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Therapeutic Drugs > Onco > Flashcards

Onco Flashcards

1
Q

Carboplatin

A

Alkylating antineoplastic agent
Platinum derivative
Mechanism:
- bind N7 of guanine on single strand, cross links DNA
- binds NH2 or SH groups on proteins
Dosed according to pt renal fnx (AUC), doesn’t cause renal dysfnx
Toxicity:
- hematopoietic toxicity mostly, less toxic to kidney and neuro

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2
Q

Cisplatin

A

Alkylating antineoplastic agent
Platinum derivative
Mechanism:
- bind N7 of guanine on single strand, cross links DNA
- binds NH2 or SH groups on proteins
Requires hydration otherwise get renal damage
Toxicity:
- renal toxicity mostly, less neuro toxic
- ototoxicity

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3
Q

Cyclophosphamide

A

Alkylating antineoplastic agent
Mustard
Prodrug - requires hepatic activation - modify dose based on LFTs
Toxicity:
- alkylating common: myelosuppression, mucositis, alopecia, impaired wound healing, impaired growth in children, reduced resistance to infxn, nausea/vomit, sterility, TERATOGENIC, carcinogenic
- leukopenia and thrombocytopenia; recovers in about 20 days
- mucositis
- bladder toxic in high or prolonged oral dosing; give MESNA with hydration to protect bladder
- high doses - cardiotoxicity, SIADH, lung toxicity

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4
Q

Dacarbazine

A

Alkylating antineoplastic agent
Emetogenic
Toxicity:
- alkylating common: myelosuppression, mucositis, alopecia, impaired wound healing, impaired growth in children, reduced resistance to infxn, nausea/vomit, sterility, TERATOGENIC, carcinogenic

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5
Q

Melphalan

A

Alkylating antineoplastic agent
Mustard
Toxicity:
- alkylating common: myelosuppression, mucositis, alopecia, impaired wound healing, impaired growth in children, reduced resistance to infxn, nausea/vomit, sterility, TERATOGENIC, carcinogenic

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6
Q

Mechlorethamine

A

Alkylating antineoplastic agent
Nitrogen Mustard
Toxicity:
- alkylating common: myelosuppression, mucositis, alopecia, impaired wound healing, impaired growth in children, reduced resistance to infxn, nausea/vomit, sterility, TERATOGENIC, carcinogenic
- leukopenia and thrombocytopenia, recover after 20 days
- vesicant
- emetogenic

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7
Q

Oxaliplatin

A

Alkylating antineoplastic agent
Platinum derivative
Mechanism:
- bind N7 of guanine on single strand, cross links DNA
- binds NH2 or SH groups on proteins
Toxicity:
- mostly neurotoxic, little renal toxicity

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8
Q

Procarbazine

A 
Alkylating antineoplastic agent
Oral bioavailability
CNS penetration
Hodgkin's lymphoma use
use in gliomas/brain tumors
Toxicity:
- CNS toxicity: somnolence, mood swings
- alkylating common: myelosuppression, mucositis, alopecia, impaired wound healing, impaired growth in children, reduced resistance to infxn, nausea/vomit, sterility, TERATOGENIC, carcinogenic
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9
Q

Temozolomide

A

Alkylating antineoplastic agent
Alkylate O6 position of guanine - distinct repair pathway
Alkylguanine alkyl transfer - low leves are a predictive marker
Use in glioma
Toxicity
- alkylating common: myelosuppression, mucositis, alopecia, impaired wound healing, impaired growth in children, reduced resistance to infxn, nausea/vomit, sterility, TERATOGENIC, carcinogenic

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10
Q

Bleomycin

A

Antibiotic antineoplastic agent
Binds iron - produces free radicals that damage DNA
Toxicity increased by presence of O2
Renal clearance - reduce dose in renal dysfnx
Toxicity:
- pulmonary and cutaneous, especially with decreased renal fnx - increased toxicity with cumulative dose; underlying pulmonary disease and radiation make this worse
- persists in lungs fatal activation of lung toxicity during surgery with high O2
- raynaud’s phenomenon
For Hodgkins and Germ cell

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11
Q

Dactinomycin

A 
Antibiotic antineoplastic agent
Intercalate into DNA helix - inhibit RNA and protein synthesis
Use in pediatric neoplasm regimens
Toxicity:
- myelosuppression
- mucositis
- diarrhea
- nausea/vomit
- vesicant - damages skin if gets outside the vein - avoid extravasation
- radiation recall
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12
Q

