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P&T Block 2 > Anti-neoplastic drugs > Flashcards

Anti-neoplastic drugs Flashcards

(78 cards)

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1
Q

-abine

A

cytosine analog (antimetabolite)

S phase active

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2
Q

-nib

A

kinase inhibitor

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3
Q

-platin

A

DNA damaging heavy metal (alkylating agent) bind N7 of guanine on single strand

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4
Q

-rubicin

A

anthracyclines (topo II directed agents)

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5
Q

-tecan

A

topo I directed agents

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6
Q

Dactinomycin

A

antibiotic

intercalates into DNA helix and inhibits RNA/protein synthesis

ADR: myelosuppression, nausea, mucositis, diarrhea, vesicant, radiation recall (skin reaction)

USE: pediatric cancers

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7
Q

Ado-trastuzumab emtansine

A

Anti-Her2 antibody conjugated with cytotoxin

ADR: cytopenias, liver damage, and cardiomyopathy (decreased EF)

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8
Q

alpha-interferon

A

cytokine

ADR: fever, chills, fatigue, cytopenias

USES: melanoma, myeloproliferative neoplasms

SAFE DURING PREGNANCY

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9
Q

Anastrazole

A

hormonal oncologic–> nonsteroidal (type II) cyp450 aromatase antagonist

acts in liver to prevent downstream production of estrogen

ADR: bone loss; fatigue

USE: breast cancer

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10
Q

Anti-metabolites are all active during which phase?

A

S phase

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11
Q

Arsenic Trioxide

A

generates free radicals–> cytotoxic

ADR: prolonged QT syndrome, hepatic, renal

USES: Acute promyelocytic leukemia

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12
Q

Azacytidine

A

antimetabolite (pyrimidine analog)

S phase active

cytosine analong; incorporation results in inhihibition of synthesis

hypomethylating agent which leads to increase in transcription

–> apoptosis

ADR: myelosuppression

metabolized by enzyme in tissue so useful for patients with hepatic or renal impairment

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13
Q

Bevacuzimab

A

Anti-VEGF antibody potentiates action of chemotherapy

ADR: bleeding/clotting, HTN, seizures/altered mental status, perforated viscus

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14
Q

Bleomycin

A

Antibiotic

produces free radicals and binds Fe–> damages DNA renal clearance

ADR: lungs and skin lack enzyme that clears bleomycin from tissue–> pulm and cutaneous toxicities fatal lung toxicity with high O2 (surgery risk) Raynaud’s syndrome, hypersensitivity

Use: hodgkin’s and germ cell cancers

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15
Q

Blinatumomab

A

Bispecific T cell engaging (BiTE) antibody against CD19 (on tumor cells) and CD3 (on T cells)–> acts as a bridge

ADR: cytokine release syndrome, neurotoxicity

Use: refractory B-precursor ALL

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16
Q

Bortezomib

A

proteasome inhibitor

ADR: thrombocytopenia, neuropathy, altered GI function

USES: Multiple myeloma

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17
Q

Brentuximab vedotin

A

Anti-CD30 antibody conjugated with cytotoxin

ADR: peripheral neuropathy, cytopenias, and upper respiratory symptoms

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18
Q

Carboplatin

A

Alkylating Agent–> DNA damaging heavy metal; crosslinks DNA

dose by AUC (patient’s renal function)

ADR: heme>>>>renal/neuro

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19
Q

Cetuximab

A

Anti-EGFR antibody–> blocks signaling and activates immune system

ADR: diarrhea, rash

Uses: Colon cancer (wt for ras); squamous head and neck cancer

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20
Q

Cisplatin

A

Alkylating Agent–> DNA damaging heavy metal; crosslinks DNA

requires hydration to avoid renal toxicity

ADR: renal > neuro/oto> heme

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21
Q

Common ADR of microtubule agents

A

myelosuppression, neuropathy

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22
Q

Cyclophosphamide

A

Alkylating Agent (Mustard)

PO

Prodrug- activated in liver

ADR: metabolites are toxic to bladder (high doses given with MESNA and hydration) high doses are cardiotoxic common- myelosuppression, alopecia, sterility, mucositis, carcinogenic, pulmonary fibrosis USES: non-hodgkin’s lymphoma

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23
Q

Cytarabine (Ara-C)

A

antimetabolite (pyrimidine analog)

S phase active

cytosine analog; inhibits synthesis –> apoptosis

ADR: myelosuppression, nausea, rash, mucositis, ocular irritation, and cerebellar toxicity at high doses

metabolized by enzyme in tissue so useful for patients with hepatic or renal impairment

USES: AML remission induction

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24
Q

Dacarbazine (DTIC)

A

Alkylating Agent–> alkylates O6 of guanine ADR: vomiting common- myelosuppression, alopecia, sterility, mucositis, carcinogenic, pulmonary fibrosis

