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Drug Table - Complete Flashcards

1
Q

Alkylating Agents Mechanism

A

Produce strong electrophiles throughcarbonium or ethyleneimonium ionintermediates, which covalently bond viaalkylation of nucleophilic moieties in DNA(mostly N7 position of guanine); Cell CycleNon-Specific (CCNS)

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2
Q

Alkylating Agents Important Side Effects

A

Bone marrow, mucosal toxicity,nausea and vomiting, toxic effectson reproductive systems,increased leukemia risk

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3
Q

Alkylating Agents Miscellaneous

A

Resistance may occur due to:decreased permeability or uptake;increased rates of catabolism;enhanced DNA repair; increasedglutathione production (inactivatesvia conjugation)

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4
Q

List 11 Alkylating Agents

A

Mechlorethamine (Mustargen)Cyclophosphamide (Cytoxan)Ifosfamide (Ifex)Carmustine (Gliadel)Lomustine (Ceenu)Dacarbazine (DTIC)Procarbazine (Matulane)Temozolomide (Temodar)Cisplatin (Platinol)Carboplatin (Paraplatin)Oxaliplatin (Eloxatin)

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5
Q

Mechlorethamine class

A

(Mustargen)Nitrogen mustard

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6
Q

Mechlorethamine mechanism

A

Alkylating agent; spontaneous conversion to active metabolites in body fluids orenzymatically converted in liver

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7
Q

Mechlorethamine Therapeutics

A

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

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8
Q

Mechlorethamine “Other” side effects

A

Severe nausea and vomiting,myelosuppression (leucopenia,thrombocytopenia)

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9
Q

Mechlorethamine Misc

A

Don’t use much anymore due to sterility

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10
Q

Cyclophosphamide(Cytoxan)Class

A

Nitrogen mustard

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11
Q

Cyclophosphamide(Cytoxan)Mechanism

A

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

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12
Q

Cyclophosphamide(Cytoxan)Therapeutics

A

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

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13
Q

Cyclophosphamide(Cytoxan)Important Side Effects

A

Hemorrhagic cystitis (bladderirritation) due to acrolein (toxicdrug metabolite); adequatehydration and administration ofMESNA (2-mercaptoethanesulfonate) minimizes problem

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14
Q

Cyclophosphamide(Cytoxan)”Other” Side Effects

A

Nausea, vomiting,myelosuppression

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15
Q

Cyclophosphamide(Cytoxan)Miscellaneous

A

Relatively long plasma half-life (7-15 hrs); taken orally

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16
Q

Difference between Ifosfamide and Cyclophosphamide

A

TherapeuticsIfos is used for Sarcoma and testicular cancerCyclophosphamide is the most widely used

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17
Q

Carmustine (Gliadel)Lomustine (Ceenu)Class

A

Nitrosoureas

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18
Q

Carmustine (Gliadel)Lomustine (Ceenu)Mechanism

A

Alkylating agent

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19
Q

Carmustine (Gliadel)Lomustine (Ceenu)Therapeutics

A

Brain tumors (cross blood-brain barrier)

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20
Q

Carmustine (Gliadel)Lomustine (Ceenu)Imp Side Effects

A

Renal toxicity, pulmonary fibrosis

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21
Q

Carmustine (Gliadel)Lomustine (Ceenu)Other side effects

A

Profound myelosuppression,severe nausea and vomiting

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22
Q

Dacarbazine (DTIC)class

A

Triazenes

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23
Q

Dacarbazine (DTIC)Mechanism

A

Alkylating agent; prodrug activated by livercytochromes

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24
Q

Dacarbazine (DTIC)Therapeutics

A

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

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25
Q

Dacarbazine (DTIC)”Other” Side Effects

A

Nausea and vomiting,myelosuppression (neutropenia, thrombocytopenia), flu-likesymptoms (fever, fatigue)

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26
Q

Dacarbazine (DTIC)Miscellaneous

A

IV administration

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27
Q

Procarbazine(Matulane)class

A

Triazenes

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28
Q

Procarbazine(Matulane)Mechanism

A

Alkylating agent; forms free radicals

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29
Q

Procarbazine(Matulane)Therapeutics

A

Hodgkin’s lymphoma

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30
Q

Procarbazine(Matulane)Important side effects

A

May cause leukemia

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31
Q

Temozolomide(Temodar)class

A

Triazenes

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32
Q

Temozolomide(Temodar)Mechanism

A

Alkylating agent; nonenzymatic conversionto methylhydrazine at physiologic pH

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33
Q

Temozolomide(Temodar)Therapeutics

A

Malignant gliomas

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34
Q

Temozolomide(Temodar)”Other” Side Effects

A

Nausea and vomiting,myelosuppression (neutropenia,thrombocytopenia), flu-likesymptoms (fever, fatigue)

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35
Q

Temozolomide(Temodar)Miscellaneous

A

Taken orally

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36
Q

Cisplatin (Platinol)class

A

Platinum analogs

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37
Q

Cisplatin (Platinol)Mechanism

A

Alkylating agents that do not formcarbonium ion intermediates or formallyalkylate DNA; covalently bind nucleophilicsites on DNA (e.g., guanine N7); convertedto active cytotoxic forms by reacting withwater to form (+)charged, hydratedintermediates that react with DNA guanine,forming inter- and intrastand cross-links

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38
Q

Cisplatin (Platinol)Therapeutics

A

Testicular, ovarian, cervical, andbladder cancers; also useful intreatment of head and neck cancer,and lung carcinoma

