Pharm- Antineoplastic Agents 10/25 Flashcards

1
Q

Nitrogen mustards, prototype

A

cyclophosphamide

ifosfamide

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

alkyl sulfonate, prototype

A

busulfan

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

platinum coordination complexes, prototype

A

cisplatin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

vinca alkaloids, prototype

A

vinblastine

vincristine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

taxanes, prototype

A

paclitaxel

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

epipodophyllotoxins, prototype

A

etoposide

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

antibiotics, prototype

A

bleomycin, doxorubicin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

enzymes, prototype

A

L-asparaginase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

folic acid analogs, prototype

A

methotrexate (MTX)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

pyrimidine analogs, prototype

A

fluorouracil (5-fluorouracil, 5-FU)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

purine analogs, prototype

A

mercaptopurine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

differentiating agents, prototype

A

tretinoin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

biological response modifiers, prototype

A

interferon-alfa

interleukin-2

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

immunomodulators, prototype

A

thalidomide

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

rescue agents, prototype

A

leucovorin

mesna

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

protein tyrosine kinase inhibitors, prototype

A

dasatinib
erlotinib
imatinib
lapatinib

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

proteasome inhibitor, prototype

A

bortezomib

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

monocolonal antibodies, prototype

A

bevacizumab
cetuximab
rituximab
trastuzumab

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

agents used to minimize adverse effects, prototype

A
erythropoietin 
serotonin antagonists (ondansetron)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

primary induction therapy

A

main treatment that provides the best possible outcome, also called first-line therapy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

neoadjuvant therapy

A

treatment given BEFORE primary induction therapy in order to improve outcome

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

adjuvant therapy

A

additional therapy given CONCOMITANTLY or AFTER primary induction therapy in order to reduce the probability of relapse

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

cell cycle specific agents, definition

A

cytotoxic for cells during specific phases of the cell cycle

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

cell cycle non-specific agents, definition

A

cytotoxic regardless of whether the cells are cycling or resting in G0 compartment (although cycling cells are more sensitive)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

growth fraction

A

the ratio of proliferating cells to resting cells (G0). It is a determinant of responsiveness to chemotherapy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

cells with high growth fraction

A

bone marrow
GI tract
hair follicles
sperm-forming cells

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

log cell kill hypothesis

A

a fraction (not an absolute number) of cells are killed. A three-log cell kill eliminates 99.9% of cells

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

primary resistance

A

an absence of response on the first drug exposure, thought to be d/t genomic instability

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

acquired resistance

A

develops in response to exposure to a given antineoplastic agent; often highly specific to a single drug, or class of drugs, and is usually d/t an increased expression of 1+ genes

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

Multi-drug resistance

A

P-glycoprotein: ATP-dependent efflux pump that actively pumps antineoplastic agents out of cells, confers resistance to a broad range of agents

Anthracyclines, vinca alkaloids, etoposide, paclitaxel, and dactinomycin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
31
Q

purpose of hematopoietic agents in treatment

A

for treating neutropenia
thrombocytopenia
anemia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
32
Q

purpose of administering ondansetron

A

serotonin receptor antagonists for emetogenic effects

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
33
Q

purpose of administering bisphosphonates

A

delay skeletal complications

34
Q

five major types of alkylating agents

A
  1. nitrogen mustards
  2. nitrosoureas
  3. alkyl sulfonates
  4. methylhydrazine derivatives
  5. triazines
    * * Also included are platinum compounds**
35
Q

Alkylating agents, MOA

A

form covalent linkages with DNA, both intra- and inter-strand. Prevents DNA from unwinding, therefore inhibits transcription and translation

36
Q

biotransformation of cyclophosphamide

A

forms acrolein, which causes hemorrhagic cystitis

37
Q

Mesna

A

inactivates acrolein and is used for prophylaxis of chemotherapy-induced cystitis

38
Q

busulfan toxicity

A

pulmonary fibrosis

39
Q

cisplatin toxicity

A

renal tubular damage

ototoxicity

40
Q

cyclophosphamide toxicity

A

hemorrhagic cystitis

41
Q

general toxicities of alkylating agents

A
direct vesicant (blistering) effects and tissue damage at injection site (consider oral administration)
acute toxicity: N/V w/i 30min
delayed toxicity: bone marrow depression with leukopenia, thrombocytopenia, nephrotoxicity, alopecia, mucosal ulceration, intestinal denudation
42
Q

three major types of antimetabolites

A
  1. folic acid analogs
  2. pyrimidine analogs
  3. purine analogs
43
Q

Antimetabolites, MOA

A

structural analogs to compounds necessary for cell proliferation, block or subvert pathways that are involved in (or lead to) cell replication

44
Q

Antimetabolites, cell cycle specific or non-specific?

A

Cell cycle specific (S phase)

45
Q

Alkylating agents, cell cycle specific or non-specific?

