Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

MOD II > TBL 9 - Cancer Chemotherapy Primer > Flashcards

TBL 9 - Cancer Chemotherapy Primer Flashcards

1
Q

What is HER-2/neu (erbB-2)?

A

A growth factor receptor.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What is ras?

A

A signal transduction molecule.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What is myc?

A

A transcription factor.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What is src?

A

A protein tyrosine kinase.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What is hTERT?

A

An enzyme that functions in DNA replication.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What is Bcl-2?

A

A membrane associated protein that functions to prevent apoptosis.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What is ABL?

A

A nonreceptor tyrosine kinase.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

What is chemotherapy?

A

A drug treatment that uses powerful chemicals to kill fast-growing cells in the body and is most often used to treat cancer.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What is immunotherapy?

A

A form of cancer treatment that uses the power of the body’s own immune system to prevent, control, and eliminate cancer.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What is an example of genetic alterations in colon carcinoma?

A

1) APC is inactivated early in tumor development.
2) Mutations of rasK frequently occur and are found in early-stage adenomas.
3) Mutations in MADR2 and p53 are associated with later stages.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What areas of cells are particularly affected by cytostatic agents?

A

Cells in the bone marrow, GI tract, gonads, hair follicles, and skin.

(Rapidly dividing cells).

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What drugs exert their actions on the S phase of the cell cycle?

A
  • Cytarabine
  • 6-mercaptopurine
  • 6-thioguanine
  • 5-fluorouracil
  • Methotrexate
  • Hydroxyurea
  • Irinotecan (blocks topoisomerase I)
  • Etoposide (blocks topoisomerase II)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What drugs exert their actions on the G2 phase of the cell cycle?

A
  • Bleomycin
  • Bortezomib
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What drugs exert their actions on the M phase of the cell cycle?

A
  • Vinblastine
  • Vincristine
    (Blocks tubular polymerization)
  • Paclitaxel (Blocks depolymerization of microtubules)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

What drugs exert their actions on the G1 phase of the cell cycle?

A
  • Asparaginase
  • -tinibs
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What drugs are non-cell-cycle specific?

A
  • Alkylating agents (cyclophosphamide, cisplatin, and procarbazine)
  • Antitumor antibiotics (doxorubicin and Daunorubicin)
  • Nitrosoureas (lomustine and carmustine)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

When are cell-cycle specific drugs most effective and when are non-cell-cycle specific drugs most effective?

A

CCS drugs are most effective in high growth fraction tumors while CCNS drugs are more useful in low growth fraction solid tumors.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Define “log kill.”

A

Using first order kinetics, a given dose of drug will destroy a constant fraction or proportion of a cell population rather than a constant number of cells.

Will kill a fixed percentage of tumor cells, not a fixed number.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

What clinical setting is primary induction therapy used?

A

Treatment of hematologic cancers and advanced solid tumors of which no alternative treatment exists.

Before surgery.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

What clinical setting is neoadjuvant chemotherapy used?

A

Chemotherapy in patients with localized cancer with alternative therapy such as surgery.

Before surgury.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

What clinical setting is adjuvant chemotherapy used?

A

Chemotherapy of many solid tumors adjuvant to local treatment such as surgery or radiation.

After surgery.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

What is included in the ABVD regimen and what is it used for?

A

Doxorubicin (Adriamycin), Bleomycin, Vincristine, Dacarbazine, and Prednisone.

Used to treat Hodgkin’s Lymphoma

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

What is included in the CHOP regimen and what is it used for?

A

Cyclophosphamide, Doxorubicin, Vincristine, and Prednisone plus Rituximab.

Used to treat Non-Hodgkin’s Lymphoma.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

What combination of drugs is used to treat Acute Lymphocytic Leukemia (ALL) in children?

A

Prednisone, Vincristine, and Asparaginase or an anthracycline, plus Intrathecal Methotrexate.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

What combination of drugs is used to treat breast cancer?

A

Cytotoxic agents, hormonal therapy with tamoxifen or an aromatase inhibitor (anastrozole), and Trastuzumab.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

What combination of drugs is used to treat Acute Myelogenous Leukemia (AML) in adults?