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39
Q

Cisplatin (Platinol)Imp Side Effects

A

Nephrotoxicity, ototoxicity,peripheral motor and sensoryneuropathy at high doses

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40
Q

Cisplatin (Platinol)Other side effects

A

Severe nausea and vomiting,mild to moderatemyelosuppression

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41
Q

Carboplatin(Paraplatin)Class

A

Platinum analogs

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42
Q

Carboplatin(Paraplatin)Mechanism

A

Alkylating agents that do not formcarbonium ion intermediates or formallyalkylate DNA; covalently bind nucleophilicsites on DNA (e.g., guanine N7); convertedto active cytotoxic forms by reacting withwater to form (+)charged, hydratedintermediates that react with DNA guanine,forming inter- and intrastand cross-links

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43
Q

Carboplatin(Paraplatin)Therapeutics

A

Ovarian cancer

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44
Q

Carboplatin(Paraplatin)Other side effects

A

Myelosuppression(thrombocytopenia)

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45
Q

Oxaliplatin (Eloxatin)class

A

Platinum analogs

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46
Q

Oxaliplatin (Eloxatin)Mechanism

A

Alkylating agents that do not formcarbonium ion intermediates or formallyalkylate DNA; covalently bind nucleophilicsites on DNA (e.g., guanine N7); convertedto active cytotoxic forms by reacting withwater to form (+)charged, hydratedintermediates that react with DNA guanine,forming inter- and intrastand cross-links

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47
Q

Oxaliplatin (Eloxatin)Therapeutics

A

Gastric and colorectal cancer

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48
Q

Oxaliplatin (Eloxatin)Imp Side effects

A

Peripheral sensory neuropathy(cold-induced)

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49
Q

Oxaliplatin (Eloxatin)Other side effects

A

Neutropenia

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50
Q

Antimetabolites in general

A

Structural analogs of folic acid or of thepurine/pyramidine bases found in DNA; actin S-phase (cell cycle specific)

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51
Q

Antimetabolites list

A

Methotrexate (Trexall)Pemetrexed (Alimta)5-Fluorouracil (5-FU, Carac)Cytarabine (AraC, Depocyt)Gemcitabine (dFdC, Gemzar)6-Mercaptopurine (Purinethol)

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52
Q

Methotrexate (Trexall) class

A

Folate analogs

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53
Q

Methotrexate (Trexall) mech

A

Inhibits dihydrofolate reductase (DHFR),which converts dietary folate totetrahydrofolate (THF) needed for thymidineand purine synthesis; given orally orintrathecally

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54
Q

Methotrexate (Trexall) Therapeutics

A

Childhood ALL and choriocarcinoma;combination therapy for Burkitt’slymphoma and carcinomas of breast,ovary, head and neck, and bladder;administered intrathecally formeningeal leukemia and meningealmetastases of tumors (can’t crossBBB); high-dose for osteosarcoma

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55
Q

Methotrexate (Trexall) Imp Side effects

A

Renal toxicity (crystallization inurine at high doses), hepatotoxicity(long-term, fibrosis/cirrhosis),reproductive (defective oogenesisor spermatogenesis, abortion)

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56
Q

Methotrexate (Trexall) Other side effects

A

Bone marrow(myelosuppression,spontaneous hemorrhage); GItoxicity (oral ulceration,stomatitis)

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57
Q

Methotrexate (Trexall) Misc

A

Can use leucovorin to prevent toxiceffects of MTX, as healthy cells cantake it up a lot better than tumor cells

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58
Q

Pemetrexed (Alimta) class

A

Folate analogs

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59
Q

Pemetrexed (Alimta) Mech

A

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

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60
Q

Pemetrexed (Alimta) Therapeutics

A

Colon cancer, mesothelioma, non-smallcell lung cancer, pancreatic cancer

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61
Q

5-Fluorouracil (5-FU, Carac) class

A

Pyramidine analogs

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62
Q

5-Fluorouracil (5-FU, Carac) Mech

A

5-FU is converted to active metabolites: 5-FdUMP inhibits TS; 5-FdUTP incorporatesinto RNA & interferes with RNA function;prodrug [capesitabine] ribosylated and phophosrylated into5-FdUMP

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63
Q

5-Fluorouracil (5-FU, Carac) Therapeutics

A

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

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64
Q

5-Fluorouracil (5-FU, Carac) Imp Side Effects

A

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

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65
Q

5-Fluorouracil (5-FU, Carac) Other side effects

A

Anorexia and nausea; mucosalulcerations, stomatitis, diarrhea;thrombocytopenia and anemia

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66
Q

5-Fluorouracil (5-FU, Carac) Misc

A

Leucovorin can potentiate effects of5-FU; must be given IV (GI toxicityand rapid degradation + metabolismin gut and liver)

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67
Q

Cytarabine (AraC, Depocyt) Class

A

Pyramidineanalogs

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68
Q

Cytarabine (AraC, Depocyt) Mech

A

Ara-C converted by deoxycytidine kinase toAra-CMP –> Ara-CTP; terminates DNAsynthesis as Ara-CTP

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69
Q

Cytarabine (AraC, Depocyt) Therapeutics

A

AML (most effective treatment), ALLand blast phase CML

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70
Q

Cytarabine (AraC, Depocyt) Other side effects

A

Severe myelosuppression(leucopenia, thrombocytopenia,anemia), GI tract toxicity(ulceration, stomatitis, diarrhea)

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71
Q

Gemcitabine (dFdC, Gemzar) class

A

Pyramidineanalogs

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72
Q

Gemcitabine (dFdC, Gemzar) Mech

A

Converted to active metabolites: dFdCDPinhibits ribonucleotide reductase (lowersdeoxyribonucleotide); dFdCTP incorporatesinto DNA, terminating DNA synthesis