Daunorubicin

A 
Topo II inhibitor antineoplastic agent
- topo II makes double strand break, drug binds and stabilizes
Anthracycline
Radiation sensitive
Elimination by liver
Toxicity:
- myelosuppression
- mucositis
- alopecia
- cardiac toxicity - due to free radical generation
- vesicant - extravasation damage
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13
Q

Doxorubicin

A 
Topo II inhibitor antineoplastic agent
- topo II makes double strand break, drug binds and stabilizes
Anthracycline
Radiation sensitive
Elimination by liver
Toxicity:
- myelosuppression
- mucositis
- alopecia
- cardiac toxicity - due to free radical generation
- vesicant - extravasation damage
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14
Q

Etoposide

A 
Topo II inhibitor antineoplastic agent
- topo II makes double strand break, drug binds and stabilizes
Reduce dose with creatinine clearance
Used in lung cancers
Toxicity:
- neutropenia, thrombocytopenia
- alopecia
- not much end organ damage
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15
Q

Mitoxantrone

A

Topo II inhibitor antineoplastic agent
- topo II makes double strand break, drug binds and stabilizes
Less cardiotoxic and less emetogenic than anthracyclines
Toxicity:
- myelosuppression, mucositis, GI

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16
Q

Idarubicin

A 
Topo II inhibitor antineoplastic agent
- topo II makes double strand break, drug binds and stabilizes
Anthracycline
Radiation sensitive
Elimination by liver
Toxicity:
- less cardio-toxic than the others on a weight basis - preferred in adults
- myelosuppression
- mucositis
- alopecia
- cardiac toxicity - due to free radical generation
- vesicant - extravasation damage
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17
Q

Bevacuzimab

A 
Antibody antineoplastic agent
Anti-VEGF
- prevents angiogenesis
Use: tumors expressing VEGF
Toxicity:
- hypertension
- clotting
- bleeding
- perforation of viscus
- CNS dysfnx
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18
Q

Cetuximab

A 
Antibody antineoplastic agent
Anti-EGFR
- blocks immune activation 
Use: colon, head and neck cancer
Toxicity
- infusion rxn - fever, chills, hypotension, bronchospasm
- cutaneous - rash
- diarrhea
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19
Q

Rituximab

A

Antibody antineoplastic agent
Anti-CD20
- blocks CD20 on B cells, inhibit lymphocyte signaling and immune activation
Use: non-Hodgkin’s lymphoma
Toxicity:
- infusion rxn - fever, chills, SOB, hypotension

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20
Q

Trastuzumab

A

Antibody antineoplastic agent
Anti-Her2/neu
- inhibits signaling and immune activation
Use: Her2 positive breast cancer
Toxicity:
- infusion rxn - fever, chills, SOB, hypotension
- cardiomyopathy - decreased EF

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21
Q

Blinatumomab

A

Antibody antineoplastic agent
Conjugated antibody
Bi-specific T cell engager for CD3 and CD19 BiTE
- bridges T cells and tumor B cells in ALL
Toxicity:
- cytokine release syndrome
- neurotoxicity

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22
Q

Ado-trastuzumab emtansine

A 
Antibody antineoplastic agent
Anti-Her2 
Toxicity:
- cytopenia
- liver damage
- heart failure
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23
Q

Ipilimumab

A 
Antibody antineoplastic agent
Anti-CTLA4
CTLA4 is a negative signal to T cell activation (like PD1)
Use: melanoma
Toxicity:
- autoimmune: gut, hepatic
- renal, thyroid
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24
Q

Brentuximab vedotin

A

Antibody antineoplastic agent
Conjugated antibody - has cytotoxic molecule attached
Anti-CD30 (on Reed Sternberg cells)
Use: Hodgkin’s lymphoma

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25
Q

Pembrolizumab

A 
Antibody antineoplastic agent
Anti-PD1 receptor
PD1 - tumor antigen that makes cancer cells invisible to immune system
Use: melanoma
Toxicity:
- auto-immune: gut, hepatic
- renal, thyroid
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26
Q

Nivolumab

A 
Antibody antineoplastic agent
Anti-PD1 receptor
PD1 - tumor antigen that makes cancer cells invisible to immune system
Use: melanoma
Toxicity:
- auto-immune: gut, hepatic
- renal, thyroid
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27
Q