A

Cytarabine and Idarubicin or Daunorubicin.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

What combination of drugs is used to treat Chronic Myelogenous Leukemia (CML)?

A

Imatinib and Interferon

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

What combination of drugs is used to treat colon carcinoma?

A

Fluorouracil, Leucocorvin, and Oxaliplatin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

What combination of drugs is used to treat ovarian cancer?

A

Paclitaxel and Carboplatin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

What combination of drugs is used to treat pancreatic cancer?

A

Gemcitabine and Erlotinib

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
31
Q

What combination of drugs is used to treat prostatic carcinoma?

A

GnRH Agonist or Antagonist and an Androgen Receptor Antagonist.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
32
Q

What combination of drugs is used to treat lung carcinoma?

A

Carboplatin, Paclitaxel, and Bevacizumab.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
33
Q

What main group are the alkylating agents cyclophosphamide and mechlorethamine part of?

A

Nitrogen mustards

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
34
Q

What main group is the alkylating agent Carmustine part of?

A

Nitrosoureas

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
35
Q

What main group is the alkylating agent Busulfan part of?

A

Alkyl Sulfonate

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
36
Q

What hepatic mechanism does cyclophophamide require in order to be converted to its active form?

A

CYP450

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
37
Q

What is the MOA of Alkylating Agents?

A

Attaches an alkyl group to N7 of the purine base guanine, cross-linking DNA and creating ring cleavage.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
38
Q

What is the toxic metabolite of cyclophosphamide?

A

Acrolein

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
39
Q

What is acrolein responsible for in terms of adverse effects?

A

Hemorrhagic cystitis with symptoms of suprapubic pain, hematuria, and cystoscopy findings.

NVD, depression of BC counts, loss of appetite, and alopecia.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
40
Q

What is used to prevent hemorrhagic cystitis caused by acrolein (cyclophosphamide)?

A

MESNA (mercaptoethanesulfonate)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
41
Q

What is the MOA of procarbazine?

A

A reactive agent that forms hydrogen peroxide , which generates free radicals that cause DNA strand scission.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
42
Q

What are the adverse effects of procarbazine?

A
  • Myelosuppression
  • GI irritation
  • CNS dysfunction
  • Peripheral neuropathy
  • Skin reactions
  • Disulfiram-like reactions
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
43
Q

What is the MOA of the nitrosoureas Carmustine, Lomustine, and Semustine and what is their clinical application?

A

Acts by cross-linking (DNA alkylation) and is highly lipid soluble, allowing for it to cross the BBB which is useful for the treatment of CNS cancers.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
44
Q

Can temozolomide penetrate the CNS?

A

Yes

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
45
Q

What are the toxic effects of Busulphan?

A
  • Adrenal insufficiency
  • Skin pigmentation
  • Acute liver injury
  • Pulmonary fibrosis
  • Alveolar hemorrhage (“Bulsulphan Lung”)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
46
Q

What are the toxic effects of Melphalan?

A

Multiple myeloma

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
47
Q

What drugs are included in the MOPP regimen?

A
  • Mechlorathamine
  • Oncovin
  • Procarbazine
  • Prednisone
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
48
Q

What drugs are considered platinum-based chemotherapeutic agents?

A

Cisplatin, Carboplatin, and Oxaliplatin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
49
Q

What is the MOA of platinum-based chemotherapeutic agents?

A

Damages DNA by binding at N7 of guanine and causing DNA crosslinking.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
50
Q

What are platinum-based chemotherapeutic agents used for?

A

Testicular, bladder, lung, and ovarian cancers.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
51
Q

What are the toxic effects of platinum-based chemotherapeutic agents?

A
  • Neurotoxicity
  • Nephrotoxicity (can be prevented with adequate hydration and diuresis)
  • Ototoxicity (hearing loss)
  • Highly emetic (induces vomiting)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
52
Q

What drug protects against renal toxicity caused by cisplatin?

A

Amifostine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
53
Q

What 4 drugs are considered to be antitumor antibodies?