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73
Q

Gemcitabine (dFdC, Gemzar) Therapeutics

A

Pancreatic cancer; effective againstnon-small cell lung cancer, ovarian,bladder, esophageal, and head andneck cancer

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74
Q

Gemcitabine (dFdC, Gemzar) Other side effects

A

Myelosuppression (leucopenia,thrombocytopenia, anemia), flulike

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75
Q

Gemcitabine (dFdC, Gemzar) Misc

A

More effective against solid tumorsthan cytarabine

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76
Q

6-Mercaptopurine (Purinethol) Class

A

Purine analogs(antimetabolites)

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77
Q

6-Mercaptopurine (Purinethol) Mech

A

Prodrug metabolized by hypoxanthineguaninephosphoribosyl transferase(HGPRT) to 6-thioinosinic acid (TIMP);TIMP inhibits first step of de novo purinebase synthesis and the formation of AMPand xanthinylic acid from inosinic acid,reducing purine levels. As well, TIMP isconverted to thio-guanine ribonucleotides,inhibiting DNA and RNA synthesis

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78
Q

6-Mercaptopurine (Purinethol) Therapeutics

A

Maintain remission in acute ALL

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79
Q

6-Mercaptopurine (Purinethol) Imp side effects

A

Hepatotoxicity in prolonged use

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80
Q

6-Mercaptopurine (Purinethol) Other side effects

A

Bone marrow suppression

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81
Q

6-Mercaptopurine (Purinethol) Misc

A

Drug interaction with allopurinol (forgout), which inhibits xanthineoxidase; decrease 6-MP dose toavoid drug accumulation andtoxicities

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82
Q

DNA Intercalating Agents General Mechanism

A

Bind DNA through intercalation betweenspecific bases, blocking DNA, RNA or bothsynthesis; cause DNA strands to break andinterfere with cell replication; CCNS

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83
Q

Dactinomycin (Actinomycin D, Cosmegen) Mech

A

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

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84
Q

Dactinomycin (Actinomycin D, Cosmegen) Therapeutics

A

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

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85
Q

Dactinomycin (Actinomycin D, Cosmegen) Imp Side effects

A

Hematopoietic suppression withpancytopenia

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86
Q

Dactinomycin (Actinomycin D, Cosmegen) Other side effects

A

Anorexia, nausea, vomiting

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87
Q

Daunorubicin (Cerubidine) Class

A

Anthracyclines

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88
Q

Daunorubicin (Cerubidine) Mech

A

Intercalate between DNA base pairs anddonate electrons to O2 to form superoxide;superoxide reacts with itself to form H2O2 –> cleaved in the presence of Fe to form OHradical, which cleaves DNA

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89
Q

Daunorubicin (Cerubidine) Therapeutics

A

AML

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90
Q

Daunorubicin (Cerubidine) Imp Side effects

A

Irreversible dose-dependentcardiotoxicity; alopecia

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91
Q

Daunorubicin (Cerubidine) Other side effects

A

Myelosuppression(neutropenia), stomatitis, GIdisturbances

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92
Q

Daunorubicin (Cerubidine) Misc

A

Dexrazoxane is cardio-protective

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93
Q

Idarubicin (Idamycin) Class

A

Anthracyclines

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94
Q

Idarubicin (Idamycin) Mech

A

Intercalate between DNA base pairs anddonate electrons to O2 to form superoxide;superoxide reacts with itself to form H2O2 –> cleaved in the presence of Fe to form OHradical, which cleaves DNA

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95
Q

Idarubicin (Idamycin) Therapeutics

A

AML

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96
Q

Idarubicin (Idamycin) Imp Side effects

A

Irreversible dose-dependentcardiotoxicity; alopecia

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97
Q

Idarubicin (Idamycin) Other side effects

A

Myelosuppression(neutropenia), stomatitis, GIdisturbances

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98
Q

Idarubicin (Idamycin) Misc

A

Dexrazoxane is cardio-protective

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99
Q

Doxorubicin (Adriamicin, Doxil) class

A

Anthracyclines

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100
Q

Doxorubicin (Adriamicin, Doxil) Mech

A

Intercalate between DNA base pairs anddonate electrons to O2 to form superoxide;superoxide reacts with itself to form H2O2 –> cleaved in the presence of Fe to form OHradical, which cleaves DNA

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101
Q

Doxorubicin (Adriamicin, Doxil) Therapeutics

A

Sarcomas, breast and lung carcinomas,malignant lymphomas

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102
Q

Doxorubicin (Adriamicin, Doxil) Imp side effects

A

Irreversible dose-dependentcardiotoxicity; alopecia

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103
Q

Doxorubicin (Adriamicin, Doxil) Other side effects

A

Myelosuppression(neutropenia), stomatitis, GIdisturbances

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104
Q

Doxorubicin (Adriamicin, Doxil) Misc

A

Dexrazoxane can be used to preventcardiotoxic effects

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105
Q

Epirubicin (Ellence) Class

A

Anthracyclines

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106
Q

Epirubicin (Ellence) Mech

A

Intercalate between DNA base pairs anddonate electrons to O2 to form superoxide;superoxide reacts with itself to form H2O2 –> cleaved in the presence of Fe to form OHradical, which cleaves DNA

