Breast Cancer and Uterine Drugs Flashcards Preview

Pharm Exam IV > Breast Cancer and Uterine Drugs > Flashcards

Flashcards in Breast Cancer and Uterine Drugs Deck (26):
1

oxytocin (indication, mech, toxicity)

synthetic version of endogenous hormone.
Indication: labor induction, augmentation of dysfunctional labor, control post-partum hemorrhage.
Mech: binds to oxytocin receptor, alters transmembrane potential, increasing uterine (smooth muscle) contraction.
Note: uterus is more sensitive to oxytocin during gestation, and even more during labor.
Tox: Uterine tachysystole

2

oxytocin (indication, mech, toxicity)

synthetic version of endogenous hormone.
Indication: labor induction, augmentation of dysfunctional labor, control post-partum hemorrhage.
Mech: binds to oxytocin receptor, alters transmembrane potential, increasing uterine (smooth muscle) contraction.
Note: uterus is more sensitive to oxytocin during gestation, and even more during labor.
Tox: Uterine tachysystole

3

Misoprostol (indication, mech, tox)

prostaglandin used off-label to induce labor, prevent post-partum hemorrhage; induce contractions after missed or incomplete miscarriage in early pregnancy.
CI: prev C-section

4

Methylergometrine (indication, toxicity)

used to prevent post-partum hemorrhage after dilation and curettage. Vasoconstrictive- increases uterine motor activity and leads to sustained contraction at high doses.
Tox: Do not use if HTN.

5

Tocolytic agents: def, indication

Relaxes uterus. Used to delay preterm delivery for administration of corticosteroids for fetal lung development.

6

Tocolytic agents: examples

Mg Sulfate; Tertbutaline; Ca channel blockers, NSAIDs

7

Magnesium sulfate

Used to prevent seizures in preeclampsia. Neuroprotective for fetus. Mech is Ca-channel blockade.

8

Magnesium sulfate

Used to prevent seizures in preeclampsia. Neuroprotective for fetus. Mech is Ca-channel blockade.

9

Tamoxifen (indication, mech, tox)

for ER+ breast cancer in pre AND post menopausal women. Mechanism is blockade of alpha ER in breast (partial agonist in endometrium).
Tox: menopausal sx; vaginal discharge, cataracts, nausea. Black Box: Inc. risk of DVT, endometrial cancer
30-40% become resistant in 5 yrs (down regulation of ER-alpha)

10

Tamoxifen (indication, mech, tox)

for ER+ breast cancer in pre AND post menopausal women. Mechanism is blockade of alpha ER in breast (partial agonist in endometrium).
Tox: menopausal sx; vaginal discharge, cataracts, nausea. Black Box: Inc. risk of DVT, endometrial cancer
30-40% become resistant in 5 yrs (down regulation of ER-alpha)

11

Cyp2D6 and tamoxifen

Tamoxifen is activated and metabolized by Cyp2D6, for which there are many polymorphisms. Poor metabolizers had worse survival than other genotypes. FDA used to recommend screening, but no longer does.

12

Tamoxifen (indication, mech, tox)

for ER+ breast cancer in pre AND post menopausal women. Mechanism is blockade of alpha ER in breast (partial agonist in endometrium).
Tox: menopausal sx; vaginal discharge, cataracts, nausea. Black Box: Inc. risk of DVT, endometrial cancer
30-40% become resistant in 5 yrs (down regulation of ER-alpha)
CI if Hx of DVT, PE, pregnancy. do not combine w/ SSRIs (inhibit cyp2D6).

13

Cyp2D6 and tamoxifen

Tamoxifen is activated and metabolized by Cyp2D6, for which there are many polymorphisms. Poor metabolizers had worse survival than other genotypes. FDA used to recommend screening, but no longer does.

14

Raloxifene

SERM to treat breast cancer in POST menopausal women with ER+ cancer only. Less efficacious than tamoxifen, but not a pro-drug so does not require activation by CYP2D6.
**Lower risk of endometrial cancer
CI in DVT, pregnancy.

15

Anastrozole

Indicated for Tx of ER+ breast cancer in POST-menopausal women (only)
REVERSIBLE Aromatase inhibitor- reduces conversion of testosterone to estrogen.
Used as an adjuvant monotherapy for up to 5 years (after 5 years of Tx with a SERM).

