Androgens

Question 1

Name the natural androgens (4)

Answer 1

• Testosterone
• Dihydrotestosterone (DHT)
• Androstenedione
• Dehydroepiandroesterone (DHEA)

Question 2

Most potent natural androgen

Answer 2

DHT

Question 3

Benefit of synthetic androgens

Answer 3

Longer half-life (like all synthetic hormones)

Question 4

Metabolic conversions of Testosterone (2)

Answer 4

• 5 alpha reductase –> DHT
• Aromatase –> Estrogen
• Aromatase might change androstenedione into estrogen instead of testosterone

Question 5

Basic Mechanism of Action of Androgen (3 steps)

Answer 5

• Testosterone diffuses into cell and binds to intracellular androgen receptor
• Hormone receptor complex dimerizes in cell nucleus and binds to specific hormone-response elements on DNA, along with a complex of co-activator or co-repressor proteins
• Promotion or inhibition of transcription of specific genes, resulting in physiologic effect.

Question 6

Reproductive actions of Androgens (4)

Answer 6

• primary and secondary sex male characteristics
• Early stages of breast and pubertal development in girls (adrenarche)
• spermatogenesis (with help of FSH)
• Stimulate libido

Question 7

Anabolic actions of Androgens (3)

Answer 7

• Increase protein synthesis
• Increased lean body mass
• DEC Fat

*similar to GH

Question 8

Effect of Androgens on growth (2)

Answer 8

• Skeletal growth and closure of epiphyses of long bones during puberty and adolescence
• Growth of larynx –> Voice Deepening

Question 9

Metabolic/hematologic actions of androgens (6)

Answer 9

• Erythropoiesis
• Decreased clotting factors production (opposite of estrogen)
• Increased skin sebum
• Decrease HDL but INC LDL :-(
• Androgenic alopecia (male pattern baldness)
• Increases bone density

Question 10

Consequences of androgen deficiency in men (6)

Answer 10

1. Decreased libido; erectile dysfunction
2. Decreased lean muscle mass w/INC Fat
3. Decreased axillary / pubic hair
4. Anemia
5. Osteoporosis
6. Decreased energy, sense of well being

Question 11

Therapeutic uses of androgens (3)

Answer 11

-HRT in primary or secondary hypogonadism
(gonads must be responsive)
-Delayed puberty
-Male Osteoporosis

Question 12

Which androgens are used in hormone replacement therapy? (2)

Answer 12

• Testosterone enanthate

- Testosterone cypionate

Question 13

Clinical indication of Testosterone enanthate and Testosterone cypionate

Answer 13

hypOgonadism

Question 14

Effect of Testosterone enanthate and Testosterone cypionate (2)

Answer 14

• [Primary and Secondary Sex Characteristics]

- Alterations in body musculature such as Fat distribution

Question 15

SEs of Testosterone enanthate and Testosterone cypionate (7)

Answer 15

CLAP for (H)arry (B)arry

• Cholestatic jaundice sundrome (protein synthesis in liver)
• Liver carcinoma
• Benign prostatic hyperplasia
• Prostate CA
• Gynecomastia
• Acne
• Headache

Question 16

Contraindication of Testosterone enanthate and Testosterone cypionate (3)

Answer 16

• Breast cancer in men
• Prostate cancer
• Pregnancy when used in women

Question 17

Delivery routes and formulations of Testosterone enanthate and Testosterone cypionate (4)

Answer 17

• Intramuscular
• Transdermal
• Topical gel
• Oral

*The transdermal is preferred to prevent first pass hepatic metabolism

Question 18

[Drug class/MOA] of Flutamide

Answer 18

[Androgen R Blocker] –> prevents DHT & Testosterone from binding

Question 19

Clinical indications of Flutamide (2)

Answer 19

• Metastatic Prostate Cancer

- BPH

Question 20

Side Effects of Flutamide (4)

Answer 20

• Hepatotoxicity
• Hematopoietic disorders
• Rash
• Constitutional (HA/Nausea)

Question 21

Contraindication of Flutamide

Answer 21

Severe Liver Dz

Question 22

Compare efficacy between Flutamide and other tx in prostate cancer

Answer 22

Flutamide > [DES and Leuprolide] which shut down LH and FSH to block androgen synthesis

Question 23

Effectiveness of Flutamide

Answer 23

Excellent when combined with medical or surgical castration

Question 24

[Drug class/MOA] of spironolactone (2)

Answer 24

Androgen R Blocker & Aldosterone R Blocker

Question 25

Drug indications of spironolactone (7)

Answer 25

"Spironolactone (H)as (P)owerful HACEK " - Hirsutism - HTN - Acne vulgaris - Edema 2º to heart failure - Cirrhosis or nephrotic syndrome - Kalemia (hypOkalemia) - Primary aldosteronism

Question 26

Side Effects of spironolactone (6)

Answer 26

"Spironolactone speared at me like a DHAGGA" - Dyspepsia - Hyperkalemic metabolic acidosis - [Agranulocytosis systemic lupus erythematosus] - Gynecomastia - GI Hemorrhage - Abnormal menstruation and also... - Lethargy - Impotence - Rash - Breast cancer - not yet established

Question 27

Contraindications of spironolactone (3)

Answer 27

- Anuria - Hyperkalemia - Acute renal insufficiency

Question 28

[Drug class/MOA] of Finasteride

Answer 28

[5 alpha reductase II inhibitor] --> Inhibits Peripheral Testosterone conversion to DHT

Question 29

Drug indications of Finasteride (2)

Answer 29

- BPH | - Androgenic alopecia

Question 30

Side Effects of Finasteride (4)

Answer 30

"Finesse too much --> BLEP" - Breast CA in males - Libido DEC - Erectile Dysfunction & Ejaculation problems - Breast TTP

Question 31

Contraindications of Finasteride (2)

Answer 31

- Known or suspected pregnancy | - Women and children

Question 32

Effects of Finasteride on the prostate

Answer 32

-Improves urine flow (especially in large prostates) * alternative to transurethral resection of prostate (TRUP) * up to 25% reduction in prostate size when consistently used for one year

Question 33

Which organs can [5 alpha reductase II] be found? (3)

Answer 33

- Prostate - Liver - Skin