Decitabine

A

Antimetabolite antineoplastic agent
DNA hypomethylating agent (methylation silences genes, increased in tumorigenesis)
Nucleoside
Mechanism:
- incorporation into DNA leads to inactivation of DNA methyl transferase - alters gene expression
Not orally bioavailable
Use: sickle cell anemia, acute myeloid leukemia, myelodysplastic syndrome
Toxicity:
- myelosuppression

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28
Q

Azacytidine

A

Antimetabolite antineoplastic agent
DNA hypomethylating agent (methylation silences genes, increased in tumorigenesis)
Nucleoside
Mechanism:
- incorporation into DNA leads to inactivation of DNA methyl transferase - alters gene expression
Not orally bioavailable
Use: sickle cell anemia, acute myeloid leukemia, myelodysplastic syndrome
Toxicity:
- myelosuppression

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29
Q

Cytarabine

A

Antimetabolite antineoplastic agent
- S phase active, get incorporated into DNA/RNA and result in cell death - inhibit normal nucleotide synthesis
Inhibits DNA synth from deoxyribonucleotides
Cytosine analog
Metabolized by cytidine deaminase - useful in hepatic and renal dysfnx
Toxicity:
- myelosuppression especially with continuous IV
- hand foot
- eye irritation
- cerebellar

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30
Q

Fluorouracil

A

Antimetabolite antineoplastic agent
- S phase active, get incorporated into DNA/RNA and result in cell death - inhibit normal nucleotide synthesis
Inhibits DNA synth from deoxyribonucleotides
Mechanism:
- inhibit thymidine synthesis, forms covalent complex with folate and thymidylate synthase
Useful in hepatic and renal impairment
Enhance activity by giving leucovorin with 5FU
Metabolized by dihydropyrimidine dehydrogenase; if DHPD deficiency, severe toxicity - rescue via uridine
Toxicity:
- myelosuppression
- GI
- cerebellar and neurocognitive at high doses
- coronary spasms - rare

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31
Q

Gemcitabine

A

Antimetabolite antineoplastic agent
- S phase active, get incorporated into DNA/RNA and result in cell death - inhibit normal nucleotide synthesis
Cytosine analog
Metabolized by cytidine deaminase - useful in hepatic and renal dysfnx
Toxicity:
- myelosuppression especially with continuous IV
- hand foot prominent
- eye irritation
- cerebellar

32
Q

Methotrexate

A

Antimetabolite antineoplastic agent
- S phase active, get incorporated into DNA/RNA and result in cell death - inhibit normal nucleotide synthesis
Inhibits ribonucleotide synthesis from purines at high doses
Inhibits DNA synth from deoxyribonucleotides at all doses
Mechanism:
- inhibits dihydrofolate reductase, blocking DNA/RNA precursor formation
Toxicity:
- myelosupprsion
- mucositis
- hepatic toxicity in chronic exposure
- pulmonary fibrosis/interstitial lung disease
If giving high dose - use leucovorin and hydration/alkalinize urine

33
Q

Paclitaxel

A 
Anti-microtubular antineoplastic agent
Microtubule polymer stabilizer
Taxane
Mechanism:
- stabilize microtubules, but they are abnormal and poorly functional
Toxicity:
- myelosuppression
- neuropathy
- fluid retention - due to vehicle
- taxane specific: fluid retention/vascular leak; hypersensitivity rxn to vehicle
34
Q

Vinblastine

A 
Anti-microtubular antineoplastic agent
Mitotic inhibitor
Vinca Alkaloid
Mechanism:
- disassemble microtubules
Toxicity:
- myelosuppression - more myelo than neuro
- neuropathy
- fluid retention - due to vehicle
35
Q

Vincristine

A 
Anti-microtubular antineoplastic agent 
Mitotic inhibitor
Vinca Alkaloid
Mechanism:
- disassemble microtubules
Toxicity:
- myelosuppression
- neuropathy - more neuro than myelo
- fluid retention - due to vehicle
36
Q

Erythropoietin

A

Growth/CS factor antineoplastic agent
Toxicity:
- clotting
- may promote tumor growth

37
Q

Sargramostim

A 
Growth/CS factor antineoplastic agent
Toxicity:
- high incidence of fever
- chills
- bone pain
- exacerbate inflammatory states
38
Q

