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Pharmacology Unit 1 > Drugs > Flashcards

Drugs Flashcards

1
Q

Mechlorethamine (Mustargen) (1)

A

Nitrogen mustard Alkylating agent; spontaneous conversion to active metabolites in body fluids or enzymatically converted in liver

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2
Q

Mechlorethamine (Mustargen) (2)

A

Hodgkin’s disease, topically for treatment of cutaneous T-cell lymphoma

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3
Q

Mechlorethamine (Mustargen) (3)

A

Severe nausea and vomiting, myelosuppression (leucopenia, thrombocytopenia)

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4
Q

Cyclophosphamide (Cytoxan) 1

A

Nitrogen mustard Alkylating agent; conversion by hepatic cytochrome P450 to active metabolite phosphoramide mustard

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5
Q

Cyclophosphamide (Cytoxan) 2

A

Most widely used alkylating agent (broad clinical spectrum); singly or in combination for ALL, CLL, non-Hodgkin’s lymphoma, and breast, lung, and ovarian cancer

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6
Q

Cyclophosphamide (Cytoxan) 3

A

Hemorrhagic cystitis (bladder irritation) due to acrolein (toxic drug metabolite); adequate hydration and administration of MESNA (2-mercaptoethane sulfonate) minimizes problem

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7
Q

Ifosfamide (Ifex) 1

A

Nitrogen mustard Alkylating agent; conversion by hepatic cytochrome P450 to active metabolite phosphoramide mustard

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8
Q

Ifosfamide (Ifex) 2

A

Sarcoma and testicular cancer

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9
Q

Ifosfamide (Ifex) 3

A

Hemorrhagic cystitis (bladder irritation) due to acrolein (toxic drug metabolite); adequate hydration and administration of MESNA (2-mercaptoethane sulfonate) minimizes problem

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10
Q

Carmustine (Gliadel) 1

A

Nitrosoureas Alkylating agent

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11
Q

Carmustine (Gliadel) 2

A

Brain tumors (cross blood-brain barrier)

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12
Q

Carmustine (Gliadel) 3

A

Renal toxicity, pulmonary fibrosis

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13
Q

Lomustine (Ceenu) 1

A

Nitrosoureas Alkylating agent

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14
Q

Lomustine (Ceenu) 2

A

Brain tumors (cross blood-brain barrier)

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15
Q

Lomustine (Ceenu) 3

A

Renal toxicity, pulmonary fibrosis

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16
Q

Dacarbazine (DTIC) 1

A

Triazenes Alkylating agent; prodrug activated by liver cytochromes

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17
Q

Dacarbazine (DTIC) 2

A

Part of ABVD for Hodgkin’s disease; also, malignant melanoma

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18
Q

Dacarbazine (DTIC) 3

A

None

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19
Q

Procarbazine (Matulane) 1

A

Triazenes Alkylating agent; forms free radicals

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20
Q

Procarbazine (Matulane) 2

A

Hodgkin’s lymphoma

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21
Q

Procarbazine (Matulane) 3

A

May cause leukemia

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22
Q

Temozolomide (Temodar) 1

A

Triazenes Alkylating agent; nonenzymatic conversion to methylhydrazine at physiologic pH

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23
Q

Temozolomide (Temodar) 2

A

Malignant gliomas

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24
Q

Temozolomide (Temodar) 3

A
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25
Q

Cisplatin (Platinol) 1

A

Platinum analogs Alkylating agents that do not form carbonium ion intermediates or formally alkylate DNA; covalently bind nucleophilic sites on DNA (e.g., guanine N7); converted to active cytotoxic forms by reacting with water to form (+)charged, hydrated intermediates that react with DNA guanine, forming inter- and intrastand cross-links

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26
Q

Cisplatin (Platinol) 2

A

Testicular, ovarian, cervical, and bladder cancers; also useful in treatment of head and neck cancer, and lung carcinoma

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27
Q

Cisplatin (Platinol) 3

A

Nephrotoxicity, ototoxicity, peripheral motor and sensory neuropathy at high doses

