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Pharm Exam 8 > L18-19 Antineoplastics > Flashcards

L18-19 Antineoplastics Flashcards

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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
If you need to treat a brain tumor, what are 2 drugs to think of?
Carmustine (BCNU) | Lomustine (CCNU)
26
Darcarbazine
DNA cross-linker Activated by P450 IV Hodgkin's disease, malignant melanoma, sarcomas Temozolomide and Procarbazine are similar
27
Temozolomide
DNA cross-linker Activated by P450 IV Used for glioma and astrocytoma
28
Procarbazine
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
29
What drug is known for having a metabolite that inhibits MOA?
Procarbazine
30
Methotrexate
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
31
Leucovorin
Given after methotrexate to rescue normal cells from damage from dihydrofolate reductase inhibition Also used with 5-FU to increase its effectiveness
32
Pemetrexed
Similar to Methotrexate Inhibits thymidilate synthase Used with Cusplatin for mesothelioma and non-small cell lung cancer Causes hand-foot disease and myelosuppression
33
What drug is assoc. c hand-foot disease?
Pemetrexed | 5-FU
34
What does rifampin do to P450?
Induces
35
What drug is converted by P450 to its active form?
Cyclophosphamide
36
How do purine analogues work?
Converted to nucleotides by HGPRT that then prevent synthesis of purines and stop DNA/RNA synthesis Not cell cycle specific Myelosuppressive
37
Mercaptopurine (Purinethol)
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
What drug interacts with Mercaptopurine and how?
Allopurinol | Inhibits xanthine oxidase which metabolizes Mercaptopurine and therefore would cause toxicity
39
What is Xanthine oxidase?
Enzyme used in the production of uric acid | It is the target of Allopurinol to treat hyperuricemia
40
Thioguanine
Similar to Mercaptopurine but not metabolized by xanthine oxidase Treats AML
41
Pentostatin, Cladribine, Fludarabine
Purine analogues like Mercaptopurine
42
What drug is metabolized by xanthine oxidase?
Mercaptopurine
43
What is Thymidylate Synthase?
Enzyme involved with production of Thymidine | Blocking it causes deficiency in Thymidine and buildup of precursor molecules that both damage DNA
44
5-Fluorouracil (5-FU, Adrucil)
``` 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
Capesitabine
5-FU prodrug more selective for tumor and less side effects | Purine group
46
Cytarabine
``` Antimetabolite Purine drug Competes with Cytosine for DNA incorporation stopping DNA synthesis Used in leukemias Severe marrow suppression ```
47
What drug causes radiation recall?
Hydroxyurea
48
Doxorubicin, Daunorubicin
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
What drug causes cardiomyopathy?
Doxorubicin
50
What drug causes red urine?
Daunorubicin
51
Dexrazoxane
Iron chelator used to decrease cardiotoxicity of Doxorubicin
52
Bleomycin (Blenoxane)
``` 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
What drug did Lance Armstrong not want to take for testicular cancer because it can cause pulmonary fibrosis?
Bleomycin
54
Dactinomycin (Actinomycin D)
Antibiotic binds DNA and breaks it Strong vesicant Radiation recall
55
Vincristine/ Vinblastine
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
Paclitaxel (Taxol)
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
Topoisomerase Inhibitors
Prevents the uncoiling of DNA
58
Etoposide (Teniposide)
Topoisomerase II inhibitor DNA strand breaks Testicular cancer Causes leukopenia
59
Topotecan, Ironotecan
Topoisomerase I inhibitor Cell cycle arrest Topotecan: ovarian cancer Ironotecan: broad spectrum Myelosuppression!
60
Asparaginase (Elspar)
Breaks down asparagine that is required by leukemia cells | Hypersensitivity reactions
61
Drugs that end in -tinib are?
Tyrosine Kinase inhibitors | All metabolized by CYP3A4
62
Imatinib (Gleevec)
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
Erlotinib
Blocks ATP binding to HER1/EGFR tyrosine kinase | Non-small cell lung cancer (2nd line) and pancreatic cancer
64
Gefitinib
Inhibits EGFR tyrosine kinase | Diarrhea
65
Cetuximab
EGF receptor antibody blocks cell growth | Anaphylactoid reactions
66
Bevacizumab
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
PD-1 inhibitors
PD-1 secreted by tumors to prevent immune system from seeing them Blocking it allows immune system to attack them
68
Nivolumab, Pembrolizumab
Inhibit PD-1 | Allow T-cells to see tumors
69
Prednisone
Lymphomas and Leukemias
70
Tamoxifen
Block estrogen receptor in breast Can cause uterine hyperplasia Must be activated by CYP2D6
71
What drugs inhibit CYP2D6? What cancer drug might this affect?
Fluoxetine, Paroxetine | Prevents activation of Tamoxifen
72
Trastuzumab (Herceptin)
Antibody to HER2 receptor | Cardiotoxic, do not combine with doxorubicin
73
Flutamide
Anti-androgen for prostate cancer
74
What drugs cause Radiation Recall?
Dactinomycin Hydroxyurea Doxorubicin Daunorubicin
75
What drugs cause Pulmonary fibrosis?
Bleomycin | Busulfan
76
What drugs cause peripheral neuropathy?
Vincristine Vinlablastine Paclitaxel
77
What drugs cause hyperuricemia?
6-Mercaptopurine (remeber Allopurinol affects metabolism) | Busulfan
78
What drugs cause acoustic nerve damage?
Cisplatin
79
What drugs cause red urine?
Daunorubicin
80
What drugs cause hepatotoxicity?
Methotrexate 6-Mercaptopurine BCNU CCNU
81
What drugs cause hemorrhagic cystitis?
Cyclophosphamide | Ifofsphamide (MESNA) reverses it
82
What drugs cause Cardiomyopathy?
Doxorubicin, Daunorubicin, Trastuzumab | Reversed with Dezrazoxane

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