Androgens and Anabolic

Steroids

Objectives
1. Discuss effects of endogenous androgens.
2. Discuss uses and effects of exogenous
androgens and anabolic steroids.
3. Describe potential consequences of abusing
androgens and anabolic steroids.
4. Counsel clients about the physiologic effects
of the dietary supplements androstenedione
and dehydroepiandrosterone (DHEA).

PENDAHULUAN
Androgens are male sex hormones secreted by
the testes in men, the ovaries in women, and the
adrenal cortices of bothsexes.
Like the female sex hormones, the naturally
occurring male sex hormones are steroids
synthesized from cholesterol.
The sex organs and adrenal glands can produce
cholesterol or remove it from the blood.
Cholesterol then undergoes a series of
conversions to progesterone, androgenic
prehormones, and testosterone.

 The androgens produced by the ovaries have

little androgenic activity and are used mainly as
precursor substances for the production of
naturally occurring estrogens.
The adrenal glands produce several androgens,
including androstenedione and
dehydroepiandrosterone (DHEA).
Androstenedione and DHEA are weak
androgens with little masculinizing effect that are
mainly converted to estrogens.

Testosterone
Testosterone is normally the only important male
sex hormone.
It is secreted by the Leydigs cells in the testes in
response to stimulation by luteinizing hormone
from the anterior is normally the only important
male sex hormone.
It is secreted by the Leydigs cells in the testes in
response to stimulation by luteinizing hormone
from the anterior pituitary gland

 The main functions of testosterone are

related to the development of male sexual
characteristics, reproduction, and
metabolism

EFFECTS OF TESTOSTERONE
ON BODY TISSUES: FETAL
Large amounts of chorionic gonadotropin are produced
by the placenta during pregnancy.
Chorionic gonadotropin is similar to luteinizing hormone
(LH) from the anterior pituitary gland. It promotes
development of the interstitial or Leydigs cells in fetal
testes, which then secrete testosterone. Testosterone
production begins the second month of fetal life.
When present,testosterone promotes development of
male sexual characteristics (eg, penis, scrotum, prostate
gland, seminal vesicles, and seminiferous tubules), and
suppresses development of female sexual
characteristics. In the absence of testosterone, the fetus
develops female sexual characteristics.

EFFECTS OF TESTOSTERONE
ON BODY TISSUES: FETAL
Testosterone also provides the stimulus for the
descent of the testes into the scrotum.
This normally occurs after the seventh month of
pregnancy, when the fetal testes are secreting
relatively large amounts of testosterone.
If the testes do not descend before birth,
administration of testosterone or gonadotropic
hormone, which stimulates testosterone
secretion, produces descent in most cases

EFFECTS OF TESTOSTERONE
ON BODY TISSUES: ADULT
Little testosterone is secreted in boys until 11 to 13 years
of age.
At the onset of puberty, testosterone secretion increases
rapidly and remains at a relatively high level until about
50 years of age,after which it gradually declines.
The testosterone secreted at puberty acts as a growth
hormone to produce enlargement of the penis, testes,
and scrotum until approximately 20 years of age.
The prostate gland,seminal vesicles, seminiferous
tubules, and vas deferens also increase in size and
functional ability.
Under the combined influence of testosterone and
follicle-stimulatinghormone (FSH) from the anterior
pituitary gland, sperm production is initiated and
maintained throughout the mans reproductive life.

EFFECTS OF TESTOSTERONE
ON BODY TISSUES: ADULT
Skin. Testosterone increases skin thickness and
activity of the sebaceous glands. Acne in the
male adolescent is attributed to the increased
production of testosterone.
Voice. The larynx enlarges and deepens the
voice of theadult man.
Hair. Testosterone produces the distribution of
hair growthon the face, limbs, and trunk typical of
the adult man. In men with a genetic trait toward
baldness, large amounts of testosterone cause
alopecia (baldness) of the scalp.

EFFECTS OF TESTOSTERONE
ON BODY TISSUES: ADULT
Skeletal muscles. Testosterone is largely
responsible for the larger, more powerful
muscles of men. This characteristic is caused by
the effects of testosterone on protein
metabolism. Testosterone helps the body retain
nitrogen, form new amino acids, and build new
muscle protein. At the same time, it slows the
loss of nitrogen and amino acids formed by
theconstant breakdown of body tissues. Overall,
testosterone increases protein anabolism
(buildup) and decreases protein catabolism
(breakdown).

