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Repro > Breast Cancer Pharm > Flashcards

Breast Cancer Pharm Flashcards

(53 cards)

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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?

23
Q

What is the route of administration of Goserelin?

Study These Flashcards
A

SC every 28 days in the upper abdominal wall

24
Q

What is the MOA of Goserelin?

Study These Flashcards
A

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

25
What are the adverse effects of Goserelin?
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
What drug causes an initial transient disease flare involving bone pain, hypercalcemia, & breast pain/tenderness?
Goserelin
27
What are the Her2/neu antibodies?
Pertuzumab, Trastuzumab, & Ado-Trastuzumab Emtasine
28
What is the route of administration of the Her2/neu antibodies?
IV every 21 days
29
What is the MOA of pertuzumab?
binds extracellular dimerization domain blocking ligand-dependent heterodimerization of HER2 w/ other epidermal growth factor receptors
30
What is the MOA of Trastuzumab?
Binds the juxtaglomerular region of the extracellular domain of HER2
31
What is the MOA of Ado-Trastuzumab Emtasine?
Binds to the HER2 receptor & allows the thioester-linked chemotherapeutic to act on microtubules upon internalization preventing cell division
32
What are the adverse effects of Pertuzumab?
Gi upset, asthenia, blood dyscrasias, fatigue, alopecia, loss of appetite, decreased LVEF, neutropenia, leukopenia
33
What drugs are often used in combination with a taxane to treat breast cancer?
Pertuzumab & Trastuzumab
34
What are the adverse effects of Traztuzumab?
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
What are the BBWs for Pertuzumab?
pregnancy
36
What are the BBWs for Trastuzumab?
cardiomyopathy, infusion reactions, pregnancy, respiratory distress syndrome, & respiratory insufficiency
37
What are the BBWs for Ado-Trastuzumab Emtasine?
heart failure, hepatic disease, pregnancy, & ventricular dysfunction
38
What oral TKI treats breast cancer?
Lapatinib
39
MOA of Lapatinib?
inhibits HER1 & HER2 by binding the intracellular domain of ErbB1 & ErbB2 receptors & competes with ATP ultimately preventing receptor activation
40
What are the adverse effects of Lapatinib?
Gi issues, anemia, thrombocytopenia, hand-foot syndrome, rash, HA, backache, interstitial lung disease, pneumonitis, QT prolongation
41
What breast cancer drug has extensive hepatic metabolism and requires monitoring of LFTs?
Lapatinib
42
What TKI has a BBW for liver disease?
Lapatinib
43
What mTOR inhibitor is given orally to treat breast cancer?
Everolimus
44
What is the MOA of Everolimus?
Binds FKBP12 to block mTOR action thus preventing cell proliferation & survival
45
What breast cancer drug has the serious adverse effects of increased opportunistic infections, neoplasia, lymphoma, & SCC?
Everolimus
46
What breast cancer drug can inhibit CYP3A4, CYP2D6, & P-gp?
Everolimus
47
What 2 drugs are used to treat endometrial cancer?
Medroxyprogesterone & Megestrol
48
What is the MOA of Medroxyprogesterone?
Binds progestin receptors & blocks GnRH release
49
What ist he MOA of Megestrol?
Suppresses pituitary LH release, enhances estrogen degradation, & promotes differentiation/maintenance of endometrial tissue
50
What are the adverse effects of medroxyprogesterone?
amenorrhea, anorexia, edema, weakness
51
What are the adverse effects of megestrol?
weight gain, hot flashes, malaise, asthenia, leathery, diaphoresis, rash, thrombophlebitis, thrombo- or pulmonary embolism; tumor flare, & hypercalcemia in pts w/ bone metastases
52
What endometrial cancer drug can also be used to treat breast cancer or anorexia/cachexia?
Megestrol
53
What breast cancer drug has the adverse effects of hyperglycemia, hyperlipidemia, & Hypertriglyceridemia?
Everolimus

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