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Pharmacology > Chemotherapeutics > Flashcards

Chemotherapeutics Flashcards

1
Q

Nitrogen mustards?

A

Mechlorethamine, Cyclophosphamide, Ifosfamide

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2
Q

Cause hemorrhagic cystitis?

A

Cyclophosphamide & Ifosfamide

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3
Q

Toxic metabolite in hemorrhagic cystitis?

A

Acrolein

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4
Q

Use to counter hemorrhagic cystitis?

A

Hydration and MESNA

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5
Q

Used for Hodgkin’s disease and topically for cutaneous T-cell lymphoma?

A

Mechlorethamine

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6
Q

Rarely used alkylating agent due to sterility?

A

Mechlorethamine

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7
Q

Alkylating agents that cross BBB?

A

Nitrosureas (Carmustine & Lomustine)

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8
Q

Carmustine & Lomustine side effects?

A

Renal toxicity, Pulmonary Fibrosis

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9
Q

Triazines?

A

Dacarbazine, Temozolomide

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10
Q

Treats malignant gliomas?

A

Temozolomide

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11
Q

Dacarbazine treats?

A

Hodgkin’s (ABVD), malignant melanoma

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12
Q

Cisplatin side effects?

A

Ototoxicity, nephrotoxicity, sensory neuropathy

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13
Q

Platinum analogs?

A

Cisplatin, Carboplatin, Oxaliplatin

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14
Q

Cold-induced peripheral sensory neuropathy?

A

Oxaliplatin

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15
Q

Oxaliplatin treats?

A

Gastric and colorectal cancer

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16
Q

Platinum analogs that treats ovarian cancer?

A

Cisplatin and Carboplatin

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17
Q

Folate analogs?

A

Methotrexate and Pemetrexed

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18
Q

Treats colon cancer, mesothelioma, non-small cell lung cancer, pancreatic cancer?

A

Pemetrexed

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19
Q

Used to prevent toxic effects of methotrexate?

A

Leucovorin

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20
Q

Methotrexate inhibits this enzyme?

A

Dihydrofolate Reductase

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21
Q

Side effects of methotrexate?

A

Renal toxicity, hepatotoxicity, reproductive toxicity

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22
Q

Inhibits THF-dependent enzymes (DHFR, TS) as a polyglutamate form?

A

Pemetrexed

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23
Q

Methotrexate treats?

A

Childhood ALL, choriocarcinoma, head & neck, Burkitt’s, breast, bladder, ovary, osteosarcoma, meningeal leukemia and meningeal metastases

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24
Q

Oral form of 5-Fluorouracil?

A

Capecitabine

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25
Q

Hand-foot syndrome?

A

5-Fluorouracil

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26
Q

Pyrimidine analogs?

A

5-Fluorouracil, cytarabine, gemcitabine

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27
Q

Most effective treatment of AML?

A

Cytarabine

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28
Q

Treats AML, ALL, blast phase CML?

A

Cytarabine

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29
Q

Gemcitabine: S-phase specific?

A

No.

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30
Q

5-Fluorouracil used topically for?

A

Basal Cell Carcinoma

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31
Q

Gemcitabine treats?

A

Pancreatic, non-small cell lung, ovarian, bladder, esophageal, head and neck

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32
Q

Treats esophageal cancer?

A

Gemcitabine

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33
Q

Maintains remission in acute ALL?

A

6-Mercaptopurine

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34
Q

Drug interaction with alopurinol?

A

6-Mercaptopurine

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35
Q

6-Mercaptopurine metabolized by what enzyme to what, to inhibit what?

A

HGPRT to TIMP, inhibits first step of de novo purine synthesis and formation of AMP and xanthinylic acid frominosinic acid

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36
Q

Derived from strains of Streptomyces?

A

DNA intercalating agents

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37
Q

Cardio-protective against anthracyclines?

A

Dexrazoxane

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38
Q

Dose-dependent cardiotoxicity?

A

Anthracyclines

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39
Q

Dactinomycin treats?

