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135 Cards in this Set
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antimitotic drug
|
vinblastine
vincristine vinorelbine paclitaxol docetaxel topetecam irinotecan etoposide teniposide |
|
inhibitors of growth factors
|
imatinab
gefitinib erlotinib bortezomib |
|
antibodies to tumor cells antigens
|
rituximab
alementuzumab tratuzumab cetuximab bevacizumab gemtuzumab ozagamicin |
|
antimitotic drugs:
interfere w/ --- process by altering --- formation or ---- --- phase specific |
mitotic
spindle degradation m-phase |
|
antimitotic:
inhibition of the -------- enzyme. topoisomerase 1 breaks and reseals ----- stranded dna topoisomerase 2 does the same on --- stranded dna -- phase specific |
topoisomerase 1 or 2
single double |
|
vinblastine alkaloid from vinca rosea --- plant
|
periwinkle
|
|
vincrisitne structural analog of ---
|
vinblastine
|
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paclitaxel --- form bark of western yew tree
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alkaloid
|
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docetaxel --- from needles of european yew tree
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alkaloid
|
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etoposide semisynthetic ------ derived from mayapple or mandrake plant
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podophyllotoxins
|
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teniposide structural analog of ---
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etoposide
|
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topotecan synthetic --- from camptotheca acuminata
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camptothecin
|
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mitotic agent interfere w/ ----
prevent --- of dna strands in cell arrest --- ---- |
microtubules
separation cell division |
|
mitotic agent
stopping cell division leads to -- --- |
cell death
|
|
vinca alkaloid route
|
iv
|
|
t/f
vinca alkaloid enters cns |
f
does not |
|
vinca alkaloid goes thru extensive ----
|
metabolism
|
|
vinca alkaloid
--- excretion |
biliary
|
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ex of vinca alkaloid
|
vincristine
vinblastine |
|
vincristine tx:
|
lymphomas
acute lympocytic leukemia hodgkin's some solid tumors |
|
vincristine part of the --- tx
|
MOPP
vincristine = oncovine |
|
vinblastine used to tx
|
hodgkin's
bladder breast ovarian testicular |
|
vinblastine part of the --- tx
|
ABVD
vinblastine = velbane |
|
which is used more for solid tumors:
vincristine or vinblastine |
vinblastine
|
|
tox of vinca alkaloids
rapid --- effects and cell ---- leads to hyper------ due to oxidation of the purine to --- acid use: |
cytotoxic
cell destruction hyperuricemia uric acid use allopurinol to prevent buildup |
|
vinca alkaloids:
strong ------ |
vesicants
|
|
tx of vesicant action of vinca alkaloids
|
heat
hyaluronidase (to disperse drug) |
|
vincristine tox
dose limiting --- toxicity peripheral ----- of hands and feet may affect both --- and ---- nerves |
neurotoxicity
periphral neuropahty sensory and motor nerves might be affected |
|
vincristine tox
suppresion of --- ----- -- nerve damage may cause -- pain face ----- |
suppresion of deep tendon reflexes
cranial nerve damage jaw pain face palsies |
|
vincristine tox
--- neuropathies |
autonomic
|
|
vincristine tox
may cause --- suppression |
myelosuppression
|
|
main vincristine tox
|
hand and glove
|
|
vinblastine tox
dose limiting ------ less --- toxic -- --- --- |
mylesuppression
neurotoxic n/v/d |
|
vinorelbine --------- ---- ca
|
non small cell lung ca
|
|
vinorelbine is a semisynthetic analog of ---
|
vinblastine
|
|
vinorelbine tox
---suppression -- --- -- -- tox |
myelosuppresion
