Anabolic Steroids: Everything You Ever Wanted to Know

mrkavin

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Q: What are "anabolic steroids" and do they really build muscle? - Technical

A: "Anabolic steroids" is the familiar name for synthetic substances related to the male sex hormones (androgens). They
promote the growth of skeletal muscle (anabolic effects) and the development of male sexual characteristics (androgenic
effects), and also have some other effects.
Some anabolic steroids are taken orally, others are injected intramuscularly, and still others are provided in gels or
creams that are rubbed on the skin. Doses taken by abusers can be 10 to 100 times higher than the doses used for medical
conditions.
Anabolic steroids are drugs that resemble androgenic hormones (sometimes called male hormones) such as testosterone (Figure
1). Athletes consume them in the hope of gaining weight, strength, power, speed, endurance, and aggressiveness. They are
widely used by athletes involved in such sports as track and field (mostly the throwing events), weight lifting, and
American football. However, in spite of their tremendous popularity, their effectiveness is controversial. The research
literature is divided on whether anabolic steroids enhance physical performance. Yet, almost all athletes who consume these
substances acclaim their beneficial effects. Many athletes feel that they would not have been as successful without them.
There are several possible reasons for the large differences between experimental findings and empirical observations. An
incredible mystique has arisen around these substances, providing fertile ground for the placebo effect. The use of
anabolic steroids in the "real world" is considerably different from that in rigidly controlled, double-blind experiments
(in a double blind study, neither the subject nor experimenter knows who is taking the drug). Most studies have not used
the same drug dosage used by athletes. Institutional safeguards prohibit administration of high dosages of possibly
dangerous substances to human subjects. Subjects in research experiments seldom resemble accomplished weight-trained
athletes. Under these conditions, we must assess the results of sound research studies, as well as clinical and empirical
field observations, in order to obtain a realistic profile of the use, effects on performance, and side effects of these
substances.

How Anabolic Steroids Work.

Male hormones, principally testosterone, are partially responsible for the tremendous developmental changes that occur
during puberty and adolescence. Male hormones have androgenic and anabolic effects. Androgenic effects are changes in
primary and secondary sexual characteristics. These include enlargement of the penis and testes, voice changes, hair growth
on the face, axilla, and genital areas, and increased aggressiveness. The anabolic effects of androgens include accelerated
growth of muscle, bone, and red blood cells, and enhanced neural conduction.
Anabolic steroids have been manufactured to enhance the anabolic properties (tissue building) of the androgens and minimize
the androgenic (sex-linked) properties. However, no steroid has eliminated the androgenic effects because the so-called
androgenic effects are really anabolic effects in sex-linked tissues. The effects of male hormones on accessory sex glands,
genital hair growth, and oiliness of the skin are anabolic processes in those tissues. The steroids with the most potent
anabolic effect are also those with the greatest androgenic effect.

Steroid Receptors:
Steroid hormones work by stimulation of receptor molecules in muscle cells, which activate specific genes to produce
proteins (see Figure 1). They also affect the activation rate of enzyme systems involved in protein metabolism, thus
enhancing protein synthesis and inhibiting protein degradation (called an anti-catabolic effect).

How a Steroid Hormone Works:
Heavy resistance training seems to be necessary for anabolic steroids to exert any beneficial effect on physical
performance. Most research studies that have demonstrated improved performance with anabolic steroids used experienced
weight lifters who were capable of training with heavier weights and producing relatively greater muscle tension during
exercise than novice subjects. The effectiveness of anabolic steroids is dependent upon unbound receptor sites in muscle.
Intense strength training may increase the number of unbound receptor sites. This would increase the effectiveness of
anabolic steroids.

Anti-Catabolic Effects Of Anabolic Steroids:
Many athletes have said that anabolic steroids help them train harder and recover faster. They also said that they had
difficulty making progress (or even holding onto the gains) when they were off the drugs. Anabolic steroids may have an
anti-catabolic effect. This means that the drugs may prevent muscle catabolism that often accompanies intense exercise
training. Presently, this hypothesis has not been fully proven.
Anabolic steroids may block the effects of hormones such as cortisol involved in tissue breakdown during and after
exercise. Anabolic steroids may prevent tissue from breaking down following of an intense work-out. This would speed
recovery. Cortisol and related hormones, secreted by the adrenal cortex, also has receptor sites within skeletal muscle
cells. Cortisol causes protein breakdown and is secreted during exercise to enhance the use of proteins for fuel and to
suppress inflammation that accompanies tissue injury.
Anabolic steroids may block the binding of cortisol to its receptor sites, which would prevent muscle breakdown and
enhances recovery. While this is beneficial while the athlete is taking the drug, the effect backfires when he stops taking
it. Hormonal adaptations occur in response to the abnormal amount of male hormone present in the athlete's body. Cortisol
receptor sites and cortisol secretion from the adrenal cortex increase.
Anabolic steroid use decreases testosterone secretion. People who stop taking steroids are also hampered with less male
hormone than usual during the "off" periods. The catabolic effects of cortisol are enhanced when the athlete stops taking
the drugs and strength and muscle size are lost at a rapid rate.
The rebound effect of cortisol and its receptors presents people who use anabolic steroids with several serious problems:
(1) psychological addiction is more probable because they become dependent on the drugs. This is because they tend to lose
strength and size rapidly when off steroids. To stave off deconditioning, athletes may want to take the drugs for long
periods of time to prevent falling behind. (2) Long-term administration increases the chance of serious side-effects. (3)
Cortisol suppresses the immune system. This makes steroid users more prone to diseases, such as cold and flu, during the
period immediately following steroid administration.