EFFECTS OF TESTOSTERONE
ON BODY TISSUES: ADULT
Bone. Testosterone makes bones thicker and
longer. After puberty, more protein and calcium
are deposited and retained inbone matrix. This
causes a rapid rate of bone growth. The height
of a male adolescent increases rapidly for a
time, then stops as epiphyseal closure occurs.
This happens when the cartilage at the end of
the long bones in the arms and legs
becomesbone. Further lengthening of the bones
is then prevented.

INDIKASI ANDROGEN
When male sex hormones or androgens are
given from exogenous sources for therapeutic
purposes, they produce the same effects as the
naturally occurring hormones.
These effects include inhibition of endogenous
sex hormones and sperm formation through
negative feedback of pituitary luteinizing
hormone (LH) and follicle stimulating hormone
(FSH).

 Male sex hormones given to women antagonize

or reduce the effects of female sex hormones.
Thus, administration of androgenic or anabolic
steroids to women suppresses menstruation and
causes atrophy of the endometrial lining of the
uterus.
Several dosage forms of androgens are
available; they differ mainly in route Of
administration and pharmacokinetics.

 Naturally occurring androgens are given

by injection because they are metabolized
rapidly by the liver if given orally.
Some esters of testosterone have been
modified to slow the rate of metabolism
and thus prolong action. For example,
intramuscular (IM) testosterone cypionate
and testosterone enanthate have slow
onsets of action and last 2 to 4 weeks.

 Oral testosterone is extensively metabolized in

its first pass through the liver, so that nearly half
of adose is lost before it reaches the systemic
circula-tion.
As a result, doses as high as 400 mg/day may
be needed to produce adequate blood levels for
full replacement therapy.
Methyltestosterone is a syn-thetic formulation
that is less extensively metabolized by the liver
and more suitable for oral administration

 Several transdermal formulations of

testosterone are available. They have a
rapid onset of action and last
approximately 24 hours. A topical gel (a
10-g dose delivers 100 mg) produces
normal serum testosterone levels within 4
hours after application, and absorption of
testosterone into the blood continues for
24 hours.

 When the gel is discontinued, serum testosterone levels

remain in the normal range for 24 to 48 hours, but
decrease to pretreatment levels within about 5 days.
With Testoderm, the serum testosterone concentration
reaches a maximum level within 2 to 4 hours and
declines within 2 hours after the skin patch is removed
Testoderm must be applied to the scrotum to achieve
adequate blood levels; scrotal skin is much more
permeable to testosteronethan other skin areas.
Testoderm TTS is applied to skin on the arm, back, or
buttocks.

 Androderm is also applied to nonscrotal

skin, and testosterone is continuously
absorbed for 24 hours, with normal blood
levels achieved during the rst day of drug
use. Applying the patch at night produces
serum testosterone levels similar to those
in healthy young men (ie, higher
concentrations in the morning and lower
ones in the evening).

 Danazol is a synthetic drug with weak androgenic activity. It is given orally, has a half-life of 4 to 5 hours, and
ismetabolized in the liver.
Route of excretion is unknown. All synthetic anabolic
steroids are weak androgens.
Consequently, giving these drugs for anabolic effects
also produces masculinizing effects. This characteristic
limits the clinical usefulness of these drugs in women
and children.
Profound changes in growth and sexual development
may occur if these drugs are given to young children.

Indications for Use

With male sex hormones, the most clear-cut indication
for use is to treat androgen deciency states (eg,
hypogonadism,cryptorchidism, impotence, oligospermia)
in boys and men.
Hypogonadism may result from hypothalamic-pituitary or
testicular dysfunction.
In prepubertal boys, administration of the drugs
stimulates the development of masculine characteristics.
In postpubertal men who become androgen decient, the
hormones re-establish and maintain masculine
characteristics and functions.

Indications for Use

In women, danazol (Danocrine) may be used to prevent
or treat endometriosis or brocystic breast disease.
Anabolic steroids are more often abused for bodybuilding purposes than used for therapeutic effects.
Although some drug literature still lists metastatic breast
cancer and some types of anemia as indications for use,
androgens have largely been replaced by newer drugs
for these purposes.
In breast cancer, for example, androgens are secondline
hormonal agents, after anti-estrogens (eg, tamoxifen).
Inanemia associated with renal failure, synthetic
erythropoietin is more effective and likely to be used.

Contraindications to Use
Androgens and anabolic steroids are
contraindicated during pregnancy (because of
possible masculinizing effects on a female
fetus), in clients with preexisting liver disease,
and in men with prostate gland disorders.
Men with enlarged prostates may have
additional enlargement, and men with prostatic
cancer may experience tumor growth.
Although not contraindicated in children, these
drugs must be used very cautiously