A

Choriocarcinoma, rhabdomyosarcoma, Ewing’s sarcoma, Wilms’ tumor

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40
Q

Anthracyclines that treat AML?

A

Idarubicin, Daunorubicin

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41
Q

Form reactive hydroxyl species?

A

Anthracyclines

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42
Q

DNA intercalating agent that causes pancytopenia?

A

Dactinomycin

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43
Q

Lung, breast, sarcomas, malignant lymphomas treatable with?

A

Doxorubicin

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44
Q

Anthracycline that treats metastatic breast and gastric cancer?

A

Epirubicin

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45
Q

DNA intercalating agent that acts in G2?

A

Bleomycin

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46
Q

Pulmonary, cutaneous toxicity with hyperthermia?

A

Bleomycin

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47
Q

Bleomycin treats?

A

Testicular tumors, Hodgkin’s disease, squamous cell carcinomas, lymphomas

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48
Q

Vinca alkaloids?

A

Vinblastine, Vincristine

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49
Q

Block depolymerization of microtubules?

A

Taxanes (Paclitaxel, Docetaxel)

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50
Q

Microtubule inhibitor side effect?

A

Peripheral neuropathies (except vinblastine)

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51
Q

With bleomycin and cysplatin to treat what?

A

Vinblastine, metastatic testicular tumor

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52
Q

Paclitaxel treats?

A

Metastatic breast, ovarian, lung, head and neck?

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53
Q

Docetaxal treats but paclitexal does not?

A

Hormone refractory prostate cancer

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54
Q

Topoisomerase inhibitors classes?

A

Epipodophyllotoxins (II), Capthothecin analogs (I)

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55
Q

Treats advanced colorectal cancer, brain, ovarian and lung cancer?

A

Irinotecan

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56
Q

Topoisomerase II inhibitors?

A

Etoposide, Teniposide

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57
Q

Etoposide treats?

A

Testicular carcinoma, lung cancer, non-Hodgkin’s

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58
Q

Epipodophyllotoxin that treats ALL?

A

Teniposide

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59
Q

Camptothecin analog that treats ovarian and small cell lung cancer?

A

Topotecan

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60
Q

Glucocorticoids?

A

Prednisone, Dexamathasone

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61
Q

Reduces edema in brain and spinal cord tumors?

A

Dexamethasone

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62
Q

Prednisone treats?

A

ALL, CLL, multiple myeloma, lymphomas

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63
Q

SERM?

A

Tamoxifen

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64
Q

Tamoxifen competes with?

A

Estradiol

65
Q

Fulvestrant is?

A

Selective ER Downregulator

66
Q

Aromatase inhibitor with significant toxicity?

A

Aminoglutethamide

67
Q

3rd generation aromatise inhibitor?

A

Anastrazole

68
Q

Leuprolide and Goserelin?

A

GnRH analogs

69
Q

Used in androgen ablation therapy with GnRH analogs?

A

Androgen-receptor blockers (Flutamide, Bicalutamide)

70
Q

Flutamide and what are AR blockers?

A

Bicalutamide

71
Q

Imatinib treats?

A

CML, GIST

72
Q

Treat imatinib-resistant CML?

A

Dasatinib, Nilotinib

73
Q

TKI with QT prolongation?

A

Nilotinib

74
Q

Pulmonary arterial HTN from this TKI?

A

Dasatinib

75
Q

Inhibit EGFR may help?

A

Non-small lung cancer

76
Q

Treat non-small lung cancer with these EGFR inhibitors?

A

Gefitinib, Erlotinib

77
Q

CD20 B-cell antibody?

A

Rituximab

78
Q

Rituximab side effects?

A

TLS, PML, mucocutaneous reactions

79
Q

Refractory, relapsed Non-Hodgkin’s?

A

Rituximab

80
Q

Trastuzumab treats?

A

HER2/neu overexpressing metastatic breast cancer, gastric, GE junction cancers

81
Q

Combined with taxanes to treat breast cancer?