Romidepsin

A

Histone De-Acetylase inhibitor antineoplastic agent
Mechanism:
- blocks HDAC which would normally silence transcription; downregulates genes associated with growth, upregulates genes associated with inhibition of cell proliferation, leads to differentiated fnxs
Use: Cutaneous T cell Lymphoma
Toxicity:
- cardiac
- myelosuppression

39
Q

Anastrazole (Arimidex)

A 
Hormonal oncologic antineoplastic agent
Aromatase inhibitor Type II - nonsteroidal
Mechanism:
- blocks estrogen synthesis at cyp450 aromatase
Use: 
- breast/endometrial cancer
Toxicity:
- bone loss
- fatigue
40
Q

Goserelin

A

Hormonal oncologic antineoplastic agent
LHRH analog
Mechanism:
- hypothalamic stimulator of continuous LH release therefore lose normal pulsatile release and decrease net LH release
- therefore decrease testosterone production

41
Q

Letrozole

A 
Hormonal oncologic antineoplastic agent
Aromatase inhibitor Type II - nonsteroidal
Mechanism:
- blocks estrogen synthesis at cyp450 aromatase
Use: 
- breast/endometrial cancer
Toxicity:
- bone loss
- MSK fatigue
42
Q

Prednisone

A 
Hormonal oncologic antineoplastic agent
Mechanism:
- induce apoptosis via glucocorticoid receptor action
Use:
- leukemia
Toxicity (related to glucocorticoid excess):
- hyperglycemia
- fluid retention
- gastric irritation
- Cushing's syndrome
- myopathy
- CNS changes
- increased opportunistic infxns
43
Q

Tamoxifen

A 
Hormonal oncologic antineoplastic agent
Anti-estrogen
Mechanism:
- blocks estrogen receptor, estradoil cannot bind ER
Toxicity:
- bone loss
- thrombogenic with DVT and large organ thromboses
- uterine neoplasms
44
Q

Irinotecan

A 
Topo I inhibitor antineoplastic agent
- topo I makes single strand break
Prodrug of SN38 - made in liver
Toxicity:
- diarrhea: early onset - atropine sensitive; late onset - reflects clearance of SN38
- myelosuppression
- alopecia
- nausea/vomit
- fatigue
45
Q

Erlotinib

A

Tyrosine kinase inhibitor antineoplastic agent
Target: EGF receptor
Use: non-small cell lung cancer and pancreatic
More specific binding to kinase has more specific inhibitor action
Toxicity:
- cutaneous - rash
- GI - diarrhea

46
Q

Imatinib

A

Tyrosine kinase inhibitor antineoplastic agent
Target: p210bcr-abl, kit
Use: chronic myelogenous leukemia with bcr-abl
More specific binding to kinase has more specific inhibitor action
Toxicity:
- cytopenias
- liver abnormalities
- fluid retention
- rare cardiomyopathy

47
Q

Sorafenib

A

Tyrosine kinase inhibitor antineoplastic agent
Multikinase antagonist
Targets: VEGF receptor, raf (FLT3)
Use: renal cell and hepatocellular carcinoma
More specific binding to kinase has more specific inhibitor action
Toxicity - related to vascular system:
- hypertension
- proteinuria
- perforated viscus (spontaneous)
- clotting/bleeding
- hand/foot syndrome due to extravasation
- rash
- diarrhea

48
Q

Sunitinib

A 
Tyrosine kinase inhibitor antineoplastic agent
Multikinase antagonist
Targets: VEGF receptor, PDGF, kit (FLT3)
Use: renal cell carcinoma
More specific binding to kinase has more specific inhibitor action
Toxicity - related to vascular system:
- hypertension
- proteinuria
- perforated viscus (spontaneous)
- clotting/bleeding
- hand/foot syndrome due to extravasation
- rash
- diarrhea
49
Q

Hydroxyurea

A 
Oncologic antineoplastic agent
DNA directed agent
Orally bioavailable
Mechanism:
- reversible inhibition of ribonucleotide reductase by chelation of non-heme iron at reactive center
- decreases dNTP pools, stalls replication
Toxicity:
- myelosuppression
- mucosal damage
- enhanced effect in renal failure
50
Q

Leucovorin

A

Antidote to folic acid antagonists

  • reduced folate, does not require dihydrofolate reductase for action
  • rescues normal cells, loads cancer cells with MTX
  • also used to enhance 5FU toxicity to cancer cells
51
Q

