Week 11 - Androgens and Anti-Androgens Flashcards
Testosterone: function
Principle endogenous androgen responsible for promoting growth and development of male sex organs and maintaining secondary sex characteristics
Testosterone: indications
- Male (primary) hypogonadism
- Male (hypogonadotropic) hypogonadism
- Delayed male puberty
- Hormone therapy in transgender males (off label use)
- Endometriosis and some postmenopausal symptoms in women (not FDA approved)
- Male climacteric (male version of menopause)
Effects of testosterone on the skin
- Hair growth
- Collagen growth
Effects of testosterone on the muscles
- Muscle growth
- Increased strength
- Increased endurance
Effects of testosterone on the bones
Bone mass density maintenance
Effect of testosterone on the brain
- Increased sex drive
- Improved mood
- Confidence
- Memory function
Effects of testosterone on the bone marrow
RBC production
Effects of testosterone on the sex organs
- Sperm production
- Erectile function
- Prostate growth
S/s of androgen deficiency
- Low libido
- Decreased morning erections
- Low bone mineral density
- Gynecomastia
- Small testes
- Loss of body hair
- Fatigue, depression, anemia, reduced muscle mass, increased fat mass
- Low morning (8-10 AM) serum testosterone
When is testosterone therapy indicated?
ONLY for testosterone deficiency; NOT impaired spermatogenesis
- Can suppress spermatogenesis if [testosterone] is normal
Testosterone: clinical effects
- Virilization/sexual function
- Improved muscle strength and reduced fat mass
- Improves bone density
When will patients start seeing effects from testosterone therapy?
3-6 months except bone density which won’t be seen until 24 months
Testosterone: ADR
- Acne
- Prostate disorders
- Sleep apnea
- Erythrocytosis
- Hepatitis, hepatic neoplasm, cholestatic hepatitis, jaundice, hepatocellular carcinoma
Men: gynecomastia, reduced sperm levels, decreased libido at high levels, depression
Women: menstrual irregularities, virilization
True/False: providers should recommend against testosterone use on “trial” basis in healthy, middle-aged men
True
Testosterone: formulations
- Gel (AndroGel, Testim, Fortesta)
- Transdermal (no longer available in U.S.)
- Intramuscular (enanthate, cypionate)
- SQ injection and pellet
NOT given orally b/c testosterone is metabolized rapidly by the liver
Testosterone: contraindications
- Prostate cancer
- Male breast cancer
- Severe lower urinary tract symptoms
- Erythrocytosis (HCT over 50)
- Increased blood clot risk
- Severe, untreated sleep apnea
- If on CPAP, can start testosterone therapy
- Uncontrolled CHF
- Increased sodium retention
- Pregnancy (category X) and lactation
Testosterone: drug interactions
- Anticoagulants (e.g. warfarin)
- Diabetic agents
- Corticosteroids
Testosterone: monitoring
- Testosterone level 2-3 months after starting therapy and when changing doses
- Once stable, check every 6-12 months
- Endocrine Society recommends reevaluation for prostate cancer at 3 months and 1 year after starting treatment
- PSA and DRE
- Check HCT 3-6 months after starting treatment, then annually
- Lipids, liver function, CBC
5-alpha reductase inhibitors: example
Finasteride (Proscar, Propecia)
5-alpha reductase inhibitors (finasteride): indications
- BPH
- Male pattern baldness
5-alpha reductase inhibitors (finasteride): MOA
Inhibits enzymes that converts testosterone to DHT
5-alpha reductase inhibitors (finasteride): caution
Prostate evaluation required for any increase in PSA while on medication
GnRH analogues: example
Leuprolide (Lupron)
GnRH analogues (leuprolide): MOA
- LH-releasing hormone antagonist
- Creates reversible chemical orchiectomy state in males
- Creates reversible chemical oophorectomy state in females