Tox: Hot flashes, osteopenia, osteoporosis.

Won't work on pre-menopausal women due to effect of functional ovaries.

16

Anastrozole

Indicated for Tx of ER+ breast cancer in POST-menopausal women (only)
REVERSIBLE Aromatase inhibitor- reduces conversion of testosterone to estrogen.
Used as an adjuvant monotherapy for up to 5 years (after 5 years of Tx with a SERM).

Tox: Hot flashes, osteopenia, osteoporosis.

Won't work on pre-menopausal women due to effect of functional ovaries.

17

Exemestane

Indicated for Tx of ER+ breast cancer in POST-menopausal women (only)
IRREVERSIBLE Aromatase inhibitor- reduces conversion of testosterone to estrogen.
Used as an adjuvant monotherapy for up to 5 years (after 5 years of Tx with a SERM).

Tox: Hot flashes, osteopenia, osteoporosis.

Won't work on pre-menopausal women due to effect of functional ovaries.

18

Leuprolide

Indicated for PREmenopausal ER+ breast cancer. Can give with SERM.

Mech: disrupts normal pulsatile stimulatoin of GnRH receptor leading to desensitization. Result is decreased FSH, LH and decreased Estrogen synthesis.

Tox: hot flashes, osteoporosis, sexual dysfunction, CI inpregnancy. Note: early transient increase in FSH and LH worsens cancer.

19

Trastuzumab

Treatment of HER2+ breast cancer.
Mech: MAb against HER2 receptor, prevents dimerization, RAS-MapK pathway. Sensitizes cell for cytotoxic therapy, antibody-dependent cellular cytotoxicity

Tox: infusion rxn/hypersensitivity is COMMON (tx w/ acetaminophen, diphenhydramine, meperidine), nephrotic syndrome, interstitial lung disease; black box warning for cardiomyopathy, fatal acute resp. syndrome.

20

Trastuzumab

Treatment of HER2+ breast cancer.
Mech: MAb against HER2 receptor, prevents dimerization, RAS-MapK pathway. Sensitizes cell for cytotoxic therapy, antibody-dependent cellular cytotoxicity

Tox: infusion rxn/hypersensitivity is COMMON (tx w/ acetaminophen, diphenhydramine, meperidine), nephrotic syndrome, interstitial lung disease; black box warning for cardiomyopathy, fatal acute resp. syndrome.

21

Trastuzumab-emtansine

"Armed" monoclonal antibody for Tx of HER2+ BC resistant to trastuzumab alone. Ab is combined with DM1(emantasine) which is a mitotic spindle poison that is endocytosed after Ab binding. Binds and inhibits alpha tubulin.
Tox: hepatotoxicity, cardiotoxicity, embryotoxicity

22

Trastuzumab-emtansine

"Armed" monoclonal antibody for Tx of HER2+ BC resistant to trastuzumab alone. Ab is combined with DM1(emantasine) which is a mitotic spindle poison that is endocytosed after Ab binding. Binds and inhibits alpha tubulin.
Tox: hepatotoxicity, cardiotoxicity, embryotoxicity

23

Pertuzumab

Tx for HER2+ breast cancer, used in conjunction with trastuzumab and docetaxel.

Mech: monoclonal antibody that binds to HER2 extracellular domain an dprevent ligand dependent dimerization with other HER2 family members.

Tox: cardiotoxicity, hypersensitivity (anaphylaxis), embryotoxic.

24

Pertuzumab

Tx for HER2+ breast cancer, used in conjunction with trastuzumab and docetaxel.

Mech: monoclonal antibody that binds to HER2 extracellular domain an dprevent ligand dependent dimerization with other HER2 family members.

Tox: cardiotoxicity, hypersensitivity (anaphylaxis), embryotoxic.

25

MammaPrint

genetic screen for breast cancer reoccurance risk: approved for pts under 61 w/ LN neg breast cancer, w/ tumor

26

Oncotype Dx

Test for LN negative ER positive OR LN positive ER positive AND post-menopausal who will be receiving adjuvant tamoxifen