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Flashcards in Voight Targeted 2 Deck (15)
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1
Q

Leuprolide

A

Lupron
GnRH agonist – stimulate negative feedback mechanism; 2-3 weeks to realize decrease in testosterone production
MOA: GnRH agonist —> Decreased LH/FSH —> Decreased Testosterone —> Decreased Prostate Cancer Growth

TOX: ECG changes, peripheral edema, hot flashes, weakness, Bone pain

2
Q

Goserelin

A

Zoladex
GnRH agonist – stimulate negative feedback mechanism; 2-3 weeks to realize decrease in testosterone production
MOA: GnRH agonist —> Decreased LH/FSH —> Decreased Testosterone —> Decreased Prostate Cancer Growth

TOX: ECG changes, peripheral edema, hot flashes, weakness, Bone pain

3
Q

Degarelix

A

Firmagon
GnRH antagonist – directly blocks pathway
MOA: GnRH antagonist —> Decreased LH/FSH —> Decreased Testosterone —> Decreased Prostate Cancer Growth

TOX: injection related reactions (SubQ), hot flashes, weight gain

4
Q

Flutamide

A

Eulexin
MOA: Block androgen receptor (competitive inhibitor)
↑ estrogen release (potential for gynecomastia)
TOX: gynecomastia, ↓ libido, diarrhea, nausea, liver abnormalities

5
Q

Nilutamide

A

Nilandron
single daily oral dose is effective

MOA: Block androgen receptor (competitive inhibitor)
↑ estrogen release (potential for gynecomastia)
TOX: gynecomastia, ↓ libido, diarrhea, nausea
visual disturbances, alcohol intolerance

6
Q

Bicalutamide

A

Casodex - highest affinity = lowest risk of toxicities (out of Flutamide, Nilutamide, Bicalutamide)
single daily oral dose is effective

MOA: Block androgen receptor (competitive inhibitor)
↑ estrogen release (potential for gynecomastia)
TOX: gynecomastia, ↓ libido, diarrhea, nausea

7
Q

Enzalutamide

A

Xtandi - strongest/highest affinity out of the 4
Single once daily dose
MOA: Androgen receptor (AR) competitive inhibitor —> Blocks trans-location of AR to nucleus and interaction of AR with DNA
- Avoid use with CYP2C8, CYP3A4 inhibitors
TOX: Risk of seizures (CNS penetration – through GABA(a) inhibition)
Pregnancy category X

8
Q

Abiraterone Acetate

A

Zytiga - inhibitor of steroid synthesis - oral - once daily
[adrenal gland, testes, prostate cancer cells]
MOA: inhibits CYP17A1 (17α-hydroxylase and 17,20-lyase) —> ↓ Testosterone production —> decreases in levels of DHEA, testosterone, and dihydrotestosterone (DHT).

  • highly protein bound (>99%)
  • metabolised in the liver by CYP3A4 and SULT2A1 to inactive metabolites
  • excreted in feces (~88%) and urine (~5%)

TOX: Joint swelling, hypokalemia, muscle discomfort, Hypertension, Hot flushes

9
Q

Estramustine

A

Emcyt
Selective uptake into prostate cells (decrease in cytotoxic effects of non-prostate cells)

MOA: Binds to β-tubulin and microtubules —> Microtubule disassembly —> arrests prostate cancer cells in the G2/M phase

TOX: Myelosuppression

SEs: Hypercalcemia
HSR → angioedema
Gynecomastia
***↑ risk of thrombosis***
Fluid retention
10
Q

Tamoxifen

A

Nolvadex (tablets) / Soltamox (oral solution)
- competitive partial agonist inhibitor of estradiol at the estrogen receptor
MOA: Formation of active metabolites (through 2D6) — N-desmethyltamoxifen + 4-hydroxytamoxifen (more potent for ER)

  • Antagonist in breast tissue
  • Agonist in bone, liver and endometrium
  • – Increase in bone density
  • – Decrease production of cholesterol in liver
  • – Increase proliferation of endometrial cells -> endometrial/ovarian cancer

TOX: Increased risk of thrombosis, hot flashes, menstrual irregularities, vaginal bleeding

11
Q

Raloxifene

A

Evista
- competitive partial agonist inhibitor of estradiol at the estrogen receptor

MOA: Antagonist in breast and uterus (endometrial cells)
— Compared to tamoxifen

Agonist in bone, liver

  • – Increase in bone density
  • – Decrease production of cholesterol in liver

TOX: Increased risk of thrombosis, hot flashes, leg cramps

12
Q

Megestrol

A
Megace
- Inhibition of  Pituitary gonadotropin release (↓ estrogen secretion)
- Agonist bind to progesterone receptor
- Turns off estrogen-responsive genes
- Partial Agonist at androgen receptor
Antagonist = anti-androgenic effect
- Agonist at glucocorticoid receptor
--- Cushing’s
--- Adrenal insufficiency

-Renal excretion

Toxicity – weight gain, thromboembolism, nausea, vomiting, glucose intolerance
pregnancy category X

13
Q

Anastrozole

A
Arimidex
- Non-steroidal
MOA: Aromatase (P4502C19) inhibitors (decreased estrone/estradiol)
***Placenta, ovaries
- Bind reversibly to heme

TOX: vaginal bleeding, hot flashes, hair thinning, nausea
Decrease bone density

Letrozole (hot flashes, hair thinning, nausea)

14
Q

Letrozole

A

Femara
MOA: Aromatase (P4502C19) inhibitors (decreased estrone/estradiol)
***Placenta, ovaries
- Bind reversibly to heme

TOX: hot flashes, hair thinning, nausea

15
Q

Exemestane

A

Aromasin
- Aromatase inhibitor (P4502C19)

MOA: ***irreversibly inactivates P4502C19 via reactive intermediate formation

TOX: vaginal bleeding, hot flashes, nausea, fatigue