Androgens Flashcards
Where are androgens synthesized?
95% testis (Leydig cells)
5% adrenal glands
Androgens are synthesized by circulating____
cholesterol
What are the metabolic effects of androgens?
Erythropoiesis
Decreased synthesis of clotting factors
Decrease HDL, increase LDL
Therapeutic uses of androgens
HRT in primary or secondary hypogonadism
Induction of puberty in delayed matruation
Osteoporosis in males
Testosterone enanthate/ Testosterone cypionate
Indication
Hypogonadism
Testosterone enanthate/ Testosterone cypionate
MOA (i.e. effects on the body)
Growth/maturation of prostate, seminal vesicles, penis, scrotum Development of male hair distribution Laryngeal development Vocal cord thickening Alterations in body musculature Fat distribution
Testosterone enanthate/ Testosterone cypionate
Side Effects
Cholestatic jaundice syndrome Liver carcinoma Benign prostatic hyperplasia Prostate cancer Gynecomastia Acne Headache
Testosterone enanthate/ Testosterone cypionate
Contraindications
Breast cancer in men
Prostate cancer
Pregnancy
Testosterone enanthate/ Testosterone cypionate
Which route of administration is preferred?
Transdermal to prevent first pass hepatic metabolism
Androgen Receptor Antagonists
Flutamide
Spironolactone
Androgens used in HRT
Testosterone enanthate/ Testosterone cypionate
Flutamide (androgen receptor antagonist) indication
Metastatic prostate cancer
BPH
Flutamide (androgen receptor antagonist) MOA
Competitive inhibitor of DHT and T binding to receptor
Flutamide (androgen receptor antagonist) Side Effects
Hepatotoxicity** Hematopoietic disorders* Diarrhea Nausea Rash Hot flashes
Flutamide (androgen receptor antagonist) Contraindication
Severe hepatic impairment
Which is the best for the treatment of prostate cancer?
A. Leuprolide
B. DES
C. Flutamide
Flutamide
Spironolactone (Androgen receptor antagonist) Indications
Hirsutism Hypertension Acne Edema (CHF) Cirrhosis /nephrotic syndrome Hypokalemia
Spironolactone (Androgen receptor antagonist) MOA
Competitive inhibition of DHT and T binding to receptor
Spironolactone (Androgen receptor antagonist) Side Effects
Gastrointestinal hemorrhage Hyperkalemic metabolic acidosis* Agranulocytosis SLE Gynecomastia Dyspepsia Lethargy Abnormal menstruation Impotence Rash
Spironolactone (Androgen receptor antagonist) Contraindications
Anuria
Hyperkalemia
Acute renal insufficiency
Spironolactone (Androgen receptor antagonist) Therapeutic consideration
An aldosterone receptor antagonist and also an androgen receptor antagonist
Inhibitors of Peripheral Testosterone Conversion to DHT
Finasteride
Finasteride (inhibitor of Peripheral Testosterone Conversion to DHT) Indication
BPH
Androgenic alopecia
Finasteride (inhibitor of Peripheral Testosterone Conversion to DHT) MOA
Selective inhibition of type II 5-a reductase (converts T to DHT in prostate, liver, skin)
Finasteride (inhibitor of Peripheral Testosterone Conversion to DHT) side effects
Breast tenderness
Decreased libido
Erectile dysfunction
Ejaculatory disorder
Finasteride (inhibitor of Peripheral Testosterone Conversion to DHT) Contraindication
Pregnancy
Women
Finasteride (inhibitor of Peripheral Testosterone Conversion to DHT) therapeutic consideration
Improves urine flow
Alternative to tranurethral resection of prostate (TURP)
25% reduction of prostate size
Most effective on large prostates
