Block 9 Drugs - Sex Hormones Flashcards
Ethinyl estradiol
MOA: Estrogen receptor agonist
Regulates gene transcription
USE: Hormone replacement
Contraception
S/E:
↑ clotting factors
↑ risk of CV events
CI: ↑ risk of breast, endometrial cancer
Contraindicated with CV disease
Unique: Use with progestin for hormone replacement therapy
Fulvestrant
MOA: Estrogen receptor antagonist
Regulates gene transcription
USE: Breast and uterine cancer
S/E: Menopausal symptoms
CI: Don’t use during pregnancy
Unique: Causes degradation of ERα
Levonorgestrel, Etonogestrel
MOA: Progesterone receptor agonist
Regulates gene transcription
USE: Hormone replacement
Contraception
Endometriosis
Unique: Many different progestins available
Tamoxifen
MOA: Selective ER modulator
Regulates gene transcription
USE: Breast cancer
S/E: Menopausal symptoms
CI: ↑ risk of endometrial cancer
Unique: Tissue specific effects on the ER
Mainly used for antagonist properties
Raloxifene
MOA: Selective ER modulator
Regulates gene transcription
USE: Breast cancer
Osteoporosis
S/E: Menopausal symptoms
CI: ↓ risk of endometrial cancer compared to Tamoxifen
Letrozole
MOA: Aromatase inhibitor
USE: Breast cancer
S/E: Menopausal symptoms
Osteoporosis
Anastrozole
MOA: Aromatase inhibitor
USE: Breast cancer
S/E: Menopausal symptoms
Osteoporosis
Flutamide
MOA: Androgen receptor antagonist
USE: Prostate cancer
S/E: GI issues
nausea
tiredness
Bicalutamide
MOA: Androgen receptor antagonist
USE: Prostate cancer
BPH
S/E: GI issues
nausea
tiredness
Testosterone
MOA: Androgen receptor agonist
USE: Hormone replacement therapy
S/E: ↑risk of prostate cancer, testicular atrophy, acne
CI: Derivatives abused for performance enhancement
Finasteride
MOA: 5-α-reductase inhibitor
USE: Prostate cancer
BPH
S/E: Decreases DHT levels
Clomiphene (Clomid)
MOA: Estrogen receptor antagonist in brain
USE: Fertility drug - blocks negative feedback by Estrogen
S/E: Multiple births
Ovarian Enlargement
Nausea
Mifepristone (RU-486)
MOA: Progesterone receptor antagonist
USE: Induce abortion
S/E: Nausea
Vomiting
Abdominal pain
Unique: Doesn’t work after week 7-10
Plan B (a progestin)
MOA: Progesterone receptor agonist
USE: Prevent pregnancy after intercourse
S/E: Nausea
Vomiting
Abdominal pain
Unique: Must be taken within 72 hrs
Ella One
MOA: Progesterone receptor agonist
USE: PRevent pregnancy after intercourse
S/E: Nausea
Vomiting
Abdominal pain
Unique: Works up to 5 days
