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Repro Pharm > Breast & Endometrial Cancer > Flashcards

Breast & Endometrial Cancer Flashcards

1
Q

MOA of Aromatase Inhibitors

A

Aromatase; Blocks production of estrone & estradiol

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2
Q

Aromatase Inhibitors (3)

A

Anastrozole, Exemestane, Letrozole

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3
Q

Aromatase Inhibitor Tox

A

Hot flashes; nausea; hair thinning; NO effect on adrenal steroids, thyroid, or other hormones; More arthralgia & diarrhea than tamoxifen but fewer gynecologic symptoms

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4
Q

Aromatase Inhibitors Metabolism

A

Hepatic

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5
Q

SERMs (3)

A

Raloxifene, Tamoxifen, Toremifene

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6
Q

Raloxifene MOA

A

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

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7
Q

Tamoxifen MOA

A

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

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8
Q

Toremifene MOA

A

SERM; Tamoxifen derivative w/ anti-estrogenic properties

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9
Q

Raloxifene Tox & BBW

A

Increased bone mineral density; Decreases serum cholesterol, LDL, & lipoproteins; Increases apolipoprotein-A1; Retinal degeneration at high doses

BBW= Thromboembolic Dz (DVT/PE) & Stroke

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10
Q

Raloxifene Admin

A

Monthly IM

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11
Q

SERMs & Pregnancy?

A

No, teratogens

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12
Q

Tamoxifen Tox & BBW

A

Increased bone mineral density; Decreases serum cholesterol, LDL, & lipoproteins; Increases apolipoprotein-A1; Retinal degeneration at high doses

BBW= Endometrial Hypertrophy, vaginal bleeding, endometrial cancer, thromboembolic dz (DVT/PE), stroke

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13
Q

Tamoxifen Admin

A

Daily PO

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14
Q

Toremifene Tox & BBW

A

Similar AE’s to tamoxifen; Avoid w/ Hx of endometrial cancer/hyperplasia & thromboembolic dz

BBW= QT Prolongation (avoid in pre-existing conditions);

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15
Q

Toremifene Admin

A

Daily PO

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16
Q

Toremifene DDI

A

Avoid w/ CYP3A4 inhibitors

17
Q

SERD (1)

A

Fulvestrant

18
Q

Fulvestrant MOA

A

SERD; Pure antagonist, no estrogenic effects; Bulky substituent prevents dimerization of ER’s in nucleus=sustained downregulation of ER expression

19
Q

Fulvestrant Tox

A

Postmenopausal symptoms: nausea, asthenia, pain, vasodilation (hot flashes), and h/a

20
Q

Fulvestrnat PK

A

Hepatic metabolism; monthly IM-sustained plasma levels

21
Q

Fulvestrnat use

A

Tx for ER+ metastatic BC in PM women w/ dz progression following anti-estrogen therapy

22
Q

Trastuzumab MOA

A

HER2/neu Antibody; Binds to the juxtaglomerular region of the extracellular domain of HER2

23
Q

Trastuzumab Tox

A

Caution- HSR w/ initial dose; Common=GI upset, asthenia, blood dyscrasias, fatigue, peripheral edema, rash, wt gain, dizziness, URTIs, pharyngitis; Rare= cardiomyopathy & HF, renal failure, hepatotox, pneumonia, respiratory failure; BBWs

24
Q

Trastuzumab BBW

A

BBWs=Cardiomyopathy, Infusion Rxns, Pregnancy, Respiratory Distress Syndrome, Respiratory Insufficiency

25
Q

Lapatinib MOA

A

TKI

26
Q

Lapatinib Tox

A

Common= GI tox, anemia, thrombocytopenia, hand-foot syndrome, rash pain, h/a, backache; Serious= interstitial lung dz/pneumonitis, QT prolongation

27
Q

Lapatinib PK

A

Extensive hepatic metabolism- 3A4 + 3A5

28
Q

Lapatinib DDI

A

CI’d w/ concurrent use of drugs that have AE’s associated w/ pulmonary tox & QT prolongation

29
Q

Lapatinib BBW

A

BBW=Liver Dz (b/c will lead to increased drug levels)- LFT monitoring required

30
Q

Everolimus MOA

A

mTOR Inhibitor; Prevents cell proliferation & survival

31
Q

Everolimus Tox & BBW

A

Non-infectious pneumonitis (sometimes fatal); Blood dyscrasias, hyperglycemia, hyperlipidemia, hypertriglyceridemia, elev creatinine, elev liver enzymes; N/V, diarrhea, pain, constipation

Also BBW - opportunistic infections & neoplasia

32
Q

Everolimus PK

A

3A4 & Pgp substrate; Inhibits 3A4, 2D6, & Pgp

33
Q

What should you monitor when a patient is on everolimus

A

Monitor: blood glucose, CBC w/ differential, LFTs, serum bilirubin-creatinine-lipid profile- phosphate-triglyceride

34
Q

Everolimus use

A

Tx in combo w/ Exemestane for advanced ER+/HER2- tumors

35
Q

Which AI is steroidal, which non-steroidal?

A

Steroidal - exemestane

non-steroidal - letrozole, anastrazole

36
Q

Non steroidal AI is reversible or irreversible?

A

reversible inhibitor

37
Q

Steroidal AI is reversible or irreversible?

A

irreversible

38
Q

Which drugs are given in combo with a taxane?

A

Pertuzumab & Trastuzumab

Repro Pharm (7 decks)

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