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120 Cards in this Set
- Front
- Back
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antineo:
two types of agents |
synthetic
natural |
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synthetic antineo
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alkylating agents
antimetabolites |
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alkylating agents:
alkylate ---/--- bases blocks --- ---- |
purine
pyrimidine blocks dna synthesis |
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structural analogs of purine and pyridamine
or cofactors needed for dna |
antimetabolites
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antimetabolites are structural analogs of -- and --
or --- needed for dna |
purine
pyridamine cofactors |
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natural products for antineo
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plant alkaloids
antibiotics biological response modifiers immunostimulants |
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plant alkaloids inhibit --- ---- formation, or inhibit --- ----
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mitotic spindle
topoisomerase 2 |
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antibiotics bind to --- ----- base pairs, breaking --- strands
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intercalate dna
dna |
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bio reponse modifiers: --, --- , and ---- inhibitors
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antibodies
kinase growth factor |
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hormonal agents: inhibit ------ sensitive --- -----
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hormone
tumor growth |
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immunostimulants: stimulate -- ---
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immune system
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abx squeez btw two strands of ------ and inhibit
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dna
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alkylating agents
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nitrogen mustards
nitrosource platinum cooridination complexes others |
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nitrogen mustards
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mechlorethamine
cyclophosphamide ifosfamide chlorambucil melphalan |
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nitrosource
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carmusitine
lomustine streptozosine (targets pancreatic b cells) |
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platinum coordination complexes
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cisplatin
carboplatin oxaliplatin |
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other alkylating agents
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dacarbazine
procarbazine temozolomide altretamine busulfan |
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alkylating agents:
--- to rapidly diving cells |
cytotoxic
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alkylating agents:
t/f cell cycle specific |
f
not cell cycle specific: G1 and S |
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alkylating agents
---genic |
mutagenic
carcinogenic teratogenic |
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alkylating agents
has significant -- ---- |
bone marrow suppression
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alkylating agents has --- cell damage
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epithelial
oral and GI mucosa |
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alkylating agents cause ---hea and decreased ----genesis
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amenorrhea
spermatogenesis |
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alkylating agents has cns mediated -- and ---
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n/v
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alkylating agents causes secondary -----
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tumors
leukemia (usu not til later in life) |
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alkylating agents
all cause: |
pulmonary fibrosis
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alkylating agents
---suppression |
immunosuppresion
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moa of alkylating agents
form -- ion or transtion ---- |
carbonium
intermediates |
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alkylating agents
alkylate the --- atom at position 7 of |
nitrogen
guanine |
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alkylating agents
alkylate the n at positions 1 and 3 of ---- |
adenosine
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alkylating agents
alkylate 3 N of ----- and the 6 O of ----- |
cytosine
guanine |
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alkylating agents
formation of cross links w/ adjacent ---- decrease --- replication |
bases
DNA |
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alkylating agents
what increases dna strand breaks |
cross links
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alkylating agents increase --- gene activity
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p53
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alkylating agents
causes abnormal pairing of -- w/ ---- |
guanine
thymidine so leads to misreading of dna |
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alkylating agents causes de----
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purination.. .. removal from sugar backbone of dna
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alkylating agents
causes increased --- cleavage due to binding non-functional ----- decrease -- for dna synthesis |
ring
guanine purines |
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n mustard
has strong ---- actions w/ significant --- --- |
vesicant
tissue damage |
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mechlorethamine
route |
IV
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mechlorethamine
quick ---- |
activation
inactivation |
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mechlorethamine used in --- disease part of --- regimen
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hodgkin's disease
MOPP's |
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MOPP's
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mechlorethamine
oncovin prednisone procarbazine |
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s/s of mechlorethamine
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n/v
myelosuppression decreased reproductive fxs (men and women) |
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what do you tx extravasation w/ for mechlorethamine
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Na Thiosulfate
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route of cyclophosphamide
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oral
iv |
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cyclophosphamide used to treat
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breast
lung testicular ovarian sarcoma nonHodgkin's CLL lymphoma |
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se of cyclophosphamide
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n/v
alopecia cystitis pulmonary fibrosis |
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cyclophosphamide causes -----
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immunosuppression
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metabolite of cyclophosphamide, acrolein, will cause ---
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cystitis
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what will prevent cystitis
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mercaptoethane sulfonate
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which is less potent
ifosfamide or cyclophosphamide |
ifosfamide
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ifosfamide used to treat
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sarcoma
testicular ca |
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se of ifosfamide
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same as cyclophosphamide
+ neurotoxicity . .. hallucinations, confusion, depression cuz more lipid soluable |
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se of ifosfamide
> --- suppression and ---toxic than cyclophosphamide |
platelet
nephrotoxic |
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what's used w/ ifosfamide to prevent cystitis
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mercaptoethane sulfonate
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melphan used to tx
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multiple myeloma
ovarian marrow ablation in transplant |
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t/f
melphan causes hair loss |
f
no hair loss |
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toxicity of melphan
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bone marrow suppression
less n/v leukemia's (secondary) tertogenic |
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chlorambucil used to tx
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chronic lymphocytic leukemia (cll)
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route of chlorambucil
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orally
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t/f
chlorambucil cause fast suppression of bone marrow |
f
slow suppression |
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toxicity of chlorambucil