n/v/d neurotoxicity |
|
paclitaxel/docetaxel
1971: spindle poison increasae tubulin ------ decrease ------ |
polymerization
disassembly |
|
paclitaxel/docetaxel
cell division stopped in ---- |
m phase
|
|
paclitaxel/docetaxel txs
|
metastatic ovarian breast, lung, esophageal, head/neck tumors
|
|
paclitaxel tox
-- suppresion ---- rxns -- ---- sensory neuropathy ---gia |
myelosuppresion
hypersensitivity rxn stocking-glove sensory neuropathy myalgia |
|
docetaxol tox
---penia less sever -- pathy less -- rxn ---- |
neutropenia
less severe neuropathy less hypersensitivity rxns edema |
|
etoposide/teniposide
cell cycle spicific for: |
S-G2
|
|
etoposide/teniposide
------ breaks and reseals dna breaks during uncoiling |
topoisomerase 2
|
|
etoposide/teniposide
agenst blocks enzymes leading to --- ---- |
strand breaks
|
|
route of etoposide
|
oral
IV |
|
etoposide 40% excreted unchanged via
|
urine
|
|
tenipside is extensively ---
|
metabolized
|
|
etoposide txs
|
testicular
lung nonhodgkin's lymphoma |
|
etoposide:
often given in combo w/ |
cisplatin
|
|
teniposide route
|
IV
|
|
tenoposide txs
|
acute lymphocytic leukemia
neuoblastoma |
|
teniposide:
check --- fx |
liver
|
|
etoposide/teniposide tox
---cia ----/---- dose limiting ------ |
alopecia
n/v dose limiting myelosuppression |
|
etoposide leads to unusual -- ---- -- due to alteration in chromosome ----
|
nonlymphocytic leukemia
chromosome 11 usu 1-3 yrs after tx after childhood acute lymphoblasitic leukemia |
|
chormosome 11: ---- ---- leukemia gene
|
MLL: mixed lineage leukemia gene
|
|
unusual nonlymphocytic leukemia occurs after what disease
|
acute lymphoblastic leukemia
|
|
irinotecan/topotecan
synthetic ---- |
camptothecins
|
|
irinotecan/topotecan
greater activity than --- --- |
natural alkaloid
|
|
irinotecan/topotecan
inhibits ----- causing -- strand breaks in dna |
topoisomerase 1
single |
|
irinotecan
metabolized and excreted in --- |
bile
|
|
topotecan
-- excretion |
renal
|
|
irinotecan used to tx
|
colorectal
breast cervical gastric lung |
|
topotecan used to tx
|
lung
ovarian cml |
|
irinotecan/topotecan tox
dose-limiting ------ |
myelosuppression
|
|
which causes more diarrhea
irinotecan or topotecan |
irinotecan>>>topotecan
|
|
irinotecan/topotecan tox
--- ---- --- cia |
n/v
alopecia |
|
irinotecan
has decreases --- activity |
cholinesterase
so increased ACTH acitvity increased muscarinic type effects |
|
biological response modifers. . .protein kinases:
genomoe codes for ----- protein kinases and 130 ---- ----- |
550
protein phosphatases |
|
protein kinases:
critical part of the --- -----pathways |
signal transduction
|
|
two types of protein kinases
|
receptor tyrosine kinases (humans-90)
enzymatic tyrosine kinases (humans - 32) |
|
rtk stimulates ----
leads to proliferatin of cells |
RAS
|
|
myeloid tyrosine kinase inhibitor:
|
Imatinib
|
|
-nib
|
tyrosine inhibitor
|
|
imatinib used to tx:
|
cml
cmml |
|
imatinib decrease --- --- responsible for cell proliferation
|
myeloid TK's
|
|
se of imatinab
|
n/v
edema |
|
epidermal growth factor tyrosine kinase inhibitor:
|
gefitinib
|
|
gefitinib txs
|
nonsmall cell lung
|
|
gefitinib se
|
diarrhea
rash nausea vomiting dry skin |
|
biological response modifiers blocks recpetors so growth factors can't bind ot stimulate -- --
|
tyrosine kinase
|
|
HER1/EGFR tyrosine kinase inhbitor
|
erlotib
|
|
erlotnib used to tx
|
mestatic non small cell lung ca
pancreatic head neck |
|
se of erlotnib
|
diarrhea
rash elevated liver enzymes |
|
ErbB1, ErbB2 TK inhibtors
|
lapatinib
|
|
lapatinib route
|
oral
|
|
lapatinib approved for
|
metastatic breast ca no longer sensitive to transtuzumab
|
|
lapatinib used in combo w/
|
capecitabine
increased time for tumor growth from ~ 4.4 to 8 mo |
|
t/f
lapatinib used for both her1 and 2 |
t
|
|
t/f
