Alkylating Agents

Front 1

In general, Alkylating agents
MOA:
uses:
S/E:

Back 1

MOA: bind to ds DNA
uses: slow growing cancer
S/E: n/v

Front 2

clue for slow growing cancer

Back 2

did not appear til >40 y/o

Front 3

How can we treat the n/v these pts will inevitibly get?

Back 3

Ondansetron

Front 4

Cyclophosphamide
MOA:
uses:
S/E:
reverse:

Back 4

MOA: require bioactivation by liver (pro-drug); covalently link DNA interstrand (x-link) at guanine N-7.

uses: Non-Hodgkins, Ovaries, Breast, Wegner's, Polyarterits Nodosa
"NOB"

tox: hemorrhagic cystitis

reverse tox with Mesna

Front 5

Nitrosoureas
examples:
MOA:
uses:
S/E:

Back 5

examples: -mustines, streptozocin
MOA: require bioactivation by liver (pro-drug); alkylate DNA; crosses
BBB

uses: brain tumors (esp. glioblastoma multiforme), Hodgkins

tox: neurotox

Front 6

Cisplatin, Carboplatic
MOA:
uses:
S/E:

Back 6

MOA: cross-link DNA
uses: bladder, ovary, lung, testicles
"BOLT"
tox: nephrotox, ototox

Front 7

Busulfan
MOA:
uses:
S/E:

Back 7

MOA: alkylates DNA
uses: CML, transplant of hemopoetic cells
S/E: pulmonary fibrosis, hyperpigmentation

Front 8

Adriamycin/ Doxorubacin/ Daunorubacin
MOA:
uses:
S/E:

Back 8

MOA: generate free rads and squeeze into (intercalte in) DNA; create breaks in DNA strand to dec replication
uses: Myeloma, Hodgkins, Sarcoma, Solid tumors
"My heart so sick"
tox: cardiotoxic (dilated cardiomyopathy), alopecia

Front 9

Dactinomycin/ Actinomycin D
MOA:
uses:
tox:

Back 9

MOA: intercalates in DNA
uses: Ewings, Wilm's, Rhabdomyosarcoma
tox: BM suppression

Front 10

Bleomycin
MOA:
uses:
tox

Back 10

MOA: generate free rads and squeeze into (intercalte in) DNA; create breaks in DNA strand to dec replication
uses: Hodgkins, Testicular
Tox: Pulm fibrosis, skin changes, minimal BM suppression

Front 11

Alkylating agents that cause
1) pulm fibrosis
2) skin changes (i.e. darker)

Back 11

bleomycin, busulphan

Front 12

Alkylating agents that cause
cardiomyopathy

Back 12

1) adriamycin (Doxyrubacin/ Donarubacin)
2) Transtuzimab

Front 13

Alkylating agents that cause
damage to renal PCT

Back 13

Cisplatin

Front 14

Alkylating agents that cause
hemorrhagic cystitis

Back 14

cyclophosphamide, isophosphomide

Front 15

Alkylating agents that block ETC
(antimitochondria)

Back 15

Antimycin

Front 16

Alkylating agent used for Multiple Myeloma

Back 16

Melphalan

Front 17

Alkylating agents used for Hodgkins
2 treatment regimens

Back 17

1st line:Mechlorethamine, Procarbazine, Dacarbazine,
other: Vinblastine, Vincristine, Adriamycin, Transtuzamab, Bleomycin, Prednisone

regimen: Mustine, Oncovin (vincristine), Procarbazine, Prednisone
"MOPP"

regimen: Adriamycin, Bleomycin, Vinblastin, Decarbazine
"ABVD"

Front 18

MC used alkylating agent

Back 18

Chlorambucil

Front 19

Toxicity of chlorambucil

Back 19

Neuro (seizures, tremors, hallucinations, confusion)

Front 20

Rescue for
1) adriamycin
2) cyclophosphomide
3) cisplatin

Back 20

1) Desroxzasane
2) mesna
3) amifastine

Front 21

Hydroxyurea
MOA:
uses:
S/E:

Back 21

MOA: S phase; inh ribonucleotide reductase (thus dec DNA synth)

uses: Sickle cell (inc HbF),
melanoma, CML

S/E: BM suppression, GI upset

Front 22

Etoposide (VP-16)
MOA:
uses:
S/E:

Back 22

MOA: late S phase, early G2 phase; inh topoisomerase II; inc DNA degredation
uses: small cell CA of lung, prostate, testicular
S/E: allopecia

Front 23

Raloxifene, Tamoxifene
MOA: (in general)
3 sites cells with estrogen rec;
at which sites is it agonist, partial agonist, antagonist

uses:
S/E:

Back 23

MOA: binds estrogen receptors found in breast, bone, uterus

agonist:
-Ralox & Tamox: bone
antagonist:
-Ralox & Tamox: breast
-Ralox- endometrium
partial agonist:
-Tamox- endometrium

uses: breast cancer, prevent osteoporosis

S/E: hot flashes, Tamox may increase risk of endometrial cancer.