Psychological Effects:
Some researchers have speculated that the real effect of anabolic steroids is the creation of a "psychosomatic state"
characterized by sensations of well being, euphoria, increased aggressiveness and tolerance to stress, allowing the athlete
to train harder. Such a psychosomatic state would be more beneficial to experienced weight lifters who have developed the
motor skills to exert maximal force during strength training. Diets high in protein and calories may also be important in
maximizing the effectiveness of anabolic steroids.

Anabolic Steroids and Performance:
The effects of anabolic steroids on physical performance are unclear. Well controlled, double blind studies have rendered
conflicting results. In studies showing beneficial effects, body weight increased by an average of about four pounds, lean
body weight by about six pounds (fat loss accounts for the discrepancy between gains in lean mass and body weight), bench
press increased by about 15 pounds, and squats by about 30 pounds (these values represent the average gains for all studies
showing a beneficial effect). Almost all studies have failed to demonstrate a beneficial effect on maximal oxygen
consumption or endurance capacity. Anabolic steroid studies have typically lasted six to eight weeks and have usually used
relatively untrained subjects.
Most changes in strength during the early part of training are neural: increased strength is mainly due to an improved
ability to recruit motor units. Anabolic steroids affect processes associated with protein synthesis in muscle. Studies
lasting six weeks (typical study length) would largely reflect neural changes and could easily miss the cellular effects of
the drugs.
The gains made by athletes in uncontrolled observations have been much more impressive. Weight gains of thirty or forty
pounds, coupled with thirty percent increases in strength, are not unusual. Such case studies lack credibility because of
the absence of scientific controls. However, it would be foolish to completely disregard such observations because the
"subjects" have been highly trained and motivated athletes.Please see the articles on pharmacology of sport and sports
medicine in the countries of the former Soviet Union for more information on anabolic steroids. Steroid abusers typically
"stack" the drugs, meaning that they take two or more different anabolic steroids, mixing oral and/or injectable types and
sometimes even including compounds that are designed for veterinary use. Abusers think that the different steroids interact
to produce an effect on muscle size that is greater than the effects of each drug individually, a theory that has not been
tested scientifically.

Possible Health Consequences of Anabolic Steroid Abuse
Hormonal system:

men


infertility
breast development
shrinking of the testicles

women

enlargement of the clitoris
excessive growth of body hair

both sexes

male-pattern baldness
Musculoskeletal system
short stature
tendon rupture
Cardiovascular system
heart attacks
enlargement of the heart's left ventricle
Liver
cancer
peliosis hepatis
Skin
acne and cysts
oily scalp
Infection
hepatitis
Psychiatric effects
homicidal rage
mania
delusions

Anabolic steroid abuse has been associated with a wide range of adverse side effects ranging from some that are physically
unattractive, such as acne and breast development in men, to others that are life threatening, such as heart attacks and
liver cancer. Most are reversible if the abuser stops taking the drugs, but some are permanent.
Most data on the long-term effects of anabolic steroids on humans come from case reports rather than formal epidemiological
studies. From the case reports, the incidence of life-threatening effects appears to be low, but serious adverse effects
may be under-recognized or under-reported. Data from animal studies seem to support this possibility. One study found that
exposing male mice for one-fifth of their lifespan to steroid doses comparable to those taken by human athletes caused a
high percentage of premature deaths.

Hormonal system:
Steroid abuse disrupts the normal production of hormones in the body, causing both reversible and irreversible changes.
Changes that can be reversed include reduced sperm production and shrinking of the testicles (testicular atrophy).
Irreversible changes include male-pattern baldness and breast development (gynecomastia). In one study of male
bodybuilders, more than half had testicular atrophy, and more than half had gynecomastia. Gynecomastia is thought to occur
due to the disruption of normal hormone balance. In the female body, anabolic steroids cause masculinization. Breast size
and body fat decrease, the skin becomes co****, the clitoris enlarges, and the voice deepens. Women may experience
excessive growth of body hair but lose scalp hair. With continued administration of steroids, some of these effects are
irreversible.