lapatinib enters cns |
t
so effective for cns metastasis |
|
lapatinib tox
|
rash
nausea fatigue anorexia |
|
t/f
lapatinib allows gf to bind but not tf |
t
|
|
proteosome inhibitor
|
bortezomib
|
|
bortezomib increase -- and decrease ----- -----
|
increase IkB (inhbits NFKB. .. survival factor)
IkB prevents survival of Ca cells decrease NFkB and NFkB cell survior promoter genes |
|
bortezomib used for
|
multiple myeloma
trials in solid tumor |
|
bortezomib tox
------ ------penia ----thy ---- pain |
fatigue
thrombocytopenia neuropathy limb pain |
|
rituximab
chimeric human-murine antibody to --- antigen on -- lymphocytes |
CD20
B |
|
90% of ---- cells expressed on CD20 antigen
|
non-hodgkin's lymphoma
|
|
CD20 regulates steps in -- ---- activation
|
cell-cycle
|
|
blocking CD20:
complement mediated: |
lysis
apoptosis antibody mediated cytotoxicity |
|
rituximab given as 4 --- infusions
|
weekly
|
|
rituximab tox:
infusion related --- -- syndrome -- --- --ria --spasm mild ----- |
flu like syndrome
n/v uticaria bronchospasm mild myelosuppression |
|
alemtuzumab binds CD--- antigen on -- and --- lymphomas
|
CD52
T B |
|
alemtuzumab induces cellular ----
|
cytotoxicity
|
|
indications for alemtuzumab
|
lympomas
CLL |
|
alemtuzumab tox
-- rxn decreased --- --- infections |
infusion
decreased T cells opportunistic infections |
|
trastuzumab recombinant human --- antibody to human --- --- ---- 2
|
monoclonal
epidermal growth factor 2 (her 2/neu, erbB2) |
|
trastuzumab antibody prevents binding of --- ----
can also down regulate --- ---- ---- |
growth factor
growth facotr receptor |
|
trastuzumab used for
|
metastatic breast tumors over expressing HER2 (erbB2)oncogene
|
|
trastuzumab used w/
|
doxorubicin
taxol |
|
trastuzumab
--- overexpression in 25-30% primary -- --- |
protein
breast ca |
|
trastuzumab tox
--- --- (weekly infusion) what do u tx w/ |
fever
chills tx: apap, diphnehydamine, meperidine |
|
trastuzumab tox
----- ------ --ache ---ness --nia --- --myopathy |
n/v
ha dizziness dyspnea cough cardiomyopathy |
|
cetuximab
antibody to --- --- --- |
epidermal growth factor
|
|
cetuximab tx:
|
metastatic colorectal ca
head neck |
|
cetuximab tox
-- rxn skin rash |
infusion
skin rash |
|
bevacizumab
antibody to ----- --- growth factor |
vascular-endothelial
(VEGF) |
|
bevacizumab prevents
|
agiogeneis
block bl supply to tumor. . .slows growth |
|
bevacizumab indications:
|
metastatic colorectal
breast lung renal pancreatic |
|
bevacizumab tox:
severe ---- ---uria --- |
severe htn
proteinuria CHF |
|
gentuzumab ozogamicin antibody to --- antigen linked to ozagamicin
|
cd33
|
|
gentuzumab ozogamicin
indication |
cd33 positive acute myelogenous leukemia in first relapse
|
|
gentuzumab ozogamicin tox
--- rxn -- and -- suppression |
infusion rxn
hepatic and bone marrow suppression |
|
gentuzumab ozogamicin
is a --- drug |
combo of angibody w/ antitumor abx
target tumor them kills |
|
t/f
gentuzumab ozogamicin is 1st line |
f
|
|
D,L-Asparaginase
---- required for protein synthesis |
asparagine
|
|
D,L-Asparaginase
--- cells take up from plasma anc can synthesize |
norm
|
|
--- tumors have low levels of asparagine synthetase
so must take up ---- |
lymphoid
asparagine |
|
---- depletes asparagine for protein synthesis in ca cells
|
asparaginase
|
|
D,L-Asparaginase
used in |
childhood acute lympocytic leukemia
|
|
D,L-Asparaginase used in combo w/
|
methotrexate
doxorubicin vincristine |
|
what's given first methotrexate or D,L-Asparaginase
|
methotrexate
D,L-Asparaginase stops protein synthesis and prevents methotrexate from working |
|
D,L-Asparaginase causes
--- rxn |
allergic
|
|
D,L-Asparaginase tox
--- hemorrhage ----tis |
intracranial hemorrhage
pancreatitis |
|
D,L-Asparaginase
decrease --- factors |
clotting
|
|
D,L-Asparaginase
---- toxicity |
ammonia
|