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

Anti-neoplastic drugs Flashcards

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
Q

Daunorubucin

A

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

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26
Q

Decitabine

A

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

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27
Q

Doxorubicin

A

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

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28
Q

Erlotinib

A

tyrosine kinase inhibitor

EGF-R

ADR: diarrhea, rash

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29
Q

Etoposide (VP-16)

A

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

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30
Q

Fluorouracil

A

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

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31
Q

Gemcitabine

A

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”

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32
Q

Goserelin

A

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
Q

Hydroxyurea

A

USES: AML hyperleukocytosis

ADR: myelosuppression, mucositis

34
Q

Idarubicin

A

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
Q

IL-2

A

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
Q

Imatinib

A

tyrosine kinase inhibitor

Bcr-abl, kit

ADR: fluid retention, hepatic, myelosuppression, rare cardiomyopathy

USES: CML, GIST

37
Q

Ipilimumab

A

Anti-CTLA4–> stimulates immune system

ADR: infusion rxn (chills, fever, SOB, hypotension), exaggerated autoimmunity especially gut and hepatic dysfunction

38
Q

Irinotecan (CPT 11)

A

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
Q

Letrozole

A

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
Q

Leucovorin

A

Reduced folate

potentiates activity of 5-FU

rescue/protexts normal cells from methotrexate

41
Q

Mechlorethamine

A

Alkylating Agent–> nitrogen mustard parent drug of class (chemical warfare)

ADR: blistering agent, vomiting common- myelosuppression, alopecia, sterility, mucositis, carcinogenic, pulmonary fibrosis

42
Q

Melphalan

A

Alkylating Agent (Mustard)

PO

ADR: common- myelosuppression, alopecia, sterility, mucositis, carcinogenic, pulmonary fibrosis

43
Q

Methotrexate

A

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
Q

Mitoxantrone

A

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
Q

Nivolumab

A

Anti- PD1 directed antibody

ADR: autoimmune like side effects including gut, hepatic, renal, thyroid

46
Q

Ondansetron

A

type 3 serotonin antagonist

USES: nausea associated with chemo

47
Q

Oxaliplatin

A

Alkylating Agent–> DNA damaging heavy metals; crosslinks DNA

ADR: neuro>>heme>>>>>renal

48
Q

Paclitaxel

A

anti-microtubular agent

stabilizes tubules and prevents breakdown –> no progression to M phase

ADR: myelosuppression, neuropathy, vascular leak (=fluid retention), hypersentiviity to vehicle

49
Q

Pembrolizumab

A

Anti-PD1 directed antibody

ADR: autoimmune like side effects including gut, hepatic, renal, thyroid

50
Q

Prednisone

A

glucocorticoid receptor antagonist

ADR: glucocorticoid excess- hyperglycemia, fluid retention, gastric irritation, cushing’s syndrome, increased opportunitistic infections, myopathy, CNS changes

51
Q

Procarbazine

A

Alkylating Agent

PO

crosses BBB

ADR: mood swings, somnolence common- myelosuppression, alopecia, sterility, mucositis, carcinogenic, pulmonary fibrosis

52
Q

Rituximab

A

Anti-CD20 antibody–> inhibits lymphocyte signaling and activates immune response

ADR: infusion reaction (chills, fever, shortness of breath, hypotension)

Uses: B cell lymphomas

53
Q

Romidepsin

A

Histone De-Acetylation (HDAC) Inhibitor

inhibits histone deacetylation –> apoptosis

ADR: cardiac, myelosuppression

54
Q

Safe for pregnancy

A

Interferon Alpha

55
Q

Sorafenib

A

tyrosine kinase inhibitor

VEGF-R, raf

ADR: HTN, proteinuria, rash, diarrhea, clotting/bleeding, hand-foot syndrome, rare hepatic

USES: Renal cell carcinoma

56
Q

Sunitinib

A

tyrosine kinase inbihitor

VEGF-R, PDGF, kit

ADR: HTN, proteinuria, rash, clotting/bleeding, hand-foot syndrome, and rare hepatic

USES: Renal cell carcinoma

57
Q

Tamoxifen

A

hormonal oncologic–> estrogen receptor antagonist; acts in cancer cell to prevent binding of estrogen to receptor

ADR: bone loss, thrombogenic, uterine neoplasms

58
Q

Temozolomide

A

Alkylating Agent–> alkylates O6 of guanine

PO

crosses BBB

ADR: common- myelosuppresion, alopecia, sterility, mucositis, carcinogenic, pulmonary fibrosis

59
Q

Toxicities common to alkylating agents

A

toxic to rapidly dividing cells–> myelosuppression, GI damage (mucositis), alopecia, impaired wound healing, impaired growth in children, immunosuppression, sterility, teratogenic, carcinogenic

60
Q

Toxicities of anthracyclines

A

myelosuppression, vesicant, mucositis, GI, dose related cardiac toxicity

61
Q

Trastuzumab

A

Anti-her2/neu antibody–> inhibits signaling (Herceptin)

ADR: cardiomyopathy (decrease EF), infusion reaction

Uses: Her2/neu + breast cancer (- hormone receptor)

62
Q

Tretinoin (ATRA)

A

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
Q

Vinblastine

A

Vinca alkaloid–> anti-microtubular agent

binds tubulin in M phase and blocks mitosis

ADR: myelosuppression; neuropathy

(in ABVD)

64
Q

Vincristine

A

vinca alkaloid–> anti-microtubular agent

binds tubulin in M phase and blocks mitosis

ADR: neuropathy > myelosuppression

65
Q

CAR

A

recognizes antigen on cancer cell, independent of MHCI

ADR: cytokine release syndrome (treat with antibody to IL-6)

USES: ALL

66
Q

ABVD

A

A= Adriamycin= doxorubicin

B= bleomycin

V= vinblastine

D= dacarbazine

67
Q

Hand Foot Syndrome

A

Gemcitabine

68
Q

Cerebellar toxicity at high doses

A

Cytarabine

69
Q

Uterine neoplasms

A

Tamoxifen

70
Q

Prolonged QT

A

arsenic trioxide

71
Q

Dosed according to UGT allele status (b/c of myelosuppression)

A

Irinotecan

72
Q

Less cardiogenic anthracycline

A

mitoxantrone

73
Q

Useful for patients with hepatic/renal impairment

A

cytosine analogs

fluorouracil

74
Q

3 Drugs that are anti-VEGF

A

Sunitinib

Sorafenib

Bevacizumab

75
Q

Asparaginase

A

treatment of ALL

ADR: thrombosis, pancreatitis

76
Q

refractory B cell ALL

A

blinatumomab

77
Q

major side effect of ATRA and treatment

A

differentiation syndrome- fever, pleural effusions, pericardial effusions, hypotension, etc.

dexamethasone

78
Q

2 cycles of diarrhea

A

irinotecan

P&T Block 2 (4 decks)

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