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FPP > Anti-neoplastic Drugs > Flashcards

Anti-neoplastic Drugs Flashcards

1
Q

cell cycle non-specific drugs

A

nonspecific cytotoxicity; kill cells in any stage of cell cycle even G0; kill normal and neoplastic cells equally. e.g alkylating agents

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2
Q

cell cycle specific phase specific drugs

A

most active at specific phase of cell cycle; some selectivity of action (more cytotxic for neoplastic cells than normal cells); given by continuous infusion or frequent small doses

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3
Q

G1 phase specific agents

A

prednisone

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4
Q

S phase specific agents

A

cytarabine, fluorouracil, methotrexate, mercaptopurine, hydroxyurea

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5
Q

G2 phase specific agents

A

bleomycin, etoposide, paclitaxel

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6
Q

M phase specific agents

A

vinblastine, vincristine

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7
Q

Cell cycle specific, phase non-specific

A

prefer killing proliferating neoplastic cells but in any phase; given in large doses to spare normal cells in G0; drawback = solid tumors often have lots of cells in G0

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8
Q

examples of Cell cycle specific, phase non-specific

A

cyclophosphamide, cisplatin, doxorubicin

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9
Q

alkylating agents

A

introduce alkyl groups into DNA, RNA and/or proteins; causes DNA crosslinks and strand breaks. cell cycle nonspecific. SE: hematopoiesis suppression, damage to intestinal mucosa, N/V, alopecia

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10
Q

classes of alkylating agents

A

nitrogen mustards (mechlorethamine, cyclophosphamide), nitrosoureas (carmustine),

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11
Q

mechlorethamine

A

nitrogen mustard. alkylating agent, produces DNA crosslinks. used for hodgkin’s and non-hodgkin’s lymphoma

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12
Q

cyclophosphamide

A

oral or parenteral, cycle-specific phase-nonspecific. activation by liver P450 to phosphoramide mustard–> toxic side product acrolein (Mesna!), broad spectrum of activity. SE: sterile hemorrhagic cystitis

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13
Q

carmustine

A

IV. highly lipophilic = good for brain tumors

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14
Q

Antimetabolites

A

analogs of compounds required for intermediary metabolism, many are phase-specific (often S), best with rapid cell proliferation

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15
Q

methotrexate

A

folate analog. binds DHFR prevents THF formation. in high doses follow with Leucovorin rescue. binds to serum albumin (CI w drugs that will displace it from albumin). SE: bone marrow suppression, renal tubular necrosis. TX: ALL, choriocarcinoma

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16
Q

pyrimidine analogs

A

fluorouracil, cytarabine

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17
Q

fluorouracil

A

activated in cells to FUTP (inhibits RNA synth), FdUMP (interferes w thymidylate synthetase & DNA synth). S-phase specific. TX: IV for GI cancers, topical for basal cell carcinomas. SE: N, anorexia, diarrhea, delayed myelosuppression

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18
Q

cytarabine

A

cytidine analog, competes for phosphorylation to dCTP, competes with dCTP for incorporation –> chain termination. s-phase specific. SE: myelosuppression & neurotoxicity. Tx: acute leukemias

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19
Q

mercaptopurine

A

purine analog, converted to ribonucleotide, inhibits RNA and DNA synthesis. S phase specific. Tx: acute leukemia. SE: bone marrow depression, N/V, anorexia, jaundice

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20
Q

hydroxyurea

A

miscellaneous antimetabolie, inhibits ribonucleotide reductase to block DNA synth. arrests cells at G1/S interface. tx: granuclocytic leukemia, head & neck cancer. SE: hematopoietic depression, GI disturbances

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21
Q

vinca alkaloids

A

bind to tubulin, inhibit proper formation of microtubules and mitotic spindle, arrests cells in metaphase. M phase specific. ex: vinblastine, vincristine

22
Q

vinblastine

A

tx: hodgkin’s and non-hodgkin’s lymphoma, breast cancer. SE: strongly myelosuppressive, epithelial ulcerations

23
Q

vincristine

A

tx: ALL, hodgkin’s and non-hodgkin’s, Wilm’s, neuroblastoma, rhabdomyosarcoma. SE: alopecia, neuromuscular abnormalities (peripheral neuropathy), less BM suppression

24
Q

taxanes

A

block late in G2 phase (G2/M interface). enhance assembly and stability of microtubules by binding to tubulin’s beta-subunit.

25
Q

paclitaxel

A

tx: refractory ovarian cancer, breast. SE: dose-limiting leukopenia, peripheral neuropathy, myalgia/arthralgia. SE: dose-limiting leukopenia, peripheral neuropathy, myalgia/arthralgia

26
Q

antitumor antibiotics

A

doxorubicin, bleomycin

27
Q

doxorubicin

A

intercalates btwn DNA base paird, distorts DNA helix. causes lipid peroxidation and free radical damage. binds to DNA and topoisomerase II. cycle-specific, phase non-specific. SE: CARDIOMYOPATHY, BM depression, alopecia, GI probs.