Front 24

Transtuzumab
MOA:
uses:
tox:

Back 24

MOA: monoclonal Ab against HER-2 (erb-2); kills cancer via Ab dependent cytotoxicity (type 2 HPY)

uses: METASTATIC breast cancer,
Myeloma, Hodgkins, Sarcoma, Solid tumors
"my heart so sick"

Tox: cardiomyopathy

Front 25

Vincristine/Vinblastine
MOA:
uses:
tox:

Back 25

MOA: M phase; block formation (polymerization) of microtubules
uses: ChorioCA, Hodgkins, Wilm's tumor
"CHW"
tox:
-Vincristine: neurotoxic, paralytic ileus
-Vinblastin: *BLASTS BM

Front 26

Imatinib (Gleevac)
MOA:
uses:
tox:

Back 26

MOA: inh corrupt tyrosine kinase activity of bcr-abl
uses: CML, GI stroma tumors
tox: fluid retention

Front 27

Paclitaxel, -taxol
MOA:
uses:
tox:

Back 27

MOA: M phase; hyperstabilize microtubles that have already been formed (polymerized); ANAphase cannot occur.
uses: ovarian, breast
tox: BM supp, hypersensitivity

Front 28

Prednisone:
MOA:
uses:
tox:

Back 28

MOA: triggers apoptosis (anti-neoplastic); also in phospholipase A breakdown (immunosupprent)

uses:
1) anti-neoplastic quality used in CLL, Hodgkins (not treated by 6MP)
2) immunosupp quality used in autoimmune dz's

tox:
1) high cortisol/stress effects:
Cushing's-like symps, immunosuppress, acne, PUD, hyperglycemia, demargination (inc WBC), K low (has aldosterone effects)
HTN= "PICK'D HAG"
2) other: cataracts, osteoporosis, psychosis= "COP"

"COP PICK'D HAG"

Front 29

L-asparaginase
MOA:
S/E:

Back 29

MOA: knocks out asparigine (takes cells source of nutrition away, to try to kill them)
S/E: ***anaphylaxis

Front 30

Which drug treats CLL?

Back 30

Prednisone

Front 31

Which two drugs are pro-drugs (need activation by liver?

Back 31

1) cyclophosphamide needs oxidation by CYP450 to be activated
2) nitrosureas (mustines) "must" be activated by ?????

Front 32

Which drugs treat CML?

Back 32

Busulfan
Hydroxyurea
Imatinib

Front 33

Which drugs are S phase specific?

Back 33

Antimetabolites (esp 5FU and 6MP)

Front 34

Which drugs are G2 phase specific?

Back 34

Etoposide (late S, early G2)
Bleomycin
Vincristin
Vinblastin

Front 35

Which drugs are M phase specific?

Back 35

Paclitaxel

Front 36

Which drugs treat NonHodgkins?

Back 36

Cytarabine (antimetabolite)
Cyclophosphomide (alkylating agent)

Front 37

Which drugs treat Choriocarcinoma?

Back 37

Vincristin/Vinblastin (alkylating agents)
Methotrexate (antimetabolite)

Front 38

1st and 2nd sign of doxyrubicin assoc cardiomyopathy

Back 38

1st: swelling of sarco retic
2nd: loss of cardiomyocytes ("myofibrillar dropout")

Front 39

Dexrazoxane
MOA:
uses:

Back 39

MOA: Fe-chelating agent; decreases formation of oxygen free rads
uses: antidote for doxorubicin

Front 40

Aromatase inh
ex:
MOA:
uses:

Back 40

ex: anastrozole, letrozole, exmestane
MOA: inh the synthesis of Estrogen from from androgens
uses:
*** equivalent or SUPERIOR to Tamoxifen in treatment of breast cancer