A

1) Bleomycin
2) Mitomycin
3) Anthracyclines - Doxorubicin and Daunorubicin

54
Q

What are the MOAs for the anthracyclines (Doxorubicin and Daunorubisin)?

A
  • Inhibits topoisomerase II to cleave DNA
  • Binds with iron to generate free radicals
  • Causes intercalating between base pairs
  • Induces histone eviction from the chromatin

Overall, inhibits DNA and RNA synthesis.

55
Q

What are the uses of anthracyclines (doxorubicin and daunorubicin)?

A
  • Breast, lung, endometrial, and ovarian cancer
  • Part of the ABVD regimen for Hodgkin’s lymphoma
  • ALL
  • Multiple myeloma
  • Non-Hodgkin lymphoma
56
Q

What are the adverse effects of anthracyclines (doxorubicin and daunorubicin)?

A
  • Bone marrow suppression
  • Cardiotoxicity (dilated cardiomyopathy and congestive heart failure)
  • Alopecia
57
Q

What medication is used to protect against cardiotoxicity caused by the anthracyclins?

A

Dexrazoxane

58
Q

What is the MOA of Dexrazoxane?

A

Binds free iron or removes iron from the doxorubicin-iron complex, thereby preventing oxygen free radical formation

59
Q

What phase of the cell cycle does Bleomycin act on?

A

G2 Phase

60
Q

What is the MOA of Bleomycin?

A
  • Intercalates DNA via an iron-bleomycin complex that produces free radicals causing DNA single and double strand breaks.
61
Q

When is Bleomycin used?

A
  • Included in the ABVD regimen for Hodgkin’s lymphoma.
  • Also used to treat Non-Hodgkin’s lymphoma, and testicular, head, neck, and skin cancers.
62
Q

What are the adverse effects of Bleomycin?

A
  • Pneumonitis
  • Pulmonary fibrosis (cough, dyspnea, crackles, infiltrates on chest x-ray)
  • Low bone marrow suppression
63
Q

What phase of the cell cycle does Methotrexate act on?

A

S phase

64
Q

What type of drug is methotrexate?

A

Antimetabolite

65
Q

What is the MOA of Methotrexate?

A

DNA synthesis inhibitor.

Inhibits dihydrofolate reductase which inhibits the conversion of folic acid to reduced folate cofactors, which in turn inhibits thymidylate synthesis.

Also, reduces T cell proliferation.

66
Q

What is Methotrexate used for?

A
  • Leukemias
  • Lymphomas
  • Breast cancer
  • Rheumatoid arthritis
  • Psoriasis
  • Immunosuppressant
  • Ectopic pregnancies -> Abortion
67
Q

What are the adverse effects of Methotrexate?

A
  • Bone marrow suppression
  • Hepatotoxicity
  • Aphthous ulcers
  • Renal and GI upset
68
Q

What drug is used to circumvent the blocked tetrahydrofolate synthesis caused by Methotrexate?

A

Leucovorin

69
Q

What is the MOA of Leucovorin?

A

Supplies reduced folate directly, bypassing the metabolic block caused by Methotrexate.

70
Q

What is another name for Leucovorin?

A

Folinic acid-N5-formyl-FH4

71
Q

What type of drug is 5-fluourouracil (5-FU)?

A

A pyrimidine analogue and prodrug that is included in the antimetabolite group.

72
Q

What is the MOA of 5-FU?

A

5-FU is converted into an abnormal dUMP (5-FdUMP) which is an irreversible inhibitor of thymidylate synthase, inhibiting the formation of thymine causing cellular death.

Inhibits DNA synthesis and inhibits RNA processing.

73
Q

What part of the cell cycle does 5-FU act on?

A

S phase

74
Q

What effect does Leucovorin have on 5-FU?

A

Increases the efficacy of it.

75
Q

What is 5-FU used for?

A

Breast, ovarian, colon, head, and neck cancers.

76
Q

What are the adverse effects of 5-FU?

A
  • Bone marrow suppression
  • Neurotoxicity
  • NVD
  • Mucositis
  • Cerebral ataxia
  • Coronary vasospasm
77
Q

What type of drug is 6-Mercaptopurine (6-MP)?

