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Winter 2021 Finals > Pharm - Antineoplastics > Flashcards

Pharm - Antineoplastics Flashcards

1
Q

Antineoplastic drug classes

A

Cytotoxic, targeted antineoplastics, hormonal therapy, immunotherapy, other

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2
Q

Limitations of antineoplastic care

A
  • Tumor cell resistance
  • Host toxicity
  • Inability to suppress metastasis
  • Drug resistance
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3
Q

Induction chemotherapy

A
  • given to induce remission

- treatment of acute leukemia

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4
Q

Consolidation chemotherapy

A
  • given once remission is achieved to sustain it

- treatment of acute leukemia

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5
Q

Maintenance chemotherapy

A
  • given in lower doses for prolonged time to prolong remission
  • only acute leukemia, sometimes lung and colorectal
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6
Q

Myoablative chemotherapy

A
  • high dose to obliterate bone marrow

- followed by bone marrow or stem cell transplant to rebuild bone marrow

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7
Q

Adjuvant chemotherapy

A
  • to destroy any microscopic spread of cancer cells after primary tumor is removed
  • given to prevent recurrence
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8
Q

Neoadjuvant chemotherapy

A
  • given prior to surgery, often attempting to shrink tumor
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9
Q

Chemoradiosensitization

A
  • small doses given during radiation therapy to increase effectiveness
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10
Q

Palliative chemotherapy

A
  • given to address sxs without expecting significant reduction in cancer
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11
Q

Administration of cytotoxic agents

A
  • intermittent combination regimes
  • optimizes synergistic effect of drugs while minimizing toxicity
  • occasionally single agents are used
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12
Q

Administration of targeted agents

A
  • continuously or intermittently

- alone or in combination with cytotoxic agents

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13
Q

Classes of cytotoxic agents

A
  • cell cycle specific - DNA synthesis inhibitors, topoisomerase inhibitors, mitotic inhibitors
  • cell cycle non-specific - DNA alkylating agents, DNA intercalating agents
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14
Q

General cytotoxic drug toxicity

A
  • bone marrow: leukopenia, thrombocytopenia, anemia
  • GI epithelium: oral mucositis, gastroenteritis
  • hair follicles: alopecia
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15
Q

DNA synthesis inhibitors classes

A
  • folate antagonists, purine/ pyrimidine analogues
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16
Q

Folate antagonist exemplar

A

Methotrexate

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17
Q

Folate antagonist mechanism

A
  • inhibits dihydrofolate activity –> prevents production of nucleotides
  • S phase specific
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18
Q

Methotrexate indications

A
  • acute leukemia, breast cancer, osteosarcoma, trophoblastic tumors
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19
Q

Purine/ pyrimidine analogue exemplar

A

Fluorouracil

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20
Q

Fluorouracil indications

A
  • breast, colorectal, gastric cancer
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21
Q

Fluorouracil mechanism

A
  • structural analogue of uracil –> prevents biosynthesis of nucleotides –> DNA strand breaks/ premature chain termination
  • active metabolite interferes with RNA function
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22
Q

DNA synthesis inhibitors toxicity

A
  • Myelosuppression (primary dose-limiting)
  • oral mucositis
  • diarrhea, hepatic and renal toxicity (methotrexate), alopecia (fluorouracil)
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23
Q

DNA alkylating agents classes

A

Nitrogen mustards, platinum compounds

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24
Q

Nitrogen mustard exemplar

A

cyclophosphamide

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25
Q

Platinum compounds exemplar

A

cisplatin

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26
Q

cyclophosphamide mechanism

A
  • prodrug converted into phosphoramide mustard (alkylating) and acrolein (toxic metabolite)
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27
Q

DNA alkylating agents mechanism

A
  • cross link DNA by binding alkyl groups into DNA bases –> interrupt synthesis, transcription, DNA repair, development of lethal mutations
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28
Q

Cisplatin mechanism

A
  • no alkyl group, but crosslink DNA via guanine residues
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29
Q

Cisplatin indications

A

Lung and ovarian cancer

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30
Q

Cyclophosphamide toxicity

A
  • Myelosuppression (dose limiting)
  • severe N/V
  • alopecia
  • hemorrhagic cystitis
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31
Q

Cisplatin toxicity

A
  • myelosuppression (milder)
  • Severe N/V, emetogenic
  • alopecia
  • nephrotoxicity, ototoxicity, sensory peripheral neuropathy
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32
Q

DNA intercalating agent classes

A
  • Anthracyclines, other
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33
Q

Anthracycline exemplar

A
  • Doxorubicin
34
Q

Doxorubicin mechanism

A
  • bind to DNA –> deformation and uncoiling
  • Inhibit topoisomerase II –> strand breaks
  • generate free radicals –> cleave DNA
35
Q

Other DNA intercalating exemplar

36
Q

Bleomycin info / indications

A
  • greatest effect in G2 effect

- Hodgkin’s disease and testicular cancer

37
Q

Doxorubicin toxicity

A
  • Myelosuppression (dose limiting)
  • N/V (moderate sever)
  • oral mucositis, alopecia
  • cardiotoxicity (dose limiting)
38
Q

