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Exam 1
Lecture 8- antitopsoimerases
38
Archaeology
5th Grade
01/27/2014

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Term
topoisomerases are?
they are in what organisms? -2
Definition
nucelar enzymes
prokaryotes, eukaryotes
Term
what is the action of topoisomerases?
Definition
catalyze intervoncersion of DNA/ nick closing enzyme
Term
topoisomerases are requireed for cell viability (neg DNA superhelix?)**
Definition
Term
Type 1 topoisomerases MOA-
Definition
nicks a strnad of DNA, then prevent rotation -> passes other strnad through and cuts the end
Term
the end result of type 1 topoisomerases-
Definition
1 less neg supercoil on the DNA
Term
topoisomerases solve what problems?
by untangling _ for replication and seperating_
Definition
topological
positive supercoils; catananes
Term
topoisomerases nicks DNA but then reseals it; is essential for replicaiton (sepearting strnads and replicaiton!**** look at slide 6
Definition
Term
Ttopoisomerases 1 break _ chains
what does 2 do?
Definition
1
breaks both DNA chains
Term
Topo 1 and topt2 similar func is?
topo 2 has what other one?
Definition
removes psotive supercoils during trnascription
-seperates chromosomes in mitosis
Term
without anti-neoplastic agent the Topo has equilibrium btwn what two things?
which the antineoplastic agents whihc one has more?
Definition
cleavage
religation
cleavage
Term
ask someone about slide 9 before test
Definition
Term
MOA of antitopoisomerases agents0
Definition
cause accumulation of DNA cleavages-> apoptpsis
Term
what are the Top II inhibitors-2
Definition
etoposide
teniposide
(epidophyllotxins)
Term
*podophyllintox bidns with tublulin, etoposide does not alter microtubules
Definition
Term
epidophyllotxins (etoposide and teniposide) are CCS or CCNS
Definition
CCS
Term
what cycel phase doe epipodophyllotxins wrok-2
Definition
M
G2
Term
where do epidophyllotxins stop cell replicaiton at?
Definition
pre-mitotic
Term
etoposide used for-3
Definition
lung, testicular, lymphomas
Term
tenopside is used in
Definition
pedatric leukemia
Term
which is elminated slower, etoposide or tenoposide?
which has higher hypersens and why?
Definition
teniposide (also mroe potent)
teniposide, bc of castor oil formulation
Term
ADes of tenoposide and etoposide-2
Definition
nuetropenia, meylosuppresion
Term
admin of etoposide nad teniposide are for how mnay days?
Definition
1-5 days
Term
what drugs do you need ot reduce dose for low Cr cl?-2
Definition
tenoposide
etoposide
Term
TOPO 1 inhibitors-3
Definition
camptothecin
irinotecan
topotecan
Term
are the thecins CCS or CCNS
Definition
CCNS
Term
the thecins are water soluble/insoluble and admin by_
Definition
water soluble
IV
Term
irinothecan was approved for what cancer-2
Definition
5-FU refracotry colorecal
also pedatric tumors
Term
topothecan was approved for-
Definition
ovarian cancer (2nd line)
Term
the thecans are metab thru?
Definition
hydrolysis
Term
half life longer for topthecan or inriothecan
Definition
irinotecan
Term
ADes of topotecan-3
Definition
meylosupp, neutropenia, N/D
Term
for Cr Cl of 40-60, topotecan dose reduced to-
Definition
0.75 mg/m^2
Term
if pt had neutropenia > 3 d, dose of topotecan reduce to-
Definition
0.25 mg/m^2
Term
whcih thecan is a prodrug and needs to be metaboliccly activated to 7-ehtyl, hydroxycamptotjeic (SN-38)?
Definition
irinotecan
Term
*irinotecan pts can have dirrhea within hrs of infusion
Definition
Term
consider _ when irinotecan pt has cholinergic symtpoms with their diarrhea?
Definition
atropine
Term
ADEs of irinotecan-3
Definition
myelosuppre
n/v
mucositis
Term
to controll delayed onset odiarreha with inriotecan, cang ive oral dose of _ q 2 hr in day and q4h at night
Definition
loperamide
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