A

cell cycle non-specific

46
Q

methotrexate, MOA

A

inhibits dihydrofolate reductase (DHFR), thereby inhibiting cell proliferation

47
Q

indications for methotrexate

A

cancer
RA
psoriasis

48
Q

leucovorin

A

reduced folate can bypass DHFR
used to rescue normal cells from high-dose MTX
antidote for accidental MTX overdose

49
Q

fluorouracil, MOA

A

active compound (FdUMP): covalently binds thymidylate synthetase and blocks de novo synthesis of thymidylate. incorporated into both DNA and RNA (FdUTP into DNA, and FUTP into RNA).

50
Q

Can leucovorin rescue 5-FU?

A

no, upstream of the enzyme

51
Q

6-mercaptopurine, MOA

A

prodrug, inhibition of several enzymes of de novo purine nucleotide synthesis, incorporates into DNA and RNA

52
Q

6-MP and Allopurinol

A

6-MP normally undergoes first pass effect in the liver by xanthine oxidase.
allopurinol inhibits xanthine oxidase. administering allopurinol with oral 6-MP results in increased levels of 6-MP and increased toxicity

53
Q

anti-metabolites, cell cycle specific or non-specific?

A

cell cycle specific (S-phase)

54
Q

common toxicities of anti-metabolites

A

N/V/D, myelosuppression, immunosuppression, thrombocytopenia, leukopenia, hepatotoxicity

55
Q

vinca alkaloids, ADRs

A

alopecia
myelosuppression (vinblastine > vincristine)
vincristine exhibits neurotoxicity (numbness/tingling in extremities, loss of DTRs, motor weakness, autonomic dysfunction)

56
Q

vinca alkaloids, MOA

A

bind to beta-tubulin and inhibit microtubule assembly

57
Q

vinca alkaloids, cell cycle specific or non-specific?

A

cell cycle specific (M-phase)

58
Q

taxanes, MOA

A

bind to beta-tubuline and stabilize microtubule assembly.

59
Q

taxanes, cell cycle specific or non-specific?

A

cell cycle specific (M-phase)

60
Q

taxanes, ADRs

A

Paclitaxel: hypersensitivity reactions in hands and toes, change in taste
Docetaxel: greater cellular uptake; retained intracellularly longer than paclitaxel permitting smaller dose, which reduces AEs, hypersensitivity, neutropenia, alopecia

61
Q

topoisomerase inhibitors, cell cycle specific or non-specific?

A

cell cycle specific (primarily S phase, also G1 and G2). EXCEPTION: anthracyclines

62
Q

anthracyclines, MOA

A

inhibit topoisomerase, intercalate DNA, oxygen free-radicals bind to DNA, causing single- and double-stranded DNA breaks

63
Q

anthracyclines, cell cycle specific or non-specific?

A

cell cycle non-specific (but cycling cells are most susceptible)

64
Q

anthracyclines, ADR

A

free radicals are linked to significant cardiotoxicity

cumulative cardiac damage can lead to arrhythmias and heart failure

65
Q

bleomycin, class

A

anti-tumor antibiotic

66
Q

bleomycin, MOA

A

free radicals cause single- and double-stranded DNA breaks

67
Q

bleomycin, cell cycle specific or non-specific?

A

cell cycle specific (G2 arrest)

68
Q

bleomycin, ADR

A

pulmonary toxicity, minimal myelosuppression

69
Q

Imatinib

A

a small molecule inhibitor of ABL tyrosine kinase, can also inhibit the RTKs PDGFR and c-KIT.
BCR-ABL fusion protein results from t(9:22) translocation, found in 95% of CML patients

70
Q

erlotinib and gefitinib, MOA

A

inhibit EGFR, a receptor tyrosine kinase.

71
Q

erlotinib and gefitinib, ADR

A

dermatologic toxicities

72
Q

Target for trastuzumab and lapatinib

A

HER2/neu (breast CA)

73
Q

trastuzumab, ADR

A

cardiovascular complications (decreased LVEF, HF)

74
Q

Pegaspargase, drug class

A

Natural Product- Enzyme

75
Q

Teniposide, drug class

A

Natural Product- Epipodophyllotoxins

76
Q

Daunorubicin, drug class

A

Natural Product- Antibiotic

77
Q

Dacarbazine, drug class

A

Alkylating Agents- Triazenes

78
Q

Streptozocin, drug class

A

Alkylating Agents- Nitrosoureas

79
Q

Oxaliplatin, drug class

A

Platinum Coordination Complex

80
Q

Cytarabine (Cytosine arabinoside; Ara-C), drug class

A

Antimetabolite, Pyrimidine analogs

81
Q

Pentostatin, drug class

A

Antimetabolite, Purine analogs

82
Q

Chlorambucil, drug class

A

Alkylating Agents, nitrogen mustards