28
Q

bleomycin

A

glycopeptide mixtures bind to DNA, cause oxidative-like damage to DNA, DNA strand breaks. phase specific for G2 (and M). SE: dose-related pulmonary toxicity, vesiculation of skin/skin hyperpigmentation, minimal myelosuppression and immunosuppression

29
Q

epipodophyllotoxins

A

etoposide

30
Q

etoposide

A

stabilizes DNA topo II causing dsDNA breaks. late G2 (also late S). SE: leukopenia, N/V, diarrhea, alopecia

31
Q

biological response modifiers (BRM)

A

agents that affect patient’s biological response to neoplasm beneficially. includes agents that act indirectly to mediate antitumor effects or that act directly on tumor cells

32
Q

filgrastim

A

G-CSF, stimulates granulocyte (PMN) production by marrow. given after myelosuppressive agents. SE: bone pain

33
Q

trastuzumab

A

MAB that binds to HER2 receptor, used in cancers that overexpress HER2. SE: cardiomyopathy, hypersensitivity, infusion reactions

34
Q

cisplatin

A

platinum coordination complex, activated species causes DNA crosslinks. promotes apoptosis. cycle-specific phase-nonspecific (sometimes S phase specific). wide antitumor spectrum. SE: nephrotoxicity, ototoxic, peripheral neuropathy, electrolyte disturbances, N/V

35
Q

procarbazine

A

activated in vivo to methylating agent that causes chromosomal damage. G1 & S phase. TX: Hodgkin’s. SE: myelosuppression, N/V

36
Q

hormones and antagonists

A

some tumors are steroid hormone-dependent. can do steroid hormone receptor assay to ID patients for endocrine therapy

37
Q

prednisone

A

adrenocorticosteroid. binds to steroid receptors, depress RNA synth of growth-related genes, induces nucleases that modulate cell lysis. arrests cells at G1. anti-emetic, palliative therapy. limited myelosuppression but long term use bad. ALL, CLL, hodgkin’s & non-hodgkin’s

38
Q

tamoxifen

A

estrogen receptor antagonist. antiestrogen, blocks ER alpha, activated by CYP2D6. TX: breast cancer, prophylaxis if high risk. SE: hot flashes, fatigue, N/V, bone/musculoskeletal pain

39
Q

letrozole

A

aromatase inhibitor. inhibits androgen to estrogen conversion in all tissues. 1st line for breast cancer in post-menopausal women. SE: bone pain, musculoskeletal pain, fatigue

40
Q

leuprolide

A

synthetic peptide analog of GnRH. initial testosterone surge followed by desensitized GnRH signaling, inhibition of LH/FSH secretion and drop in testosterone synth to castration level. Tx: prostate. SE: hot flash, impotence

41
Q

flutamide

A

antiandrogen, blocks androgen receptors. tx: metastatic prostate cancer. SE: gynecomastia, diarrhea, hepatotoxicity.

42
Q

reasons for resistance

A

resting cells. toxicity limits dose. spontaneous mutations. clinical resistance. selection & overgrowth (small fraction of cells in tumor resist & keep growing). MDR (drug efflux pumps)

43
Q

strategies to circumvent resistance

A

increase dose. multi-drug regimens. co-administer agents that defeat resistance. give drugs with different metabolism/mech/both. recruit cells out of resting phase.

44
Q

advantages to combo therapy

A

maximal cell kill within range of tolerable toxicity. broader range of coverage for de novo resistance. prevent or slow new resistance development.

45
Q

principles of combination chemotherapy

A

use multiple agents likely to be effective vs various cell types. include drugs active as single agents. use agents w non-overlapping toxicities. use each drug at its optimal dose and schedule. give combos at consistent intervals. use drugs with different mechanisms of action.

46
Q

sequential blockade

A

simultaneous action of two inhibitors acting on different enzymes of a linear metabolic pathway. ex: hydroxyurea + cytarabine; methotrexate + fluorouracil

47
Q

concurrent inhibition

A

inhibitors block two separate paths leading to same end product

48
Q

complementary inhibition

A

one inhibitor affects function of end product, other affects synthesis of that end product. ex: cytarabine + doxorubicin

49
Q

rescue

A

rescue patient’s normal cells from the treatment. ex: leucovorin after MTX; autologous BM transplant

50
Q

synchronization

A

tumor cells are synchronized to one phase for max effect from agent specific for that phase

51
Q

recruitment

A

mobilize slowly- or non-proliferating cells into more rapid proliferation. initiate therapy w cell cycle-nonspecific drugs to reduce tumor bulk and recruit non-dividing cells into active DNA synthesis, follow w cycle-specific agents

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