Pharma - 4th Asessment - Androgens - 5 Feb 2007

ANDROGENS  Testosterone  Androstenedione  Dehydroepiandrosterone  Dehydroepiandrosterone Sulfate

Hypothalamus

-

GnRH Anterior pituitary

FSH

LH

Gonadotropins

Inhibin Androgen-binding protein

Testes Sertoli cell

Leydig cell

Sperm

Testosterone

NUCLEUS CYTOSOLIC RECEPTOR DNA TRANSCORTIN

mRNA

STEROID NEW PROTEIN

RIBOSOMES

Schematic model of the mechanism of action of glucocorticoids

ANDROGENS – BINDING PROTEIN  SHBG – 58 %  Albumin – 40 %

ANDROGENS - Metabolism H3 C

 Androsterone (20%)

H3 C O

 Etiocholanolone (20%)

A

C

OH

D

B

Testostersone

 Dihydrotestosterone (40%)  Conjugates – Glucuronides, Sulfate (50%)

ANDROGENS - TSSUES Testosterone

Dihydrotestosterone

• Muscle

• Penis, Secrotum

• Liver

• Prostate

• Kidney

• Skin, sweat glands

• Bone

• Hair cells

ANDROGENS - ACTION  Spermatogenesis  Sexual Development   Libido   Bone Density   Muscle Mass   Erythrocyte Mass

ANDROGENS – REPLACEMENT THERAPY  Hypogonadism  Impotence  Cryptorchidism

ANDROGENIC STEROIDS – ANDROGENIC REPLACEMENT  Testosterone (Oreton) 1M 3 x Week  Testosterone Cypionate (DEPO-Testosterone) 1M 2-4 week  Fluoxymesterone (Haotestin) PO-Daily  Testosterone Enanthate IM

ANABOLIC STEROIDSCLINICAL USES  Protein Catabolic States  Short Stature  Anemia  Oesteoporosis  Breast Cancer  Endometriosis  Angioneuratic Edema

ANDROGEN ANALOGS – ANABOLIC STEROIDS  Stanozol (Winstrol) PO  Nandrolone Phenopropionate (Durabolin) 1M  Ethylestrenol (Maxibolin) PO  Danazol PO

ANDROGEN – SIDE EFFECTS  Growth of Facial Hair  Male Pattern Baldness  Acne  Priapisim  Impotence

ANDROGEN – SIDE EFFECTS (cont’d)  Gynocomastia  Growth Disturbances (Children)  Premature Coronary Artery Disease ( LDL)  Edema and Hepatotoxicity  Azoospermia

ANTIANDROGENS  Cyproterone Acetate  Flutamide (Eulexin)  Spironolactone (Aldactone)  Finasteride (Proscar)  Leuprolide  Ketoconazol

ANTIANDROGENS – THERAPEUTIC USES  Hairsutism (Female)  Prostatic Carcinoma  Benign Prostatic Hypertrophy  Precocious Puberty (Children)  Hypersexuality

MALE CONTRACEPTIVES  Gossypol  19 - Nortestosterone

MALE SEXUAL PERFORMANCE  Papaverine  Phentolamine  Prostaglandin E1 (Alpostadil)  Sildenafil