Musculoskeletal system:
Rising levels of testosterone and other sex hormones normally trigger the growth spurt that occurs during puberty and
adolescence. Subsequently, when these hormones reach certain levels, they signal the bones to stop growing, locking a
person into his or her maximum height.
When a child or adolescent takes anabolic steroids, the resulting artificially high sex hormone levels can signal the bones
to stop growing sooner than they normally would have done.

Cardiovascular system:
Steroid abuse has been associated with cardiovascular diseases (CVD), including heart attacks and strokes, even in athletes
younger than 30. Steroids contribute to the development of CVD, partly by changing the levels of lipoproteins that carry
cholesterol in the blood. Steroids, particularly the oral types, increase the level of low-density lipoprotein (LDL) and
decrease the level of high-density lipoprotein (HDL). High LDL and low HDL levels increase the risk of atherosclerosis, a
condition in which fatty substances are deposited inside arteries and disrupt blood flow. If blood is prevented from
reaching the heart, the result can be a heart attack. If blood is prevented from reaching the brain, the result can be a
stroke.
Steroids also increase the risk that blood clots will form in blood vessels, potentially disrupting blood flow and damaging
the heart muscle so that it does not pump blood effectively.

Liver:
Steroid abuse has been associated with liver tumors and a rare condition called peliosis hepatis, in which blood-filled
cysts form in the liver. Both the tumors and the cysts sometimes rupture, causing internal bleeding.

Skin:
Steroid abuse can cause acne, cysts, and oily hair and skin.

Infection:
Many abusers who inject anabolic steroids use nonsterile injection techniques or share contaminated needles with other
abusers. In addition, some steroid preparations are manufactured illegally under non-sterile conditions. These factors put
abusers at risk for acquiring life-threatening viral infections, such as HIV and hepatitis B and C. Abusers also can
develop infective endocarditis, a bacterial illness that causes a potentially fatal inflammation of the inner lining of the
heart. Bacterial infections also can cause pain and abscess formation at injection sites.

Mechanism of Action:
First, let's take the broadest view possible, but at the molecular level. Consider one molecule of an anabolic/androgenic
steroid (AAS) in the bloodstream, bound to a molecule of testosterone binding globulin (TeBG). A receptor on the outside of
the muscle cell will bring the TeBG/AAS into the cell. This process itself stimulates the metabolism of the cell by
increasing cyclic AMP, but that is not the major effect of AAS use.
Alternatively, the AAS molecule may be free in the bloodstream, not bound to anything. If so, it can easily diffuse into
the cell through the cell membrane, rather like water soaking through paper.
Next, inside the cell, the molecule of AAS binds to a molecule of androgen receptor (AR), which is inside the cell, not in
the cell membrane. The androgen receptor is a very large molecule and is made of about a thousand amino acids. Thus, it is
far larger than the molecule of AAS. The AR has a "hinge" region, and can be folded into either of two shapes. When it
binds a molecule of AAS, the AR folds at the hinge, and is activated.
Think of the AR as being a machine that does nothing unless it is turned on. The AR either has an AAS bound to it, and is
thereby switched on; or it does not, and is switched off. There is no intermediate condition that might cause an AAS to
give a weak effect – there is no being "halfway folded" at the hinge. The only question is, How long does the AR stay
activated before the AAS leaves? The answer, generally, is in the range of a couple of hours.
After the AAS leaves, the AR returns to its original state, and is ready to be used again.
Since the AR can only be either activated or not activated, it is just as much activated by say a bound molecule of
methenolone (from Primobolan) as it is by a bound molecule from any other AAS.
This is not to say that differing AAS may give differing results for other reasons.
Once a molecule of AAS is bound to the AR, the receptor now travels to the nucleus of the cell, and forms a dimer (pair)
with another activated AR. The dimer then binds to certain parts of the DNA, and certain genes then start producing more
mRNA. This is a way for the body to selectively activate only certain genes. In this case, only those genes associated with
androgens are activated, or have their activity increased.
mRNA is different for each gene, and carries the information the cell needs to make specific proteins. Myosin and actin,
which are major components of muscle, are examples of proteins, and these are made, ultimately, as a result of mRNA
production from the genes for those proteins.
At last: muscle protein, our goal. The molecule of AAS ultimately causes the muscle cell to make more of certain proteins,
helping the user to get bigger. (There were steps needed to get from the mRNA to the protein, but we will skip them.)
Does each binding of AAS to an AR result in exactly one extra molecule of protein produced? No. Because even though the AR
is fully activated by any AAS, that does not mean that it always succeeds in binding to DNA. And differing amounts of mRNA
might be produced, because an AR remains active as long as an AAS remains bound to it. If many mRNA molecules are produced,
then, generally, they will cause many corresponding protein molecules to be produced.
So the amount of extra growth per extra activated AR can vary.