Androgens And Anabolic Steroids

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3 major Sex Steroid Hormones produced in men and females:

Back 1

1. Estrogen
2. Progestin
3. androgens

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Male primary sex organ:

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testis

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female primary sex organ:

Back 3

ovaries

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What are androgens?

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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.

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5-alpha-reductase converts testosterone to the more potent hormone:

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DHT (dihydro-testosterone)

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Levels of androgens according to age:

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1. @ gestation/infancy: fluctuate
2. @ childhood: low
3. @ puberty/adult: high
4. @ old age: decline

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Androgens circulate in 3 major forms:

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1. Free testosterone (2%)
2. Tightly bound to sex hormone binding globulin (SHBG) (40%)
3. Weakly bound to albumin (60%)

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% Bioavailable androgens

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62%
(40% weakly bound to albumin, 2% free)

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why do androgens have a high half-life?

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because they are lipophilic

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Major functions of Testosterone

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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

Front 11

Natural androgen sources

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1. testes
2. ovary
3. adrenal cortex

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main androgen produced in testes:

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testosterone

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main androgens produced in ovaries:

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testosterone and androstendione at similar concentrations

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main androgens produced in adrenal cortex:

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DHEA: dehydro-epi-androsterone
-weak androgen
-DHEA decreases fatigue
-antiaging claims

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Hypogonasism in males is due to:

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1. failure of testes to produce adequate testosterone.
2. Klinefelter's syndrome
3. Infection in testes (viral/bacterial)
4. Radiation, chemoterapy, injury, undescended testes

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Klinefelter's syndrome

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genetic disease that causes primary hypogonadism due to an extra X-chromosome

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Secondary Hypogonadism

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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)

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therapeutic uses of Androgens (Testosterone)

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1. Hypo-gonadism (males)
2. hypo-pituitarism (males/females)
3. Menopause/Andropause (males/females)
4. Breast cancer (+anticancer drugs)
5. Anabolic effects

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What is cryptorchidism?

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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

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Androgens are contraindicated in:

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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)

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Androgens Adverse Effects in males only:

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1. prostate/breast enlargement
2. Impotence
3. testicular atrophy
4. azoospermia

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Androgens Adverse Effects in females only:

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1. viralization
2. breast diminution
3. clitoral enlargement

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Androgens Adverse Effects in males and femalles:

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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

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Androgen abused by athletes to improve performance

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DHEA (de-hydro-epi-androsterone)

effects:
-higher RBC count
-increased hematopoiesis

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Androgen (Testosterone) drug preparations:

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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)

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ADME of androgen (testosterone preparations):

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1. well absorbe by all routes
2. readyly converted to inactive metabolites
3. Prolonged absorption and activity in esters
4. Synthetic derivatives active orally

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treatment for Hypogonadism in males:

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Androgens (testosterone):
1. Testo-sterone
2. Methyl-testo-sterone
3. Fluoxyme-sterone (Halotestin)
4. Methandro-sterone (dianabo)
5. Ethyl-estrenol (Maxabolin)

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treatment for Hypogonadism in females:

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1. Conjugated estrogens
2. Ethyl estradiol
3. Estradiol esters

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Drugs to treat Prostate Cancer:

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1. F-lutamide
2. Bica-lutamide
3. Finasteride
4. Amino-Glute-Thimide

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Pharmacology of Flutamide/Bica-lutamide:
(use,MofA,AE)

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use: Metastatic PROSTATE CANCER

MofA: Androgen Receptor Antagonist, Anti-androgen

Adverse Effects: Hepatotocity

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Pharmacology of Finasteride:
(use,MofA,AE)

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use:
1. Benign PROSTATE HYPERPLASIA
2. baldness (in males)
3. Hairsutism (in females)

MofA: 5-alpha reductase inhibitor, Anti-androgen

Adverse Effects: N/A

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Pharmacology of Amino-Glute-timide:
(use,MofA,AE)

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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

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Weak androgen-Receptor Inhibitor used to treat HYPERTENSION

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Sipirolactone

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Spirolactone therapeutic used

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1. hypertension
2. Hirsutism
3. Edema

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Spirolactone mode of action:

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1. Synthetic steroid,
2. weak androgen-receptor inhibitor
3. acts as a K-sparing diuretic

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Anti-androgen that causes hepatoxicity:

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1. flutamide
2. bica-lutamide

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5-alpha-reductase inhibitor used to treat bening prostate tumor

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finasteride

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what is hairsutism?

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excessive hairiness, esp. in women.

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Androgen-receptor antagonist

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1. Flutamide
2. Bica-lutamde

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What is Cushing's syndrome?

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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).

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propecia

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A trademark for the drug finasteride, used to treat male pattern baldness

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Finasteride therapeutic used:

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1. PROSTATE CANCER
2. BREAST CANCER
3. ADRENAL TUMORS
4. CUSHING'S SYNDROME

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Flutamide and bica-lutamide are given together with __ to treat prostate cancer

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GnRH

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Treatment for Hirsutism (in women):

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1. Finasteride
2. Spironolactone

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Male hormonal contraception

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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)

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Danazol consists of

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LH + FSH hormones

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Gossypol

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Cottonseed oil, alters seminiferous epithelium affecting sperm production. treatment is long term and reversible