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Medical Pharmacology > Antineoplastic Agents > Flashcards

Antineoplastic Agents Flashcards

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USMLE® Step 1 flashcards
1
Q

Cyclophosphomide

A

alkylating agent, bischloroethylamine
directly damages DNA
prodrug of Mechloroethylamine

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2
Q

Mechlorethamine

A

alkylating agent, bischloroethylamine
directly damages DNA
Super toxic old school chemo agent

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3
Q

Nitrosoureas (Class)

A

alkylating agent
little cross-resistance w/ other chemo agents
directly damages DNA
can cross the BBB

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4
Q

Procarbazine

A

alkylating agent
prodrug
little cross-resistance
leukemogenic

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5
Q

Cisplatin

A

Platinum Coordination Complex
forms x-linked w/DNA
nephrotoxicity/acoustic nerve dysfunction

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6
Q

Methotrexate

A 
anti-tumor antimetabolite
Inhibits DNA precursor synthesis
folic acid analogue
inhibits DHFR
can be rescued w/ folinic acid
multiple resistance mechanisms
S-phase specific
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7
Q

6-Mercaptopurine

A

anti-tumor antimetabolite, purine antagonist
inhibits DNA synthesis
Converted to active form by HGPRT
downregulation of HGPRT is common resistance mechanisms
metabolized by xanthine oxidase
allopurinol inactivates xanthine oxidase, increases activity
S-phase specific

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8
Q

6-thioguanine

A

anti-tumor antimetabolite, purine antagonist
inhibits DNA synthesis
Converted to active form by HGPRT
downregulation of HGPRT is common resistance mechanisms

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9
Q

5-fluorouracil

A

antitumor antimetabolite, pyrimidine antagonist
metabolites (f-dUMP) inhibt thymidylate synthetase
F-U, F-DUMP

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10
Q

Capecitabine

A

antitumor antimetabolite, pyrimidine antagonist
oral prodrug of 5-FU
good for CC and refractory BC

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11
Q

Cytarabine

A

antitumor antimetabolite, pyrimidine antagonist
cytosine arabinoside (araC)
converted to araCMP and araCTP by deoxycytidine kinase
DCK loss tumor cell resistance

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12
Q

Daunorubicin

A

Antitumor antibiotic, anthracycline
DNA intercalation
Topo II inhibition
irreversible toxicity at high doses

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13
Q

Doxorubicin

A

Antitumor antibiotic, anthracycline
DNA intercalation
Topo II inhibition
irreversible toxicity at high doses

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14
Q

Bleomycin

A

antitumor antibiotic
DNA strand scission
active against broad spectrum
PULMONARY FIBROSIS/ANAPHYLACTIC REACTIONS

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15
Q

Vinblastine

A 
Mitotic Spindle Poison, vinca alkyloid
inhibits tubule poly
acute nausea, vomiting and DD bone marrow suppression
(blastin' bone marrow?)
super effective against lymphomas
resistance by tubulin gene mutations
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16
Q

Vincristine

A

Mitotic Spindle Poison, vinca alkyloid
inhibits tubule poly
milder side-effects than ‘blastine, significant neurotoxicity
resistance by tubulin gene mutations

17
Q

Paclitaxel

A

mitotic spindle poison, plant alkyloid
ENHANCES TUBULINE POLY, BLOCKS DISAssembly (compare w/ ‘blastine & ‘cristine)
good for the ovarian cancers

18
Q

Topotecan

A

topo inhibitor, camptothecans
binds to topo I, blocks relegation of single strand break
works during S-phase

19
Q

Irinotecan

A

topo inhibitor, camptothecans
binds to topo I, blocks relegation of single strand break
works during S-phase

20
Q

Etoposide

A

topo inhibitor
binds topo II, blocks relegation of single strand break
S-phase specific

21
Q

Tamoxifen

A

selective estrogen response modulator (SERM)
competitive inhibition of estrogen binding
partial agonist of Es Rec
efficacy varies according to tissue-specific expression of ER
low toxicity
good for breast and endomet cancer
risk of thrombosis/uterine cancer

22
Q

Raloxifen

A

selective estrogen response modulator (SERM)
competitive inhibition of estrogen binding
good for breast and endomet cancer in presence of osteoporosis
risk of thrombosis/uterine cancer?

23
Q

Letrozole

A

aromatase inhibitor
blocks androgen conversion to estrogen
good for post-menopausal women cause compensatory ovarian production of estrogen
more effective than tamoxifen
no inc. risk of thrombosis/uterine cancer

24
Q

Anastrozole

A

aromatase inhibitor
blocks androgen conversion to estrogen
good for post-menopausal women cause compensatory ovarian production of estrogen
more effective than tamoxifen
no inc. risk of thrombosis/uterine cancer

25
Q

Exemestane

A

aromatase inhibitor
blocks androgen conversion to estrogen
good for post-menopausal women cause compensatory ovarian production of estrogen
more effective than tamoxifen
no inc. risk of thrombosis/uterine cancer

26
Q

Leuprolide

A

Synthetic analogue of GnRH
pulsatile dose elevates levels of androgens
continuous high dose lowers androgen level
as effective as estrogen therapy or orchiectomy in treatment of prostate cancer

27
Q

Flutamide

A

Androgen receptor antagonist

Used in conjunction with Leuprolide to block the pulse of androgens at start of therapy

28
Q

Erlotinib

A

Small molecule inhibitor of EGFR kinase
lung cancer
head and neck cancer

29
Q

Cetuximab

A

chimeric EGFR antibody
colon cancer
head and neck cancer

30
Q

Trastuzumab

A

chimeric HER2 ab

breast cancer

31
Q

Imatinib

A

Small molecule inhibitor of BCR/Abl

approved for CML

32
Q

Brentuximab Vedotin

A

Chimeric Anti-CD30 ab conjugated to Vedotin

super toxic mit spin poison

Medical Pharmacology (26 decks)

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