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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
Trastuzumab (Herceptin) mechanism
Unknown HER2/neu (ErbB2) receptor antibody mechanism (enhanced receptorendocytosis or blocking homo- orheterodimerization)
26
Trastuzumab (Herceptin) therapeutics
HER2/neu-overexpressing metastatic breast cancer
27
Trastuzumab (Herceptin) Imp side effects
Hypersentivity reaction; ventriculardysfunction
28
Trastuzumab (Herceptin) misc
Usually combined with taxanes; enhances doxorubicin cardiotoxicity
29
Cetuximab (Erbitux) class
Monoclonal antibody
30
Cetuximab (Erbitux) mechanism
EGFR1 (ErbB1)
31
Cetuximab (Erbitux) therapeutics
EGFR-positive metastatic colorectal cancer
32
Cetuximab (Erbitux) imp side effects
Allergic reactions, sudden cardiac death, dermatologic problems, infections, renal failure, electrolyte abnormalities
33
Cetuximab (Erbitux) other side effects
Asthenia/malaise, fever,nausea, constipation, interstitialpneumonitis
34
Cetuximab (Erbitux) misc
Clinical trials, probably combine withcisplatin
35
Ipilimumab (Yervoy) class
Human monoclonal antibody
36
Ipilimumab (Yervoy) mechanism
Cytotoxic T-Lymphocyte Antigen 4 inhibitor; stimulates immune system
37
Ipilimumab (Yervoy) therapeutics
Melanoma
38
Vemurafenib (Zelboraf) class
Serine/threonine kinase inhibitor
39
Vemurafenib (Zelboraf) mechanism
Inhibits oncogenic BRAF kinase
40
Vemurafenib (Zelboraf) therapeutics
Unresectable Stage III and IV or metastatic melanomas w/BRAF mutations
41
Vemurafenib (Zelboraf) imp side effects
Arthralgia, fatigue, photosensitivity, nausea, alopecia, diarrhea, QT prolongation
42
Vemurafenib (Zelboraf) other side effects
Cutaneous squamous cellcarcinoma, keratoacanthoma, new primary cutaneous melanoma
43
Dabrafenib (Tafinlar) class
Serine/threonine kinase inhibitor
44
Dabrafenib (Tafinlar) mechanism
Inhibits oncogenic BRAF kinase
45
Dabrafenib (Tafinlar) therapeutics
Unresectable Stage III and IV ormetastatic melanomas w/BRAF mutations
46
Dabrafenib (Tafinlar) imp side effects
Serious febrile drug reactions, uveitis and iritis, hyperglycemia, hyperkeratosis
47
Trametinib (Mekinist) mechanism
Inhibits MEK
48
Trametinib (Mekinist) therapeutics
Unresectable Stage III and IV ormetastatic melanomas w/BRAF mutations
49
Trametinib (Mekinist) imp side effects
Cardiomyopathy, retinal disorders,interstitial lung disease, serious skin toxicities
50
Trametinib (Mekinist) other side effects
Rash, diarrhea, stomatitis,hypertension, pruritis
51
Hydroxyurea (Hydrea) mechanism
Inhibits ribonucleoside diphosphate reductase
52
Hydroxyurea (Hydrea) therapeutics
CML (replaced by Imatinib),polycythemia vera, essentialthrombocythemia; treatment for sicklecell disease (increases Hb-F)
53
Retinoids Mechanism
ATRA induces terminal differentiation inmalignant immature promyelocytes, which subsequently apoptose
54
Retinoids Therapeutics
APL
55
Retinoids imp side effects
"Leukocyte Activation Syndrome"(LAS), an increase in WBCs (fever,weight gain, respiratory distress,serosal effusion, renal failure)
56
Retinoids misc
Combined w/anthracyclines;corticosteroids used to block "LAS"
57
Arsenic Trioxide (Trisenox) Therapeutics
Relapsed APL
58
Thalidomide (Thalomid) Therapeutics
Multiple myeloma and myelodysplasticsyndromes
59
Interferons
Hairy-cell leukemia, CML, and AIDS related Kaposi's sarcoma

Pharmacology Unit 1 (7 decks)

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