--- discomfort -- fibrosis --- ---itis ---genic --lity |
gi discomfort
pulmonary fibrosis seizures dermatitis bone marrow suppression tertogenic infertility |
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carmustine (bcnu IV), lomustine (ccnu oral), streptozocin
----- activated |
non-enzymatically
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carmustine (bcnu IV), lomustine (ccnu oral), streptozocin
--- dna and ----- proteins |
alkylate dna
carbamoylate proteins |
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t/f
carmustine (bcnu IV), lomustine (ccnu oral), streptozocin hydrophilic |
f
lipophilic |
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carmustine (bcnu IV), lomustine (ccnu oral), streptozocin
used for |
brain tumors
melamona nonHodgkin's lymphoma |
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se of carmustine (bcnu IV), lomustine (ccnu oral), streptozocin
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n/v
increased myelosuppression fibrosis renal toxicity secondary leukemia |
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carmustine (bcnu IV), lomustine (ccnu oral), streptozocin
causes -- toxicity |
renal
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dacarbazine (dtic IV)/procarbazine (matulane oral)
activation by ------ to ---- |
p-450
diazomethane |
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dacarbazine (dtic iv)/procarbazine (matuline oral )
diazomethane is a --- agent procarbazine has several metabolites including including ---- and ---- |
cytotoxic
H2O2 formaldehyde |
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dacarbazine (dtic iv)/procarbazine (matuline oral ) txs
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hodgkin's disease
malignant melanoma |
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dacarbazine (dtic iv)/procarbazine (matuline oral )
part of what regimen |
dacarbazine (dtic iv) . . . ABVD
procarbazine (matuline oral ) . . . MOPP |
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dacarbazine (dtic iv)/procarbazine (matuline oral )
toxicity severe -- and ----- --- suppression --cia --- --- syndrome |
severe n/v
myelosuppressio alopecia flu-like syndrome |
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dacarbazine (dtic iv)/procarbazine (matuline oral )
toxicity -- depression -- and -- toxicity --genic --- suppresant --ity |
cns depression
renal and hepatotoxicity leukogenic immunosuppression infertility |
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toxicity by darcabazine
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severe n/v
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toxicity by procarbazine
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cns depression
immunosuppressant leukogenic |
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toxicity by both dacarbazine (dtic iv)/procarbazine (matuline oral )
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myelosuppresion
alopecia |
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doc for malignant gliomas together w/ radiation
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temozolomide
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temozolomide mechanism similar to -----
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darcarbazine
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temozolomide
prodrug |
MTIC
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temozolomide
similar toxicity to |
dacarbazine
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atretamine route
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oral
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temozolomide route
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oral
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atretamine activated to ----
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alkylating agent
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t/f
atretamine 1st line for ovarian ca |
f
second line |
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atretamine
causes ----suppression |
myelosuppression
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atretamine
causes --toxicity |
neurotoxicity
ataxia, depressio, confusion, hallucinations |
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thiotepa converted to ---
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tepa
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thiotepa --- to dna
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cross links
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thiotepa has multiple ----- many of which are ---
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metabolites
active |
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tthiotepa used to tx
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bladder
breast hodgkin's ablation of bone marrow before transplant |
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toxicity of thiotepa
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alopecia
hematological immunological coma seizures |
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busulfan route
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oral
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busulfan
alkyl sulfonate acts like -- |
mustard
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busulfan
causes acute --- |
myelosuppression
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busulfan
used to tx |
chronic myelogenous leukemia (CML)
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busulfan used w/ ---- to ablate marrow before transplant
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cyclophosphamide
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busulfan se
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d/mild n/v
sizures myelosuppression secondary malignancies infertility teratogenic |
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busulfan
what can be fatal |
bisulfan lung. . . pulmonary fibrosis
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cisplatin route
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IV
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cisplatin --- activated
doesn't formally --- ---- dna |
water
formally alkylate |
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cisplatin will cross link ---- on guanine or ------ w/in same strand
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nitrogen
adenine |
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cisplatin
treats |
bladder
cervical ovarian testicular melanoma non-small cell lung tumor |
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cisplatin reacts w/ -- groups
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sulfhydral group
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cisplatin
--- some tumors to ----- |
sensitizes
radiation makes more effective to radiation. . . so less radiation needed. ..less damage to norm cells |
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toxcity of cisplatin
severe --- ----- ---toxicity ---toxicity mild ----- |
n/v
nephrotoxicity . . . limiting ototoxicity mild myelosuppression |
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what's used to prevent nephrotoxicity in cisplatin
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hydrate pt. . . 1-2 L of saline
amifostine thiophosphate renal protective agent |
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what will limit toxicity of cisplatin
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sulfhydryl rescue - a thiosulfate to limit toxicity
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carboplatin used to tx
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ovarian
non-small and small cell lung ca bone marrow ablation |
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carboplatin route
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IV
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carboplatin requires -----
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activation
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which is slower, less reacitve than cisplatin
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carboplatin
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toxicity of carboplatin
moderate --- --- dose limiting ------ ---genic |
moderate n/v
dose limiting myelosuppression (more than cisplatin) teratogenic |
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t/f
carboplatin can damage hearing |
t
not as much as cisplatin |
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oxaliplatin used to tx
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gi
colorectal ovarian head and neck ca testicular breast pancreatic |
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oxaliplatin ---- neuropathy
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peripheral
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toxicity
mild --- ------ --- suppression --- suppression --- shock ------- rxns --edema |
mild n/v
myelosuppression hematological suppression anaphylactic shock hypersensitivity rxn angioedema |
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development of resistance:
decrease ability to --- --- decreased activation and conversion of ----- |
enter cells
prodrug |
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development of resistance
increased intracellular --- to bind --- agent increased --- --- mechanism |
glutathione
alkylating DNA repair |
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when does resistance develop rapidly
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when used alone
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