Androgens & Anabolic Steroids

   1. Androgens (Male Sex Hormone):

   - development of secondary sex characters in male

   - it was isolated as testicular hormone

   - commercial sources: urine of male, female and testicular extracts

   - it is also a product of the adrenal cortex

   - androgen is able to develop secondary sex characteristics in castrated male

   - e.g. testosterone

Secretion and Regulation-

   - secreted by interstitial cells/Leydig cells of testes

   - FSH stimulation on testes causes testosterone secretion

Pharmacological Actions-

   - growth of genitalis (penis, scrotum, seminal vesicle)

   - growth of hairs (pubic, axillary, beard, etc)

   - thickening of the skin

   - veins look prominent since subcutaneous fat is lost

   - larynx grows & voice deepens 

   - penile erection and physical aggression

   - development of the male phenotype

   - spermatogenesis and maturation of spermatozoa

   - rapid bone growth

   - fusion of epiphysis in boys as well as girls by Estradiol formed by testosterone.(@Extradiol-visit our social media platforms for more)

   - Muscle building

   - Induces erythropoiesis

Mechanism of action-

   - Testosterone acts via androgen receptor present in the target cell as shown in the figure below:

Pharmacokinetics-(ADME)

 A - Oral: inactive due to faster first-pass metabolism in the liver

   - hence, IM route is preferred

 D - 98% testosterone bound to sex hormone-binding globulin ( SHBG ) & to     albumin

   - SHBG testosterone is inactive due to tight binding

 M - major metabolic products are androsterone and etiocholanolone

 E - mostly as a conjugate with glucuronic acid and sulfate

   - estradiol also formed from testosterone by aromatization

   * T½ 10-20 min

   * Methyltestosterone and fluoxymesterone(synthetic androgens) are get metabolized slowly & longer action but less potent

   * Estrogens are not produced by DHT & fluoxymesterone

Side Effects-

   - acne in males and females

   - excess body hairs

   - irregular menstruation

   - testicular atrophy (if prolonged use)

   - hepatic carcinoma (if long term use of methyltestosterone)

   - gynecomastia

   - premature sexual behaviors

   - lowering of HDL and rise in LDL especially with α-alkylated analogs of testosterone.

   - cholestatic jaundice

   - salt retention and edema

   - oligozoospermia

Contraindications-

   - carcinoma of prostate and male breast

   - liver and kidney disease

   - during pregnancy (masculinization of the Female fetus)

   - in >65 years aged men

   - CHF or coronary artery disease

Uses-

   1. Testicular failure

   2. Hypopituitarism

   3. AIDS-related muscle wasting

   4. Hereditary angioneurotic edema

   5. Ageing

2. Anabolic Steroids (Synthetic Androgens):

   - having higher anabolic and lower androgenic activity

   - drugs e.g. Nandrolone, Oxymetholone, Stanozolol, Methandienone

Side Effects-

   - jaundice

   - can worsen lipid profile

Contraindications-

   - same as testosterone

   - migraine

Uses-

   - Hypoplastic and hemolytic anemia

   - To enhance physical ability in athletes

   - Osteoporosis

   - Acute illness, severe trauma (catabolic states)

   - Malignancy-associated and anemia

   - sub-optimal growth in boys

   - renal insufficiency