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107
Q

Epirubicin (Ellence) Therapeutics

A

Metastatic breast cancer, gastriccancer

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108
Q

Epirubicin (Ellence) Imp side effects

A

Irreversible dose-dependentcardiotoxicity; alopecia

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109
Q

Epirubicin (Ellence) Other side effects

A

Myelosuppression(neutropenia), stomatitis, GIdisturbances

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110
Q

Epirubicin (Ellence) Misc

A

Dexrazoxane can be used to preventcardiotoxic effects

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111
Q

Bleomycin (Blenoxane) Mech

A

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

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112
Q

Bleomycin (Blenoxane) Therapeutics

A

Combination therapy for testiculartumors or Hodgkin’s disease;squamous cell carcinomas andlymphomas

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113
Q

Bleomycin (Blenoxane) Imp side effects

A

Pulmonary toxicity (pulmonaryfibrosis); cutaneous toxicity(hyperpigmentation,hyperkeratosis, erythema);hyperthermia

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114
Q

Bleomycin (Blenoxane) Other side effects

A

Minimally myelo- andimmunosuppressive (often usedin combo therapy); headache,nausea, vomiting

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115
Q

Bleomycin (Blenoxane) Misc

A

Dexrazoxane can be used to preventcardiotoxic effects

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116
Q

Microtubule Inhibitors

A

Inhibit mitosis and cause metaphase arrestby interfering with microtubule function(tubulin (de)polymerization); CCS

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117
Q

Vinblastine (Velban) Class

A

Vinca alkaloids

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118
Q

Vinblastine (Velban) Mech

A

Block tubulin polymerization intomicrotubules

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119
Q

Vinblastine (Velban) Therapeutics

A

Metastatic testicular tumors (withbleomycin, cisplatin); component ofABVD used for Hodgkin’s disease

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120
Q

Vinblastine (Velban) Other side effects

A

Myelosuppression, nausea,vomiting

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121
Q

Vincristine (Oncovin) Class

A

Vinca alkaloids

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122
Q

Vincristine (Oncovin) Mech

A

Block tubulin polymerization intomicrotubules

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123
Q

Vincristine (Oncovin) Therapeutics

A

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

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124
Q

Vincristine (Oncovin) Important side effects

A

Dose-limiting neurotoxicity(peripheral neuropathy)

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125
Q

Vincristine (Oncovin) Other side effects

A

Relatively low bone marrowtoxicity

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126
Q

Paclitaxel (Taxol, Abraxane) Class

A

Taxanes

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127
Q

Paclitaxel (Taxol, Abraxane) Mech

A

Block microtubule depolymerization intotubulin

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128
Q

Paclitaxel (Taxol, Abraxane) Therapeutics

A

Metastatic breast, ovarian, lung, andhead and neck cancers

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129
Q

Paclitaxel (Taxol, Abraxane) Imp side effects

A

Peripheral neuropathy

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130
Q

Paclitaxel (Taxol, Abraxane) other side effects

A

Neutropenia; hypersensitivityreactions

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131
Q

Docetaxel (Taxotere) class

A

Taxanes

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132
Q

Docetaxel (Taxotere) Mech

A

Block microtubule depolymerization intotubulin

133
Q

Docetaxel (Taxotere) Therapeutics

A

Metastatic breast, ovarian, lung, andhead and neck cancers; hormonerefractory prostate cancer

134
Q

Docetaxel (Taxotere) Important side effects

A

Peripheral neuropathy

135
Q

Docetaxel (Taxotere) Other side effects

A

Neutropenia; hypersensitivityreactions

136
Q

Etoposide (Etopophos) class

A

Epipodophyllotoxins

137
Q

Etoposide (Etopophos) mechanism

A

Inhibits topoisomerase II

138
Q

Etoposide (Etopophos) Therapeutics

A

Testicular carcinoma, lung cancer, andnon-Hodgkin’s lymphoma

139
Q

Etoposide (Etopophos) other side effects

A

Dose-limiting myelosuppression(neutropenia), oral mucositis

140
Q

Teniposide (Vumon) Class

A

Epipodophyllotoxins

141
Q

Teniposide (Vumon) Mechanism

A

Inhibits topoisomerase II

142
Q

Teniposide (Vumon) Therapeutics

143
Q

Teniposide (Vumon) Other side effects

A

Dose-limiting myelosuppression(neutropenia), oral mucositis

144
Q

Irinotecan (Camptosar) Class

A

Camptothecinanalogs

145
Q

Irinotecan (Camptosar) Mechanism

A

Inhibits topoisomerase I

146
Q

Irinotecan (Camptosar) Therapeutics

A

Advanced colorectal cancer; lung,ovarian, cervical and brain tumors

147
Q

Irinotecan (Camptosar) Other side effects

A

Severe neutropenia, severediarrhea

148
Q

Topotecan (Hycamtin) Class

A

Camptothecinanalogs

149
Q

Topotecan (Hycamtin) Mechanism

A

Inhibits topoisomerase I

150
Q

Topotecan (Hycamtin) Therapeutics

A

Ovarian and small cell lung cancer

151
Q

Topotecan (Hycamtin) Other side effects

A

Severe neutropenia, severediarrhea

152
Q

Prednisone (Meticorten) Class

A

Glucocorticoids

153
Q

Prednisone (Meticorten) Mechanism

A

Inhibit mitosis in lymphocytes

154
Q

Prednisone (Meticorten) Therapeutics

A

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

155
Q

Dexamethasone (Decadron) Class

A

Glucocorticoids

156
Q

Dexamethasone (Decadron) Mechanism

A

Inhibit mitosis in lymphocytes

157
Q

Dexamethasone (Decadron) Therapeutics

A

Reduces edema in brain and spinalcord tumors with radiation therapy

158
Q

Tamoxifen (Soltamox) Class

A

Selectiveestrogen-receptormodulators(SERMs)

