Pharmacology of Androgens and Anabolic Steroids

Question 1

Testosterone acts as a prohormone for

Answer 1

1. 5alpha-dihydrotestosterone production ctalyzed by 5alpha-reductase enzyme
2. Estrogen production catalyzed by aromatase enzyme

Question 2

5alpha-DHT acts as the mediator of

Answer 2

the actions of testosterone in certain target tissues in which the 5alpha-reductase is expressed

Question 3

What does the removal of methyl group in the 19 position of the androgen molecule do?

Answer 3

enhances its anabolic effects

Question 4

Degradation and excretion of androgens

Answer 4

Androgens are metabolized in the liver to inactive 17-ketosteroids; 17-ketosteroids are excreted as conjugates of glucuronic and sulfuric acids

Question 5

Effective systemic concentrations of exogenously administered native testosterone cannot be maintained for a considerable length of time because;

Answer 5

it is inactivated readily in the liver when given orally; also it is absorbed quickly and degraded quickly in liver when administered parenterally

Question 6

Type A androgen preparation

Answer 6

esterified androgens

Question 7

Type B androgen preparation

Answer 7

17alpha-alkylated androgens

Question 8

Type C androgen preparation

Answer 8

androgens with changes in the ring structure

Question 9

Some androgenic steroids

Answer 9

1. Testosterone cypionate
2. Testosterone propionate
3. Testosterone enanthate
4. Methyltestosterone

Question 10

Some anabolic steroids

Answer 10

1. Nandrolone decanoate
2. Oxandrolone
3. Oxymetholone
4. Fluoxymesterone
5. Stanozolol

Question 11

Clinical uses of androgenic and anabolic steroids

Answer 11

1. Androgen replacement therapy in men
2. As protein anabolic agents
3. Growth stimulators
4. Endometriosis
5. Osteoporosis
6. Stimulation of erythropoiesis

Question 12

Women respond to androgens with

Answer 12

hirsutism, acne, amenorrhea, clitoral enlargement, deppening of voice

Question 13

Contraindications and cautions for the use of androgens

Answer 13

1. Androgenic steroids should not be used in pregnant women or women who may become pregnant
2. Male patients with carcinoma or prostate or breast
3. Avoid the use of androgens in infants

Question 14

Antiandrogens are useful in the management of

Answer 14

1. hyperplasia and carcinoma of the prostate
2. acne
3. baldness
4. virilizing syndromes in females
5. precocious puberty in boys
6. inhibition of sex drive in men who are sex offenders

Question 15

Antiandrogens that inhibit androgen synthesis

Answer 15

1. Gonadotropin Releasing Hormone
2. Spironolactone
3. Ketoconazole

Question 16

Antiandrogens that block androgen action

Answer 16

1. Cyproterone acetate
2. Flutamide
3. Finazteride (inhibits 5alpha-reductase)

Question 17

MOA of GnRh as an antiandrogen

Answer 17

uncoupling of GnRH receptors from their effectors; internalization of GnRH receptors; depletion of LH stores in pituitary gonadotrophs

Question 18

Therapeutic uses of GnRH as an antiandrogen

Answer 18

to manage prostate metastatic carcinoma and precocious puberty

Question 19

Abiraterone as an antiandrogen

Answer 19

inhibits activity of 17alpha-hydroxylase; used to treat prostate cancer

Question 20

Spironolactone as an antiandrogen

Answer 20

aldosterone antagonist; inhibits the activity of CP-450 enzymes involved in androgen synthesis

Question 21

Ketoconazole as an antiandrogen

Answer 21

blocks adrenal and testicular androgen synthesis

Question 22

Two types of antiandrogens that block androgen action

Answer 22

1. drugs that compete for binding of testosterine and DHT to the androgen receptor
2. inhibitors of 5alpha-reductase

Question 23

Cyproterone Acetate

Answer 23

Progestin; potent androgen antagonist; used to treat acne, baldness, hirsutism, virilizing of syndromes, precocious puberty, prostatic hypertrophy and carcinoma, inhibition of libido in men

Question 24

Flutamide

Answer 24

competes with androgens for the androgen receptor; used for the treatment of prostatic cancer usually in conjunction with GnRH analogs

Question 25

Bicalutamide

Answer 25

competes with androgens for the androgen receptor; treatment of early stages of prostate carcinoma and hirsutism

Question 26

Nilutamide

Answer 26

treatment of advanced stage prostate cancer; competes with androgens

Question 27

Cimetidine

Answer 27

used primarily in the treatment of peptic ulcer disease; H2 antagonist; competes

Question 28

Drugs that inhibit 5alpha-reductase

Answer 28

Finasteride and Dutasteride

used to treat BPH