ANDROGENS / ESTROGENS

  1. What are the transport mechanisms of Androgens?
    • Testosterone-Estrogen binding protein (30%)
    • Albumin bound (68%)
    • Free (2%)
    • Active fraction = free + albumnin-bound
  2. What are the actions of Testosterone?
    • Androgen receptors
    • Converted to DHT via 5a-reductase
    • Converted to estrogen via aromatase
  3. What's the treatment for Hypogonadism?
    Testosterone supplement
  4. what's the cause of congenital adrenal hyperplasia?
    Tx?
    • 21-Hydroxylase deficiency
    • Tx: hydrocortisone & fludrocortisone
  5. What's the clinical presentation of Andropause?
    Decreased testosterone concentration from 30-70 y/o
  6. What are disorders with testosterone replacement as a treatment?
    Andropause, Catabolic (AIDS) Wasting, Anemia
  7. What kind of drug is Flutamide?
    • Androgen receptor antagonist
    • Sequential rise in LH --> testosterone increase
    • More toxic
  8. What kind of drug is Bicalutamide?
    • Androgen receptor antagonist
    • Sequential rise in LH --> testosterone increase
    • Less toxic
  9. What kind of drug is Cyproterone Acetate?
    • Weak androgen recpetor antagonist
    • Tx for hitsutism in women
  10. What kind of drug is Finasteride?
    • Block type II 5a-reductase --> inhibit DHT production in prostate
    • Tx for BPH
  11. What kind of drug is Dutasteride?
    Block type I &II 5a-reductase --> inhibit DHT production in prostateTx for BPH
  12. What kind of drugs are:
    Estradiol-17, Estriol, Estrone, Premarin
    • Estradiol-17: is the main estrogen produced by the ovary
    • Estriol: a weak estrogen
    • Estrone: a weak estrogen
    • Premarin: from pregnant mare urine
  13. What kind of drug is 17a ethunyl estradiol?
    Orally active estrogen therapy
  14. What kind of drug is equilin?
    • Equine estrogen therapy
    • Conjugation with SO4 results in avoidance of first pass metabolism
  15. What kind of drug is ethinyl estradion/ norethindrone acetate? What's the clinical result?
    • Estrogen and Progesterone combined
    • Decreased risk of colon CA, bone fracture
    • Increased risk of MI, CVA, clots, breast CA
  16. What kind of drug is Tamoxifen?
    • Partial estrogen receptor agonist
    • Agonist: endometrium & Bone
    • Antagonist: Breast
  17. What kind of drug is Raloxifene?
    • Partial estrogen receptor agonist
    • Agonist: Bone
    • Antagonist: Breast & endometrium
  18. What kind of drug is Letrozole?
    • Aromatase inhibitor
    • Tx for breast CA to block local production of estrogen
Author
eschott
ID
77386
Card Set
ANDROGENS / ESTROGENS
Description
Drugs
Updated