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Pharmacology Unit 1 > Misc. Agents > Flashcards

Misc. Agents Flashcards

1
Q

Imatinib (Gleevac) Class

A

Tyrosine Kinase inhibitor

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2
Q

Imatinib (Gleevac) Mechanism

A

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

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3
Q

Imatinib (Gleevac) Therapeutics

A

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

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4
Q

Imatinib (Gleevac) Side effects

A

Nausea and vomiting, fluid retention, muscle cramps,arthralgia, myelosuppression

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5
Q

Gefitinib (Iressa) Class

A

Tyrosine Kinase inhibitor

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6
Q

Gefitinib (Iressa) Mechanism

A

Inhibit epidermal growth factor receptor (EGFR) tyrosine kinase

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7
Q

Gefitinib (Iressa) Therapeutics

A

Non-small lung cancer

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8
Q

Erlotinib (Tarceva) Class

A

Tyrosine Kinase inhibitor

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9
Q

Erlotinib (Tarceva) Mechanism

A

Inhibit epidermal growth factor receptor(EGFR) tyrosine kinase

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10
Q

Erlotinib (Tarceva) Therapeutics

A

Non-small lung cancer

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11
Q

Nilotinib (Tasigna) class

A

Tyrosine Kinase inhibitor

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12
Q

Nilotinib (Tasigna) Mechanism

A

Inhibits Abl kinase

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13
Q

Nilotinib (Tasigna) Therapeutics

A

Imatinib-resistant CML

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14
Q

Nilotinib (Tasigna) Imp side effects

A

Myelosuppression, QT prolongation, hepatotoxicity,electrolyte abnormalities

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15
Q

Dasatinib (Sprycel) class

A

Tyrosine Kinase inhibitor

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16
Q

Dasatinib (Sprycel) mechanism

A

Inhibits Abl & Src kinases

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17
Q

Dasatinib (Sprycel) therapeutics

A

Imatinib-resistant CML

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18
Q

Dasatinib (Sprycel) Imp side effects

A

Myelosuppression, bleeding, fluidretention, pulmonary arterial hypertension, Diarrhea, nausea and vomiting,weakness, infections

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19
Q

Rituximab (Rituxan) class

A

Monoclonal antibody

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20
Q

Rituximab (Rituxan) mechanism

A

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

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21
Q

Rituximab (Rituxan) therapeutics

A

Non-Hodgkin’s lymphomas

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22
Q

Rituximab (Rituxan) imp side effects

A

Infusion reactions, tumor lysis syndrome (TLS), severe mucocutaneous reactions, progressive multifocal leukoencephalopathy (PML)

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23
Q

Rituximab (Rituxan) other side effects

A

Skin reactions, irregularheartbeat, muscle or joint pain

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24
Q

Trastuzumab (Herceptin) class

A

Monoclonal antibody

25
Q

Trastuzumab (Herceptin) mechanism

A

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

26
Q

Trastuzumab (Herceptin) therapeutics

A

HER2/neu-overexpressing metastatic breast cancer

27
Q

Trastuzumab (Herceptin) Imp side effects

A

Hypersentivity reaction; ventriculardysfunction

28
Q

Trastuzumab (Herceptin) misc

A

Usually combined with taxanes; enhances doxorubicin cardiotoxicity

29
Q

Cetuximab (Erbitux) class

A

Monoclonal antibody

30
Q

Cetuximab (Erbitux) mechanism

A

EGFR1 (ErbB1)

31
Q

Cetuximab (Erbitux) therapeutics

A

EGFR-positive metastatic colorectal cancer

32
Q

Cetuximab (Erbitux) imp side effects

A

Allergic reactions, sudden cardiac death, dermatologic problems, infections, renal failure, electrolyte abnormalities

33
Q

Cetuximab (Erbitux) other side effects

A

Asthenia/malaise, fever,nausea, constipation, interstitialpneumonitis

34
Q

Cetuximab (Erbitux) misc

A

Clinical trials, probably combine withcisplatin

35
Q

Ipilimumab (Yervoy) class

A

Human monoclonal antibody

36
Q

Ipilimumab (Yervoy) mechanism

A

Cytotoxic T-Lymphocyte Antigen 4 inhibitor; stimulates immune system

37
Q

Ipilimumab (Yervoy) therapeutics

38
Q

Vemurafenib (Zelboraf) class

A

Serine/threonine kinase inhibitor

39
Q

Vemurafenib (Zelboraf) mechanism

A

Inhibits oncogenic BRAF kinase

40
Q

Vemurafenib (Zelboraf) therapeutics

A

Unresectable Stage III and IV or metastatic melanomas w/BRAF mutations

41
Q

Vemurafenib (Zelboraf) imp side effects

A

Arthralgia, fatigue, photosensitivity, nausea, alopecia, diarrhea, QT prolongation

42
Q

Vemurafenib (Zelboraf) other side effects

A

Cutaneous squamous cellcarcinoma, keratoacanthoma, new primary cutaneous melanoma

43
Q

Dabrafenib (Tafinlar) class

A

Serine/threonine kinase inhibitor

44
Q

Dabrafenib (Tafinlar) mechanism

A

Inhibits oncogenic BRAF kinase

45
Q

Dabrafenib (Tafinlar) therapeutics

A

Unresectable Stage III and IV ormetastatic melanomas w/BRAF mutations

46
Q

Dabrafenib (Tafinlar) imp side effects

A

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

47
Q

Trametinib (Mekinist) mechanism

A

Inhibits MEK

48
Q

Trametinib (Mekinist) therapeutics

A

Unresectable Stage III and IV ormetastatic melanomas w/BRAF mutations

49
Q

Trametinib (Mekinist) imp side effects

A

Cardiomyopathy, retinal disorders,interstitial lung disease, serious skin toxicities

50
Q

Trametinib (Mekinist) other side effects

A

Rash, diarrhea, stomatitis,hypertension, pruritis

51
Q

Hydroxyurea (Hydrea) mechanism

A

Inhibits ribonucleoside diphosphate reductase

52
Q

Hydroxyurea (Hydrea) therapeutics

A

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

53
Q

Retinoids Mechanism

A

ATRA induces terminal differentiation inmalignant immature promyelocytes, which subsequently apoptose

54
Q

Retinoids Therapeutics

55
Q

Retinoids imp side effects

A

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

56
Q

Retinoids misc

A

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

57
Q

Arsenic Trioxide (Trisenox) Therapeutics

A

Relapsed APL

58
Q

Thalidomide (Thalomid) Therapeutics

A

Multiple myeloma and myelodysplasticsyndromes

59
Q

Interferons

A

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

Pharmacology Unit 1 (7 decks)

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