Chemotherapy Flashcards

1
Q

MTX

A

S-specific
folic acid analog –> inhib DHFR
dec dTMP –> dec DNA and protein synthesis
SE: myelosuppression –> leucovorin rescue
liver macrovesicular fatty changes
mucositis
teratogenic

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2
Q

Neoplastic uses of MTX

A

leukemias
lymphomas
choriocarcinoma
sarcoma

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3
Q

Non-neoplastic uses of MTX

A
abortion
ectopic prego
RA
psoriasis
IBD
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4
Q

5-FU

A

S-specific
pyrimidine analog –> activates to 5F-dUMP –> complexes folic acid
complex inhibits thymidylate synthase (dec dTMP)
SE: myelosuppression –> not revers by leucovorin
overdose: rescue with uridine
photosensitivity

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5
Q

Uses of 5-FU

A

colone cancer
pancreatic cancer
basal cell Ca (topical)

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6
Q

Cytarabine

A
S-specific
Pyrimidine analog --> inhib DNA pol
SE: leukopenia
thrombocytopenia
megaloblastic anemia
use for leukemias and lymphomas
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7
Q

Azathioprine, 6-mercaptopurine

A

S-specific
purine analog –> activated by HGPRT –> dec de novo purine synthesis
use in preventing organ rejection
RA
SLE (azathioprine)
leukemia
IBD (6-MP)
metal by XO –> inc toxicity with allopurinol
also has bone marrow, liver, and GI toxicity

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8
Q

6-thioguanine (6-TG)

A

S-specific
purine analog –> activated by HGPRT –> dec de novo purine synthesis
use in IBD and leukemia

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9
Q

Actinomycin D

A
intercalates DNA
use in Wilms tumor
Ewing sarcoma
rhabdomyosarcoma 
(basically childhood tumors)
can cause myelosuppression
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10
Q

Doxorubicin

A

generates free radicals
intercalates DNA –> causes breaks –> dec replication
use in solid tumors, leukemias and lymphomas

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11
Q

Doxorubicin SE

A

CARDIOTOXIC –> dilated cardiomyopathy
use DEXRAZOXANE (iron chelator) to prevent myopathy
myelosuppression
alopecia

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12
Q

Bleomycin

A

induces free radical formation –> DNA strand breaks
use in testicular cancer and Hodgkin lymphoma
can cause PULMONARY FIBROSIS
skin changes
mucositis
MINIMAL myelosuppression

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13
Q

Cyclosphosphamide

A
alkylating agent  --> X-link DNA at guanine n-7
requires hepatic bioactivation
use in solid tumors
lymphomas
some brain cancers
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14
Q

Cyclophosphamide SE

A

myelosuppression
hemorrhagic cystitis
can be partially prevented by MENSA
same for ifosfamide

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15
Q

Ifosfamide

A
alkylating agent  --> X-link DNA at guanine n-7
requires hepatic bioactivation
use in solid tumors
lymphomas
some brain cancers
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16
Q

Nitrosoureas (-ustines) / Streptozocin

A
alkylating agent
cross-links DNA
is bioactivated and crosses the BBB
use in gliomablastoma multiforme and other brain tumors
can cause CNS toxicity
17
Q

Busulfan

A
alkylating agent 
cross-links DNA
use in CML or to ablate BM before transplant
SEVERE myelosuppression
pulmonary fibrosis
hyperpigmentation
18
Q

Vincristine

A

microtubule inhibitor
bind beta-tubulin and inhibit its polymerization
prevents spindle formation and M-phase
use in solid tumors, leukemias, and lymphomas
can cause neurotoxicity and paralytic ileus

19
Q

Vinblastine

A

microtubule inhibitor
bind beta-tubulin and inhibit its polymerization
prevents spindle formation and M-phase
use in solid tumors, leukemias, and lymphomas
causes bone marrow suppression

20
Q

Paclitaxel (taxols)

A
hyperstabilize tubules --> spindles cannot break down --> cannot progress to anaphase
use in ovarian and breast Ca
causes myelosuppression
alopecia
hypersensitivity
21
Q

Cisplatin

A

cross-links DNA
use in testicular / bladder / ovarian / lung Ca
can cause nephrotoxicity and acoustic nerve damage
prevent nephro with AMIFOSTINE (free radical scavenger)
and Cl- diuresis

22
Q

Carboplatin

A

cross-links DNA
use in testicular / bladder / ovarian / lung Ca
can cause nephrotoxicity and acoustic nerve damage
prevent nephro with AMIFOSTINE (free radical scavenger)
and Cl- diuresis

23
Q

Etoposide

A

inhib topoisomerase II –> inc DNA degradation
testicular and small cell lung cancer / leukemias / lymphomas
SE: GI irritation / myelosuppression / alopecia

24
Q

Teniposide

A

inhib topoisomerase II –> inc DNA degradation
testicular and small cell lung cancer / leukemias / lymphomas
SE: GI irritation / myelosuppression / alopecia

25
Q

Irinotecan

A

inhib tobopisomerase I –> prevents DNA unwinding and replication
used in colon cancer / ovarian cancer
can cause severe myelosuppression and diarrhea

26
Q

Topotecan

A

inhib tobopisomerase I –> prevents DNA unwinding and replication
used in small cell lung cancer / ovarian cancer
can cause severe myelosuppression and diarrhea

27
Q

Hydroxyurea

A

inhib ribonucleotide reductase –> inhib DNA synthesis
use for melanoma, CML and sickle cell (inc HbF)
SE: BM suppression and GI upset

28
Q

Prendisone / Prednisolone

A

may trigger apoptosis
use in CLL, non-Hodgkin lymphomas
also used as immunosuppressants
SE: Cushing-like Sx

29
Q

Tamoxifen

A

selective estrogen receptor modulator (SERMs)
blocks binding of estrogen to ER+ cells
use for breast cancer
SE: endometrium partial agonist –> inc risk of endometrial cancer
hot flashes

30
Q

Raloxifene

A

selective estrogen receptor modulator (SERMs)
blocks binding of estrogen to ER+ cells
use to prevent osteoporosis
not an endometrial antagonist

31
Q

Trastu(2)zumab

A

Ab against HER-2 –> tyrosine kinase receptor
use for HER-2 + breast cancer and gastric cancer
can cause CARDIOTOXICITY

32
Q

Imatinib

A

tyrosine kinase inhib of bcr-able and c-Kit
use in CML and GI stromal tumors
can cause fluid retention

33
Q

Rituximab

A
Ab against CD20 (B-cell neoplasms)
non-Hodgkin lymphoma
RA (in combo with MTX)
ITP
SE: inc risk of multifocal leukoencephalopathy
34
Q

Vemurafenib

A

small molec inhib of B-Raf kinase with the V600E mutation

use for metastatic melanoma

35
Q

Bevacizumab

A

Ab against VEGF –> inhib angiogenesis
use with colorectal and renal cell Ca
risk of hemorrhage and impaired wound healing