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25
Daunorubucin
Anthracycline--\> Topo II inhibitor forms complex with DNA and Topo II and prevents re-ligation resulting in breaks in DNA --\> apoptosis ADR: interaction with radiation therapy common anthracycline- myelosuppression, vesicant, mucositis, GI, dose related cardiac toxicity
26
Decitabine
anti-metabolite (pyrimidine analog) S phase active cytosine analog; incorporation inhibits synthesis hypomethylating agent resulting in increased transcription --\> apoptosis ADR: myleosuppression metabolized by enzyme in tissue, so good for patients with hepatic or renal impairment
27
Doxorubicin
Anthracycline--\> Topo II inhibitor forms complex with DNA and Topo II and prevents re-ligation resulting in breaks in DNA--\> apoptosis ADR: common anthracycline- mucositis, myelosuppression, vesicant, GI, dose related cardiac toxicity
28
Erlotinib
tyrosine kinase inhibitor EGF-R ADR: diarrhea, rash
29
E**topo**side (VP-16)
Topo II inhibitor forms complex with DNA and Topo II and prevents re-ligation resulting in further breaks in DNA--\> apoptosis ADR: myelosuppression, alopecia reduce dose in proportion to creatinine clearance
30
Fluorouracil
antimetabolite (pyrimidine analg) S phase active inhibits thymidine synthesis by forming complex with folate and thymidylate synthase ADR: myelosuppression, mucositis, CNS at high doses Increased activity with Leucovorin metabolized in tissue by DHPD, so good for patients with renal or hepatic dysfunction
31
Gemcitabine
Antimetabolite (pyrimidine analog) S phase active cytosine analog; inhibirs synthesis --\> apoptosis metabolized by enzyme in tissue, so useful for patients with hepatic and renal impairment ADR: myelosuppression, "hand foot syndrome"
32
Goserelin
hormonal ongologic--\> LHRH analog which results in disruption of normal pulsatile release and feedback mechanisms --\> downregulation of testosterone and estrogen ADR: bone pain, decreased sex drive
33
Hydroxyurea
USES: AML hyperleukocytosis ADR: myelosuppression, mucositis
34
Idarubicin
Topo II inhibitor-- anthracycline complexes with DNA and Topo II to prevent re-ligation resulting in further DNA breaks--\> apoptosis less cardiotoxic than other anthracyclines ADR: myelosuppression, vesicant, mucositis, GI
35
IL-2
cytokine--\> induces T cell response, cytolytic for tumors ADR: fever, chills, fatigue, cytopenias, infusion reactions with hypotension and vascular leak syndrome; altered mental status; cardiopulmonary USES: high dose for metastatic renal tumors and melanoma
36
Imatinib
tyrosine kinase inhibitor Bcr-abl, kit ADR: fluid retention, hepatic, myelosuppression, rare cardiomyopathy USES: CML, GIST
37
Ipilimumab
Anti-CTLA4--\> stimulates immune system ADR: infusion rxn (chills, fever, SOB, hypotension), exaggerated autoimmunity especially gut and hepatic dysfunction
38
Irinotecan (CPT 11)
Topo-I inhibitor forms complex with DNA and Topo I, preventing re-ligation; breaks in DNA--\> apoptosis Prodrug of SN38 Dose according to UGT allele status ADR: myelosuppression, nausea, diarrhea (early and late onset), fatigue, alopecia
39
Letrozole
hormonal oncologic--\> nonsteroidal (type II) cyp450 aromatase antagonist; acts in liver to prevent downstream production of estrogen ADR: bone loss; musculoskeletal fatigue USE: breast cancer
40
Leucovorin
Reduced folate potentiates activity of 5-FU rescue/protexts normal cells from methotrexate
41
Mechlorethamine
Alkylating Agent--\> nitrogen mustard parent drug of class (chemical warfare) ADR: blistering agent, vomiting common- myelosuppression, alopecia, sterility, mucositis, carcinogenic, pulmonary fibrosis
42
Melphalan
Alkylating Agent (Mustard) PO ADR: common- myelosuppression, alopecia, sterility, mucositis, carcinogenic, pulmonary fibrosis
43
Methotrexate
antimetabolite (folate antagonist) S phase active inhibits dihydrofolate reductase and thereby DNA synthesis ADR: mucositis, myelosuppression, hepatic w/ chronic exposure rescure/protect normal cell with Leucovorin Renal clearance
44
Mitoxantrone
