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Pharm Exam 8 > L18-19 Antineoplastics > Flashcards

L18-19 Antineoplastics Flashcards

1
Q

What characteristics of tumor cells will increase the likelihood of a successful treatment?

A

Fast growing tumors
High % of cells in growth stage
Small tumors–better penetration
Early detection

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2
Q

What are some ways that tumors become resistant to drug treatment?

A 
Change levels/affinity of target enzymes
Decrease drug activation
Increase DNA repair
Increase salvage pathways for purines and pyrimidines
Decrease drug uptake
Increase efflux through P-glycoprotein
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3
Q

What does P-glycoprotein do?

A

Increases drug efflux causing tumor resistance to treatment

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4
Q

Cancer drugs target fast reproducing cells. What cells in the body will also be damaged?

A 
Bone marrow leading to increased bleeding and depressed immunity
Gi tract–N/V
Hair follicles
Renal
Reproduction
Teratogenesis
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5
Q

What was one of the first cytotoxic agents used to treat cancer?

A

Mustard gas used to treat lymphoma

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6
Q

How do alkylating agents work?

A

Very reactive agent that alkylates the DNA and causes miscoding, breaking, and crosslinking
Not cell-cycle specific
Most effective on rapidly growing cells

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7
Q

Alkylating agent toxicity

A

Vesicant: tissue damage at injection site (mustard gas damages tissue)
Affects rapidly proliferating cells–hair, marrow, sperm, GI
Traditional toxicities

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8
Q

Cisplatin (Platinol)

A 
Platinum alkylating agent
Cross-links DNA
Sensitizes cells to radiation
Broad spectrum
Used in testicular cancer
Toxicity: renal (amifostin prtects), acoustic nerve damage, anaphylaxis, nausea and vomiting bad
Carboplatin and Oxalaplatin similar
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9
Q

What alkylating agent causes acoustic nerve damage leading to tinnitus?

A

Cisplatin (Platinol)

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10
Q

Carboplatin

A

Same function and effects as Cisplatin

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11
Q

Oxalaplatin

A

Same function and effects as Cisplatin

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12
Q

Mechlorethamine (Mustargen)

A 
Nitrogen Mustard alkylating agent
One of the first drugs
Most effective in G1 and M phase
Used often in Hodgkin's Disease
Toxicity: vesicant!, hyperuricemia from massive tumor cell lysis, renal damage, N/V, sterility & teratogenicity
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13
Q

Cyclophosphamide (Cytoxan)

A

Nitrogen mustard alkylating agent
Must know this drug!
Oral–unique
Pro-drug that is activated by P-450
Metabolized into Acrolein that causes hemorrhagic cystits–to protect against this give MESNA
Broad spectrum, used for immun suppression
Toxicities: not a vesicant, alopecia bad, SIADH, N/V, anorexia

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14
Q

What drug causes hemorrhagic cystitis and how is this prevented?

A

Cyclophosphamide (Cytoxan)

Co-administer MESNA

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15
Q

What drug causes SIADH?

A

Cyclophosphamide (Cytotoxan)

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16
Q

Ifosfamide

A

Similar to Cyclophosphamide, combined with MESNA, also causes hemorrhagic cystitis

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17
Q

Chloranbucil

A 
Alkylating agent
Oral, slow action
Used for CLL
Very non-toxic
Used for years–a long-term drug
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18
Q

Thiotepa

A

Alkylating agent
Used for bladder cancer
Not oral

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19
Q

Bendamustine

A

Alkylating agent

Used for CLL and non-hodgkins lymphoma

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20
Q

What drug is often used to counter the hyperuricemia in cancer patients?

A

Allopurinol with hydration

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21
Q

Busulfan–Myleran

A

Alkylating agent
CML
Known for hyperuricemia

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22
Q

What are Nitrosoureas?

A

Alkylating agents that have ability to form 2 rings to attack DNA/RNA synthesis

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23
Q

Carmustine (BCNU)

A

Nitrosourea drug
Known for high lipid solubility making it effective for brain tumors
Vesicant–burns on admin.

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24
Q

Lomustine (CCNU)

A

Nitrosourea drug
Known for high lipid solubility making it effective for brain tumors
Vesicant–burns on admin.

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25
Q

If you need to treat a brain tumor, what are 2 drugs to think of?

