Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

GI part 2 > Chemotherapy Pharm > Flashcards

Chemotherapy Pharm Flashcards

1
Q 
class 1 agents
class 2 agents
class 3 agents
A

• Class 1: all cells killed
; ex: nonspecific alkylating agents, nitrogen mustard

• Class 2: cell cycle specific; plateaus
ex: vinblastine, methotrexate

•	Class 3 agents: non-cycle specific but slower rate of kill than class 1; 
example: daunorubicin
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

survival curves are ____

what does that mean?

A

logarithmic

-a given dose kills a constant fraction of cells

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

MDR

A

multidrug resistance

over production of glycoproteins that pump drugs out of cells

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

nitrogen mustards def and mechanism (4 are?)

A

Mech: DNA is alkylated –> causes misreading and strand breaks

MICC - melphalan, ifosfamide, chlorambucil, cyclophasphamide

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

melphalan and chlorambucil

A

nitrogen mustards; phenylalanine derivatives

orally; 1.5-2 hr half life

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

clyclophosphamide

A

nitrogen mustard –>activated to aldophosphamide by hepatic cyt p450 –> hydrolized to active phosphoramide mustard in target cells

-inactivated by aldehyde dehydrogenase 

reduced hepatotoxicity BUT -->
o	Toxicities (different than the others) – immunosuppression, pulmonary fibrosis, cystitis, water retention, alopecia, carcinogenesis
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

ifosfamide

A

Cyclophosphamide derivative for testicular cancer

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

2 chloroethyl nitrosureas

A

carmustine

lomustine

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

nitrosureas

A

carmustine and lomustine
Mech: Alkylation, DNA crosslinking, and carbamoylation of proteins
o lipid soluble –> disappear rapidly from plasma into lipids/CNS = long half-life

toxicities: delayed/severe hematopoietic depression;

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

which nitrosurea can be implantable wafer for treatment of malignant glioma.

A

carmustine

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

cisplatin

A

platinum coordinate; only the cis-dichloro form is active. Used for testicular/ovarian cancer, and head/neck cancers.
• Mechanism: alkylation by dissociation of Cl- ions leaving a + charged complex –> crosslinks are formed.

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

3 platinum coordination complex drugs

A

cisplatin
oxaliplatin
carboplatin

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

which form of cisplatin is active?

inactive?

A

cis-dichloro is active

plasma bound drug is inactive

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

oxaliplatin

A

cisplatin analogue used to treat colorectal cancer.

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

toxicity of platinum coordinator complexes

A

myelosuppression, nephrotoxicity, ototoxicity; nephrotoxicity can be attenuated by administration of the free radical scavenger amifostine.

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

carboplatin

A

platinum coordinator complex with less renal toxicity; dose is limited by leukopenia and thrombocytopenia

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

procarbazine

A 
nonspecific alkylator (DNA, RNA, protein)
•	treat Hodgkin's lymphoma.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

classes of alkylating agents

A

nitrosureas
platinum coordinators
nitrogen mustards
procarbazine

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

vinca alkaloids

A

Vincristine and vinblastine

potent plant-derived antitumor agents
• Mechanism: INHIBITS microtubule formation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

vincristine - class? toxicity?

A

vinca alkaloid

neurotoxicity and stimulates ADH release

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

vinblastine - class? toxicity?

A

vinca alkaloid

myelosuppression and mucositis

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

2 taxanes?

A

paclitaxel and docetaxel

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

paclitaxel

A

taxane from yew tree Taxus; inhibits microtubule reorganization

24
Q

which taxane is natural? which is semisynthetic?

A

docetaxel is semisynthetic

paclitaxel is natural

25
Q

ixabepilone

A

binds directly to β-tubulin and, in contrast to the vinca alkaloids, promotes polymerization/stabilizes microtubules, arresting cells in G2/M.
o Used for treatment of taxane- and anthracycline-resistant breast cancer.

26
Q

2 Epipodophylotoxins

A

Etoposide and teniposide

27
Q

etoposide and teniposide

A

from mandrake plant podophyllotoxin
• Uses: Hodgkin’s lymphoma, diffuse histiocytic lymphoma and lung small cell carcinoma
• Mechanism: Inhibit topoisomerase II 

• Toxicities: leukopenia, thrombocytopenia

28
Q

2 derivatives from the plant alkaloid camptothecin

their mechanism?

