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Unit 1: Pharm > Miscellaneous Agents > Flashcards

Miscellaneous Agents Flashcards

1
Q

What class of drug is Imatinib (Gleevac)?

A

Tyrosine Kinase Inhibitor

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2
Q

What is the mechanism of action of Imatinib?

A

It inhibits Abl kinase by binding where ATP should go

It also inhibits PDGFR and c-kit

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3
Q

How is Imatinib metabolized?

A

Cytochrome P450

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4
Q

What is Imatinib used to treat?

A

CML (first line therapy)

Gastrointestinal tumor

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5
Q

What are the major side effects of Imatinib?

A

Nausea and vomiting

Fluid Retention

Muscle Cramps

Arthraligia

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6
Q

What are the minor side effects Imatinib?

A

Myelosuppression

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7
Q

How is imatinib administered?

A

Orally`

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8
Q

What class of drug is Gefitinib (Iressa)?

A

Tyrosine kinase inhibitor

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9
Q

What is the mechanism of action of Gefitinib?

A

Inhibits the epidermal growth factor recepto tyrosine kinase

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10
Q

What is gefitinib used to treat?

A

Non- small lung cancer

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11
Q

What calass of drug is Erlotinib (Tarceva)?

A

Tyrosine kinase inhibitor

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12
Q

What is the mechanism of action of Erlotinib?

A

Inhibits epidermal growth factor receptor tyrosine kinase

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13
Q

What is erlotinib used to treat?

A

Non-small lung cancer

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14
Q

What class of drug is Nilotinib (Tasigna)?

A

Tyrosine kinase inhibitor

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15
Q

What is the mechanism of action of nilotinib?

A

Inhibits Abl kinase

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16
Q

What is nilotinib used to treat?

A

Imatinib-resistant CML

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17
Q

What are the major and minor side effects of nilotinib?

A

Major: Myelosupression

Minor: QT prolongation, hepatotoxicity, electrolyte abnormalitis

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18
Q

What class of drug is dasatinib (Sprycel)?

A

Tyrosine kinase inhibitor

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19
Q

What is the mechanism of action of dasatinib?

A

Inhibits Abl and Src kinases

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20
Q

What is dasatinib used to treat?

A

Imatinib-resistant CML

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21
Q

Major and minor side effects of dasatinib?

A

Major: Myelosupresion, bleeding, fluid retention, pulmonary arterial hypertension

Minor: Diarrhea, nausea and vomiting, weakness and infections

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22
Q

How are dasatinib and nilotinib administered?

A

Orally

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23
Q

What class of drug is rituximab?

A

Monoclonal antibody

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24
Q

What is the mechanism of action of rituximab?

A

CD20 B-cell antibody that can directly activate apoptosis, compliment or cell mediated cytotoxicity

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25
Q

What is rituximab used to treat?

A

Non-hodgkin’s lymphoma

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26
Q

Major side effects of rituximab?

A

Infusion reactions, tumor lysis syndrome, severe mucocutaneous reactions, PML

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27
Q

What are the minor side effects of rituximab?

A

Skin reactions, irregular heartbeat, muscle or joint pain

28
Q

What class of drug is trastuzumab?

A

Monoclonal antibody

29
Q

What is the mechanism of action of trasuzumab?

A

mechanism is not completely known. But it is known that it interacts somehow with the HER2/neu receptor.

Theories include: enhanced receptor endocytosis or blocking homo- or heterodimerization

30
Q

What is trastuzumab used to treat?

A

HER2/ neu overexpressing metastatic breast cancer

31
Q

Side effects of trastuzumab?

A

Hypersensitivity reaction; ventricular dysfunction

32
Q

What is trastuzumab usually administered with?

A

Usually combined with taxanes ( )

33
Q

What happens when trastuzumab is given with doxorubicin?

A

It enhances the cardiotoxicity of doxorubicin

34
Q

What type of agent is cetuximab (Erbiux)?

A

Monoclonal Antobody

35
Q

What is the mechanism of action of cetuximab?