A

Carmustine (BCNU)

Lomustine (CCNU)

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26
Q

Darcarbazine

A

DNA cross-linker
Activated by P450
IV
Hodgkin’s disease, malignant melanoma, sarcomas
Temozolomide and Procarbazine are similar

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27
Q

Temozolomide

A

DNA cross-linker
Activated by P450
IV
Used for glioma and astrocytoma

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28
Q

Procarbazine

A

DNA cross-linker
Activated by P450
IV
Used for Hodgkin’s and non-hodgkin’s lymphomas, brain tumors
Metabolite is an MAO inhibitor–careful with antidepressants and linezolid

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29
Q

What drug is known for having a metabolite that inhibits MOA?

A

Procarbazine

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30
Q

Methotrexate

A

Inhibits dihydrofolate reductase to inhibit production of folic acid and thereby inhibit production of thymidylate which eventually prevents DNA synthesis and damages DNA
Can be used for immune suppression in low doses
For cancer: high doses but only few times
Leucovorin: given after to rescue the normal cells from damage
Toxicity: precipitates in kidney–hydration important, hepatotoxicity

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31
Q

Leucovorin

A

Given after methotrexate to rescue normal cells from damage from dihydrofolate reductase inhibition

Also used with 5-FU to increase its effectiveness

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32
Q

Pemetrexed

A

Similar to Methotrexate
Inhibits thymidilate synthase
Used with Cusplatin for mesothelioma and non-small cell lung cancer
Causes hand-foot disease and myelosuppression

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33
Q

What drug is assoc. c hand-foot disease?

A

Pemetrexed

5-FU

34
Q

What does rifampin do to P450?

A

Induces

35
Q

What drug is converted by P450 to its active form?

A

Cyclophosphamide

36
Q

How do purine analogues work?

A

Converted to nucleotides by HGPRT that then prevent synthesis of purines and stop DNA/RNA synthesis
Not cell cycle specific
Myelosuppressive

37
Q

Mercaptopurine (Purinethol)

A

Purine analogue that inhibits purine synthesis
Metabolized by xanthine oxidase–important drug interaction with Allopurinol and other drugs that affect XO
Used for leukemia

38
Q

What drug interacts with Mercaptopurine and how?

A

Allopurinol

Inhibits xanthine oxidase which metabolizes Mercaptopurine and therefore would cause toxicity

39
Q

What is Xanthine oxidase?

A

Enzyme used in the production of uric acid

It is the target of Allopurinol to treat hyperuricemia

40
Q

Thioguanine

A

Similar to Mercaptopurine but not metabolized by xanthine oxidase
Treats AML

41
Q

Pentostatin, Cladribine, Fludarabine

A

Purine analogues like Mercaptopurine

42
Q

What drug is metabolized by xanthine oxidase?

A

Mercaptopurine

43
Q

What is Thymidylate Synthase?

A

Enzyme involved with production of Thymidine

Blocking it causes deficiency in Thymidine and buildup of precursor molecules that both damage DNA

44
Q

5-Fluorouracil (5-FU, Adrucil)

A 
Inhibits thymidylate synthase–blocks DNA synthesis
Purine group
Needs folic acid to work so adding Leucovorin added to help with this
Cell cycle specific–G1 and S phases
Broad spectrum of use
Colorectal cancer
Topical for basal cell carcinoma
Causes hand-foot disease
45
Q

Capesitabine

A

5-FU prodrug more selective for tumor and less side effects

Purine group

46
Q

Cytarabine

A 
Antimetabolite
Purine drug
Competes with Cytosine for DNA incorporation stopping DNA synthesis
Used in leukemias
Severe marrow suppression
47
Q

What drug causes radiation recall?

A

Hydroxyurea

48
Q

Doxorubicin, Daunorubicin

A

Antibiotic
Logdes itself in the DNA and breaks it and causes dysfunction
Generates free-radicals leading to cardiomyopathy especially with Herceptin which is also cardiotoxic
Cardio effects increased by Iron–decreased by iron chelator Dexrazoxane
Used for Thyroid and Breast cancers and many others
Daunorubicin can also cause red urine and is used for some leukemias

49
Q

What drug causes cardiomyopathy?

A

Doxorubicin

50
Q

What drug causes red urine?

A

Daunorubicin

51
Q

Dexrazoxane

A

Iron chelator used to decrease cardiotoxicity of Doxorubicin

52
Q

Bleomycin (Blenoxane)

A 
Antibiotic
Binds DNA and breaks it
Most active in G2 and M phase
Good for testicular and ovarian cancer and many others
Little myelosuppression
Does cause pulmonry fibrosis
Can cause anaphylactoid Sx
53
Q

What drug did Lance Armstrong not want to take for testicular cancer because it can cause pulmonary fibrosis?