A

Purine analog

78
Q

How are azathioprine and 6-MP related?

A

Azathioprine is the prodrug of 6-MP.

79
Q

What is the MOA of 6-MP?

A

Inhibits numerous enzymes of purine nucleotide conversion, inhibiting purine, DNA, and RNA synthesis.

80
Q

What compound does 6-MP need to be converted to in order to be active and what compound metabolizes this action?

A

6-MP must be metabolized by hypoxanthine guanine phophoribosyl transferase (HGPRT) to 6-thioinosinic acid.

81
Q

How do some cancer cells have resistance to 6-MP?

A

They have a decreased activity of HGPRT.

82
Q

Where is 6-MP metabolized and what is it metabolized by?

A

Metabolized in the liver by xanthine oxidase.

83
Q

What drug does 6-MP interact with that causes 6-MP to be less effective?

A

Allopurinol

84
Q

What drug class does 6-MP interact with that causes 6-MP toxicity?

A

Thiopurines

85
Q

What is 6-MP used for?

A
  • Childhood acute lymphocytic leukemias
  • Chronic myeloid leukemia
86
Q

What are some adverse effects caused by 6-MP?

A
  • Bone marrow suppression
  • Hepatic dysfunction (cholestasis, jaundice, and necrosis)
  • Mucositis
  • Diarrhea
87
Q

What kind of drugs are Gemcitabine and Cytarabine?

A

Pyrimidine analogs

88
Q

What is the MOA of Gemcitabine?

A

Is a fluorinated cytidine analog that acts on the S-phase of the cell cycle and is an inhibitor of DNA synthesis.

89
Q

What is Gemcitabine used for?

A
  • Pancreatic carcinoma
  • Non-small cell lung cancer
  • Breast and ovarian cancers
90
Q

What are some adverse effects of Gemcitabine?

A
  • Myelosuppression
  • Oral and GI ulceration
  • NV
  • High doses can damage the liver, heart, and other organs.
91
Q

What is the MOA of Cytarabine?

A

Activated by kinases to AraCTP which inhibits DNA polymerase and incorporates itself into DNA and RNA.

92
Q

What are some adverse effects of Cytarabine?

A
  • NV
  • Myelocuppression
  • Neutropenia
  • Thrombocytopenia
  • Cerebellar ataxia
93
Q

What is Cytarabine used for?

A
  • AML
  • ALL
  • CML in blast crisis
94
Q

What type of drug is Hydroxyurea?

A

Antimetabolite

95
Q

What is the MOA of Hydroxyurea?

A

Inhibits the ribonucleotide reductase enzyme and shifts globulin gene transcription from beta to gamma, which increases the levels of HbF and decreases HbB.

96
Q

What is Hydroxyurea used for?

A

Sickle cell disease.

Fetal hemoglobin is not affected by the sickle cell mutation.

97
Q

What are some adverse effects of Hydroxyurea?

A
  • Myelosuppression
  • Megaloblastic anemia
  • Pancytopenia
98
Q

What type of drug is all-trans retinoic acid (ATRA)?

A

Differentiating agent

99
Q

What is the MOA of ATRA?

A

Promotes differentiation of promyelocytes.

100
Q

What is ATRA used for?

A

Acute promyelocytic leukemia

101
Q

What are some adverse effects of ATRA?

A
  • “Differentiation syndrome” with respiratory distress
  • Pleural and pericardial effusions
  • CNS symptoms
102
Q

What is the MOA of vinblastine and vincristine?

A

Binds to B-tubulin and causes inhibition of microtubular polymerization in the M phase of the cell cycle.

103
Q

What is vinblastine used for?

A

ABVD protocol for Hodgkin lymphoma.

104
Q

What is vincristine used for?

A

Hodkin lymphoma, AL leukemias, Wilms tumor, rhabdomyosarcoma, neuroblastoma, and breast cancer.

105
Q

What are the side effects of vinblastine and vincristine?