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28
Q

Carboplatin (Paraplatin) 1

A

Platinum analogs Alkylating agents that do not form carbonium ion intermediates or formally alkylate DNA; covalently bind nucleophilic sites on DNA (e.g., guanine N7); converted to active cytotoxic forms by reacting with water to form (+)charged, hydrated intermediates that react with DNA guanine, forming inter- and intrastand cross-links

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29
Q

Carboplatin (Paraplatin) 2

A

Ovarian cancer

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30
Q

Carboplatin (Paraplatin) 3

A
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31
Q

Oxaliplatin (Eloxatin) 1

A

Platinum analogs Alkylating agents that do not form carbonium ion intermediates or formally alkylate DNA; covalently bind nucleophilic sites on DNA (e.g., guanine N7); converted to active cytotoxic forms by reacting with water to form (+)charged, hydrated intermediates that react with DNA guanine, forming inter- and intrastand cross-links

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32
Q

Oxaliplatin (Eloxatin) 2

A

Gastric and colorectal cancer

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33
Q

Oxaliplatin (Eloxatin) 3

A

Peripheral sensory neuropathy (cold-induced)

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34
Q

Methotrexate (Trexall) 1

A

Folate analogs Inhibits dihydrofolate reductase (DHFR), which converts dietary folate to tetrahydrofolate (THF) needed for thymidine and purine synthesis; given orally or intrathecally

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35
Q

Methotrexate (Trexall) 2

A

Childhood ALL and choriocarcinoma; combination therapy for Burkitt’s lymphoma and carcinomas of breast, ovary, head and neck, and bladder; administered intrathecally for meningeal leukemia and meningeal metastases of tumors (can’t cross BBB); high-dose for osteosarcoma

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36
Q

Methotrexate (Trexall) 3

A

Renal toxicity (crystallization in urine at high doses), hepatotoxicity (long-term, fibrosis/cirrhosis), reproductive (defective oogenesis or spermatogenesis, abortion)

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37
Q

Pemetrexed (Alimta) 1

A

Folate analogs Polyglutamate forms that inhibit THF-dependent enzymes (e.g., DHFR, TS); metabolized to polyglutamate forms that inhibit THF-dependent enzymes (e.g., DHFR, thymidylate synthase (TS))

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38
Q

Pemetrexed (Alimta) 2

A

Colon cancer, mesothelioma, non-small cell lung cancer, pancreatic cancer

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39
Q

Pemetrexed (Alimta) 3

A
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40
Q

5-Fluorouracil (5-FU, Carac) 1

A

Pyramidine analogs 5-FU is converted to active metabolites: 5-FdUMP inhibits TS; 5-FdUTP incorporates into RNA & interferes with RNA function; prodrug ribosylated and phophosrylated into 5-FdUMP

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41
Q

5-Fluorouracil (5-FU, Carac) 2

A

Combination therapy for breast, colorectal, gastric, head and neck, cervical and pancreatic cancer; topically for basal cell carcinoma

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42
Q

5-Fluorouracil (5-FU, Carac) 3

A

Hand-foot syndrome (erythema, sensitivity of palms and soles), cardiac toxicity (acute chest pains)

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43
Q

Cytarabine (AraC, Depocyt) 1

A

Pyramidine analogs Ara-C converted by deoxycytidine kinase to Ara-CMP –> Ara-CTP; terminates DNA synthesis as Ara-CTP

44
Q

Cytarabine (AraC, Depocyt) 2

A

AML (most effective treatment), ALL and blast phase CML

45
Q

Cytarabine (AraC, Depocyt) 3

A
46
Q

Gemcitabine (dFdC, Gemzar) 1

A

Pyramidine analogs Converted to active metabolites: dFdCDP inhibits ribonucleotide reductase (lowers deoxyribonucleotide); dFdCTP incorporates into DNA, terminating DNA synthesis

47
Q

Gemcitabine (dFdC, Gemzar) 2

A

Pancreatic cancer; effective against non-small cell lung cancer, ovarian, bladder, esophageal, and head and neck cancer

48
Q

Gemcitabine (dFdC, Gemzar) 3

A
49
Q

6-Mercaptopurine (Purinethol) 1

A

Purine analogs (antimetabolites) Prodrug metabolized by hypoxanthine-guanine phosphoribosyl transferase (HGPRT) to 6-thioinosinic acid (TIMP); TIMP inhibits first step of de novo purine base synthesis and the formation of AMP and xanthinylic acid from inosinic acid, reducing purine levels. As well, TIMP is converted to thio-guanine ribonucleotides, inhibiting DNA and RNA synthesis

50
Q

6-Mercaptopurine (Purinethol) 2

A

Maintain remission in acute ALL

51
Q

6-Mercaptopurine (Purinethol) 3

A

Hepatotoxicity in prolonged use

52
Q

Dactinomycin (Actinomycin D, Cosmegen) 1

A

Intercalates G-C base pairs of DNA, interfering with DNA-dependant RNA polymerase; also causes ssDNA breaks

53
Q

Dactinomycin (Actinomycin D, Cosmegen) 2

A

Pediatric tumors (Wilms’ tumor, rhabdomyosarcoma Ewing’s sarcoma); choriocarcinoma in women

54
Q

Dactinomycin (Actinomycin D, Cosmegen) 3

A

Hematopoietic suppression with pancytopenia

55
Q

Daunorubicin (Cerubidine) 1

A

Anthracyclines Intercalate between DNA base pairs and donate electrons to O2 to form superoxide; superoxide reacts with itself to form H2O2 –> cleaved in the presence of Fe to form OH radical, which cleaves DNA

56
Q

Daunorubicin (Cerubidine) 2

A

AML

57
Q

Daunorubicin (Cerubidine) 3

A

Irreversible dose-dependent cardiotoxicity; alopecia

58
Q

Idarubicin (Idamycin) 1

A

Anthracyclines Intercalate between DNA base pairs and donate electrons to O2 to form superoxide; superoxide reacts with itself to form H2O2 –> cleaved in the presence of Fe to form OH radical, which cleaves DNA

59
Q

Idarubicin (Idamycin) 2

A

AML

60
Q

Idarubicin (Idamycin) 3

A

Irreversible dose-dependent cardiotoxicity; alopecia

61
Q

Doxorubicin (Adriamicin, Doxil) 1

A

Anthracyclines Intercalate between DNA base pairs and donate electrons to O2 to form superoxide; superoxide reacts with itself to form H2O2 –> cleaved in the presence of Fe to form OH radical, which cleaves DNA

62
Q

Doxorubicin (Adriamicin, Doxil) 2

A

Sarcomas, breast and lung carcinomas, malignant lymphomas

63
Q

Doxorubicin (Adriamicin, Doxil) 3

A

Irreversible dose-dependent cardiotoxicity; alopecia

64
Q

Epirubicin (Ellence) 1

A

Anthracyclines Intercalate between DNA base pairs and donate electrons to O2 to form superoxide; superoxide reacts with itself to form H2O2 –> cleaved in the presence of Fe to form OH radical, which cleaves DNA

65
Q

Epirubicin (Ellence) 2

A

Metastatic breast cancer, gastric cancer

66
Q

Epirubicin (Ellence) 3

A

Irreversible dose-dependent cardiotoxicity; alopecia

67
Q

Bleomycin (Blenoxane) 1

A

Acts in G2 phase of cell cycle. Binds to DNA, producing ss- and dsDNA breaks

68
Q

Bleomycin (Blenoxane) 2

A

Combination therapy for testicular tumors or Hodgkin’s disease; squamous cell carcinomas and lymphomas

69
Q

Bleomycin (Blenoxane) 3

A

Pulmonary toxicity (pulmonary fibrosis); cutaneous toxicity (hyperpigmentation, hyperkeratosis, erythema); hyperthermia

70
Q

Vinblastine (Velban) 1

A

Vinca alkaloids Block tubulin polymerization into microtubules

71
Q

Vinblastine (Velban) 2

A

Metastatic testicular tumors (with bleomycin, cisplatin); component of ABVD used for Hodgkin’s disease

72
Q

Vinblastine (Velban) 3

A
73
Q

Vincristine (Oncovin) 1

A

Vinca alkaloids Block tubulin polymerization into microtubules

74
Q

Vincristine (Oncovin) 2

A

Childhood ALL (with glucocorticoids); Hodgkin’s and non-Hodgkin’s lymphomas

75
Q

Vincristine (Oncovin) 3

A

Dose-limiting neurotoxicity (peripheral neuropathy)

76
Q

Paclitaxel/Docetaxel 1

A

Taxanes Block microtubule depolymerization into tubulin

77
Q

Paclitaxel/Docetaxel 2

A

Metastatic breast, ovarian, lung, and head and neck cancers

78
Q

Paclitaxel/Docetaxel 3

A

Peripheral neuropathy

79
Q

Etoposide/Tenoposide 1

A

Epipodophyllotoxins Inhibits topoisomerase II

80
Q

Etoposide/Tenoposide 2

A

Testicular carcinoma, lung cancer, and non-Hodgkin’s lymphoma for Etoposide. ALL for Tenoposide

81
Q

Etoposide/Tenoposide 3

A

Dose-limiting myelosuppression (neutropenia), oral mucositis

82
Q

Irinotecan/Topotecan 1

A

Camptothecin analogs Inhibits topoisomerase I

83
Q

Irinotecan/Topotecan 2

A

Ovarian and small cell lung cancer for Topotecan. Colorectal, cervical, and brain tumors in addition for Irinotecan

84
Q

Irinotecan/Topotecan 3

A

Severe neutropenia, severe diarrhea

85
Q

Prednisone (Meticorten) 1

A

Glucocorticoids Inhibit mitosis in lymphocytes

86
Q

Prednisone (Meticorten) 2

A

ALL; combination for Hodgkin’s, non-Hodkin’s, multiple myeloma, and CLL

87
Q

Prednisone (Meticorten) 3

A
88
Q

Dexamethasone (Decadron) 1

A

Glucocorticoids Inhibit mitosis in lymphocytes

89
Q

Dexamethasone (Decadron) 2

A

Reduces edema in brain and spinal cord tumors with radiation therapy

90
Q

Dexamethasone (Decadron) 3

A
91
Q

Tamoxifen (Soltamox) 1

A

Selective estrogen-receptor modulators (SERMs) Competes with estradiol for binding to estrogen receptor

92
Q

Tamoxifen (Soltamox) 2

A

ER-positive breast cancer, or as adjuvant therapy following primary breast tumor excision; prevention of breast cancer in high-risk patients

93
Q

Tamoxifen (Soltamox) 3

A

Hot flushes, hair loss; increased risk of endometrial cancer; increased risk of thromboembolic events

94
Q

Fulvestrant (Faslodex) 1

A

Selective estrogen-receptor downregulators (SERDs) Binds with much higher affinity (>100-fold) to estrogen receptor than tamoxifen, inhibiting dimerization, increasing degradation, and reducing overall ER levels

95
Q

Fulvestrant (Faslodex) 2

A

Posmenopausal women with ER-positive metastatic breast cancer

96
Q

Fulvestrant (Faslodex) 3

A
97
Q

Aminoglutethamide/Anastrozole/Letrozole/Exemestane 1

A

Aromatase inhibitors Inhibits function of aromatase

98
Q

Aminoglutethamide/Anastrozole/Letrozole/Exemestane 2

A

ER-positive breast cancer in postmenopausal women. Aminoglutethamide weak. Anastrozole front line treatment

99
Q

Aminoglutethamide/Anastrozole/Letrozole/Exemestane 3

A

None except significant for aminoglutethamide

100
Q

Leuprolide/Goserelin 1

A

GnRH analogs Binds GnRH receptor; inhibits release of FSH & LH

101
Q

Leuprolide/Goserelin 2

A

Androgen ablation therapy, along with AR blockers

102
Q

Leuprolide/Goserelin 3

A
103
Q

Flutamide/Bicalutamide 1

A

Nonsteroidal androgen-receptor blockers Competes with androgen for AR binding

104
Q

Flutamide/Bicalutamide 2

A

Androgen ablation therapy, along with GnRH analogs

105
Q

Flutamide/Bicalutamide 3

A

–

Pharmacology Unit 1 (1 decks)

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