A

Binds the EGFR1 (Erb1) receptor

36
Q

What is cetuximab used to treat?

A

EGFR- positive metastatic colorectal cancer

37
Q

What are the major ride effects associated with cetuximab?

A

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

38
Q

What are the minor side effects of cetuximab?

A

Asthenia/ malaise, fever, nausea, constipation, interstitial pneumonitis

39
Q

Is cetuxmab used as a single agent or in combination?

A

There are current clinical trials to see efficacy as a combination therapy regimen…it will probably be used with cisplatin

40
Q

What type of agent is vemurafenib (zelboraf)?

A

Serine/ theonine kinase inhibitor

41
Q

What is the mechanism of action of vemurafenib?

A

It inhibits the oncogenic BRAF kinase

42
Q

What is vemurafenib used to treat?

A

Unresectable stage III or IV or Metastatic melanomas with BRAF mutations

43
Q

Major side effects of vemurafenib?

A

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

44
Q

What are the minor side effects of vemurafenib?

A

cutaneous squamous cell carcinoma, keratoacanthoma, new primary cutaneous melanoma

45
Q

T/F: Clinical trails show that dacarbazine is better in treating unresectable stage III or IV or metastatic melanoma than vemurafenib?

A

False….vemurafenib has been shown to be the superior drug

46
Q

What type of drug is Ipilimumab ( Yervoy)?

A

Human monoclinal antibody

47
Q

What is the mechanism of action of Ipilimumab?

A

Cytotoxic T- lymphocyte antigen 4 inhibitor

It has the ability to stimulate the immune system

48
Q

What is Ipilimumab used to treat?

A

Melanoma

49
Q

What type of drug us dabrafenib (Tafinlar)? What is its mechanism of action?

A

Class: Serine/ Tyrosine kinase inhibitor

Mechanism: Inhibits oncogenic BRAF kinase

50
Q

What is dabrafenib used to treat?

A

Unresectable stage III or IV or metastatic melanomas with BRAF mutations

51
Q

What are the major side effects of dabrafenib?

A

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

52
Q

What are the less common side effects of dabrafenib?

A

Cutaneous squamous cell carcinoma, keratocanthoma, new primary cutaneous melanoma

** Has a greater risk of developing these side effects than Vemurafenib does.

53
Q

What is the mechanism of action of Trametinib (Mekinist)?

A

Inhibits MEK

54
Q

What is Trametinib used to treat?

A

unresectable stage II or IV or metastati melanomas w/ BRAF mutations

55
Q

Major side effects of Trametinib?

A

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

56
Q

Minor side effects of Trametinib?

A

Rash, diarrhea, stomatitis, hypertension, pruritis

57
Q

Which of the following can cause male infertility:

Trametinib
Dabrafenib
Vemurafenib

A

Trametinib

Dabrafenib

58
Q

What is the mechanism of action of hydroxyurea?

A

inhibits ribonucleoside diphosphate reductase

59
Q

What is hydroxyurea used to treat?

A

CML (but was replaced by imatinib)

Polycythemia vera

Essential thrombocythemia

Sickle cell disease (increases fetal Hb)

60
Q

What is the mechanism of action of retinoids?

A

all trans- retinoic acid induces terminal differentiation in malignant immature promyelocytes…which then apoptose

61
Q

What are retinoids used to treat?

A

APL

62
Q

What are the major side effects of retinoids?

A

“Leukocyte activation syndrome”:

increase in WBCs, fever, weight gain, respirator distress, serosal effusion, renal failure

63
Q

What is the combination therapy that retinoids is used in and why?

A

Combined with anthracyclines, and also corticosteroids to block the leukocyte activation syndrome (LAS)

64
Q

What is arsenic trioxide (trisenox) used to treat?

A

relapsed APL

65
Q

What is Thalidomide used to treat?

A

Multiple myeloma and myelodysplastic syndromes

66
Q

What are interferons used to treat?

A

Hairy-cell leukemia, CML and AIDS related Kaposi Sarcoma

Unit 1: Pharm (8 decks)

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