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1.11
Androgens
| Term | Definition |
|---|---|
| What is the principal androgen in males and females | testosterone |
| principle sites of production for testosterone are: | 1. gonads 2. adrenal gland |
| Other androgens in body: | 1. dihydrotestosterone (DHT) 2. androstenedione 3. dehydroepiandrosterone (DHEA) |
| biosynthesis of androgens: 85% of circulating estradiol in men is from the conversion of ___________ to _________ in the _________and _________ | testosterone to estradiol (E2) in the liver and adipose tissue |
| MOA of Androgens: Enzyme that converts testosterone to DHT | 5a reductase (type 2) |
| MOA of Androgen: DHT (or testosterone) binds to: | intracellular androgen receptor (DHT has a much higher affinity) |
| MOA of Androgen: Hormone-receptor complex is transported to __________ and binds to: | nucleus and binds to androgen response elements (ARE) on DNA |
| MOA of Androgen: final step of MOA | increase mRNA transcription and translation into specific proteins |
| enzymatic reaction: testosterone -------(5a-reductase)-----> dihydrotestosterone | proceeds to androgen receptor effects: 1. external genitalia (differentiation during gestation, maturation in puberty, adulthood prostatic diseases) 2. hair follicles (increased growth during puberty) |
| direct reaction: testosterone ------> androgen receptor | effects: 1. internal genitalia (wolffian development during gestation) 2.skeletal muscle (increase mass and strength in puberty) 3. erythropoiesis (bone??) |
| enzymatic reaction: testosterone -------(CYP19 aromatase)-----> estradiol | proceeds to estrogen receptor effects: 1. bone (epiphyseal closure increased density) 2. Libido?? |
| physiological actions of androgen (gestational period) | development and differentiation of male reproductive tract during embryonic development |
| physiological actions of androgen (during puberty) | development of secondary sex characteristics |
| physiological actions of androgen (anabolic effects during puberty) | closure of epiphyses (last event in puberty) through estrogen and estrogen receptors |
| physiological actions of androgen through life (2): | 1. stimulation of RBC production 2. induce and maintain spermatogenesis |
| anabolic steroid: | 1. bind to the same receptor 2. all anabolic steroids' are also androgenic 3. oral 17a-alkulated androgens |
| anabolic steroids: Effects | 1. increase protein synthesis (increase muscle mass, strength, masculine appearance, decrease fatigue) 2. anticatabolic activity (blocks cortisone, increase body mass) 3. anabolic effect(new proteins in muscle cells) |
| anabolic steroids': Effects (males) | 1. enhances masculinity of appearance 2. gynecomastia 3. testicular atrophy (decreased testosterone production) 4. acne 5. acceleration of male-pattern baldness |
| anabolic steroids': Effects (females) | 1. acne 2. increased facial/body hair (hirsutism) 3. coarsening of skin 4. male-pattern baldness 5. deepened voice 6. breast atrophy (shrinking of breasts) |
| anabolic steroids': Effects (youth) | premature epiphyseal closure (decrease height) |
| anabolic steroids': Effects (cardiovascular) | increases cardiac risk factors (ex: hypertension, increased LDL/HDL ration) |
| anabolic steroids': Effects (hepatic) | elevated liver enzymes |
| anabolic steroids': Effects (central acting on body) | affects aggression, sexuality, cognition, emotion and personality |
| therapeutic uses of androgens (5) | 1. male hypogonadism (testosterone deficiency) 2. male senescence or andropause (age related testosterone deficiency) 3. female hypogonadism (serum level testosterone below normal) 4. athletic performance 5. erectile dysfunction |
| Androgen preparations: side effects | 1. decrease in testicle size 2. increased production of RBC 3. gynecomastia (increased breast gland tissue-men) 4. hepatotoxicity 5. decrease HDL, increase LDL 6. advancement of benign prostatic hypertrophy/prostate cancer |
| Androgen preparations: Side effects in women and children | 1. increased facial and body hair 2. male pattern baldness 3. acne 4. children: enlargement of sex organs 5. prepubertal teens: premature closure of epiphyses and stunted growth |
| Androgen preparations: topical skin gels (3) | 1. AXIRON (transdermal solution) 2. ANDROGEL (transdermal gel) 3. TESTIM (transdermal gel) |
| Androgen preparations: testosterone esters (2) IM injection | 1. testosterone cypionate (DEPO-TESTOSTERONE) 2. Testosterone enanthate (DELATESTRYL) |
| Androgen preparations: 17-a-alkylated androgen | 1. Oxandrolone (OXANDRIN) androgenic: anabolic activity- 1:3-1:13 2. oxymetholone (ANADROL-50) |
| Androgen preparations: miscellaneous androgens | Danazol (DANOCRINE) |
| GnRH AGONIST (drugs) | Goserelin, Histrelin |
| MOA of GnRH AGONIST | -desensitize GnRH signaling pathways -non-pulsatile (constant) administration will inhibit gonadotropin secretion (LH & FSH) - initially cause a flare of LH and FSH followed by decrease levels leaving testosterone at near castration levels |
| therapeutic use of GnRH AGONIST | prostate cancer |
| GnRH ANTAGONIST (drugs) | Ganirelix, Cetrorelix |
| GnRH ANTAGONIST MOA | competitive antagonists of GnRH receptors in the anterior pituitary |
| GnRH ANTAGONIST therapeutic use | prostate cancer |
| Androgen Receptor ANTAGONISTS (drugs) | flutamide bicalutamide spironolactone |
| Androgen Receptor ANTAGONISTS: Spironolactone | mineralocorticoid with weak anti-androgenic effects |
| Androgen Receptor Antagonists: Therapeutic Uses | 1. prostate cancer (flutamide, bicalutamide, nilutamide-adjunts) 2. flutamide used in women to treat hirsutism |
| 5 a-reductase inhibitors | 5a-reductase |
| 5a-reductase inhibitors (drugs) | 1. finasteride (PROSCAR): type 2 5a-reductase 2. Dutasteride (AVODART): type 1 and 2 |
| 5a-reductase inhibitors MOA | block conversion of testosterone to DHT especially in male external genitalia |
| treatment of BPH with 5a-reductase inhibitors (other clinical uses) | 1. male pattern baldness- Finasteride (PROPECIA) 2. Hirsutism in women |
Created by:
megangodfrey97
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