159
Q

Tamoxifen (Soltamox) Mechanism

A

Competes with estradiol for binding toestrogen receptor

160
Q

Tamoxifen (Soltamox) Therapeutics

A

ER-positive breast cancer, or asadjuvant therapy following primarybreast tumor excision; prevention ofbreast cancer in high-risk patients

161
Q

Tamoxifen (Soltamox) Important side effects

A

Hot flushes, hair loss; increasedrisk of endometrial cancer;increased risk of thromboembolicevents

162
Q

Tamoxifen (Soltamox) Other side effects

A

Nausea and vomiting

163
Q

Fulvestrant (Faslodex) Class

A

Selectiveestrogen-receptordownregulators(SERDs)

164
Q

Fulvestrant (Faslodex) Mechanism

A

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

165
Q

Fulvestrant (Faslodex) Therapeutics

A

Posmenopausal women with ERpositivemetastatic breast cancer

166
Q

Aminoglutethamide (Cytadren) Class

A

Aromataseinhibitors

167
Q

Aminoglutethamide (Cytadren) Mechanism

A

Inhibits function of aromatase

168
Q

Aminoglutethamide (Cytadren) Therapeutics

A

Relatively weak, used against breastcancer

169
Q

Aminoglutethamide (Cytadren) Imp side effects

A

Significant

170
Q

Anastrozole (Arimidex) Class

A

Aromataseinhibitors

171
Q

Anastrozole (Arimidex) Mechanism

A

Inhibits function of aromatase

172
Q

Anastrozole (Arimidex) Therapeutics

A

First-line for ER-positive breast cancerin postmenopausal women

173
Q

Letrozole (Femara) class

A

Aromataseinhibitors

174
Q

Letrozole (Femara) Mechanism

A

Inhibits function of aromatase

175
Q

Letrozole (Femara) Therapeutics

A

ER-positive breast cancer inpostmenopausal women

176
Q

Exemestane (Aromasin) class

A

Aromataseinhibitors

177
Q

Exemestane (Aromasin) Mechanism

A

Steroidal inhibitor of aromatase

178
Q

Exemestane (Aromasin) Therapeutics

A

ER-positive breast cancer inpostmenopausal women

179
Q

Leuprolide (Lupron) class

A

GnRH analogs

180
Q

Leuprolide (Lupron) Mechanism

A

Binds GnRH receptor; inhibits release ofFSH & LH

181
Q

Leuprolide (Lupron) Therapeutics

A

Androgen ablation therapy, along withAR blockers

182
Q

Goserelin (Zoladex) Class

A

GnRH analogs

183
Q

Goserelin (Zoladex) Mechanism

A

Binds GnRH receptor; inhibits release ofFSH & LH

184
Q

Goserelin (Zoladex) Therapeutics

A

Androgen ablation therapy, along withAR blockers

185
Q

Flutamide (Eulexin) Class

A

Nonsteroidalandrogen-receptorblockers

186
Q

Flutamide (Eulexin) Mechanism

A

Competes with androgen for AR binding

187
Q

Flutamide (Eulexin) Therapeutics

A

Androgen ablation therapy, along withGnRH analogs

188
Q

Bicalutamide (Casodex) Class

A

Nonsteroidalandrogen-receptorblockers

189
Q

Bicalutamide (Casodex) Mechanism

A

Competes with androgen for AR binding

190
Q

Bicalutamide (Casodex) Therapeutics

A

Androgen ablation therapy, along withGnRH analogs

191
Q

Imatinib (Gleevac) Class

A

Tyrosine Kinaseinhibitor

192
Q

Imatinib (Gleevac) Mechanism

A

Inhibits Abl kinase by binding where ATPshould go; also inhibits PDGFR and c-kit;metabolized by cytochrome P450

193
Q

Imatinib (Gleevac) Therapeutics

A

First line therapy for CML; also,gastrointestinal tumor (GIST)

194
Q

Imatinib (Gleevac) Imp Side effects

A

Nausea and vomiting, fluidretention, muscle cramps,arthralgia

195
Q

Imatinib (Gleevac) Other side effects

A

Myelosuppression

196
Q

Imatinib (Gleevac) Misc

A

Oral (1/day)

197
Q

Gefitinib (Iressa) Class

A

Tyrosine Kinaseinhibitor

198
Q

Gefitinib (Iressa) Mechanism

A

Inhibit epidermal growth factor receptor(EGFR) tyrosine kinase

199
Q

Gefitinib (Iressa) Therapeutics

A

Non-small lung cancer

200
Q

Erlotinib (Tarceva) Class

A

Tyrosine Kinaseinhibitor

201
Q

Erlotinib (Tarceva) Mechanism

A

Inhibit epidermal growth factor receptor(EGFR) tyrosine kinase

202
Q

Erlotinib (Tarceva) Therapeutics

A

Non-small lung cancer

203
Q

Nilotinib (Tasigna) class

A

Tyrosine Kinaseinhibitor

204
Q

Nilotinib (Tasigna) Mechanism

A

Inhibits Abl kinase

205
Q

Nilotinib (Tasigna) Therapeutics

A

Imatinib-resistant CML

206
Q

Nilotinib (Tasigna) Imp side effects

A

Myelosuppression

207
Q

Nilotinib (Tasigna) other side effects

A

QT prolongation, hepatotoxicity,electrolyte abnormalities

208
Q

Nilotinib (Tasigna) misc

A

Oral (2/day)

