GnRH agonist (pulsatile) or GnRH antagonist (continuous)
Pulsatile: Prostate CA, Uterine fibroids, precocious puberty
Which form of testosterone can cause hepatotoxicity?
Danazol - also causes dec HDL, and inc LDL
What are some off-label uses for testosterone?
AIDS related muscle wasting
Blood dycrasias (hemolytic anemia)
What are testosterone drugs used to treat?
Endometriosis and hereditary angioedema - Danazol
Hypogonadism, develop 2˚ sex characteristics, burn recovery - Testosterone/Me-testosterone
BPH, male pattern baldness
Adverse Effects of Androgen Abuse
1. Dec. sperm production
2. Dec. testicular size
What are the natural androgens? (3)
Non-steroidal AR blocker (competitive)
Used w/ Leuprolide for Metastatic Prostate Cancer
Which anti-androgen can cause hepatic failure?
What is the mechanism of action of Sildenafil, Vardenafil, and Tadalafil? What side effect do you need to be careful of?
PDE5 Inhibitor: ↑cGMP - relaxes smooth muscle
Nitrate vasodilator combo hypotension - caution w/ adrenergic R blockers
PGE1 analog - injection/suppository ED
Where is testosterone metabolized?
Liver - high 1st pass effect
What do you use Estrogens to treat? (4)
Hypogonadism or ovarian failure
Menstural abnormalities (+ progestin)
Men w/ androgen-dependant prostate CA
SERM: Antagonist of ER in hypothalamus - block feedback inhibition
↑LH and FSH
Antagonist of Breast ER
Agonist at Uterus and bone ER
Treat and prevent recurrence of ER⊕ Breast CA
Agonist on bone ER
Antagonist at uterus ER
What is hormone replacement therapy used for? What must you not forget?
Relief or prevention of menopausal symptoms or osteoporosis
Add progesterone to avoid endometrial cancer
Anastrozole and Exemestane
Postmenopausal women w/ Breast CA
Competitive inhibitor of progestins at PR
Termination of pregnancy + Misoprostol (PGE1)
Who are OCPs CI in?
Smokers > 35 yo
Hx of thromboembolism and stroke
Hx of estrogen-dependent tumor
β2-agonist - relax uterus
↓contraction frequency during labor
What are ketoconazole and spironolactone used for?
PCOS - Prevent hirsutism
Ketoconazole: Inhibit steroid synthesis (17,20-desmolase)
Spironolactone: Inhibits steroid binding (17α-hydroxylase and 17, 20-desmolase)
α1-antagonist - BPH
Inhibits smooth muscle contraction
*α1A,D selective = prostate only*