Arsenic trioxide

A 
Hematologic antineoplastic agent
Use: Acute Promyelocytic Leukemia
Mechanism:
- receives and donates electrons, generates free radicals
Toxicity:
- heavy metal toxicity
- kidney, hepatic
- cardiac conduction problems - long QT
52
Q

IL-2

A 
Hematologic antineoplastic agent
Induces T cell response - cytolytic to tumors
Use: melaoma, renal cell carcinoma
Toxicity:
- hypotension, vascular leak
- headache/fever/chills/fatigue (flu-like)
- altered mental status
- cardiopulmonary
53
Q

alpha-interferon

A 
Hematologic antineoplastic agent
Biological response modifier
Use: adjuvant for melanoma; myeloproliferative neoplasms (CML); Kaposi's sarcoma
Safe in pregnancy
Toxicity:
- fatigue, fever, chills (flu-like)
- cytopenias
- hypotension due to vascular leak
- chronic use: depression
54
Q

Tretinoin (all-trans retinoic acid)

A

Hematologic antineoplastic agent
Mechanism:
- binds retinoic acid receptor, induces differentiation of leukemic cells
Use: Acute Promyelotic Leukemia with 15;17 translocation
Toxicity:
- teratogenic
- cutaneous - dry skin, ocular keratitis
- increased intracranial pressure - headaches, papilledema
- differentiation syndrome - differentiated tumor cells release cytokines in tissues and cause organ damage

55
Q

Bortezomib

A 
Proteosome inhbitor antineoplastic agent
Mechanism:
- Block digestion of proteins targeted for degradation, prevents cytokine action that would occur through NF-kB
Use: multiple myeloma and lymphoma
Toxicity:
- neuropathy
- thrombocytopenia
- altered GI fnx
- cardio and pulmonary toxicity (prominent)
56
Q

Cis-retinoic acid (?)

A

Hematologic antineoplastic agent

57
Q

GCSF (? same as Sargramostim)

A

Growth factor antineoplastic agent

58
Q

Ondansetron (?)

A

Anti-emetic therapy

59
Q

Cirzotinib/Xalkori (?)

A

Anti-ALK

anaplastic lymphoma kinase

60
Q

Imid

A 
Thalidomide, Lenalidomide
- alter cytokine milieu
Immunomodulator
Use: multiple myeloma
Toxicity:
- thromboses
- cytopenias
61
Q

CAR-T

A

Genetically modified T cell - given new genes that allow production of a TCR that does not need MHC
- has internal region that acts as a co-stim
- grow up the T cells with IL-2 before giving back to host
Mechanism:
- allow for non-MHC recognition of tumor antigen
Toxicity:
- cytokine release syndrome

62
Q

Alkylating agents

A 
Platinum derivatives:
- Oxiplatin, Carboplatin, Cisplatin
Cyclophosphamide
Dacarbazine
Melphalan
Mechlorethamine
Procarbazine
Temozolomide
63
Q

Antibiotics

A

Bleomycin

Dactinomycin

64
Q

Topo II inhibitors

A 
Daunorubicin
Doxorubicin
Etoposide
Mitoxantrone
Idarubicin
65
Q

Antibodies

A 
Bevacuzimab
Cetuximab
Rituximab
Trastuzumab
Blinatumomab
Ado-trastuzumab emtansine
Ipilimumab
Bretuximab
Pembrolizumab
Nivolumab
66
Q

Anti-metabolites

A 
Decitabine
Azacitidine
Cytarabine
Fluorouracil
Gemciabine
Methotrexate
67
Q

Anti-microtubule

A

Paclitaxel
Vinblastine
Vincristine

68
Q

Growth/CS factors

A

Erythropoietin

Samgramostim

69
Q

HDAC inhibitor

A

Romidepsin

70
Q

Hormonal oncologics

A 
Anastrazole
Goserelin
Letrozole
Prednisone
Tamoxifen
71
Q

Topo I inhibitors

A

Irinotecan

72
Q

Tyrosine kinase inhibitors

A

Erlotinib
Imatinib
Sorafenib
Sunitinib

73
Q

Other oncologics

A

Hydroxyurea

74
Q

Antidote to folic acid antagonists

A

Leucovorin

75
Q

Additional hematologics

A

Arsenic trioxide
IL-2
IFN-a
Tretinoin - all trans retinoic acid

76
Q

Anti-emetic therapy

A

Ondansetron

Therapeutic Drugs (7 decks)

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