209
Q

Dasatinib (Sprycel) class

A

Tyrosine Kinaseinhibitor

210
Q

Dasatinib (Sprycel) mechanism

A

Inhibits Abl & Src kinases

211
Q

Dasatinib (Sprycel) therapeutics

A

Imatinib-resistant CML

212
Q

Dasatinib (Sprycel) Imp side effects

A

Myelosuppression, bleeding, fluidretention, pulmonary arterialhypertension

213
Q

Dasatinib (Sprycel) other side effects

A

Diarrhea, nausea and vomiting,weakness, infections

214
Q

Dasatinib (Sprycel) misc

A

Oral (1/day)

215
Q

Rituximab (Rituxan) class

A

Monoclonalantibody

216
Q

Rituximab (Rituxan) mechanism

A

CD20 B-cell antibody that can directlyactivate apoptosis, activate complement, oractivate cell-mediated cytotoxicity (e.g., Tcells, NK cells)

217
Q

Rituximab (Rituxan) therapeutics

A

Non-Hodgkin’s lymphomas

218
Q

Rituximab (Rituxan) imp side effects

A

Infusion reactions, tumor lysissyndrome (TLS), severemucocutaneous reactions,progressive multifocalleukoencephalopathy (PML)

219
Q

Rituximab (Rituxan) other side effects

A

Skin reactions, irregularheartbeat, muscle or joint pain

220
Q

Rituximab (Rituxan) misc

A

Patients need careful monitoring

221
Q

Trastuzumab (Herceptin) class

A

Monoclonalantibody

222
Q

Trastuzumab (Herceptin) mechanism

A

Unknown HER2/neu (ErbB2) receptorantibody mechanism (enhanced receptorendocytosis or blocking homo- orheterodimerization)

223
Q

Trastuzumab (Herceptin) therapeutics

A

HER2/neu-overexpressing metastaticbreast cancer

224
Q

Trastuzumab (Herceptin) Imp side effects

A

Hypersentivity reaction; ventriculardysfunction

225
Q

Trastuzumab (Herceptin) misc

A

Usually combined with taxanes;enhances doxorubicin cardiotoxicity

226
Q

Cetuximab (Erbitux) class

A

Monoclonalantibody

227
Q

Cetuximab (Erbitux) mechanism

A

EGFR1 (ErbB1)

228
Q

Cetuximab (Erbitux) therapeutics

A

EGFR-positive metastatic colorectalcancer

229
Q

Cetuximab (Erbitux) imp side effects

A

Allergic reactions, sudden cardiacdeath, dermatologic problems,infections, renal failure, electrolyteabnormalities

230
Q

Cetuximab (Erbitux) other side effects

A

Asthenia/malaise, fever,nausea, constipation, interstitialpneumonitis

231
Q

Cetuximab (Erbitux) misc

A

Clinical trials, probably combine withcisplatin

232
Q

Cetuximab (Erbitux) class

A

Monoclonalantibody

233
Q

Cetuximab (Erbitux) mechanism

A

EGFR1 (ErbB1)

234
Q

Cetuximab (Erbitux) therapeutics

A

EGFR-positive metastatic colorectalcancer

235
Q

Cetuximab (Erbitux) imp side effects

A

Allergic reactions, sudden cardiacdeath, dermatologic problems,infections, renal failure, electrolyteabnormalities

236
Q

Cetuximab (Erbitux) other side effects

A

Asthenia/malaise, fever,nausea, constipation, interstitialpneumonitis

237
Q

Cetuximab (Erbitux) misc

A

Clinical trials, probably combine withcisplatin

238
Q

Ipilimumab (Yervoy) class

A

Humanmonoclonalantibody

239
Q

Ipilimumab (Yervoy) mechanism

A

Cytotoxic T-Lymphocyte Antigen 4 inhibitor;stimulates immune system

240
Q

Ipilimumab (Yervoy) therapeutics

241
Q

Vemurafenib (Zelboraf) class

A

Serine/threoninekinase inhibitor

242
Q

Vemurafenib (Zelboraf) mechanism

A

Inhibits oncogenic BRAF kinase

243
Q

Vemurafenib (Zelboraf) therapeutics

A

Unresectable Stage III and IV ormetastatic melanomas w/BRAFmutations

244
Q

Vemurafenib (Zelboraf) imp side effects

A

Arthralgia, fatigue, photosensitivity,nausea, alopecia, diarrhea, QTprolongation

245
Q

Vemurafenib (Zelboraf) other side effects

A

Cutaneous squamous cellcarcinoma, keratoacanthoma,new primary cutaneousmelanoma

246
Q

Vemurafenib (Zelboraf) misc

A

Superior to dacarbazine in Phase IIItrials

247
Q

Dabrafenib (Tafinlar) class

A

Serine/threoninekinase inhibitor

248
Q

Dabrafenib (Tafinlar) mechanism

A

Inhibits oncogenic BRAF kinase

249
Q

Dabrafenib (Tafinlar) therapeutics

A

Unresectable Stage III and IV ormetastatic melanomas w/BRAFmutations

250
Q

Dabrafenib (Tafinlar) imp side effects

A

Serious febrile drug reactions,uveitis and iritis, hyperglycemia,hyperkeratosis

251
Q

Dabrafenib (Tafinlar) other side effects

A

Higher risk of developing above

252
Q

Dabrafenib (Tafinlar) misc

A

May cause male infertility

253
Q

Trametinib (Mekinist) mechanism

A

Inhibits MEK

254
Q

Trametinib (Mekinist) therapeutics

A

Unresectable Stage III and IV ormetastatic melanomas w/BRAFmutations

255
Q

Trametinib (Mekinist) imp side effects

A

Cardiomyopathy, retinal disorders,interstitial lung disease, seriousskin toxicities

