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walters drugs Flashcards

1
Q

alkylating agents MAO

A

alkylate DNA and proteins

form highly reactive intermediates

cell cycle nonspecific

1) ring opening
2) depurinization
3) miscoding: GC substitutes for AT
4) crosslinking interrupts DNA replication

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2
Q

Mechlorethamine

A

1st gen nitrogen mustard

unstable, spontaneously cyclizes on injection

part of MOPP

powerful vesicant - avoid extravasation (risk tissue necrosis)

1) side chain cyclizes
2) form ethyleniminium ion
3) form carbonium ion
4) reactive species reacts w/DNA
5) transfer alkyl group
6) form covalent bond

SE: nausea, vomiting, phlebitis, alopecia, myelosuppression

teratogen
carcinogen

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3
Q

cyclophosphamide

A

wide spectrum nitrogen mustard

not a vesicant

activated by liver

1) creates 4OH-cyclophosphamide
2) creates aldophosphamide
3) liver makes carboxyphosphamide, blood makes phosphoramide mustard and acrolein
4) phosphoramide becomes normitrogen mustard, acrolein is responsible for hemorrhagic cystitis

SE: leukopenia - tx w/Filgrastim (recombinant G-CSF) or sargramostim (GM-CSF), hemorrhagic cystitis - tx w/Mesna (nucleophilic thiol), SIADH, nasuea, vomiting, alopecia, amenorrhea, apsermia, pulmonary toxicity, cardiotoxicity, carcinogenic, mutagenic, teratogenic

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4
Q

Melphan

A

nitrogen mustard

erratic oral absorption

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5
Q

Chlorambucil

A

nitrogen mustard

myelosuppresive activity

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6
Q

Bendamustine

A

nitrogen mustard

repairable crosslinks

no cross-resistance w/other alkylating agents

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7
Q

Nitrosureas MOS

A

alkylate DNA and carbamoylate proteins

attacks #6 O of G

not phase specific

lipophilic - crosses blood-brain barrier

not a vesicant

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8
Q

Carmustine

A

1st gen nitrosureas

SE: nasuea, vomiting, meylosuppression, PULMONARY FIBROSIS, nephrotoxicity, hepatotoxicity

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9
Q

Lomustine

A

nitrosureas

no pulmonary fibrosis

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10
Q

Busulfan

A

bifunctional alkyl sulfonate alkylating agent

myelosuppresion

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11
Q

Methotrexate

A

folic acid analog

inhibits DHFR, can’t synthesize DNA

SE: neurotoxicity w/motor deficits

Leucovorin rescue - rescue healthy cells that uptake folate

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12
Q

Pralatrexate

A

folic acid analog

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13
Q

Cytarabine

A

pyrimidine analog

incorporates into DNA, improper stacking of bp, fragmentation of double helix

give w/Danorubicine

SE: myelosuppression

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14
Q

6-mercaptopurine

A

purine analog

suppress BM

analog of hypoxanthine

1) substrate for HGPRT
2) becomes 6-T-IMP
3) incorporate into DNA
4) inhibit txn/tln

give w/allopurinol inhibit metabolism to uric acid

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15
Q

6-thiogruanine

A

purine analog

suppress BM

analog of G

1) activated by HGPR
2) incorporates into DNA
3) strand breaks

allopurinol has no effect

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16
Q

fludarabine

A

purine analog

resists deamination by guanase

inhibits DNA polymerase

SE: peripheral neuropathy

**fatal pulmonary toxicity if given w/pentostatin

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17
Q

pentostatin

A

purine analog

1) inhibits ADA
2) block DNA synthesis

**fatal if given w/fludarabine

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18
Q

cladribine

A

purine analog

1) incorporates into DNA
2) strand breaks
3) deplete NAD and ATP
4) disrupts cell metabolism

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19
Q

clofarabine

A

purine analog

cladribine for children

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20
Q

vinka alkaloids MOA + resistance

A

from periwinkle plant

M phase metaplase

1) bind tubulin
2) dissolve MTs
3) metaphase arrest
4) neurotoxicity

resistance: P-glycoprotein (efflux)

excreted in bile

**intrathecal administration is deadly

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21
Q

vinchristine

A

vinca alkaloid

part of MOPP

SE: neurotoxicity, loss Achilles tendon reflex

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22
Q

vinblastine

A

vinca alkaloid

SE: leukopenia (tx w/Filgrastim), phlebitis

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23
Q

topoisomerase II inhibitors MOA

A

from mandrake plant

1) bind tubulin w/o interfering with MT structure/function
2) forms tenary complex w/DNA
3) prevents reannealing
4) ds breaks

