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47 Cards in this Set

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3 major Sex Steroid Hormones produced in men and females:
1. Estrogen
2. Progestin
3. androgens
Male primary sex organ:
testis
female primary sex organ:
ovaries
What are androgens?
A. are esteroidal hormones produced in the testis Leydig cells mainly although some also produced in ovaries and Adrenal glands. Normaly levels are higher in men than in women.
5-alpha-reductase converts testosterone to the more potent hormone:
DHT (dihydro-testosterone)
Levels of androgens according to age:
1. @ gestation/infancy: fluctuate
2. @ childhood: low
3. @ puberty/adult: high
4. @ old age: decline
Androgens circulate in 3 major forms:
1. Free testosterone (2%)
2. Tightly bound to sex hormone binding globulin (SHBG) (40%)
3. Weakly bound to albumin (60%)
% Bioavailable androgens
62%
(40% weakly bound to albumin, 2% free)
why do androgens have a high half-life?
because they are lipophilic
Major functions of Testosterone
1. develop and maintain male 2ry sexual characteristics
2. sexual function
3. normal sex drive
4. normal sperm production
5. fertility
6. maintenance of bone and muscle mass
7. metabolic rate and muscle-fat ratio
8. transcriptional regulation of some genes through androgen receptor
Natural androgen sources
1. testes
2. ovary
3. adrenal cortex
main androgen produced in testes:
testosterone
main androgens produced in ovaries:
testosterone and androstendione at similar concentrations
main androgens produced in adrenal cortex:
DHEA: dehydro-epi-androsterone
-weak androgen
-DHEA decreases fatigue
-antiaging claims
Hypogonasism in males is due to:
1. failure of testes to produce adequate testosterone.
2. Klinefelter's syndrome
3. Infection in testes (viral/bacterial)
4. Radiation, chemoterapy, injury, undescended testes
Klinefelter's syndrome
genetic disease that causes primary hypogonadism due to an extra X-chromosome
Secondary Hypogonadism
Inadequate stimulation of testes to produce testosterone due to hypothalamic or pituitary abnormality.

-hypotalamus/pituitary tumor or injury
-Kallmann's syndrome (lack GnRH)
-andropause (in old men)
therapeutic uses of Androgens (Testosterone)
1. Hypo-gonadism (males)
2. hypo-pituitarism (males/females)
3. Menopause/Andropause (males/females)
4. Breast cancer (+anticancer drugs)
5. Anabolic effects
What is cryptorchidism?
failure of one or both testes to descend into the scrotum. Occurs in 3% of all 1 year old males

treatment: hCG or LHRH for 6 wks.

Do not treat with testosterone because of negative feedback
Androgens are contraindicated in:
1. pregnant women (b/c offspring problems)
2. Males with prostate or brease cancer (b/c mitotic)
3. Cardiac disease patients predisposed to edema (b/c Na retention)
Androgens Adverse Effects in males only:
1. prostate/breast enlargement
2. Impotence
3. testicular atrophy
4. azoospermia
Androgens Adverse Effects in females only:
1. viralization
2. breast diminution
3. clitoral enlargement
Androgens Adverse Effects in males and femalles:
1. risk of stroke & CHD 2. agressiveness 3. jaundice and risk of liver tumor 4. accelerated closure of epiphisis (short person syndrome) 5. precacious puberty 6. puberty like effects (acne, gynecomastia, sex) 7. Jaundice 8. higher RBC count 9. increased hematopoiesis 10. Na retention 11. Psychologic dependence 12. Psychotic symptoms
Androgen abused by athletes to improve performance
DHEA (de-hydro-epi-androsterone)

effects:
-higher RBC count
-increased hematopoiesis
Androgen (Testosterone) drug preparations:
1. Testosterone 1:1
2. Methyl-testosterone 1:1
3. Fluoxy-mesterone 1:2 (Halotestin)
4. Meth-androstenolone 1:3 (Dianabo)
5. ethyl-esterone 1:6 (Maxabolin)
ADME of androgen (testosterone preparations):
1. well absorbe by all routes
2. readyly converted to inactive metabolites
3. Prolonged absorption and activity in esters
4. Synthetic derivatives active orally
treatment for Hypogonadism in males:
Androgens (testosterone):
1. Testo-sterone
2. Methyl-testo-sterone
3. Fluoxyme-sterone (Halotestin)
4. Methandro-sterone (dianabo)
5. Ethyl-estrenol (Maxabolin)
treatment for Hypogonadism in females:
1. Conjugated estrogens
2. Ethyl estradiol
3. Estradiol esters
Drugs to treat Prostate Cancer:
1. F-lutamide
2. Bica-lutamide
3. Finasteride
4. Amino-Glute-Thimide
Pharmacology of Flutamide/Bica-lutamide:
(use,MofA,AE)
use: Metastatic PROSTATE CANCER

MofA: Androgen Receptor Antagonist, Anti-androgen

Adverse Effects: Hepatotocity
Pharmacology of Finasteride:
(use,MofA,AE)
use:
1. Benign PROSTATE HYPERPLASIA
2. baldness (in males)
3. Hairsutism (in females)

MofA: 5-alpha reductase inhibitor, Anti-androgen

Adverse Effects: N/A
Pharmacology of Amino-Glute-timide:
(use,MofA,AE)
use:
1. Benign PROSTATE CANCER
2. BREAST CANCER
3. ADRENAL TUMORS
4. CUSHING'S SYNDROME

MofA: 1. Blocks cholesterol conversion to pregnolone (1st step in steroid synthesis). 2. aromatase inhibitor ( blocks conversion of androgen to estrogens)

Adverse Effects: N/A
Weak androgen-Receptor Inhibitor used to treat HYPERTENSION
Sipirolactone
Spirolactone therapeutic used
1. hypertension
2. Hirsutism
3. Edema
Spirolactone mode of action:
1. Synthetic steroid,
2. weak androgen-receptor inhibitor
3. acts as a K-sparing diuretic
Anti-androgen that causes hepatoxicity:
1. flutamide
2. bica-lutamide
5-alpha-reductase inhibitor used to treat bening prostate tumor
finasteride
what is hairsutism?
excessive hairiness, esp. in women.
Androgen-receptor antagonist
1. Flutamide
2. Bica-lutamde
What is Cushing's syndrome?
A syndrome caused by an excess of corticosteroids, especially cortisol, in the blood, characterized by obesity, muscle and skin atrophy, facial fullness (known as moon facies), hypertension, and other physical changes. Glucocorticoid excess is usually caused by a tumor of the adrenal cortex, excessive intake of ACTH or glucocorticoids, or increased production of ACTH from a tumor of the anterior lobe of the pituitary gland. Cushing's syndrome is named after its discoverer, American neurosurgeon Harvey Williams Cushing (1869-1939).
propecia
A trademark for the drug finasteride, used to treat male pattern baldness
Finasteride therapeutic used:
1. PROSTATE CANCER
2. BREAST CANCER
3. ADRENAL TUMORS
4. CUSHING'S SYNDROME
Flutamide and bica-lutamide are given together with __ to treat prostate cancer
GnRH
Treatment for Hirsutism (in women):
1. Finasteride
2. Spironolactone
Male hormonal contraception
1. Danazol + Testosterone
2. Androgen + Progestin or Estrogen
3. GnRH analogs (continuous dose)
4. Receptor Anti-androgen
5. GnRH Antagonist + Testosterone
6. Gossypol (cottonseed oil)
Danazol consists of
LH + FSH hormones
Gossypol
Cottonseed oil, alters seminiferous epithelium affecting sperm production. treatment is long term and reversible