Pharm - Androgens

Question 1

What tissues/cells synthesize androgens?

Answer 1

95% is from Leydig cells of tissue

5% is from adrenal glands

Question 2

What are the natural androgens?

Answer 2

Testosterone
Dihydrotestosterone (DHT)
Androstenedione
Dehydroepiandrosterone (DHEA)

Question 3

Describe the general process of androgen synthesis

Answer 3

Cholesterol is cleaved to form pregnenolone, wihch is converted to DHEA and Androstenedione. These compounds can be converted to testosterone.

Question 4

What 3 outcomes can occur once testosterone diffuses into a target cell

Answer 4

1) Binds to androgen receptor directly
2) Converted to DHT and binds androgen receptor
3) Converted to estradiol and binds estrogen receptor

Question 5

What two enzymes are responsible for converting testosterone into DHT and estradiol?

Answer 5

Aromatase converts testosterone to estrodiol

5alpha reductase converts testosterone to DHT

Question 6

What are the reproductive functions of androgens?

Answer 6

Secondary male sex characteristics
Puberty in females
Promotes spermatogenesis (with FSH)
Regulation of gonadotropin secretion

Question 7

What are the anabolic functions of androgens?

Answer 7

Increase protein synthesis, lean body mass, skeletal muscle growth and reduce fat mass
Skeletal growth and epiphyseal closure
Growth of larynx at puberty (deepening voice)

Question 8

What are the metabolic functions of androgens?

Answer 8

Erythropoiesis
Decreased synthesis of clotting factors
Increased sebum production
Decrease HDL and increase LDL
Androgenic alopecia

Question 9

Symptoms of man with androgen deficiency

Answer 9

Decreased libido and erectile dysfunction
Decreased muscle mass, increased adiposity
Decreased axillary and pubic hair
Anemia
Osteoporosis
Decreased energy, sense of well being

Question 10

What are the therapeutic uses of androgens?

Answer 10

HRT for hypogonadism
Induction of puberty
Treat osteoporosis in males

Question 11

Indication for testosterone HRT

Answer 11

Hypogonadism

Question 12

What are the major androgenic effects of androgen HRT?

Answer 12

Prostate growth/maturation
Growth of penis, scrotum, seminal vesicles
Development of male hair distribution
Laryngeal enlargement and vocal cord thickening
Increased muscle mass

Question 13

What are the side effects of androgen HRT?

Answer 13

Cholestatic jaundice syndrome
Liver carcinoma
Benign prostatic hyperplasia (BPH)
Prostate cancer
Gynecomastia
Acne
Headache

Question 14

What are contraindications of androgen HRT?

Answer 14

Breast cancer in men
Prostate cancer
Pregnancy

Question 15

What is flutamide?

Answer 15

Androgen receptor antagonist used for metastatic prostate cancer and BPH

Question 16

What is the mechanism of action of flutamide?

Answer 16

Competitive inhibition of DHT and T binding the receptor

Question 17

What is the side effect of flutamide?

Answer 17

Hepatotoxicity
Hematopoietic disorders
Diarrhea
Nausea
Rash
Hot flashes

Question 18

What are contraindications of androgen receptor antagonsists?

Answer 18

Flutamide is contraindicated in patients with severe hepatic impairment

Question 19

Flutamide, DES and leuprolide are all used for prostate cancer. Which is preferred?

Answer 19

Flutamide is better than DES and leuprolide for prostate cancer treatment. Especially effective in combination with medical or surgical castration.

Question 20

What is spironolactone?

Answer 20

Androgen receptor antagonist (and mineralocorticoid receptor antagonist) used to treat: hirsutism, hypertension, acne, edema, cirrhosis, hypokalemia

Question 21

What are the side effects of spironolactone?

Answer 21

GI hemorrhage
Hyperkalemic metabolic acidosis
Agranulocytosis SLE
Gynecomastia
Dyspepsia
Abnormal menstruation/impotence

Question 22

Contraindication for spironolactone

Answer 22

Anuria
Hyperkalemia
Acute renal insufficiency

Question 23

What is finasteride?

Answer 23

A 5alpha reductase inhibitor used to treat BPH and androgenic alopecia

Question 24

What is the mechanism of action of finasteride?

Answer 24

Prevents conversion of testosterone to DHT by inhibiting 5alpha reductase

Question 25

What are the side effects of finasteride?

Answer 25

Neoplasm of male breast
Breast tenderness
Decreased libido, erectile dysfunction, ejaculatory disorder

Question 26

What are the contraindications for finasteride treatment?

Answer 26

Pregnancy

Question 27

What benefits does finasteride have for men with BPH?

Answer 27

Improves urine flow by reducing prostate size by up to 25%. This is used as an alternative to transurethral resection of the prostate.