256
Q

Trametinib (Mekinist) other side effects

A

Rash, diarrhea, stomatitis,hypertension, pruritis

257
Q

Trametinib (Mekinist) misc

A

May cause female infertility

258
Q

Hydroxyurea (Hydrea) mechanism

A

Inhibits ribonucleoside diphosphatereductase

259
Q

Hydroxyurea (Hydrea) therapeutics

A

CML (replaced by Imatinib),polycythemia vera, essentialthrombocythemia; treatment for sicklecell disease (increases Hb-F)

260
Q

Retinoids Mechanism

A

ATRA induces terminal differentiation inmalignant immature promyelocytes, whichsubsequently apoptose

261
Q

Retinoids Therapeutics

262
Q

Retinoids imp side effects

A

“Leukocyte Activation Syndrome”(LAS), an increase in WBCs (fever,weight gain, respiratory distress,serosal effusion, renal failure)

263
Q

Retinoids misc

A

Combined w/anthracyclines;corticosteroids used to block “LAS”

264
Q

Arsenic Trioxide (Trisenox) Therapeutics

A

Relapsed APL

265
Q

Thalidomide (Thalomid) Therapeutics

A

Multiple myeloma and myelodysplasticsyndromes

266
Q

Interferons

A

Hairy-cell leukemia, CML, and AIDSrelatedKaposi’s sarcoma

267
Q

ABVD

A

Doxorubicin (adriamycin), bleomycin,vinblastine, dacarbazine

268
Q

CHOP

A

Cyclophosphamide, hydroxydoxorubicin,vincristine (oncovine), prednisone

269
Q

MOPP

A

Mechlorethamine, vincristine (oncovine),procarbazine, prednisone

270
Q

CMF

A

Cyclophosphamide, methotrexate, 5-fluorouracil

271
Q

FEC

A

5-fluorouracil, epirubicin, cyclophosphamide

272
Q

Class for:Estradiol (valerate & cypionate)Estrone sulfateEquilin sulfateQuinestrol

A

Estradiol esters(steroidal)

273
Q

Class for:Ethinyl estradiolMestranol

A

Alkyl estrogen

274
Q

Mechanism for:Estradiol (valerate & cypionate)Estrone sulfateEquilin sulfateQuinestrolEthinyl estradiolMestranol

A

Absorbed through skin, mucus membranes,GI Tract; body-wide distribution via sexhormonebinding globulin

275
Q

Therapeutics for:Estradiol (valerate & cypionate)Estrone sulfateEquilin sulfateQuinestrolEthinyl estradiolMestranol

A

Contraception, primary hypogonadism,postmenopausal hormone therapy

276
Q

Imp side effects for:Estradiol (valerate & cypionate)Estrone sulfateEquilin sulfateQuinestrolEthinyl estradiolMestranol

A

Weight gain, HTN; less commonly,may cause breast cancer, DVT,cervical and endometrial cancer

277
Q

Other side effects for:Estradiol (valerate & cypionate)Estrone sulfateEquilin sulfateQuinestrolEthinyl estradiolMestranol

A

Nausea, breast tension/pain,vaginal bleeding, headache

278
Q

Misc for:Estradiol (valerate & cypionate)Estrone sulfateEquilin sulfateQuinestrolEthinyl estradiolMestranol

A

Strongly contraindicated in breast orendometrial cancers, endometriosis,undiagnosed vaginal bleeds;relatively contradinicated inpregnancy, thromboembolic disease,HTN, hepatic disease, family historyof breast or uterine cancer

279
Q

Diethylstilbestrol class

A

Non-steroidalsynthetic estrogen

280
Q

Diethylstilbestrol Imp side effect

A

Increased risk of clear celladenocarcinoma of vagina & cervix

281
Q

Tamoxifen citrate (Nolvadex) class

A

Non-steroidal antiestrogen;selectiveestrogen receptormodifier

282
Q

Tamoxifen citrate (Nolvadex) mechanism

A

Blocks estrogen from binding ER andcausing growth in ER(+) breast cancer

283
Q

Tamoxifen citrate (Nolvadex) therapeutics

A

ER(+) breast cancer

284
Q

Tamoxifen citrate (Nolvadex) imp side effects

A

Pro-estrogenic effect on uterineepithelium (increase risk ofendometrial cancer); partialestrogen agonist in bone andendometrium

285
Q

Tamoxifen citrate (Nolvadex) misc

A

Anti-estrogenic effect on mammaryepithelium; must be used in veryhigh doses

286
Q

Clomiphene citrate (Clomid) class

A

Non-steroidal antiestrogen

287
Q

Clomiphene citrate (Clomid) mechanism

A

Blocks estrogen binding to hypothalamicreceptors (no estradiol negative feedbackon gonadotropins) –> increased secretionof gonadotropins & LH –> ovulation

288
Q

Clomiphene citrate (Clomid) therapeutics

A

Stimulate ovulation in patients whowant to get pregnant

289
Q

Clomiphene citrate (Clomid) imp side effects

A

Hot flashes, multiple pregnancy

290
Q

Clomiphene citrate (Clomid) other side effects

A

Stomach pain, headache, upsetstomach, vomit

291
Q

Clomiphene citrate (Clomid) misc

A

Cis-isomer (zuclomiphene) is a weakestrogen agonist; trans-isomer(enclomiphene) is a potent estrogenantagonist

292
Q

ClassMicronized progesteroneTransvaginal progesterone

A

Naturalprogesterone

293
Q

Therapeutics forMicronized progesteroneTransvaginal progesterone

A

Contraception, hormone replacementtherapy

294
Q

Imp side effects forMicronized progesteroneTransvaginal progesterone

A

Fatigue, drowsiness

295
Q

Misc forMicronized progesteroneTransvaginal progesterone

A

Contraindicated in thromboembolicdisorders or patients with such ahistory, liver disease (metabolised inthe liver), undiagnosed vaginalbleeding, pregnancy (atrophy ofendometrium leading to birthdefects)

