Male Pharmacology Flashcards
Testosterone –> Dihydrotestosterone
5a reductase
Testosterone –> Estradiol
Aromatase
External genitalia
Hair follicles (balding)
Prostate hyperplasia
Dihydrotestosterone – Androgen receptor
Internal genitalia
Skeletal muscle
Erythropoiesis
Testosterone – Androgen receptor
Epiphyses
Bone density
Libido
Estradiol – Estrogen receptor
Testosterone Preparations
Transdermal - Testosterone
IM injection - Cypionate (Testosterone Esters)
Oral - Stanozolol (17-alkylated compounds)
Longest 1/2 life of testosterone preparations
Esters - Cypionate (IM) –> Days
Patch –> Hours
Gel –> 1 Day
Therapeutic uses of androgens
Male hypogonadism (testosterone deficiency) Goal is to mimic normal serum testosterone concentrations
SE of testosterone
Acne
Gynecomastia
Aggressive sexual behavior
**Must assess height and growth status of the patient
Other uses of androgens
- Male senescence
- Women with low testosterone
- Muscle wasting – associated with AIDS
- Blood dycrasias – (Danazol) for hemolytic anemia and idiopathic TTP
- Angioedema – 17-alkylated androgens (Stanozolol) stimulate hepatic synthesis of the esterase inhibitor
- Danazol is used for treatment of endometriosis and fibrocystic breast disease
- Improve athletic performance
What is one concern surrounding the use of testosterone in older men with pre-existing heart disease?
Two-fold increase in the relative risk of MI
Androstenedione and DHEA
Weak androgens
Increases popularity as a mean stop increase testosterone because they are treated as nutritional supplements
Adverse effects of androgen abuse
- Decreased endogenous testosterone and sperm production resulting in diminished fertility
- Decreased testicular size (after many years)
- High doses cause erythrocytosis
- Gynecomastia (testosterone converted to estrogen)
- 17-alkylated androgens cause hepatotoxicity – also more likely to increase LDL and decrease HDL
- In women and children virilization can occur
- Boys experience phallic enlargement, and women experience clitoral enlargement
- Stunting of linear growth (children)
- Psychological disorders and sudden death d/t cardiac disease
GnRH analog
Inhibits testosterone secretion by inhibiting LH secretion
Leuprolide
Therapeutic uses of Leuprolide
Treatment of advanced prostate cancer
Endometriosis
Central precocious puberty