ANTINEOPLASTIC AGENT Flashcards
(85 cards)
1
Q
ADR: Alopecia
A
Doxorubicin, Carboplatin
2
Q
ADR: Neutrotoxic can go to BBB
A
Nitrosurea: Carmustine & Lomustine
3
Q
ADR: H/A and Peripheral neuropathy
A
Vinka alkaloids: vincristine & vinblastine
4
Q
ADR: Change in visual quality / corneal opacity
A
Tamoxifen
5
Q
ADR: Epistaxis (nosebleed)
A
Plicamycin
6
Q
ADR: Cardiotoxicity/ Bone marrow depression
A
Doxorubicin, Daunorubicin
7
Q
ADR: Pulmonary fibrosis
A
Bleomycin, Busulfan
8
Q
ADR: Liver toxicity
A
Methotrexate
9
Q
ADR: Nephrotoxic
A
Cisplatin, Carboplatin
10
Q
ADR: Myelosuppression
A
Methotrexate, 5-Flurouracil
11
Q
ADR: Hemorrhagic Cystitis
A
Cyclophosphamide
12
Q
ADR: Muscle pain, Malaise, Fever
A
Cytarabine
13
Q
New or unusual growth of tissue or tumor
may be benign or malignant cancer
A
Neoplasms
14
Q
uncontrollable growth and spread of abnormal
A
Neoplasia
15
Q
any cancer that arises form epithelium
A
Carcinoma
16
Q
cancer of connective tissue
A
Sarcoma
17
Q
cancer of the lymph nodes
A
Lymphoma
18
Q
Any abnormal swelling in or on body part
A
Tumor
19
Q
a tumor that does not invade and destroy the tissue in which it originates or spread to the distant sites in the body
A
Benign
20
Q
a tumor that does invade and destroys the tissue in which it originates and can spread to other sites in the body via the bloodstream and lymphatic system.
A
Malignant
21
Q
The distant spread of tumor from its site origin
A
Metastasis
22
Q
aka mutation: exposure to chemicals or unusual element that cause cancer and step 1
A
Initiation
23
Q
a promotor that increases mutation of the cell, can be specific or non-specific and step 2
A
Promotion
24
Q
INc. the growth -> activate tumor cell to spread
aggressive and inc malignant
A
Progression
25
Chemicals
Excess energy or macronutrients especially unsaturated fats
virus
radiation
limited antioxidant and other nutrients
causes of cancer
26
Curative
Palliative
Adjuvant therapy
salvage chemotherapy
neoadjuvant
Goals for the cancer
27
total eradication of cancer cells
lower tumor cell burden at which level host
immunological defenses may keep the cells in control
Curative
28
Alleviation of symptoms, decrease tumor size, control growth
avoidance of life-threatening toxicity
inc. survival and improved quality of life
Palliative
29
attempt to eradicate microscopic cancer after surgery
Adjuvant therapy
30
an attempt to get a patient into remission, after previous therapies have failed
salvage chemotherapy
31
chemotherapy is given to decrease the tumor burden before definitive therapy (surgery, radiation)
neoadjuvant
32
oncologists prefer to use the term complete response or remission to indicate a patient with no evidence of disease after treatment
remission
33
chemotherapeutic agents kill a constant fraction of cells (1st order kinetics), rather than specific number of cells after each dose
Log Kill hypothesis
34
significance weight ____ that indicates positive to a tumor
1 gram
35
Antimetabolites
Bleomycin
Podophyllin Alkaloids
Plant alkaloids
Cell cycle specific agent
36
Alkylating Agents
antibiotics
cisplatin
nitrosoureas
Cell cycle non-specific agent
37
guardian of the cell
tumor suppressor
p53
38
the ability of some cells to synthesize their own growth factors
Autocrine signaling
39
the programmed cell death
apoptosis
40
INB. cell division thru alkylation of DNA
Alkylating Agents
41
Nitrogen mustard
ethyleneimines
alkyl sulfonate
nitrosoureas
triazenes
Alkylating Agents
42
Prodrugs under nitrogen mustard
mechlorethamine, cyclophosphamide
43
a too-reactive agent
a vesicant
only in IV form
intermediate product: aziridine
mechlorethamine
44
Antidote for mechlorethamine toxicity
Na thiosulfate
45
use in chronic lymphocytic leukemia
acute lymphoblastic leukemia
toxic metabolite: Acrolein
hydroxylation in the liver
cyclophosphamide
46
active part of cyclophosphamide
phospharamide mustard
47
a chemical added to cyclophosphamide
concentrates the electrophilic substance in the kidney and conjugates acrolein
MESNA (2-mercaptoethansesulfonate)
48
be taken orally
least toxic nitro mustard
it slows down the reaction in the formation of
