Androgens Flashcards
In what two locations is testosterone produced in the male body? Which secretes more than the other?
Leydig cells produce about 95% and the adrenal glands make about 5%.
What is the effect of activin and inhibin in males?
Activin stimulates pituitary FSH release, while inhibin prevents it (along with testosterone).
primary enzymes involved in testosterone metabolism
5-alpha reductase
aromatase
How are testosterones excreted?
metabolized in the liver and excreted in the urine
How are adrenal androgens different from those synthesized in Leydig cells?
The are much weaker and are only intermediates of the testosterone synthesis pathway.
clinical uses of androgens
(1) andropause
(2) gynecologic disorders (endometriosis)
(3) hormone replacement in men with hypogonadism or pituitary deficiency
(4) protein anabolism (post-trauma)
Why are the 17-alkyl forms of synthetic androgens more effective orally?
Without an alkyl group at that position, testosterone is quickly metabolized and inactivated. When it is present, the alcohol cannot be converted to a ketone as a part of the metabolic process and the drug can be absorbed.
Esterification, like with estrogens, has this effect on testosterone action.
delays absorption and prolongs action with intramuscular injection
adverse effects of androgens in men
azoospermia, acne, sleep apnea, gynecomastia, increased aggressiveness/psychotic sx
adverse effects of androgens in women
hirsutism, acne, amenorrhea, clitoral enlargement, voice deepening
Finasteride
5-alpha reductase inhibitor for BPH, alopecia, PCOS
Dutasteride
5-alpha reductase inhibitor for BPH, hirsutism, PCOS, alopecia
Spironolactone
androgen receptor inhibitor (aldosterone) for hirsutism, acne, PCOS
What are two non-steroidal androgen receptor inhibitors?
flutamide and enzalutamide