296
Q

Class for:MedroxyprogesteroneNorethindroneNorgestrelMegestrol

A

Syntheticprogesterone

297
Q

Therapeutics for:MedroxyprogesteroneNorethindroneNorgestrelMegestrol

A

Contraception, hormone replacementtherapy

298
Q

Imp side effects for:MedroxyprogesteroneNorethindroneNorgestrelMegestrol

A

Edema, abdominal bloating; lesscommonly: strong androgeniceffects (hirsutism, acne)

299
Q

Other side effects for:MedroxyprogesteroneNorethindroneNorgestrelMegestrol

A

Anxiety, irritability, depression,muscular pain; increased risk ofthrombus and PE

300
Q

Misc for:MedroxyprogesteroneNorethindroneNorgestrelMegestrol

A

Contraindicated in thromboembolicdisorders or patients with such ahistory, liver disease (metabolised inthe liver), undiagnosed vaginalbleeding, pregnancy (atrophy ofendometrium leading to birthdefects)

301
Q

Class for:Monophasic Ortho-NovumBiphasic Ortho-NovumTriphasic Ortho-Novum

A

Combination pill

302
Q

Mechanism for:Monophasic Ortho-NovumBiphasic Ortho-NovumTriphasic Ortho-Novum

A

Constant level of estrogen suppresses FSH,LH surge; progesterone suppresses LHsurge, thickens cervical mucus, leads toendometrial atrophy

303
Q

Therapeutics for:Monophasic Ortho-NovumBiphasic Ortho-NovumTriphasic Ortho-Novum

A

Contraception

304
Q

Imp side effects for:Monophasic Ortho-NovumBiphasic Ortho-NovumTriphasic Ortho-Novum

A

As with synthetic estrogen andprogesterones

305
Q

Monophasic Ortho-Novum Misc

A

Consistent dose of estrogen andprogestin (only take 21 days)

306
Q

Biphasic Ortho-Novum Misc

A

Fixed estrogen, progestin increasedfor days 11-21

307
Q

Triphasic Ortho-Novum Misc

A

Fixed or variable estrogen, whileprogestin increases in 3 phases (1-7,8-14, 15-21)

308
Q

Mini-pill class

A

Progestin only

309
Q

Mini-pill mechanism

A

As progestin

310
Q

Mini-pill Therapeutics

A

Less effective than combination pill forcontraception; use when patient hasestrogen contraindication; good inlactating women (estrogen reduces milkproduction)

311
Q

Mini-pill imp side effect

A

More likely to produce irregularmenstrual cycle (estrogen requiredto provide stability to endometrium)

312
Q

Mini-pill other side effect

A

Suppresses endometrial cancer

313
Q

Levonorgestrel (Plan B) class

A

Syntheticprogestogen

314
Q

Levonorgestrel (Plan B) Mechanism

315
Q

Levonorgestrel (Plan B) Therapeutics

A

Prevent implantation

316
Q

Levonorgestrel (Plan B) Imp side effect

A

Likely the same as combinationoral contraceptives

317
Q

Levonorgestrel (Plan B) misc

A

Must be taken within 72 hours ofcoitus

318
Q

Mifepristone (RU-486, Korlym) class

A

Anti-progestin;glucocorticoidreceptorantagonist

319
Q

Mifepristone (RU-486, Korlym) Mechanism

A

Competitively binds to progesteronereceptor (leading to detachment of fetus);glucocorticoid recepter antagonist

320
Q

Mifepristone (RU-486, Korlym) Therapeutics

A

Abortion; Cushing’s Syndrome

321
Q

Mifepristone (RU-486, Korlym) Misc

A

Must take early in pregnancy (by day49); oral administration; must begiven by doctor in medical facilityprepared for surgery if abortionincomplete

322
Q

Class for:Sildenafil citrate (Viagra)Vardenafil HCl (Levitra)Tadalafil (Cialis)

A

PDE5 inhibitor

323
Q

Mechanism for:Sildenafil citrate (Viagra)Vardenafil HCl (Levitra)Tadalafil (Cialis)

A

Bind catalytic site of PDE5; inhibits PDE5breakdown of cGMP –> decreased Ca –>smooth muscle relaxation –> erection

324
Q

Therapeutics for:Sildenafil citrate (Viagra)Vardenafil HCl (Levitra)Tadalafil (Cialis)

A

Erectile dysfunction; does not trigger anautomatic erection, but improvesresponse to sexual stimulation

325
Q

Imp side effects for:Sildenafil citrate (Viagra)Vardenafil HCl (Levitra)Tadalafil (Cialis)

A

Headache, dizziness, change invision (NAION)

326
Q

Other side effects for:Sildenafil citrate (Viagra)Vardenafil HCl (Levitra)Tadalafil (Cialis)

A

Flushing, upset stomach, stuffyor runny nose, UTI, diarrhea

327
Q

Misc for:Sildenafil citrate (Viagra)Vardenafil HCl (Levitra)

A

Oral (once/day max); half-life of 4hours, peak plasma concentration in1-2 hours; contraindicated if onnitrates or α-blockers (unsafe drop inBP)

328
Q

Misc for:Tadalafil (Cialis)

A

Oral (once/day max); half-life of 17.5hours, peak plasma concentration in1-2 hours; contraindicate if onnitrates or α-blockers (unsafe drop inBP)

Pharm Drug Table (11 decks)

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