Pharmacology of Androgens and Anabolic Steroids Flashcards Preview

Pharmacology Test #5 > Pharmacology of Androgens and Anabolic Steroids > Flashcards

Flashcards in Pharmacology of Androgens and Anabolic Steroids Deck (28)
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1

Testosterone acts as a prohormone for

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

2

5alpha-DHT acts as the mediator of

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

3

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

enhances its anabolic effects

4

Degradation and excretion of androgens

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

5

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

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

6

Type A androgen preparation

esterified androgens

7

Type B androgen preparation

17alpha-alkylated androgens

8

Type C androgen preparation

androgens with changes in the ring structure

9

Some androgenic steroids

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

10

Some anabolic steroids

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

11

Clinical uses of androgenic and anabolic steroids

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

12

Women respond to androgens with

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

13

Contraindications and cautions for the use of androgens

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

14

Antiandrogens are useful in the management of

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

15

Antiandrogens that inhibit androgen synthesis

1. Gonadotropin Releasing Hormone
2. Spironolactone
3. Ketoconazole

16

Antiandrogens that block androgen action

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

17

MOA of GnRh as an antiandrogen

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

18

Therapeutic uses of GnRH as an antiandrogen

to manage prostate metastatic carcinoma and precocious puberty

19

Abiraterone as an antiandrogen

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

20

Spironolactone as an antiandrogen

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

21

Ketoconazole as an antiandrogen

blocks adrenal and testicular androgen synthesis

22

Two types of antiandrogens that block androgen action

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

23

Cyproterone Acetate

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

24

Flutamide

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

25

Bicalutamide

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

26

Nilutamide

treatment of advanced stage prostate cancer; competes with androgens

27

Cimetidine

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

28

Drugs that inhibit 5alpha-reductase

Finasteride and Dutasteride
used to treat BPH