aziridine, making oral administration possible for them
chlorambucil and melfalan
49
use in bladder cancer, ovarian cancer, breast cancer
moa: desulfuration
IM: aziridine
reactive in low ph
Thiotepa
50
use in chronic myelogenous leukemia
intermediate metabolite: 3-hydroxysulfolane
tetrahydrothiophene 1-oxide
sulfalene
Busulfan
51
____optimal for antineoplastic activity of busulfan
4-5 alkyl substituents
52
undergo spontaneous non-enzymatic degradation with formation of the 2-chloroethyl carbonium ion from diazohydroxide formed
liberates isocynate that attach carbomoyl grp to the lysine residue of protein inactive DNA
nitrosoureas
53
alkylating agent that pass thru BBB
use in brain tumor
myelosuppression is the dose-limiting effect
Nitrosurea: Carmustine & Lomustine
54
BCNU/ Bis-chloroethyl nitrosourea
Carmustine
55
CCNUU/ chloroethyl- Cyclohexyl nitrosourea
Lomustine
56
undergoes N-demethylation (liver cyp450)
forms diazomethane
can inb mao and aldehyde dehydrogenase
Dacarbazine/procarbazine
57
purine analogs
pyrimidine analogs
folic acid analogs
myelosuppression is the dose-limiting toxicity for all drugs in this class
prodrugs
target: S phase of the cell division
antimetabolite
58
mercaptopurine
thioguanine
Azathioprine
pentostatin
hypoxanthine and quanine
DNA
purine analogs
59
____convert to T-GMP (6-thioguanine mono phosphate)
_____convert T-IMP (6-thioinosine mono phosphate)
Thioguanine, mercaptopurine
60
T-GMP AND T-IMP CONVERTS INTO HGPRT BY enzyme called _____
Guanylyl kinase
61
HGPRT means
Hypoxanthine guanine phosphoribosyl transferase
62
the accumulation cases inhibition in inosinate oxygenase
HGPRT
63
used an immunosuppressive agent
and a derivative of 6 mercaptopurine
Azathioprine
64
mercaptopurine + ____will make it more toxic
Allopurinol
65
D-arabinose form D-ribose DNA polymerase inb
Vidarabine
66
addition of fluorine in D-ribose
arabirosyl- 7- fluroadenine Triphosphate
DNA polymerase inb
Fludarabine
67
chlorine incorporated in the adenine
2-chlorodeoxy adenosine triphosphate
DNA polymerase inb
Cladribine
68
Fluorouracil
Floxuridine
Cytarabine
Gemcitabine
RNA
Pyrimidine Analogs
69
1st choice for colon cancer
inb thymidtlate synthase
converted ito a fraudulent nucleotide
FDUMP
IM: 5-fluorodeoxyuridine monophosphate
5-fluorouridine triphosphate
5-Fluorouracil
70
FDUMP means
Fluorodeoxyuridine monophosphate
71
Prodrugs of 5-Fu
to reduce the catabolic inactivation of 5-FU by DPD
inb DPD
capecitabine, tegafur
72
DPD means
Dihydropyrimidine dehydrogenase
73
discovered in Europe 1960 approved by FDA june 1969
Cytosine arabinoside
1 beta-arabinofuranosylcytosine
rapid conversion into cytosine arabinoside triphosphate, which damage DNA when cell cycle holds in "S-phase"
Cytarabine
74
Cytarabine +____+____= use to treat acute nonlymphocytic leukemia
daunorubicin, thioguanine
75
replaces cytidine, during DNA replication
1st line for small lung cancer (iV)
Fluorination sugar moiety
Gemcitabine
76
Moa: blocks DNA synthesis through inb enzyme dihydrofolate reductase
pseudo irreversibile (highgher ph)
folate acid inb kills cells in the s-phase
Methotrexate
77
___is given to prevent toxicity in cells. Given 6-24 hours after treatment w/ MTX
Leucovorin
78
Daunorubicin
Doxorubicin
Dactinomycin
Idarubicin
valrubicin
bleomycin
mitomycin
Plicamycin
Streptozocin
Cytotoxic Antibiotic
79
disrupt DNA function and cell division
streptomyces
MOA: intercalation
inb topoisomerase
alkylation
strand breakage
Cytotoxic Antibiotic
80
isolated streptomyces verticillius
naturally occurring as Cu-chelates
intercalates between G-C base pairs
ROS formation from bleo-iron complex
Bleomycin
81
isolated streptomyces parvulus
inb topisomerase II
g-c base pairs
G1 and S phase
3-phenoxazone, 9-dicarboxylic acid
dactionomycin
82
a toxic anthracycline
planar oxidized anthracene nucleus fused to a cyclohexane ring that is subsequently connected to an amino sugar
doxorubicin, daunorubicin
83
a derivative of daunorubicin that is less toxic
4-demetoxy analog
idarubicin
84
an epimer derivative of doxorubicin
epirubicin
85
isolated in streptomyces peucetius
it intercalates into DNA and decreased synthesis of both DNA & RNA
Anthracycline