A
  • BMS
  • Neurotoxicity (loss of axonal transport, paresthesia/pain in fingers and feet, and distal weakness)
106
Q

What is the MOA of the taxanes (Paaclitaxel and Docetaxel)?

A
  • Blocks microtubule breakdown or degradation
  • Enhances tubulin polymerization
  • Hyperstabilizes microtubules in the M phase
107
Q

What adverse effects are caused by the taxanes?

A
  • Peripheral neuropathy (burning paresthesia of hands and feet)
  • Myelosuppression
  • Hypersensitivity
108
Q

What is Paclitaxel used for?

A
  • Ovarian cancer
  • Non-small cell lung cancer
  • Breast cancer
109
Q

What is Docetaxel used for?

A
  • Breast cancer
  • Non-small cell lung cancer
110
Q

What is Cabazitaxel used for?

A

Hormone refractory prostate cancer.

111
Q

What is the MOA of the Camptothecon class (irinotecan and topotecan) of DNA topoisomerase inhibitors?

A

Inhibits topoisomerase I which normally breaks single strands of DNA before resealing.

112
Q

What are the pharmacokinetics of irinotecan?

A

Irinotecan is a prodrug that is activated in the liver to SN-38 and eliminated in the bile and feces.

113
Q

What are the pharmacokinetics of Topotecan?

A

It is eliminated renally.

114
Q

What are Irinotecan and Topotecam used for?

A

Colon, ovarian, and small cell cancer.

115
Q

What is the adverse effect of Topotecan?

A

Myelosuppression

116
Q

What is the adverse effect of Irinotecan?

A

Diarrhea

117
Q

How is Irinotecan toxicity treated?

A
  • Acute: diarrhea
  • Delayed: loperamide which acts on the mu-opiod receptors in the mesenteric plexus of the large intestine
118
Q

What is the MOA of the Epipodophyllotoxins class (etoposide and teniposide) of DNA topoisomerase inhibitors?

A

Inhibits topoisomerase II which normally breaks double strands of DNA before resealing.

119
Q

What are the pharmacokinetics of Etoposide?

A

It is eliminated renally and dose reductions should be made in patients with renal impairment.

120
Q

What are the clinical uses of etoposide and teniposide?

A

Used in combination drug regimen for therapy of lymphoma, lung, germ cell, and gastric cancers.

121
Q

What are the adverse effects of etoposide and teniposide?

A
  • Myelosuppression
  • GI upset
  • Alopecia
122
Q

What mechanism of resistance do cancer cells have against alkylating agents and cisplatin?

A

Increased DNA repair.

123
Q

What mechanism of resistance do cancer cells have against Bleomycin, Cisplatin, and the Anthracyclines?

A

Formation of trapping agents.

124
Q

What mechanism of resistance do cancer cells have against Methotrexate?

A

Changes in target enzymes.

125
Q

What mechanism of resistance do cancer cells have against the purine and pyrimidine antimetabolites?

A

Decreased activation of prodrugs and inactivation of anticancer drugs.

126
Q

What mechanism of resistance do cancer cells have against Bleomycin and Vincristine?

A

Decreased drug accumulation via increased expression of MDR1 for the cell surface glycoprotein P-glycoprotein which is involved in the accelerated efflux of the drugs.

127
Q

What is tumor lysis syndrome?

A

An oncologic emergency that is caused by massive tumor cell lysis and the release of large amounts of potassium, phosphate, and uric acid into the systemic circulation ;eading to deposition of uric acid and/or calcium phosphate crystals in the renal tubules and acute kidney injury, oliguria, or anuria.

128
Q

What are some risk factors for tumor lysis syndrome?

A

Burkitt lymphoma and ALL.

129
Q

What agent is used to treat tumor lysis syndrome?

A

Rasburicase with correction of electrolyte abnormalities.

Also Allopurinol and febuxostat.

130
Q

What can be used prophylactically for tumor lysis syndrome?

A

IV hydration and urinary alkalinization.

131
Q

What is the MOA of Rasburicase?

A

Causes a reaction with an enzyme that turns uric acid into the inactive substance Allantoin which reduces uric acid levels.

MOD II (8 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions