Anabolic steroid Totally Explained

Everything about Anabolic Steroid totally explained

Anabolic steroids, anabolic-androgenic steroids or AAS, are a class of steroid hormones related to the hormone testosterone. They increase protein synthesis within cells, which results in the buildup of cellular tissue (anabolism), especially in muscles. Anabolic steroids also have androgenic and virilizing properties, including the development and maintenance of masculine characteristics such as the growth of the vocal cords and body hair. The word anabolic comes from the Greek: anabole, "to build up", and the word androgenic comes from the Greek: andros, "man" + genein, "to produce".
   Anabolic steroids were first isolated, identified and synthesized in the 1930s, and are now used therapeutically in medicine to stimulate bone growth and appetite, induce male puberty, and treat chronic wasting conditions, such as cancer and AIDS. Anabolic steroids also produce increases in muscle mass and physical strength, and are consequently used in sport and bodybuilding to enhance strength or physique. Serious health risks can be produced by long-term use or excessive doses of anabolic steroids. These effects include harmful changes in cholesterol levels (increased low-density lipoprotein and decreased high-density lipoprotein), acne, high blood pressure, liver damage, and dangerous changes in the structure of the left ventricle of the heart. Some of these effects can be mitigated by exercise, or by taking supplemental drugs. In particular, the use of steroid hormones pre-dates their identification and isolation: medical use of testicle extract began in the late 19th century while its effects on strength were still being studied. In 1889, the 72-year-old British neurologist Charles-Édouard Brown-Séquard injected himself with an extract of dog and guinea pig testicles, and reported at a scientific meeting that these injections had led to a variety of beneficial effects.
   This testicular hormone was first identified by Karoly Gyula David, E. Dingemanse, J. Freud and Ernst Laqueur in a May 1935 paper "On Crystalline Male Hormone from Testicles (Testosterone)." They named the hormone testosterone, from the stems of testicle and sterol, and the suffix of ketone. The chemical synthesis of testosterone was achieved in August that year, when Butenandt and G. Hanisch published a paper describing "A Method for Preparing Testosterone from Cholesterol." Only a week later, the third group, Ruzicka and A. Wettstein, announced a patent application in a paper "On the Artificial Preparation of the Testicular Hormone Testosterone (Androsten-3-one-17-ol)." Ruzicka and Butenandt were offered the 1939 Nobel Prize for Chemistry for their work, but the Nazi government forced Butenandt to decline the honor. The development of muscle-building properties of testosterone was pursued in the 1940s, in the Soviet Union and in Eastern Bloc countries such as East Germany, where steroid programs were used to enhance the performance of Olympic and amateur weight lifters. In response to the success of Russian weightlifters, the U.S. Olympic Team physician Dr. John Ziegler worked with synthetic chemists to develop an anabolic steroid for American weightlifters, resulting in the production of methandrostenolone (Dianabol). Dianabol, developed by Ciba Pharmaceuticals, was approved for use in the U.S. by the Food and Drug Administration in 1958. Dianabol had the same strength building properties as testosterone, but with reduced side effects.
   From the 1950s until the 1980s, there were doubts that anabolic steroids produced anything more than a placebo effect. In a 1972 study, participants were informed they'd receive injections of anabolic steroids on a daily basis, but instead had actually been given a placebo. They reportedly couldn't tell the difference, and the perceived performance enhancement was similar to that of subjects taking the real anabolic compounds. According to Geraline Lin, a researcher for the National Institute on Drug Abuse, these results remained unchallenged for 18 years, even though the study used inconsistent controls and insignificant doses. In a 2001 study, the effects of high doses of anabolic steroids were examined, by injecting variable doses (up to 600 mg/week) of testosterone enanthate into muscle tissue for 20 weeks. The results showed a clear increase in muscle mass and decrease in fat mass associated with the testosterone doses.

Pharmacology

Routes of administration

Anabolic steroids are primarily administered orally (by mouth) or parenterally. Some anabolic steroids may also be administered by topical or transdermal methods; however, not as much is known of these more recently developed routes of administration. The traditional routes of administration don't have differential effects on the efficacy of the drug. Studies indicate that the anabolic properties of anabolic steroids are relatively similar despite the differences in pharmacokinetic principles such as first-pass metabolism. However, the first-pass metabolism that orally-administered AAS are subjected to has been shown to produce more harmful side effects, particularly liver damage.

Anabolic and androgenic effects

As the name suggests, anabolic-androgenic steroids have two different, but overlapping, types of effects. First, they're anabolic, meaning that they promote anabolism (cell growth). Some examples of the anabolic effects of these hormones are increased protein synthesis from amino acids, increased appetite, increased bone remodeling and growth, and stimulation of bone marrow, which increases the production of red blood cells.
Second, these steroids are androgenic or virilizing, meaning in particular that they affect the development and maintenance of masculine characteristics. The biochemical functions of androgens such as testosterone are numerous. Processes affected include pubertal growth, sebaceous gland oil production, and sexuality (especially in fetal development). Some examples of virilizing effects are growth of the clitoris in females and the penis in male children (the adult penis doesn't grow even when exposed to high doses of androgens), increased growth of androgen-sensitive hair (pubic, beard, chest, and limb hair), increased vocal cord size, deepening the voice, increased libido, suppression of natural sex hormones, and impaired production of sperm.
Through a combination of these effects, anabolic steroids stimulate the formation of muscles and hence cause an increase in the size of muscle fibers, leading to increased muscle mass and strength. This increase in muscle mass is mostly due to larger skeletal muscles, and is caused by both increased production of muscle proteins as well as a decline in the breakdown rate of these proteins. A high testosterone dose also decreases the amount of fat in muscle, while increasing protein content. Anabolic steroids also decrease overall fat.

Adverse effects

Anabolic steroids can cause many adverse effects. Most of these side effects are dose-dependent, the most common being elevated blood pressure, especially in those with pre-existing hypertension, and harmful changes in cholesterol levels: some steroids cause an increase in LDL cholesterol and a decrease in HDL cholesterol. Anabolic steroids such as testosterone also increase the risk of cardiovascular disease or coronary artery disease. Acne is fairly common among anabolic steroid users, mostly due to stimulation of the sebaceous glands by increased testosterone levels. Conversion of testosterone to dihydrotestosterone (DHT) can accelerate the rate of premature baldness for those who are genetically predisposed.
   Other side effects can include alterations in the structure of the heart, such as enlargement and thickening of the left ventricle, which impairs its contraction and relaxation. Possible effects of these alterations in the heart are hypertension, cardiac arrhythmias, congestive heart failure, heart attacks, and sudden cardiac death. These changes are also seen in non-drug using athletes, but steroid use may accelerate this process. However, both the connection between changes in the structure of the left ventricle and decreased cardiac function, as well as the connection to steroid use have been disputed.
   High doses of oral anabolic steroid compounds can cause liver damage as the steroids are metabolized (17α-alkylated) in the digestive system to increase their bioavailability and stability. When high doses of such steroids are used for long periods, the liver damage may be severe and lead to liver cancer.
   There are also gender-specific side effects of anabolic steroids. Development of breast tissue in males, a condition called gynecomastia (which is usually caused by high levels of circulating estrogen), may arise because of increased conversion of testosterone to estrogen by the enzyme aromatase. Reduced sexual function and temporary infertility can also occur in males. Another male-specific side effect which can occur is testicular atrophy, caused by the suppression of natural testosterone levels, which inhibits production of sperm (most of the mass of the testes is developing sperm). This side effect is temporary: the size of the testicles usually returns to normal within a few weeks of discontinuing anabolic steroid use as normal production of sperm resumes. Female-specific side effects include increases in body hair, deepening of the voice, enlarged clitoris, and temporary decreases in menstrual cycles. When taken during pregnancy, anabolic steroids can affect fetal development by causing the development of male features in the female fetus and female features in the male fetus.
   A number of severe side effects can occur if adolescents use anabolic steroids. For example, the steroids may prematurely stop the lengthening of bones (premature epiphyseal fusion through increased levels of estrogen metabolites), resulting in stunted growth. Other effects include, but are not limited to, accelerated bone maturation, increased frequency and duration of erections, and premature sexual development. Anabolic steroid use in adolescence is also correlated with poorer attitudes related to health.

Mechanism of action

The effect of anabolic steroids on muscle mass is caused in at least two ways: first, they increase the production of proteins; second, they reduce recovery time by blocking the effects of stress hormone cortisol on muscle tissue, so that catabolism of muscle is greatly reduced. It has been hypothesized that this reduction in muscle breakdown may occur through anabolic steroids inhibiting the action of other steroid hormones called glucocorticoids that promote the breakdown of muscles. Anabolic steroids also affect the number of cells that develop into fat-storage cells, by favouring cellular differentiation into muscle cells instead.
The main way in which steroid hormones interact with cells is by binding to proteins called steroid receptors. When steroids bind to these receptors, the proteins move into the cell nucleus and either alter the expression of genes or activate processes that send signals to other parts of the cell.
In the case of anabolic steroids, the receptors involved are called the androgen receptors. The mechanisms of action differ depending on the specific anabolic steroid. Different types of anabolic steroids bind to the androgen receptor with different affinities, depending on their chemical structure. On the other hand, steroids such as oxandrolone bind tightly to the receptor and act mostly on gene expression.

Pharmacodynamics

The pharmacodynamics of anabolic steroids are unlike peptide hormones. Peptide hormones can't penetrate the cell membranes and only indirectly affect the nucleus of target cells through their interaction with the cell’s surface receptors. Conversely, as steroid hormones, anabolic steroids are membrane permeable and influence the nucleus of cells by direct action. The pharmacodynamic action of anabolic steroids begin when the exogenous hormone penetrates the permeable membrane of the target cell and binds to an androgen receptor located in the cytoplasm of that cell. From there, the entire receptor-complex moves from the cytoplasm into the nucleus by a process called translocation. Once in the nucleus, the receptor-complex interacts with the DNA by recoding the genetic information to produce more myonuclei, this is known as transcription. After the restructuring of DNA, mRNA sends the new message back into the cytoplasm where specific organelles, such as ribosomes, make new protein.

Medical and non-medical uses

Medical uses

Since the discovery and synthesis of testosterone in the 1930s, anabolic steroids have been used by physicians for many purposes, with varying degrees of success.

Bone marrow stimulation: For decades, anabolic steroids were the mainstay of therapy for hypoplastic anemias due to leukemia or kidney failure, especially aplastic anemia. Anabolic steroids have largely been replaced in this setting by synthetic protein hormones (such as epoetin alfa) that selectively stimulate growth of blood cell precursors.
Growth stimulation: Anabolic steroids can be used by pediatric endocrinologists to treat children with growth failure. However, the availability of synthetic growth hormone, which has fewer side effects, makes this a secondary treatment.
Stimulation of appetite and preservation and increase of muscle mass: Anabolic steroids have been given to people with chronic wasting conditions such as cancer and AIDS.
Induction of male puberty: Androgens are given to many boys distressed about extreme delay of puberty. Testosterone is now nearly the only androgen used for this purpose and has been shown to increase height, weight, and fat-free mass in boys with delayed puberty.
Testosterone enanthate has frequently been used as a male contraceptive and it's thought that in the near future it could be used as a safe, reliable, and reversible male contraceptive.
Anabolic steroids have been found in some studies to increase lean body mass and prevent bone loss in elderly men. However, a 2006 placebo-controlled trial of low-dose testosterone supplementation in elderly men with low levels of testosterone found no benefit on body composition, physical performance, insulin sensitivity, or quality of life.
Used in hormone replacement therapy for men with low levels of testosterone and is also effective in improving libido for elderly males.
Used to treat gender dysmorphia (the belief that one was born the wrong gender) by producing secondary male characteristics, such as a deeper voice, increased bone and muscle mass, facial hair, increased levels of red blood cells and clitoral enlargement in female-to-male patients.

Non-medical use and abuse

It is difficult to determine what percent of the population in general have actually used anabolic steroids, but the number seems to be fairly low. Studies in the United States have shown anabolic steroid users tend to be mostly middle-class heterosexual men with a median age of about 25 who are noncompetitive bodybuilders and non-athletes and use the drugs for cosmetic purposes. Another study found that non-medical use of AAS among college students was at or less than 1%. According to a recent survey, 78.4% of steroid users were noncompetitive bodybuilders and non-athletes while about 13% reported unsafe injection practices such as reusing needles, sharing needles, and sharing multidose vials, though a 2007 study found that sharing of needles was extremely uncommon among individuals using anabolic steroids for non-medical purposes, less than 1%. Another 2007 study found that 74% of non-medical anabolic steroid users had secondary college degrees and more had completed college and less had failed to complete high school than is expected from the general populace. The same study found that individuals using Anabolic steroids for non-medical purposes had a higher employment rate and a higher household income than the general population. According to one study, AAS users also distrust their physicians and in the sample 56% hadn't disclosed their AAS use to their physicians. Another 2007 study had similar findings, showing that while 66% of individuals using anabolic steroids for non-medical purposes were willing to seek medical supervision for their steroid use, 58% lacked trust in their physicians, 92% felt that the medical communities knowledge of non-medical anabolic steroid use was lacking and 99% felt that the public has an exaggerated view of the side effects of anabolic steroid use.
Anabolic steroids have been used by men and women in many different kinds of professional sports (cricket, track and field, weightlifting, bodybuilding, shot put, cycling, baseball, wrestling, mixed martial arts, boxing, football, etc.) to attain a competitive edge or to assist in recovery from injury. Such use is prohibited by the rules of the governing bodies of many sports. Anabolic steroid use occurs among adolescents, especially by those participating in competitive sports. It has been suggested that the prevalence of use among high-school students in the U.S. may be as high as 2.7%. Male students used anabolic steroids more frequently than female students and, on average, those who participated in sports used steroids more often than those who did not.

Administration

There are three common forms in which anabolic steroids are administered: oral pills, injectable steroids, and skin patches. Oral administration is most convenient, but the steroid must be chemically modified so that the liver can't break it down before it reaches the systemic circulation; these formulations can cause liver damage in high doses. Injectable steroids are typically administered into the muscle, not into the vein, to avoid sudden changes in the amount of the drug in the bloodstream. Transdermal patches (adhesive patches placed on the skin) may also be used to deliver a steady dose through the skin and into the bloodstream. Injection is the most common method used by individuals administering anabolic steroids for non-medical purposes. Some androgens are converted by the body into estrogen, a process, known as aromatisation, which has potential adverse effects described previously. Consequently, during a steroid cycle, users may also take drugs to prevent aromatisation (called aromatase inhibitors) or drugs which affect estrogen receptor binding (called selective estrogen receptor modulators or SERMs): for example, the SERM tamoxifen prevents binding to the estrogen receptor in the breast, and so it can be used to reduce the risk of gynecomastia.
To combat the natural testosterone suppression and to restore proper function of numerous glands involved, what is known as "post-cycle therapy" or PCT is sometimes used. PCT takes place after each cycle of anabolic steroid use and typically consists of a combination of the following drugs, depending on which protocol is used:

A SERM such as clomiphene citrate or tamoxifen citrate (this is the primary PCT drug).

An aromatase inhibitor such as anastrozole.

Human chorionic gonadotropin, although it's more common now to use this throughout the cycle rather than after it. The aim of PCT is to return the body's endogenous hormonal balance to its original state within the shortest period of time. People prone to the premature hair loss exacerbated by steroid use have been known to take the prescription drug finasteride for prolonged periods of time. Finasteride reduces the conversion of testosterone to DHT, the latter having much higher potency for alopecia. Finasteride is useless in the cases when steroid isn't converted into a more androgenic derivative. Since anabolic steroids can be toxic to the liver or can cause increases in blood pressure or cholesterol, many users consider it ideal to get frequent blood work tests and blood pressure tests to make sure their blood pressure or cholesterol are still within normal levels.

Controversies

Anabolic steroids, like other drugs, have been the subject of controversy. Although anabolic steroids have been frequently linked in the media to dangerous side effects and high mortality rates, they're used widely in medicine with an accepted side effect profile, providing patients are monitored for possible complications. Former assistant professor at the University of Toronto and World Wrestling Entertainment athletic physician Mauro Di Pasquale has stated, "As used by most people, including athletes, the adverse effects of anabolic steroids appear to be minimal."
In 1992, NFL football player Lyle Alzado died from brain cancer, which he attributed to the use of anabolic steroids. However, although steroids have been known to cause liver cancer, there's no published evidence that anabolic steroids cause either brain cancer or the specific type of T-cell lymphoma that caused his death.
Other purported side effects include the idea that anabolic steroids have caused many teenagers to commit suicide. While lower levels of testosterone have been known to cause depression, and ending a steroid cycle temporarily lowers testosterone levels, the hypothesis that anabolic steroids are responsible for suicides among teenagers remains unproven. Although teen bodybuilders have been using steroids since at least the early 1960s, there have been few studies examining a possible link between steroids and suicide in the medical literature. Arnold Schwarzenegger has admitted to using anabolic steroids during his bodybuilding career for many years before they were made illegal, and in 1997 he underwent surgery to correct a defect relating to his heart. Some have assumed this was due to anabolic steroids. Although anabolic steroid use can sometimes cause enlargement and thickening of the left ventricle, Schwarzenegger was born with a congenital genetic defect in which his heart had a bicuspid aortic valve; a condition that rendered his aortic valve with two cusps instead of three, which can occasionally cause problems later in life.