A

Bleomycin

54
Q

Dactinomycin (Actinomycin D)

A

Antibiotic binds DNA and breaks it
Strong vesicant
Radiation recall

55
Q

Vincristine/ Vinblastine

A

Plant alkaloid
Bind tubulin to prevent microtubule aligning in mitosis of M phase
Vincristine: leukemia, Hodgkin’s, high neurotoxicity because axonal transport requires microtubules, low myelosuppression

Vinblastine: testicular carcinoma,Hidgkin’s, more myelosuppression but less neurotoxicity

56
Q

Paclitaxel (Taxol)

A

Plant Alkaloid
Binds microtubulin stabilizing it and preventing disassembly after mitosis
Very toxic
Broad spectrum
Causes peripheral neuropathy, myelosuppression, myalgia, arthralgia, hypersensitivity–decreased by binding to albumin

57
Q

Topoisomerase Inhibitors

A

Prevents the uncoiling of DNA

58
Q

Etoposide (Teniposide)

A

Topoisomerase II inhibitor
DNA strand breaks
Testicular cancer
Causes leukopenia

59
Q

Topotecan, Ironotecan

A

Topoisomerase I inhibitor
Cell cycle arrest
Topotecan: ovarian cancer
Ironotecan: broad spectrum

Myelosuppression!

60
Q

Asparaginase (Elspar)

A

Breaks down asparagine that is required by leukemia cells

Hypersensitivity reactions

61
Q

Drugs that end in -tinib are?

A

Tyrosine Kinase inhibitors

All metabolized by CYP3A4

62
Q

Imatinib (Gleevec)

A

Inhibits Bcr-Abl fusion protein (Philadelphia chromosome) that is unique to cancer cells especially CML but also gastrointestinal stromal tumor
No severe SE’s
Can be some immunosuppression

63
Q

Erlotinib

A

Blocks ATP binding to HER1/EGFR tyrosine kinase

Non-small cell lung cancer (2nd line) and pancreatic cancer

64
Q

Gefitinib

A

Inhibits EGFR tyrosine kinase

Diarrhea

65
Q

Cetuximab

A

EGF receptor antibody blocks cell growth

Anaphylactoid reactions

66
Q

Bevacizumab

A

Angiogenesis Inhibitor
VEGF blocker?
Decreases blood supply to slow tumor growth
Bleeding and thromboembolism risk increased with systemic use
Blood vessels don’t heal well so avoid surgery

67
Q

PD-1 inhibitors

A

PD-1 secreted by tumors to prevent immune system from seeing them
Blocking it allows immune system to attack them

68
Q

Nivolumab, Pembrolizumab

A

Inhibit PD-1

Allow T-cells to see tumors

69
Q

Prednisone

A

Lymphomas and Leukemias

70
Q

Tamoxifen

A

Block estrogen receptor in breast
Can cause uterine hyperplasia
Must be activated by CYP2D6

71
Q

What drugs inhibit CYP2D6? What cancer drug might this affect?

A

Fluoxetine, Paroxetine

Prevents activation of Tamoxifen

72
Q

Trastuzumab (Herceptin)

A

Antibody to HER2 receptor

Cardiotoxic, do not combine with doxorubicin

73
Q

Flutamide

A

Anti-androgen for prostate cancer

74
Q

What drugs cause Radiation Recall?

A

Dactinomycin
Hydroxyurea
Doxorubicin
Daunorubicin

75
Q

What drugs cause Pulmonary fibrosis?

A

Bleomycin

Busulfan

76
Q

What drugs cause peripheral neuropathy?

A

Vincristine
Vinlablastine
Paclitaxel

77
Q

What drugs cause hyperuricemia?

A

6-Mercaptopurine (remeber Allopurinol affects metabolism)

Busulfan

78
Q

What drugs cause acoustic nerve damage?

A

Cisplatin

79
Q

What drugs cause red urine?

A

Daunorubicin

80
Q

What drugs cause hepatotoxicity?

A

Methotrexate
6-Mercaptopurine
BCNU
CCNU

81
Q

What drugs cause hemorrhagic cystitis?

A

Cyclophosphamide

Ifofsphamide (MESNA) reverses it

82
Q

What drugs cause Cardiomyopathy?

A

Doxorubicin, Daunorubicin, Trastuzumab

Reversed with Dezrazoxane

Pharm Exam 8 (6 decks)

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