Topo II inhibitor complexes with DNA and Topo II to prevent re-ligation resulting in further breaks in DNA--\> apoptosis less cardiotoxic than anthracycline ADR: myelosuppression, mucositis, GI
45
Nivolumab
Anti- PD1 directed antibody ADR: autoimmune like side effects including gut, hepatic, renal, thyroid
46
Ondansetron
type 3 serotonin antagonist USES: nausea associated with chemo
47
Oxaliplatin
Alkylating Agent--\> DNA damaging heavy metals; crosslinks DNA ADR: neuro\>\>heme\>\>\>\>\>renal
48
Paclitaxel
anti-microtubular agent stabilizes tubules and prevents breakdown --\> no progression to M phase ADR: myelosuppression, neuropathy, vascular leak (=fluid retention), hypersentiviity to vehicle
49
Pembrolizumab
Anti-PD1 directed antibody ADR: autoimmune like side effects including gut, hepatic, renal, thyroid
50
Prednisone
glucocorticoid receptor antagonist ADR: glucocorticoid excess- hyperglycemia, fluid retention, gastric irritation, cushing's syndrome, increased opportunitistic infections, myopathy, CNS changes
51
Procarbazine
Alkylating Agent PO crosses BBB ADR: mood swings, somnolence common- myelosuppression, alopecia, sterility, mucositis, carcinogenic, pulmonary fibrosis
52
Rituximab
Anti-CD20 antibody--\> inhibits lymphocyte signaling and activates immune response ADR: infusion reaction (chills, fever, shortness of breath, hypotension) Uses: B cell lymphomas
53
Romidepsin
Histone De-Acetylation (HDAC) Inhibitor inhibits histone deacetylation --\> apoptosis ADR: cardiac, myelosuppression
54
Safe for pregnancy
Interferon Alpha
55
Sorafenib
tyrosine kinase inhibitor VEGF-R, raf ADR: HTN, proteinuria, rash, diarrhea, clotting/bleeding, hand-foot syndrome, rare hepatic USES: Renal cell carcinoma
56
Sunitinib
tyrosine kinase inbihitor VEGF-R, PDGF, kit ADR: HTN, proteinuria, rash, clotting/bleeding, hand-foot syndrome, and rare hepatic USES: Renal cell carcinoma
57
Tamoxifen
hormonal oncologic--\> estrogen receptor antagonist; acts in cancer cell to prevent binding of estrogen to receptor ADR: bone loss, thrombogenic, uterine neoplasms
58
Temozolomide
Alkylating Agent--\> alkylates O6 of guanine PO crosses BBB ADR: common- myelosuppresion, alopecia, sterility, mucositis, carcinogenic, pulmonary fibrosis
59
Toxicities common to alkylating agents
toxic to rapidly dividing cells--\> myelosuppression, GI damage (mucositis), alopecia, impaired wound healing, impaired growth in children, immunosuppression, sterility, teratogenic, carcinogenic
60
Toxicities of anthracyclines
myelosuppression, vesicant, mucositis, GI, dose related cardiac toxicity
61
Trastuzumab
Anti-her2/neu antibody--\> inhibits signaling (Herceptin) ADR: cardiomyopathy (decrease EF), infusion reaction Uses: Her2/neu + breast cancer (- hormone receptor)
62
Tretinoin (ATRA)
binds retinoic acid receptor causes maturation of promyelocytes ADR: teratogenic, increased intracranial pressure, cutaneous, hepatic, _differentiation syndrome_ USES: Acute promyelocytic leukemia t(15;17)
63
Vinblastine
Vinca alkaloid--\> anti-microtubular agent binds tubulin in M phase and blocks mitosis ADR: myelosuppression; neuropathy (in ABVD)
64
Vincristine
vinca alkaloid--\> anti-microtubular agent binds tubulin in M phase and blocks mitosis ADR: neuropathy \> myelosuppression
65
CAR
recognizes antigen on cancer cell, independent of MHCI ADR: cytokine release syndrome (treat with antibody to IL-6) USES: ALL
66
ABVD
A= Adriamycin= doxorubicin B= bleomycin V= vinblastine D= dacarbazine
67
Hand Foot Syndrome
Gemcitabine
68
Cerebellar toxicity at high doses
Cytarabine
69
Uterine neoplasms
Tamoxifen
70
Prolonged QT
arsenic trioxide
71
Dosed according to UGT allele status (b/c of myelosuppression)
Irinotecan
72
Less cardiogenic anthracycline
mitoxantrone
73
Useful for patients with hepatic/renal impairment
cytosine analogs fluorouracil
74
3 Drugs that are anti-VEGF
Sunitinib Sorafenib Bevacizumab
75
Asparaginase
treatment of ALL ADR: thrombosis, pancreatitis
76
refractory B cell ALL
blinatumomab
77
major side effect of ATRA and treatment
differentiation syndrome- fever, pleural effusions, pericardial effusions, hypotension, etc. dexamethasone
78
2 cycles of diarrhea
irinotecan

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