A

Trastuzumab

82
Q

Trastuzumab enhances cardiotoxicity of?

A

Doxorubicin

83
Q

Trastuzumab conjugated with?

A

Emtansine (Ado-trastuzumab-emtansine)

84
Q

EGFR1 inhibitor?

A

Cetuximab

85
Q

Treasts EGFR-positive metastatic colorectal cancer and SCCHN?

A

Cetuximab

86
Q

RIsk of pulmonary embolism?

A

Cetuximab

87
Q

Cytotoxic T-Lymphocyte Antigen 4 inhibitor that stimulates the immune system?

A

Ipilimumab

88
Q

Oncogenic kinase of melanoma?

A

BRAF

89
Q

BRAF inhibitors?

A

Vemurafenib, Dabrafenib

90
Q

MEK inhibitor?

A

Trametinib

91
Q

Risk of cutaneous SCC, keratoacanthoma, new primary cutaneous melanoma?

A

Vemurafenib, Dabrafenib

92
Q

Serious febrile reactions, hyperglycemia and male infertility?

A

Dabrafenib

93
Q

Skin toxicities, female infertility, cardiomyopathy and retinal disorders?

A

Trametinib

94
Q

Relapsed AP:?

A

Arsenic Trioxide

95
Q

Inhibits ribonucleoside diphosphate reductase?

A

Hydroxyurea

96
Q

Lekocyte Activation Syndrome?

A

Retinoids

97
Q

Treats PV, ET and SC?

A

Hydroxyurea

98
Q

Multiple myeloma and myelodysplastic syndromes?

A

Thalidomide

99
Q

Interferons treat?

A

Hairy-cell leukemia, CML, AIDS-related Kaposi’s sarcoma

100
Q

Blocks LAS?

A

Corticosteroids

101
Q

FEC?

A

5-fluorouracil, epirubicin, cyclophosphamide

102
Q

CMF?

A

Cyclophosphamide, methotrexate, 5-fluorouracil

103
Q

MOPP?

A

Mechlorethamine, vincristine (oncovine), procarbazine, prednisone

104
Q

ABVD?

A

Doxorubicin (adiamycin), bleomycin, vinblastine, dacarbazine

105
Q

CHOP?

A

Cyclophosphamide, hydroxydoxorubicin, vincristine (oncovine), prednisone

106
Q

Pyrimidine analog given IV?

A

5-Fluorouracil

107
Q

Dacarbazine: oral or IV?

A

IV

108
Q

Temozolomide: oral or IV

A

Oral

109
Q

Nitrogen mustards with long half-lives?

A

Cyclophosphamide, Ifosfamide

110
Q

List the CCNS and CCS chemotherapeutics.

A

CCNS: Alkylating agents, DNA intercalating agents (except bleomycin–G2). CCS: Antimetabolites (S-phase) (except gemcitabine), MT Inhibitors (M-phase), Topoisomerase inhibitors

111
Q

Treat brain tumors?

A

Carmustine, Lomustine

112
Q

Dacarbazine class?

A

Triazene

113
Q

Temozolomide class?

A

Triazene

114
Q

Most widely used alkylating agent?

A

Cyclophospamide

115
Q

Cyclophosphamide treats?

A

ALL, CLL, breast, lung, ovarian, Non-Hodgkin’s

116
Q

Cisplatin treats?

A

Testicular, ovarian, cervical, bladder, H & N, lung

117
Q

Sarcoma and testicular cancer?

A

Ifosfamide

118
Q

5-Fluorouracil treats?

A

Breast, cervical, gastric, H & N, colorectal, pancreatic

119
Q

Non-Anthracycline DNA Intercalating agents?

A

Dactinomycin, Bleomycin

120
Q

Vinca alkaloid that treats Childhood ALL with glucocorticoids?

A

Vincristine

121
Q

Microtubule inhibitor that treats Hodgkin’s and non-hodgkin’s?

A

Vincristine

122
Q

Bicalutamide class?

A

AR-blocker

123
Q

GnRH analogs?

