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Repro > Breast Cancer Pharm > Flashcards

Breast Cancer Pharm Flashcards

1
Q

What are the aromatase inhibitors?

A

Anastrozole, Exemestane, Letrozole

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2
Q

MOA of aromatase inhibitors?

A

Blocks CYP19A1 mediated production of estrone & estradiol; actions are highly specific & no effects are observed on other organs or hormones

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3
Q

Adverse effects of aromatase inhibitors?

A

hot flashes, nausea, hair thinning, arthralgia, diarrhea

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4
Q

Route of administration of aromatase inhibitors?

A

oral

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5
Q

Which aromatase inhibitors are reversible?

A

Anastrozole & Letrozole

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6
Q

Which aromatase inhibitors are irreversible?

A

Exemestane

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7
Q

What are the SERMs?

A

Raloxifene, Tamoxifen, Toremifene

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8
Q

MOA of Raloxifene?

A

ER agonist/antagonist; estrogen effect on bone & anti-estrogen effect on mammary tissue

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9
Q

MOA of tamoxifen?

A

ER agonist/antagonist; estrogen effect on bone & anti-estrogen effect on mammary tissue

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10
Q

MOA of toremifene?

A

Derivative of tamoxifen with antiestrogenic properties

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11
Q

Route of administration of the SERMs?

A

Raloxifene is give IM monthly; Tamoxifen & Toremifene are given orally daily

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12
Q

Adverse effects of Raloxifene?

A

teratogen; decreases bone metabolism, serum cholesterol, & LDL; retinal degeneration (high doses); increases apolipoprotein A1

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13
Q

Adverse effects of Tamoxifen?

A

teratogen; decreases bone metabolism, serum cholesterol, & LDL; retinal degeneration (high doses); increases apolipoprotein A1

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14
Q

Adverse effects of Toremifene?

A

QT prolongation; teratogen

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15
Q

Which SERMs have a BBW for DVT, PE, & stroke?

A

Raloxifene & Tamoxifen

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16
Q

Which SERM has a BBW for endometrial hypertrophy, endometrial cancer, & vaginal bleeding?

A

Tamoxifen

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17
Q

Which SERM undergoes CYP3A4 metabolism?

A

Toremifene

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18
Q

What drug is a SERD?

A

Fulvestrant

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19
Q

MOA of Fulvestrant?

A

Binds ER but carries a bulky substituent that prevents crucial dimerization of ER in the nucleus thus down-regulating ER expression

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20
Q

Adverse effects of Fulvestrant?

A

nausea, asthenia, pain, vasodilation (hot flashes), HA

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21
Q

What breast cancer drug is a GnRH agonist?

A

Goserelin

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22
Q

What is the route of administration of fulvestrant?

A

IM (monthly)

23
Q

What is the route of administration of Goserelin?

A

SC every 28 days in the upper abdominal wall

24
Q

What is the MOA of Goserelin?

A

down-regulation of GnRH receptor on the pituitary gland ultimately decreasing the production of FSH & LH

25
Q

What are the adverse effects of Goserelin?

A

amenorrhea, hot flashes, decreased libido, vaginal dryness, emotional lability, depression, sweating, gynecomastia, HA, N/V, peripheral edema, lethargy, anorexia, decreased bone density, osteopenia/osteoporosis

26
Q

What drug causes an initial transient disease flare involving bone pain, hypercalcemia, & breast pain/tenderness?

A

Goserelin

27
Q

What are the Her2/neu antibodies?

A

Pertuzumab, Trastuzumab, & Ado-Trastuzumab Emtasine

28
Q

What is the route of administration of the Her2/neu antibodies?

A

IV every 21 days

29
Q

What is the MOA of pertuzumab?

A

binds extracellular dimerization domain blocking ligand-dependent heterodimerization of HER2 w/ other epidermal growth factor receptors

30
Q

What is the MOA of Trastuzumab?

A

Binds the juxtaglomerular region of the extracellular domain of HER2

31
Q

What is the MOA of Ado-Trastuzumab Emtasine?

A

Binds to the HER2 receptor & allows the thioester-linked chemotherapeutic to act on microtubules upon internalization preventing cell division

32
Q

What are the adverse effects of Pertuzumab?

A

Gi upset, asthenia, blood dyscrasias, fatigue, alopecia, loss of appetite, decreased LVEF, neutropenia, leukopenia

33
Q

What drugs are often used in combination with a taxane to treat breast cancer?

A

Pertuzumab & Trastuzumab

34
Q

What are the adverse effects of Traztuzumab?

A

Gi upset, asthenia, blood dyscrasias, fatigue, peripheral edema, rash, weight gain, dizziness, URTIs, pharyngitis, fatigue, cardiomyopathy, heart failure, renal failure, hepatotoxicity, pneumonia, respiratory failure

35
Q

What are the BBWs for Pertuzumab?

A

pregnancy

36
Q

What are the BBWs for Trastuzumab?

A

cardiomyopathy, infusion reactions, pregnancy, respiratory distress syndrome, & respiratory insufficiency

37
Q

What are the BBWs for Ado-Trastuzumab Emtasine?

A

heart failure, hepatic disease, pregnancy, & ventricular dysfunction

38
Q

What oral TKI treats breast cancer?

A

Lapatinib

39
Q

MOA of Lapatinib?

A

inhibits HER1 & HER2 by binding the intracellular domain of ErbB1 & ErbB2 receptors & competes with ATP ultimately preventing receptor activation

40
Q

What are the adverse effects of Lapatinib?

A

Gi issues, anemia, thrombocytopenia, hand-foot syndrome, rash, HA, backache, interstitial lung disease, pneumonitis, QT prolongation

41
Q

What breast cancer drug has extensive hepatic metabolism and requires monitoring of LFTs?

A

Lapatinib

42
Q

What TKI has a BBW for liver disease?

A

Lapatinib

43
Q

What mTOR inhibitor is given orally to treat breast cancer?

A

Everolimus

44
Q

What is the MOA of Everolimus?

A

Binds FKBP12 to block mTOR action thus preventing cell proliferation & survival

45
Q

What breast cancer drug has the serious adverse effects of increased opportunistic infections, neoplasia, lymphoma, & SCC?

A

Everolimus

46
Q

What breast cancer drug can inhibit CYP3A4, CYP2D6, & P-gp?

A

Everolimus

47
Q

What 2 drugs are used to treat endometrial cancer?

A

Medroxyprogesterone & Megestrol

48
Q

What is the MOA of Medroxyprogesterone?

A

Binds progestin receptors & blocks GnRH release

49
Q

What ist he MOA of Megestrol?

A

Suppresses pituitary LH release, enhances estrogen degradation, & promotes differentiation/maintenance of endometrial tissue

50
Q

What are the adverse effects of medroxyprogesterone?

A

amenorrhea, anorexia, edema, weakness

51
Q

What are the adverse effects of megestrol?

A

weight gain, hot flashes, malaise, asthenia, leathery, diaphoresis, rash, thrombophlebitis, thrombo- or pulmonary embolism; tumor flare, & hypercalcemia in pts w/ bone metastases

52
Q

What endometrial cancer drug can also be used to treat breast cancer or anorexia/cachexia?

A

Megestrol

53
Q

What breast cancer drug has the adverse effects of hyperglycemia, hyperlipidemia, & Hypertriglyceridemia?

A

Everolimus

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