Bleomycin toxicity

A
  • Myelosuppression (mild)
  • N/V (mild)
  • oral mucositis, alopecia
  • pulmonary toxicity
39
Q

Topoisomerase inhibitor classes

A
  • podophylotoxins, camptothecin analogues
40
Q

Podophylotoxin exemplar

41
Q

Etoposide mechanism

A
  • Interfere with topoisomerase II –> prevent recoiling of DNA
  • S phase
42
Q

Etoposide indications

A

Lung, gastric cancer

43
Q

Camptothecin analogue exemplar

A

Irinotecan

44
Q

Irinotecan mechanism

A

Inhibits topoisomerase I –> prevents relaxation of supercoiled DNA

45
Q

Irinotecan indications

A

Colorectal, gastro-esophageal, lung cancer

46
Q

Topoisomerase inhibitor toxicity

A
  • Myelosuppression (dose limiting)
  • N/V
  • Alopecia (etoposide)
  • Diarrhea (dose limiting in irinotecan)
47
Q

Mitotic inhibitor classes

A

Taxanes, vinca alkaloids

48
Q

Taxanes exemplar

A

Paclitaxel

49
Q

Paclitaxel indications

A

Breast, ovarian, lung

50
Q

Vinca alkaloids exemplar

A

Vincristine

51
Q

Vincristine indications

A

Acute leukemia, lymphomas, neuroblastoma

52
Q

Mitotic inhibitors mechanism

A
  • Interfere with microtubule structure, rendering them nonfunctional
  • M phase
53
Q

Mitotic inhibitors toxicity

A
  • Myelosuppression, esp neutropenia (dose limiting paclitaxel)
  • Peripheral neuropathy (dose limiting)
  • Alopecia, N/V
  • Paralytic ileus (vincristine)
  • Hypersensitivity rxns (paclitaxel)
54
Q

Targeted antineoplastics targets

A
  • Proteins more abundant in cancer cells
  • proteins that drive cancer proliferation
  • chromosome abnormalities present only in cancer cells
55
Q

Targeted agent toxicity

A
  • Most common: diarrhea, liver problems
  • Skin: acneiform rash, dry skin, nail changes, hair depigmentation
  • problems with blood clotting and wound healing
  • high BP
  • GI perforation (rare but serious)
56
Q

Targeted antineoplastic classes

A

Protein kinase inhibitors, proteasome inhibitors, monoclonal antibodies

57
Q

Protein kinase inhibitors exemplar

58
Q

Protein kinase inhibitors mechanism

A
  • impede pathways promoting malignant cell transformation
59
Q

Imatinib mechanism/ indications

A
  • Inhibits BCR-ABL tyrosine kinase

- CML

60
Q

Imatinib adverse effects

A
  • nausea, edema, rash, and diarrhea
61
Q

Proteasome inhibitors exemplar

A

Bortezomib

62
Q

Bortezomib adverse effects

A
  • fatigue
  • peripheral neuropathy (dose limiting)
  • N/V, diarrhea/ constipation
    myelosupprression
63
Q

Bortezomib indications

A

Multiple myeloma, mantle cell lymphoma

64
Q

Monoclonal antibodies exemplar

65
Q

Rituxamib mechanism

A
  • naked mAB - binds and blocks antigens in cancer cells
66
Q

Rituxamib adverse effects

A
  • hypersensitivity rxns
  • fever, chills, nausea, HA
  • myelosuppression
67
Q

Immunotherapy agent classes

A

Cytokines, immune checkpoint inhibitors

68
Q

Hormone antagonist classes

A

Estrogen antagonists, aromatase inhibitors, GnRH antagonist, androgen antagonists

69
Q

Cytokines exemplar

A

Interferon alpha

70
Q

Interferon alpha indications

A

Hairy cell leukemia, malignant melanoma, renal cell carcinoma

71
Q

Immune checkpoint inhibitors exemplar

A

Ipilimumab

72
Q

Ipilimumab mechanism

A

mAB against CTLA-4 antigen

73
Q

Ipilimumab indications

A

metastatic malignant melanoma

74
Q

Ipilimumab adverse effects

A
  • rash, fatigue, nausea

- diarrhea assoc w/ severe immune enterocolitis

75
Q

Estrogen antagonist exemplar

76
Q

Aromatase inhibitor exemplar

77
Q

GnRH agonist exemplar

A

Leuprolide

78
Q

Androgen antagonists exemplar

79
Q

Tamoxifen mechanism/ indications

A
  • selective estrogen receptor modulator

- ER + breast cancer

80
Q

Letrozole mechanism/ indications

A
  • prevents androgens –> estrone/ estradiol

- only post-menopausal ER+

81
Q

Leuprolide mechanism

A
  • after initial surge, complete inhibition of testicular/ ovarian function
82
Q

Flutamide mechanism/ indications

A
  • Prevents binding to/ downregulates T receptors –> inhibits tumor growth
  • first 2 weeks of GnRH agonist therapy or for metastatic prostate cancer

Winter 2021 Finals (6 decks)

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