Pharm #3 - Androgens

Question 1

State the physiological actions of androgens on the reproductive system

Answer 1

REPRODUCTIVE
Growth, development, maintenance of primary and secondary male sex characteristics
Puberty in females
Promote spermatogenesis (w/ FSH)
Neuroendocrine regulation of gonadotropin secretion

Question 2

State the physiological actions of androgens (anabolic)

Answer 2

ANABOLIC

Increase protein synthesis, lean body mass, skeletal muscle growth, reduce fat mass

Question 3

State the physiological actions of androgens (growth)

Answer 3

GROWTH
Stimulates skeletal growth, epiphyseal closure
Growth of larynx at puberty, voice deepening

Question 4

State the physiological actions of androgens (metabolic)

Answer 4

METABOLIC
 Erythropoiesis
 Decreased synthesis of clotting factors
 Increased sebum production in skin
 Decrease HDL; increase LDL
 Androgenic alopecia (male pattern baldness)

Question 5

CONSEQUENCES OF ANDROGEN DEFICIENCY IN MEN -6

Answer 5

1. Decreased libido, erectile dysfunction
2. Decreased skeletal muscle mass; increased adipose tissue mass
3. Decreased axillary and pubic hair
4. Anemia
5. Osteoporosis
6. Decreased energy and sense of well being

Question 6

THERAPEUTIC USES OF ANDROGENS (3)

Answer 6

HRT in primary or secondary hypogonadism

Induction of puberty in delayed maturation

Rx of osteoporosis in males (similar to estrogen on its action of bone)

Question 7

What are the 2 androgens used in HRT

Answer 7

Testosterone enanthate

Testosterone cypionate

Question 8

Testosterone enanthate
Testosterone cypionate

• INdication
• MOA

Answer 8

Hypogonadism

Replacement of testosterone produces androgenic effects, such as:
Growth and maturation of prostate
Seminal vesicles
Penis & Scrotum
Development of male hair distribution
Laryngeal enlargement
Vocal cord thickening
Alterations in body musculature, and
Fat distribution

Question 9

Testosterone enanthate
Testosterone cypionate

Side effects -7 (main 1)

Answer 9

1. Cholestatic jaundice syndrome***
   (similar to estrogen - progesterone combo)
2. Liver carcinoma
3. Benign prostatic hyperplasia
4. Prostate cancer
5. Gynecomastia (excess converted to estrogen)
6. Acne (sebaceous gland d
   evelopment)
7. Headache

Question 10

Testosterone enanthate
Testosterone cypiona

Contraindications - 3

Answer 10

Breast cancer in men (androgen is converted to estrogen = bad)

Prostate cancer

Pregnancy when used in women (stimulate estrogen production)

Question 11

Flutamide

MOA

Indication s(2)

Answer 11

Competitive inhibition of dihydrotestosterone & testosterone binding to the receptor
(androgen receptor antagonist)

Metastatic prostate cancer
Benign prostatic hypertrophy

Question 12

Flutamide

SE (2 main)

COntra -1

Answer 12

Hepatotoxicity
 Hematopoietic disorders
 Diarrhea
 Nausea
 Rash
 Hot Flashes

Contra: Severe hepatic impairment

Question 13

better for prostate cancer

- DES 
or
-leuprolide
or
- flutamide

Answer 13

Flutamide is comparatively better than DES and leuprolide in treatment of prostate cancer
Highly effective when combined with medical or surgical castration

DES  synthetic estrogen (non-aromatic)
half life is very long
offspring can result in adenocarcinoma

Leuprolide – GnRH antagonist

Question 14

Spironolactone

MOA

Answer 14

Competitive inhibition of dihydrotestosterone & testosterone binding to the receptor

Question 15

Spironolactone

indications - 6

Answer 15

Hirsutism
 Hypertension
 Acne vulgaris
 Edema associated with heart failure
 Cirrhosis or nephrotic syndrome
 Hypokalemia

Question 16

Spironolactone

SE

(10)

Answer 16

1. Gastrointestinal hemorrhage
2. Hyperkalemic metabolic acidosis
3. Agranulocytosis systemic lupus erythematosus
4. Gynecomastia
5. Dyspepsia
6. Lethargy
7. Abnormal menstruation
8. Impotence
9. Rash
10. Breast cancer – not yet established

Question 17

3 contra for spironolactone

Answer 17

Anuria
Hyperkalemia
Acute renal insuffiency

*aldosterone receptor antagonist but also acts as an androgen receptor antagonist

Question 18

Finasteride

MOA

Indications -2

Answer 18

Selective inhibition of type II 5 α-reductase, the enzyme responsible for conversion of testosterone to dihydrotestosterone in prostate, liver & skin

1. Benign prostatic hyperplasia
2. Androgenic alopecia

Question 19

Finasteride

• adverse - 5

Answer 19

All functions of DHT

1. Neoplasm of male breast (rare and not yet investigated)
2. Breast tenderness
3. Decreased libido
4. Erectile dysfunction
5. Ejaculatory disorder

Question 20

Finasteride

Contra - 1

Answer 20

Known or suspected pregnancy

Question 21

Improves urine flow (smaller cells)

Can be used as alternative to transurethral resection of prostate (TRUP)

Up to 25% reduction in prostate size when consistently used for one year

Most effective in patients with large prostates

Women should not be treated with finasteride

Answer 21

Finasteride