"Roid rage"

Another condition that's frequently discussed as a possible side effect of anabolic steroids is known as "roid rage"; however there's no consensus in the medical literature as to whether such a condition actually exists. Testosterone levels are indeed associated with aggression and hypomania, but the link between other anabolic steroids and aggression remains unclear. While some studies have shown a correlation between manic symptoms and anabolic steroid use, later studies have questioned these conclusions. Individual studies vary in their findings, with some reporting no increase in aggression or hostility with anabolic steroid use, and others finding a correlation. Including a study of two pairs of identical twins, in which one twin used anabolic steroids and the other did not, found that in both cases the steroid-using twin exhibited high levels of aggressiveness, hostility, anxiety and paranoid ideation not found in the "control" twin.
It has previously been theorized that some studies showing a correlation between angry behavior and steroid use are confounded by the fact that steroid users are likely to demonstrate cluster B personality disorders prior to administering steroids. In addition, many case studies have concluded anabolic steroids have little or no real effect on increased aggressive behavior.

Legal and sport restrictions

Legal status

The legal status of anabolic steroids varies from country to country: some have stricter controls on their use or prescription than others. In the U.S., anabolic steroids are currently listed as Schedule III controlled substances under the Controlled Substances Act, which makes the possession of such substances without a prescription a federal crime punishable by up to seven years in prison. Anabolic steroids are also illegal without prescription in Australia, Argentina, Brazil and Portugal, and are listed as Schedule 4 Controlled Drugs in the United Kingdom. On the other hand, anabolic steroids are readily available without a prescription in some countries such as Mexico and Thailand.
The history of the U.S. legislation on anabolic steroids goes back to the late 1980s, when the U.S. Congress considered placing anabolic steroids under the Controlled Substances Act following the controversy over Ben Johnson's victory at the 1988 Summer Olympics in Seoul. During deliberations, the AMA, DEA, FDA as well as the NIDA all opposed listing anabolic steroids as controlled substances, citing the fact that use of these hormones doesn't lead to the physical or psychological dependence required for such scheduling under the Controlled Substance Act. Nevertheless, anabolic steroids were added to Schedule III of the Controlled Substances Act in the Anabolic Steroid Control Act of 1990.

Distribution

In the U.S., Canada and Europe, steroids are purchased just like any other illegal drug, through dealers who are able to obtain the drugs from a number of sources. Most users would prefer to buy from legitimate sources but can't because of the legal restrictions. Instead, illegal anabolic steroids are sold at gyms, competitions, and through the mail. For the most part, these substances are smuggled, but may also be obtained through pharmacists, veterinarians, and physicians. In addition, a significant number of counterfeit products are sold as anabolic steroids, particularly via mail order from websites posing as overseas pharmacies. Individuals also produce fake steroids and attempt to sell them over the Internet, causing a wide variety of health concerns. In the U.S., black market importation continues from Mexico, Thailand, and other countries where steroids are more easily available or not illegal at all.

Movement for decriminalization

After the Anabolic Steroid Control Act of 1990 listed anabolic steroids as Schedule III controlled substances in the U.S., a small movement has arisen that's highly critical of current laws concerning anabolic steroids. On June 21, 2005, Real Sports aired a segment discussing the legality and prohibition of anabolic steroids in America. The show featured Gary I. Wadler, M.D., chairman of the U.S. Anti-Doping Agency and a prominent anti-steroid activist. When pressed for scientific evidence by correspondent Armen Keteyian that anabolic steroids are as "highly fatal" as is often claimed, Wadler admitted there was no evidence. Bryant Gumbel concluded the "hoopla" concerning the dangers of anabolic steroids in the media was "all smoke and no fire". Several other legal reviewers have criticized controlled substance status for anabolic steroids, including lawyer Rick Collins whose book, Legal Muscle, details published resources on anabolic steroids and the law. Collins opposes non-medical teen steroid use or steroid use to cheat in sports, but advocates wider discretion for physicians in the case of mature adults. In 2006, he argued at PUMPED, a steroid seminar in Manhattan, that the reporting of the risks associated with anabolic steroids in the media is biased and misinformed. He also argues that anabolic steroid criminalization increases the risks associated with anabolic steroids due to impurities in black market products. However, the U.S. government's position since the late 1980s has been and continues to be that the risks of steroid use are too great to allow them to be decriminalized or unregulated.

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