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Repro Pharm - Keith > Breast and Endometrial Cancer > Flashcards

Breast and Endometrial Cancer Flashcards

1
Q

MOA of anastrozole

A

aromatase inhibitor. non-steroidal (reversible)

prevents conversion of testosterone to E2

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2
Q

ADE of anastrozole

A

hot flashes, nausea, hair thinning.
joint stiffness
NO effects on adrenal steoids, thyroids or other homones.

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3
Q

MOA of exemestane

A

aromatase inhibitor. steroidal (irreversible)
prevents conversion of testosterone to E2

Exemestane exterminates permanently

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4
Q

ADE of exemestane

A

hot flashes, nausea, hair thinning.
joint stiffness
NO effects on adrenal steoids, thyroids or other homones.

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5
Q

MOA of letrozole

A

aromatase inhibitor. non-steroidal (reversible)

prevents conversion of testosterone to E2

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6
Q

ADE of letrozole

A

hot flashes, nausea, hair thinning.
joint stiffness
NO effects on adrenal steoids, thyroids or other homones.

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7
Q

MOA of raloxifene

A

SERM. ER agonist/antagonist depending on location.
Estrogen effect on bone
Anti-estrogen effect on mammary tissue.
Monthly IM.

Decreases bone resoprtion and lowers serum cholesterol.

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8
Q

ADE of raloxifene

A

retinal degeneration at high doses
BBW for DVT, PE, and stroke
teratogen
NO AGONISM IN ENDOMETRIUM.

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9
Q

MOA of tamoxifen

A 
SERM.  ER agonist/antagonist depending on location. 
Estrogen effect on bone
Anti-estrogen effect on mammary tissue.
Daily per oral.
CYP 2D6

Decreases bone resoprtion and lowers serum cholesterol.

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10
Q

ADE of tamoxifen

A

retinal degeneration at high doeses
teratogen
Black BOX warning for endometrial hypertrophy, vaginal bleeding, ednometiral cancer and DVT or PE and stoke

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11
Q

MOA of toremifene

A

SERM. derivative of tamoxifen with antiestrogenic properties. CYP 3A4

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12
Q

ADE of toremifene

A

Similar to SERMs but also has BLACK BOX warning for prolonged QT interval.

(retinal degeneration at high doeses
teratogen
Black BOX warning for endometrial hypertrophy, vaginal bleeding, ednometiral cancer and DVT or PE.)

CYP 3A4 metabolism

Contraindicated in endometrial cancer and thromboembolism.

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13
Q

MOA of fulvestrant

A

SERD. Pure antagonist with NO estrogenic actions.

Impairs receptor dimerization and decreases ER levels.

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14
Q

ADE of fulvestrant

A

PM symptoms (nausea, asthenia, pain, vasodilation hot flashes and headache)

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15
Q

MOA of goserelin

A

GnRH agonist. Initially increases FSH/LH leading to disease flare, but then negatively inhibits them, decreasing estradiol to PM levels within 2-4 weeks.

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16
Q

ADE of goserelin

A

initial transiet disease flare of bone pain from mets, hypercalcemia, breast enlargment and tenderness.

well tolerated long term therapy

PM side effects: hot flashes, down libido, vaginal dryness, emotional, depression, gynecomastia, decreased bone density.

17
Q

MOA of pertuzumab

A

Her-2 antibody for dimerization domain. Given IV with long half-life

18
Q

ADE of pertuzumab

A

BBW for pregnancy!

hypersensitivity reactions, GI upset, asthenia, blood dyscrasias, fatigue.

Alopecia, loss of appetite
decreased LVEF
neutropenia and leukopenia.

19
Q

MOA of trastuzumab

A

Her-2 antibody for extracellular domain

20
Q

ADE of trastuzumab

A 
peripheral edema, rash, weight gain, URTIs
BBW for:
Cardiomyopathy, HF
RENAL FAILURE
HEPATOTOXICITY
pneumonia and respiratory failure.
CID with pregancy.
21
Q

MOA of lapatinib

A

TKI. Prevents downstream signalling of HER1 and HER2. extensive hepatic metabolism and CYP3A4.

22
Q

ADE of lapatinib

A

BBW for liver disease. elevates LFTs.
GI issues, anemia, thrombocytopenia, HAND-foot Syndrome, rash
Interstitial lung disease
QT prolongation

23
Q

MOA of everolimus

A

mTOR inhibitor. mTOR regulates cell proliferation and angiogneneis. Drug binds to FKBP-12 and forms a 3-2ay complex with mTOR to inhibit it.

24
Q

ADE of everolimus

A

BBW for risk of opportunistic infections and neoplasia.

Blood dyscrasia, hyperglycemia and hyperlipidemia, high TGs and elevated creatinine and liver enzymes

NV, diarrhea, pain, constipation.

25
Q

How can resistance to tamoxifen develop?

A 
variable expression of ERa or ERb.
interference with binding
alternative splicing of ER mRNA variants
modulation of ER expression and function by EGFR1 and EGFR2 growth factors.
CYP2D6 genotype.
26
Q

Which drug should a pre-menopausal women be given?

A

tamoxifen.

If post-menopausal switch to other drugs.

Repro Pharm - Keith (11 decks)

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