
  • camptothecin analog, top I inhib
  • ovarian and small cell lung cancer
  • severe neutropenia and diarrhea
22
Q

hormones and antagonists

A
  • used for hormone dependent neoplasms
  • lymphomas, leukemias
  • breast
  • prostate
23
Q

hormones for lymphomas and leukemias

A
  • glucocorticoids-prednisone/ dexamethasone
  • cytotoxic effects on lymphocytes, inhibit mitosis in lymphocytes
  • prednisone + vincristine produce remission in ALL
  • prednisone also component of MOPP and CHOP for hodgkins and non-hodgkins
  • dexamethasone to reduce edema following radiation of brain tumors
24
Q

hormone therapy for breast cancer

A
  • usually estrogen dependent and can be suppressed by admin of estrogen antagonists
  • selective estrogen receptor modulators-tamoxifen
  • selective estrogen receptor downregulators- fulvestrant
  • aromatase inhib- aminoglutethamide, anastrozole, letrozole, exemestane
25
Q

selective estrogen receptor modulators

A
  • SERMs
  • tamoxifen
  • trt of ER positive early stage and metastatic breast cancer
  • used for prevention in high risk women
  • hot flushes, hair loss, nausea/vomiting
  • weak agonist of ER in endometrium, increased risk of endometrial cancer and thromboembolism
26
Q

selective estrogen receptor downregulators

A
  • SERDs
  • fulvestrant first FDA approved
  • binds to ER with >100 fold higher affinity of tamoxifen and inhibits hormone receptor complex formation
  • also reduces ER expression
  • post menopausal women with ER pos metastatic breast cancer
27
Q

aromatase inhibitors

A
  • aminoglutethamide (1st gen- weak and lots of tox), anastrozole (3rd gen, potent and selective), letrozole, exemestane
  • inhibit aromatase, which is necessary for estrogen synthesis
  • profound estrogen deprivation in post menopausal women
28
Q

anastrozole

A
  • first line for ER pos in postmenopausal
  • early stage and advanced
  • potent and selective
  • non steroidal reversible (with letrozole)
  • exemestane is steroidal, competes with androstenedione
  • have replaced tamoxifen
29
Q

hormones for prostate cancer

A
  • androgen deprivation therapy through surgical or medical castration is useful
  • leuprolide and coserelin
  • flutamide, bicalutamide
30
Q

leuprolide, goserelin

A
  • GnRH analogs
  • bind to GnRH and inhibit FSH and LH, reduced testicular production of testosterone
  • do not inhibit adrenal androgen syn
31
Q

flutamide, bicalutamide

A
  • non-steroidal androgen receptor blockers

- compete with natural hormone testosterone for binding with AR

32
Q

hydroxyurea

A
  • inhibits ribonucleotide reductase, no deoxyribonts
  • trt of myeloproliferative neoplasms (polycythemia vera, essential thrombocytopenia
  • sickle cell
33
Q

all trans retinoic acid

A
  • APL

- differentiation of promyelocytes

34
Q

arsenic trioxide

A

-heavy metal toxin effective in relapsed APL

35
Q

thalidomide

A
  • approved for trt of multiple myeloma and MDS
  • inhibits production of IL6, which is a GF for myeloma cells
  • inhibits angiogenesis
36
Q

interferon alpha

A

-hairy cell leukemia, CML, AIDs related kaposis

37
Q

TKIs

A
  • imatinib for CML

- gefitinib/erlotinib (EGFR inhib) for non small cell lung

38
Q

monoclonal antibodies

A
  • trastuzumab for her2 +

- cetuximab (against ErbB1) for metastatic colon cancer

39
Q

multi drug resistance

A
  • resistance to multiple drugs may occur due to increased expression of cell surface glycoproteins involved in drug efflux
  • such drug transporters use ATP to drive drug molecules out of cancer cells
  • veraparnil (Ca channel antagonist) inhibits these drug transporters
40
Q

bleomycin tox

A

-pulm fibrosis

41
Q

cisplatin tox

A

-nephro, oto, peripheral neuro

42
Q

cyclophosphamide tox

A

hemorrhagic cystitis

43
Q

anthracyclines (doxorubicin)

A

-cardio

44
Q

methotrexate

A

-renal, hepato, bone marrow

45
Q

paclitaxel

A

-peripheral neuro

46
Q

vincristine

A

-neuro- peripheral

Pharmacology Unit 1 (10 decks)

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