Chapter 52: Androgens

Question 1

Androgens

Answer 1

Produced by the testes, ovaries, and adrenal cortex
Major endogenous androgen: Testosterone
Androgens most noted for their ability to promote expression of male sex characteristics
Have significant physiologic and pharmacologic effects unrelated to sex
Primary clinical application: Management of androgen deficiency in males
Principal adverse effects: Virilization and hepatotoxicity

Question 2

Testosterone

Answer 2

Biosynthesis and secretion
Males: Testosterone
Females: Preandrogens

Effects on sex characteristics in males
Pubertal transformation
Spermatogenesis

Effects on sex characteristics in females
Clitoral growth
Maintenance of normal libido
Overproduction of androgens = virilization

Anabolic effects
Skeletal muscle

Erythropoietic effects
Synthesis of erythropoietin
Men have higher hematocrit than women

Question 3

Clinical Pharmacology of the Androgens

Answer 3

Two basic categories:
Testosterone and testosterone esters
17-Alpha-alkylated compounds

Question 4

Therapeutic uses androgens

Answer 4

Male hypogonadism
Replacement therapy
Delayed puberty
Replacement therapy in menopausal women
Wasting in patients with acquired immunodeficiency syndrome (AIDS)
Anemias

Question 5

Androgen drug schedule

Answer 5

3

Question 6

ADR of androgens

Answer 6

Virilization in women, girls, and boys
Premature epiphyseal closure
Hepatotoxicity
Effects on cholesterol levels
Use in pregnancy
Prostate cancer
Edema
Abuse potential (athletic performance)

Question 7

Androgen preparations for male patients

Answer 7

Hypogonadism
Oral androgens: Fluoxymesterone and methyltestosterone
Intramuscular testosterone esters
Transdermal testosterone patches
Transdermal testosterone gels
Transdermal testosterone under arms
Implantable subcutaneous testosterone pellets
Testosterone buccal tablets

Question 8

General considerations: topical application

Answer 8

Location for application
Skin-to-skin contact transfer
Women and children: Avoid contact
Swimming
Showering

Question 9

Androgen (Anabolic Steroid) Abuse by Athletes

Answer 9

Some athletes use anabolic steroids to enhance athletic performance

Significant risks:
Hypertension, suppression of release of LH and FSH, testicular shrinkage, sterility, gynecomastia, acne, reduction in HDL, increase in LDL
Hepatotoxicity with 17-alpha-alkylated compounds
Renal damage
Psychologic effects
Mentally healthy: Minimal impact
Psychologically unbalanced: Could intensify aggression

Amendment to the Controlled Substances Act. Schedule III drugs are defined as those with a low to moderate potential for dependence