A

Leuprolide, Goserelin

124
Q

Aromotase inhibitors?

A

Aminoglutethamide, Anastrazole

125
Q

Serine/Threonine Kinase inhibitors?

A

Vemurafenib, Dabrafenib

126
Q

Hypersensitivity, ventricular dysfunction, CHF?

A

Trastuzamab

127
Q

Uveitis, Iritis?

A

Dabrafenib

128
Q

AKA adriamycin?

A

Doxorubicin

129
Q

AKA oncovine?

A

Vincristine

130
Q

Characteristics of LAS?

A

Fever, weight gain, respiratory distress, serosal effusion, renal failure

131
Q

Important side effect of alkylating agents?

A

Leukemogenic

132
Q

Resistance to alkylating agents?

A

Decreased permeability or uptake; Increased catabolism; Increased DNA repair; Increased glutathione (inactivates alkylating agents)

133
Q

Temozolomide converted to what at physiological pH?

A

Methylhydrazine

134
Q

Can be used with myelosuppressive drugs due to limited bone marrow toxicity?

A

Vincristine

135
Q

Treats refractory and relapsed follicular lymphomas?

A

Rituximab

136
Q

Proved superior to MOPP and CHOP in Phase III trials for Hodgkin’s?

A

ABVD

137
Q

Breast cancer combinations?

A

FEC, CMF

138
Q

MOPP usually for?

A

Lymphomas

139
Q

Combined with cytarabine to treat AML?

A

Anthracyclines (EXCEPT if cardiotoxicity concerns–use Mitoxantrone)

140
Q

Activated by Cytochrome p450?

A

Cyclophasphamide, Ifosfamide

141
Q

Is Dacarbazine a prodrug?

A

Yes, activated by the liver.

142
Q

How is Temozolomide activated?

A

Nonenzymatic conversion to methylhydrazine at physiological pH

143
Q

5-FU mxn of action?

A

Prodrug. 5-dUMP inhibits TS. 5-dUTP interferes with RNA.

144
Q

Most severe side effect of cytarabine?

A

Severe myelosuppression

145
Q

Cytarabine mxn of action?

A

Ara-C to Ara-CMP via deoxycytidine kinase. Terminates DNA as Ara-CTP.

146
Q

Gemcitabine mxn of action?

A

Prodrug. dFdCDP inhibits ribonucleotide reductase. dFdCTP terminates DNA synthesis.

147
Q

First-line against pancreatic cancer?

A

Gemcitabine

148
Q

Antimetabolite with hepatotoxicity in prolonged use?

A

6-Mercaptopurine

149
Q

Dactinomycn mxn of action?

A

Intercalates G-C bps, interfering with DNA dependent RNA polymerase. Causes ssDNA breaks.

150
Q

Benefit of bleomycin side effects?

A

Minimaly myelo- and immunosuppressive.

151
Q

Bleomycin does what in G2?

A

Binds to DNA, producing ss and ds breaks.

152
Q

Contraindications of Nilotinib?

A

Long QT, hypokalemia, hypomagnesemia

153
Q

Arthralgia, fatigue, photosensitivity, nausea, alopecia, diarrhea, long QT?

A

Vemurafenib

154
Q

Allergies, sudden cardiac death, dermatologic problems, infections, renal failure, electrolyte abnormalities, pulmonary embolism, intersititial pneumonitis?

A

Cetuximab

155
Q

Retinoids treat, combined with?

A

APL, anthracyclines (or Arsenic Trioxide if unable to handle anthracyclines, although trend is toward ATRA + AT)

156
Q

Major side effect of Ado-trastuzamab-emtansine?

A

Hepatotoxicity, ventricular dysfunction

157
Q

Cetuximab approved in combination with?

A

5-FU, Irinotecan, Leucovorin

158
Q

Serious skin toxicity as most important side effect?

A

Trametinib

159
Q

Methotrexate effect on bone marrow?

A

Severe suppression

Pharmacology (46 decks)

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