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Exam 1
Lecture 3-Alkylating agents
71
Anatomy
6th Grade
01/26/2014

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Term
Cisplatin toxicites-2
Definition
renal
neurologic
Term
methotrexate toxicitie-2
Definition
renal, immunosuppressive
Term
busulfan toxicities-2
Definition
hepatic, pulmonary
Term
CYCLOPHOSAMIDE tox-3
Definition
heaptic, immunosuppresive, hemmorrhagic cystits)
Term
bleomycin tox
Definition
pulmonary
Term
procarbazine tox-2
Definition
pulmonary, leukemia
Term
what drugs have cardiac tox-2
Definition
doxorubicin, daunorubicin
Term
tox of vincristine
Definition
neurologic
Term
immunsuppresive tox of drugs-2
Definition
cytrabine, dactinomycin
Term
tox of asparginase
Definition
pancreatitis
Term
whcih drugs have the elast bone marrow suppression-4
Definition
cisplatin, bleomycin, vincristine, asparaginase
Term
alkylating agents were devloped to use as?
Definition
mustard gas
Term
alkylating agents react with electron rich/poor atoms and form _ bonds
Definition
rich; covalent
Term
alkylating groups are electrophillic/phobic?
so they interact with _ gorups. ex-2?
Definition
phillic (electron poor)
neucelophillic (e- rich)
N2, O2
Term
alkylating moeities are-
Definition
highly reactive, pos. charged alkyl intermediates
Term
what are targets for alkylation?-4
Definition
amino, phosphate, sulfahydryl (SH), hydroxyl (OH) -(on DNa, prooteins, etc)
Term
alkylating are monofuncuitonal or bufunctional?
Definition
either
Term
what are the main targets for alkylation?
what does this also msotly accoutn for? why?
Definition
DNA bases (moslty purines like guanine)
cytotoxicity; proteins and small molecules alkylating aren't harmful
Term
monofunctional alkyl agents react with _ DNA whcih invovles-2
Definition
1 strand
strnad breaking, mutagenic alkylations
Term
bifunctional aklyl agents react wiht _; produces-
Definition
atom on each DNA strnad
cross link covalently links the strnads of the double helix
Term
alkylating agents bind directly/indirectly to DNA?
therefor they are what category of anticancer med?
Definition
directly
non cell cycle specific
Term
slide 9 has chemisty of the alky;lators:
1)acitvaiton
2) nucelophillic attack on azidrine ring by E-donor
Definition
Term
outcomes of alkylating rxn-4
Definition
template misread/mispaired
cross linking prevents strand unwinding
single strnad breaks-> inhibit DNA/RNA protein synth
double strnad breaks- considereed mutagenic
Term
look at slide 12 right before test, has the alkylating groups and medds in each*
Definition
Term
what are the preffered sites for DNA alkylation-4
Definition
N7 guanine
N2 guanine
O6 guanine
04 thymine
Term
what are the monofunctional agents-4
(these induce methylation, strnad breaks, mutations)
Definition
dacarbazine, procarbazine, temozoloamide
Term
what are the bifucntional agents-4
(these have alkylation, cross links, strnad breaks, mutations
Definition
N2 mustards, cyclophosphamides, nitrosureas, melphalan
Term
Mustargen
Definition
mechlorethamine HCL
Term
indicaitons for mustargen-2
Definition
Hodgkin's, lymphosarcoma
Term
whais the probelm with mustargen
Definition
extravasation ( use thiosulfate and ice packs)
Term
which mustard gas is injeciton only?
which is the most reactive
Definition
mustargen
mustargen
Term
Alkeran
Definition
melphalan
Term
indications for melphalan-1
Definition
pallatative of multiple myeloma
Term
problem with alkeran
Definition
causes chrom abnormalites
Term
counseling for alkeran-2
Definition
oral/IV; reduce dose with low BUN
Term
what is teh most widely used alkylating agent
Definition
cyclophosmaide
Term
indications for cyclophosphamide-4
Definition
lymphomas, solid tumor: breast, ovarian, lung
Term
which drug cna be used to prevent trnasplantation rejection
Definition
cyclophosphamide
Term
clyclophosphamide can be used for non maliganant immune disease such as- and also to break _ of cancer antigens
Definition
RA
immunsuppressive actions
Term
cyclophosphamide counseling-2
Definition
oral/injection
safe with bad renal fnct
Term
what are the prodrugs metab in the liver-2
Definition
cyclophosphamide
ifophosamide
(phosphamide mystards)
Term
ask someone if needd to know enzymes for slide 18
Definition
Term
what is the toxic metab for clyclophosphamide?
what is its side effect
acrolein cna metab into-
this causes-2
Definition
acrolein
hemorrhagic cystitis
mercaptethansulfonate
suprpubic pain, heamturia
Term
clyclophosphamide-> _
Definition
aldophosphamide
Term
Leukeran
Definition
chlorambucil
(has azidirne species)
Term
indicaitons for Leukeran-2
Definition
leukemias (DOC, CLL) and lymphomas
Term
what is the least toxic nutrogen mustard compound?
so how often are blood counts?
Definition
Leukaran
weekly
Term
Leukeran is admin-
Definition
orally
Term
the counseling point with Leukeran-2
Definition
use contraception (terotegni)
major bone suppression
Term
Thoiplex
Definition
thiotepa
Term
indicaitons for thiotepa
Definition
urinary bladder papillary carcinoma
Term
admin for thiotepa
Definition
IV only
Term
MOA of thiotepa
Definition
ethylenemine radical disruptin DNA-> chain scission
Term
monitoring for thiotepa
Definition
blood counts 3 wks post cessation. high tox bone suppression
Term
nitrosureas has delayed/fast hematopoeitc tox? when is the nadir?
why?
Definition
delayed
5-6 wks post admin
damage early hematopetic precursor
Term
what drugs are a good choice for brain tumors?
why?
Definition
nitrosureas
highly lipophillic to cross BBB
Term
what are the nitrosureas-4
Definition
Nimustine, semustine, Lomustine, carmustine
Term
Myleran/Busulfux
Definition
Busulfan
Term
indicaitons for busulfan
Definition
DOC pallitative chronic myelogenous leukemia (CML)
Term
Busulfan counseling
Definition
severe mylosupression
use w/ allopurinol since can cause hyperuricemia
Term
which med is used for bone marrow ablation prior to trnasplant?
Definition
busulfan
Term
which drug has a remission rate of 90% after 1 dose
Definition
busulfan
Term
mitomycin forms-
Definition
DNA cross links
Term
mitomycin contains these groups that have cytotxicity-
Definition
quinone (free radical rxn)
aziridine (alkylator)
Term
ADEs of mitomycin-3
Definition
myelosuppr, stomatitis, N/V/D
Term
mitomycin forms _ radicals, has _ cross links, and is a _
Definition
oxygen free radical, G-G, vesicant
Term
which drug classes decompase spontaneously like nitrosureas/ produce carbonium ion-2
ex-
Definition
hydrazine
triazine
procarbazine
temozaline (oral methylating for brain tumros)
Term
def of vesicant
Definition
causes blisters/extravasation
Term
major ADEs of alkylating agents shown on slide 27
Definition
Term
whcih molecule produced in tumors inactivates alkylating agents?
Definition
glutathione (GSH) (gluathion trnasferases GSTs) are overexpressed in cancers and so make more GSH
Term
two modes of resistance to alkylating agents
Definition
GSH
enhanced DNA repair
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