L 11 androgens Flashcards
testosterone
-Most important androgen secreted by the testis
Binds to the androgen receptor and alters the rate of transcription
In men, ~8 mg of testosterone is produced daily
-95% by the Leydig cells in the testis
-5% by the adrenal glands
Plasma levels of testosterone
-In men, 0.6 μg/dL after puberty; decreases after age 50
-In women, 0.03 μg/d
circulating testosterone
-Bound to sex hormone-binding globulin (SHBG) (65%)
-Bound to albumin (33%)
-Free (2%
GnRH
gonadrotropin-releasing hormone
LH
luteinizing hormone
FSH
follicle stimulating hormone
excretion of testosterone
-occurs in the liver
-inactivated and conjugated, then excreted to the urine
adrenal androgens
-Intermediates of the testosterone synthesis pathway
-Produced in significant amounts, largely in the adrenal glands.
-Weak androgen effects
-Physiological functions are not known
-androstenedione, DHEA, DHEAS
physiologic effects of testosterone
-Responsible for many changes at puberty
-Growth-promoting properties
-Stimulation and maintenance of sexual function
-Stimulation of erythrocyte production
-Decrease in HDL levels
growth promoting properties
-Penile and scrotal growth
-Change in the skin (thicker and oilier)
-pubic, axillary, and beard hair
-Deepening of the voice
-Skeletal growth followed by epiphyseal closure
-Increase in lean body mass positive nitrogen balance
androgen replacement therapy in men
-Male hypogonadism (testosterone deficiency)
-Hypopituitarism
gynecological disorders
-Must be used with great caution due to adverse effects
-Endometriosis (danazol)
-In combination with estrogens for replacement therapy in the postmenopausal period (controversial)
-Eliminates the endometrial bleeding.
-Enhances libido
protein anabolic agents
Reverses protein loss after trauma, surgery, or prolonged immobilization in conjunction with dietary measures and exercises
clinical uses of androgens
-andropause
-protein anabolic agents
-gynecologic disorders
-androgen replacement therapy in men
synthetic androgens
-When administered orally, testosterone is readily absorbed but inactivated largely.
-17-alkyl forms (ex. methyltestosterone) are more active orally.
-Ester forms (ex. propionate, enanthate, cypionate) have prolonged absorption time
and greater activity for intramuscular administration
anabolic steroids in sports
-Used in doses 10 – 200 times larger than the daily normal production to increase
strength and aggressiveness.
-Such effects have been proven only in women
-Large doses of anabolic steroids suppress the secretion of gonadotropins. –> testicular atrophy
significant health risks by long term use of anabolic steroids
-Harmful changes in cholesterol levels (Low HDL and high LDL)
-Acne
-High blood pressure
-Hepatic dysfunction in case of 17-alkyl steroid
adverse effects of androgen in women
-Hirsutism
-Acne
-Amenorrhea
-Clitoral enlargement
-Deepening of the voice
-should not be used in infants or pregnant women because there is significant disturbances in sexual development
adverse effects of androgens in men
-Acne
-Sleep apnea
-Gynecomastia
-Azoospermia and testicular atrophy
-Increased aggressiveness and psychotic symptom
antiandrogens
-5a reductase inhibitor
-androgen receptor antagonist
5a reductase inhibitors
-block the conversion from testosterone to 5a dihydrotestosterone
-Finasteride (Proscar ®, Propecia® )
-Dutasteride (Avodart®
synthetic androgens
-Methyltestosterone (Android®, Metandren®, Testred®)
-testosterone enanthate (Delatestryl®)
-testosterone cypionate (Depo-Testosterone®
androgen receptor antagonist
-Block the binding of endogenous androgens to the receptor or inhibit the activation of the receptors
-Steroidal inhibitors
-Non-steroidal inhibitors
finasteride
-Benign prostatic hyperplasia (Proscar®)
-Male pattern baldness (Propecia ®)
-Hirsutism in women
dutasteride
-Benign prostatic hyperplasia
-Male pattern baldnes
cyproterone acetate
-Hirsutism in women
-Excessive sexual drive in men
spironolactone
-Hirsutism in women
-Acne
steroidal androgen receptor antagonist
Cyproterone acetate (Androcur®)
Spironolactone (Aldactone®)
flutamide
-Non-steroidal antiandrogen
-Prostate cancer
enzalutamide
-Non-steroidal antiandrogen
-Metastatic castration-resistant prostate cancer
nonsteroidal androgen receptor antagonist
flutamide (Eulexin®)
Enzalutamide (Xtandi®)