A

irinotecan and topotecan

inhibit topoisomerase 1

29
Q

irinotecan

A

derivative of plant alkaloid camptothecin
inhibits topoisomerase 1
treatment of metastatic colorectal cancer.

30
Q

topotecan

A

derivative of the plant alkaloid camptothecin
inhibits topoisomerase 1
Effective for treatment of ovarian and small cell lung carcinoma.

31
Q

2 anthracyclines

A

Daunorubicin and doxorubicin

32
Q

Daunorubicin and doxorubicin

A

anthracyclines

o Free radical and strand breaks formation
o Inhibition of DNA topoisomerase II

• CARDIOTOXICITY

33
Q

dexrazoxane

A

a protectant, iron chelator that inhibits free radical formation
can reduce cardiac damage from anthracyclines

34
Q

what drug do you pair with anthracyclines (daunorubicin and doxorubicin) to prevent ROS and reduce cardiac damage?

A

dexrazoxane

35
Q

bleomycin

A

antibiotic
• causes depurination and depyrimidation–> strand breaks
• NOT a substrate for MDR
• Toxicity: sub-acute or chronic pneumonitis, lesions of the skin

36
Q

what is NOT a substrate for MDR?

A

bleomycin

37
Q

an anti-metabolite?

its antidote if there is toxicity?

A

methotrexate

leucovorin

38
Q

methotrexate

A
  • folic acid analogue; inhibits dihydrofolate reductase

39
Q

folic acid analogue that is a competitive inhibitor of the enzyme dihydrofolate reductase?

A

methotrexate

40
Q

leucovorin

A

treats MTX toxicity

by supplying reduced folate to cells

41
Q

pyrimidine analogues

A

analogues of uridine or cytidine –> synthesis of defective DNA and chain termination

5GACC –> 5 fluorouracil, gemcitabine, azacitidine, capecitabine, cytosine arabinoside

42
Q

5GACC

A

the pyrimidine analogues –> synthesis of defective DNA and chain termination
5 fluorouracil, gemcitabine, azacitidine, capecitabine, cytosine arabinoside

43
Q

capecitabine

A

a 5-FU prodrug whose final step of activation is catalyzed by thymidine phosphorylase; used in metastatic breast and colon cancer.

44
Q

azacitidine

A

pyrimidine analogue

o Used to treat myelodysplastic syndrome.

45
Q

purine analogues

A

6 mercaptopurine and 6 thioguanine
converted by HPRT

S phase of cell cycle is most sensitive

46
Q

asparaginase

A

catalyzes conversion of asparagine to aspartate –> inhibition of protein synthesis.
o Toxicities: Reduction in concentration of secreted proteins (clotting factors, insulin, albumin, etc.), hypersensitivity reactions, hepatotoxicity.

47
Q

kinase inhibitors

A 
GIVES
gefitinib
imatinib mesylate
vemurafenib
erlotinib
sorafenib
48
Q

Imatinib mesylate

A

treats CML

—blocks the ATP-binding site of the c-abl tyrosine kinase

49
Q

vorinostat

A

• Histone deacetylase inhibitor; Used to treat cutaneous T cell lymphoma

50
Q

all trans retinoic acid

A

(vitamin A) - First line therapy for promyelocytic leukemia

51
Q

cetuximab

A

directed against EGF receptor

52
Q

trastuzumab

A

cell-mediated cytotoxicity;

 .


53
Q

bevacizumab

A

• Ab against VEGF; Designed to inhibit angiogenesis;

o risk of thromboembolic events;

54
Q

rituximab

A

anti-CD20 monoclonal antibody

o Toxicity: can result in HBV reactivation.

55
Q

ipilimumab?
gemtuzumab ozogamicin?
pembrolizumab?

A

TARGETs:

  • -CTLA-4 
–myeloid surface antigen CD33.
  • -PD-1 receptor (programmed cell death 1)
56
Q

intrathecal methotrexate

A

CNS prophylactic into CSF - dihydrofolate reductase inhibitor that targets CNS since chemo doesn’t cross into there but cancer can

toxicity: meningitis

GI part 2 (8 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions