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
2
Q
Mechlorethamine (Mustargen) (2)
A
Hodgkin’s disease, topically for treatment of cutaneous T-cell lymphoma
3
Q
Mechlorethamine (Mustargen) (3)
A
Severe nausea and vomiting, myelosuppression (leucopenia, thrombocytopenia)
4
Q
Cyclophosphamide (Cytoxan) 1
A
Nitrogen mustard Alkylating agent; conversion by hepatic cytochrome P450 to active metabolite phosphoramide mustard
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
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
7
Q
Ifosfamide (Ifex) 1
A
Nitrogen mustard Alkylating agent; conversion by hepatic cytochrome P450 to active metabolite phosphoramide mustard
8
Q
Ifosfamide (Ifex) 2
A
Sarcoma and testicular cancer
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
10
Q
Carmustine (Gliadel) 1
A
Nitrosoureas Alkylating agent
11
Q
Carmustine (Gliadel) 2
A
Brain tumors (cross blood-brain barrier)
12
Q
Carmustine (Gliadel) 3
A
Renal toxicity, pulmonary fibrosis
13
Q
Lomustine (Ceenu) 1
A
Nitrosoureas Alkylating agent
14
Q
Lomustine (Ceenu) 2
A
Brain tumors (cross blood-brain barrier)
15
Q
Lomustine (Ceenu) 3
A
Renal toxicity, pulmonary fibrosis
16
Q
Dacarbazine (DTIC) 1
A
Triazenes Alkylating agent; prodrug activated by liver cytochromes
17
Q
Dacarbazine (DTIC) 2
A
Part of ABVD for Hodgkin’s disease; also, malignant melanoma
18
Q
Dacarbazine (DTIC) 3
A
None
19
Q
Procarbazine (Matulane) 1
A
Triazenes Alkylating agent; forms free radicals
20
Q
Procarbazine (Matulane) 2
A
Hodgkin’s lymphoma
21
Q
Procarbazine (Matulane) 3
A
May cause leukemia
22
Q
Temozolomide (Temodar) 1
A
Triazenes Alkylating agent; nonenzymatic conversion to methylhydrazine at physiologic pH
23
Q
Temozolomide (Temodar) 2
A
Malignant gliomas
24
Q
Temozolomide (Temodar) 3
A
25
Cisplatin (Platinol) 1
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
26
Cisplatin (Platinol) 2
Testicular, ovarian, cervical, and bladder cancers; also useful in treatment of head and neck cancer, and lung carcinoma
27
Cisplatin (Platinol) 3
Nephrotoxicity, ototoxicity, peripheral motor and sensory neuropathy at high doses
28
Carboplatin (Paraplatin) 1
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
29
Carboplatin (Paraplatin) 2
Ovarian cancer
30
Carboplatin (Paraplatin) 3
---
31
Oxaliplatin (Eloxatin) 1
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
32
Oxaliplatin (Eloxatin) 2
Gastric and colorectal cancer
33
Oxaliplatin (Eloxatin) 3
Peripheral sensory neuropathy (cold-induced)
34
Methotrexate (Trexall) 1
Folate analogs Inhibits dihydrofolate reductase (DHFR), which converts dietary folate to tetrahydrofolate (THF) needed for thymidine and purine synthesis; given orally or intrathecally
35
Methotrexate (Trexall) 2
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
36
Methotrexate (Trexall) 3
Renal toxicity (crystallization in urine at high doses), hepatotoxicity (long-term, fibrosis/cirrhosis), reproductive (defective oogenesis or spermatogenesis, abortion)
37
Pemetrexed (Alimta) 1
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))
38
Pemetrexed (Alimta) 2
Colon cancer, mesothelioma, non-small cell lung cancer, pancreatic cancer
39
Pemetrexed (Alimta) 3
---
40
5-Fluorouracil (5-FU, Carac) 1
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
41
5-Fluorouracil (5-FU, Carac) 2
Combination therapy for breast, colorectal, gastric, head and neck, cervical and pancreatic cancer; topically for basal cell carcinoma
42
5-Fluorouracil (5-FU, Carac) 3
Hand-foot syndrome (erythema, sensitivity of palms and soles), cardiac toxicity (acute chest pains)
43
Cytarabine (AraC, Depocyt) 1
Pyramidine analogs Ara-C converted by deoxycytidine kinase to Ara-CMP --> Ara-CTP; terminates DNA synthesis as Ara-CTP
44
Cytarabine (AraC, Depocyt) 2
AML (most effective treatment), ALL and blast phase CML
45
Cytarabine (AraC, Depocyt) 3
---
46
Gemcitabine (dFdC, Gemzar) 1
Pyramidine analogs Converted to active metabolites: dFdCDP inhibits ribonucleotide reductase (lowers deoxyribonucleotide); dFdCTP incorporates into DNA, terminating DNA synthesis
47
Gemcitabine (dFdC, Gemzar) 2
Pancreatic cancer; effective against non-small cell lung cancer, ovarian, bladder, esophageal, and head and neck cancer
48
Gemcitabine (dFdC, Gemzar) 3
---
49
6-Mercaptopurine (Purinethol) 1
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
6-Mercaptopurine (Purinethol) 2
Maintain remission in acute ALL
51
6-Mercaptopurine (Purinethol) 3
Hepatotoxicity in prolonged use
52
Dactinomycin (Actinomycin D, Cosmegen) 1
Intercalates G-C base pairs of DNA, interfering with DNA-dependant RNA polymerase; also causes ssDNA breaks
53
Dactinomycin (Actinomycin D, Cosmegen) 2
Pediatric tumors (Wilms' tumor, rhabdomyosarcoma Ewing's sarcoma); choriocarcinoma in women
54
Dactinomycin (Actinomycin D, Cosmegen) 3
Hematopoietic suppression with pancytopenia
55
Daunorubicin (Cerubidine) 1
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
Daunorubicin (Cerubidine) 2
AML
57
Daunorubicin (Cerubidine) 3
Irreversible dose-dependent cardiotoxicity; alopecia
58
Idarubicin (Idamycin) 1
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
Idarubicin (Idamycin) 2
AML
60
Idarubicin (Idamycin) 3
Irreversible dose-dependent cardiotoxicity; alopecia
61
Doxorubicin (Adriamicin, Doxil) 1
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
Doxorubicin (Adriamicin, Doxil) 2
Sarcomas, breast and lung carcinomas, malignant lymphomas
63
Doxorubicin (Adriamicin, Doxil) 3
Irreversible dose-dependent cardiotoxicity; alopecia
64
Epirubicin (Ellence) 1
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
Epirubicin (Ellence) 2
Metastatic breast cancer, gastric cancer
66
Epirubicin (Ellence) 3
Irreversible dose-dependent cardiotoxicity; alopecia
67
Bleomycin (Blenoxane) 1
Acts in G2 phase of cell cycle. Binds to DNA, producing ss- and dsDNA breaks
68
Bleomycin (Blenoxane) 2
Combination therapy for testicular tumors or Hodgkin's disease; squamous cell carcinomas and lymphomas
69
Bleomycin (Blenoxane) 3
Pulmonary toxicity (pulmonary fibrosis); cutaneous toxicity (hyperpigmentation, hyperkeratosis, erythema); hyperthermia
70
Vinblastine (Velban) 1
Vinca alkaloids Block tubulin polymerization into microtubules
71
Vinblastine (Velban) 2
Metastatic testicular tumors (with bleomycin, cisplatin); component of ABVD used for Hodgkin's disease
72
Vinblastine (Velban) 3
---
73
Vincristine (Oncovin) 1
Vinca alkaloids Block tubulin polymerization into microtubules
74
Vincristine (Oncovin) 2
Childhood ALL (with glucocorticoids); Hodgkin's and non-Hodgkin's lymphomas
75
Vincristine (Oncovin) 3
Dose-limiting neurotoxicity (peripheral neuropathy)
76
Paclitaxel/Docetaxel 1
Taxanes Block microtubule depolymerization into tubulin
77
Paclitaxel/Docetaxel 2
Metastatic breast, ovarian, lung, and head and neck cancers
78
Paclitaxel/Docetaxel 3
Peripheral neuropathy
79
Etoposide/Tenoposide 1
Epipodophyllotoxins Inhibits topoisomerase II
80
Etoposide/Tenoposide 2
Testicular carcinoma, lung cancer, and non-Hodgkin's lymphoma for Etoposide. ALL for Tenoposide
81
Etoposide/Tenoposide 3
Dose-limiting myelosuppression (neutropenia), oral mucositis
82
Irinotecan/Topotecan 1
Camptothecin analogs Inhibits topoisomerase I
83
Irinotecan/Topotecan 2
Ovarian and small cell lung cancer for Topotecan. Colorectal, cervical, and brain tumors in addition for Irinotecan
84
Irinotecan/Topotecan 3
Severe neutropenia, severe diarrhea
85
Prednisone (Meticorten) 1
Glucocorticoids Inhibit mitosis in lymphocytes
86
Prednisone (Meticorten) 2
ALL; combination for Hodgkin's, non-Hodkin's, multiple myeloma, and CLL
87
Prednisone (Meticorten) 3
---
88
Dexamethasone (Decadron) 1
Glucocorticoids Inhibit mitosis in lymphocytes
89
Dexamethasone (Decadron) 2
Reduces edema in brain and spinal cord tumors with radiation therapy
90
Dexamethasone (Decadron) 3
---
91
Tamoxifen (Soltamox) 1
Selective estrogen-receptor modulators (SERMs) Competes with estradiol for binding to estrogen receptor
92
Tamoxifen (Soltamox) 2
ER-positive breast cancer, or as adjuvant therapy following primary breast tumor excision; prevention of breast cancer in high-risk patients
93
Tamoxifen (Soltamox) 3
Hot flushes, hair loss; increased risk of endometrial cancer; increased risk of thromboembolic events
94
Fulvestrant (Faslodex) 1
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
Fulvestrant (Faslodex) 2
Posmenopausal women with ER-positive metastatic breast cancer
96
Fulvestrant (Faslodex) 3
---
97
Aminoglutethamide/Anastrozole/Letrozole/Exemestane 1
Aromatase inhibitors Inhibits function of aromatase
98
Aminoglutethamide/Anastrozole/Letrozole/Exemestane 2
ER-positive breast cancer in postmenopausal women. Aminoglutethamide weak. Anastrozole front line treatment
99
Aminoglutethamide/Anastrozole/Letrozole/Exemestane 3
None except significant for aminoglutethamide
100
Leuprolide/Goserelin 1
GnRH analogs Binds GnRH receptor; inhibits release of FSH & LH
101
Leuprolide/Goserelin 2
Androgen ablation therapy, along with AR blockers
102
Leuprolide/Goserelin 3
---
103
Flutamide/Bicalutamide 1
Nonsteroidal androgen-receptor blockers Competes with androgen for AR binding
104
Flutamide/Bicalutamide 2
Androgen ablation therapy, along with GnRH analogs
105
Flutamide/Bicalutamide 3
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