Exam 2: Lecture X, Androgens Flashcards
In men, LH and FSH control….
test secretion and sperm production
secreted by AP gland
LH stimulate Leydig cells which…..
secrete test at start of puberty
FSH stimulates Sertoli cells which….
produce sperm
Testosterone
main natural androgen
steroid hormone, precursor is cholesterol
Testosterone is synthesized form
progesterone and dehydroepiandrosterone
Majority of testosterone produced in…
testes = 95%
Adrenal gland <5%
65% bound with SHBG (Sex hormone Binding globulin) in plasma
Testosterone converted to dihydrotestosterone by…
5a-reductase
both Test and Dihydrotest affect gene transcription
Test effects before birth
masculinizes the repro tract and external genitalia
promotes descent of testes into scrotum
Test effects upon sex-specific tissue
Promotes growth and maturation of repro system at puberty
Spermatogenesis
Maintains the repro tract throughout adulthood
Test effects other reproductive effects
sex drive at puberty
controls gonads
Test effects non-reproductive effects
protein anabolic effect
bone growth at puberty
closes epiphyseal plate
aggressive behavior
causes masculinization of a female
Test clinical uses
replace therapy in hypogonadism
stimulate RBC production
suppression of estrogen secretion in women
estrogen suppression with severe endometriosis
treatment of mammary carcinoma in women
illicit use by athletes to increase muscle mass and strenght
Androgenic/Anabolic effect ratios
Testosterone 1:1
Testosterone cypionate 1:1
Methyltestosterone 1:1
Fluoxymesterone 1:2
Oxandrolone (Oxandrin) 1:3 – 1:13
Test toxicity
largely result of masculinizing effects
Hepatotoxicity
Jaundice
Liver enzymes abnormalities
Hepatocellular carcinoma (rarely)
Priapism or impotence
Increased risk of coronary heart disease in both sexes
Dependence and withdrawal syndrome were reported
Illicit use by athletes – unpredictable rage and hostility
Antiandrogens are an important therapy for…
benign and malignant prostate disease. Drugs act at different sites in androgen pathway
Ketoconazole
An antifungal agent.
** Inhibits steroid synthesis **
Characterized by antiandrogen and anti-glucocorticoid effects.
Used to treat prostate cancer and Cushing’s syndrome.
Suppresses adrenal steroid synthesis in patients with steroid-dependent metastatic tumors.
Men treated with the drug develop reversible gynecomastia.
Finasteride (Proscar and Propecia)
inhibit 5a reductase
useful in benign prostate hyperplasia in reducing prostate size
in women may treat male-type baldness, hirsutism and possibly acne
Test Receptor Inhibitors
Cyproterone (Generic)
Flutamide (Eulexin)
Bicalutamide (Casodex)
Cyproterone (Generic)
Partial agonist at androgen receptors
Progesterone derivative
Also, affects hypothalamus and decreases GnRH synthesis
Therapy of precocious puberty in males
Masculinization and acne in women
Was proposed to use in treatment of severe hypersexuality in males
Spironolactone (Aldactone, CaroSpir)
A competitive inhibitor of aldosterone
** Also competes with dihydrotestosterone for androgenic receptors ***
Therapy of precocious puberty in boys and girls.
Used to treat hirsutism in women.
Progesterone
Inhibits GnRH secretion without effect on peripheral tissues
GnRH controls LH and FSH
All exogenous androgens, estrogens and progesterone inhibit GnRH