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24
Q

Etoposide

A

topoisomerase II inhibitor

SE: leukopenia, thrombocytopenia

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25
Q

Teniposide

A

topoisomerase II inhibitor

retained longer in cells

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26
Q

anthracyclines MOA

A

1) intercalates between 2 bps on opposite DNA strands

2) local uncoiling of double helix

27
Q

Doxorubicin

A

anthracycline

from streptomyces fungus

avoid extravasation! - local vesican action (Adriamycin flare)

SE: turns urine red, leukopenia - tx w/Filgrastim, cardiotoxicity - quinones chelate Fe and form ROS (tx w/Dexrazoxane - iron chelator)

28
Q

Danorubicin

A

anthracycline

from streptomyces fungus

SE: cardiotoxic

29
Q

Idarubicin

A

anthracycline

SE: cardiotoxic

30
Q

Epirubicine

A

anthracycline

31
Q

Mitoxantrone

A

anthracenedione derived from anthracyclines

32
Q

Bleomycin

A

from streptomyces verticillus

1) chelates copper and iron
2) create O2 radicales
3) DNA scission

SE: pulmonary toxicity&raquo_space; pulmonary fibrosis, cutaneous toxicity

no significant myelosuppression

33
Q

L-asparaginase

A

derived from E coli

1) hydrolyzes asparagine
2) deprives cells of asparagine

SE: hypersensitivity, hyperglycemia, bleeding

34
Q

Pegasparaginase

A

conjugated to PEG

35
Q

Azacitidine

A

1) incorporates into DNA
2) demethylation
3) apoptosis

SE: nausea, vomiting, myelosuppresion, GI symptoms

36
Q

Decitabine

A

induces ds breaks

37
Q

Nelarabine

A

incorporates into DNA, inhibits synthesis

38
Q

Alemtuzumab

A

monoclonal antibody

targets CD52

lysis of leukemic cells (Ab-C’ toxicity)

39
Q

90Y-ibritumomab tiuxetan

A

monoclonal antibody

binds CD20 Ag

generates free radicals
destroys from inside

40
Q

ofatumumab

A

monoclonal antibody (IgG analog)

targets CD20 Ag

Ag-C’ toxicity and apoptosis

41
Q

rituximab

A

monoclonal antibody

targets epitope on CD20
Ag-C’ toxicity and apoptosis

42
Q

tositumomab

A

monoclonal antibody

ionizing radiation (beta particles) destroy cells from inside

43
Q

interferon MOA

A

bind specific cell-surface receptors

enzyme induction
inhibition of proliferation
enhanced immune activities

BBW: neurpsychiatric, autoimmune, ischemic, infectious disorders

44
Q

interferon alpha 2a

A

interferon

antiviral w/antineoplastic activity

inhibits synthesis of ornithin decarboxylase

45
Q

peginterferon alpha 2a

A

interferon

attached to PEG to extend t1/2

46
Q

interferon alpha 2b

A

interferon

47
Q

Aldesleukin

A

recombinant interleukin2

produce LAK cells from T blasts

SE: capillary leak syndrome (tx w/leukapheresis)

48
Q

Denileukin Deftitox

A

immunotoxin

recombinant IL2 w/diptheria toxin fragment A

SE: hypersensitivity, vascular leak syndrome

49
Q

tyrosine kinase inhibitors SE

A

nausea, vomiting, diarrhea, headache, muscle cramps, joint/muscle pain, rash, edema, pulmonary fibrosis, thrombocytopenia, neutropenia

50
Q

imatinib

A

Tyr kinase inhibitor

binds closed conformation of enzyme

51
Q

nilotinib

A

Tyr kinase inhibitor

binds closed conformation of enzyme

52
Q

dasatinib

A

Tyr kinase inhibitor

binds open and closed states

53
Q

Ponatinib

A

Tyr kinase inhibitor

BBW: arterial thrombosis, hepatotoxicity

SE: hypertension, abdominal pain, fever, constipation

54
Q

Ibrutinib

A

Tyr kinase inhibitor

prevents activation of B cell pathways
inhibits proliferation/migration

55
Q

Hydroxyurea

A

analog of urea

inhibits ribonucleotide disphosphate reductase

S phase specific

56
Q

Tretinoin

A

1st gen retinoid

1) binds retinoic acid receptor
2) forms heterodime RAR-RXR
3) induce differentiation of APL cells

pregnancy category X

57
Q

bexarotene

A

retinoid

targets RXR receptor, forms heterodimers

58
Q

Arsenic Trioxide

A

DNA fragmentation and apoptosis

59
Q

Bortezomib

A

binds proteosomes

60
Q

Vorinoistate

A

1) inhibits HDACs
2) accumulation of acetylated histone
3) induces cell cycle arrest

61
Q

Thalidomide

A

inhibits angiogenesis
anti-inflammatory
decrease TNFa synthesis
inhibit leukocyte migration

pregnancy category X

62
Q

Lenalidomide

A

less teratogenic thalidomide

63
Q

pomalidomide

A

thalidomide derivative

pregnancy category X

BL (2 decks)

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