Professional Documents
Culture Documents
androgenic
androgenic
Dihydrotestosterone
Prasterone (dehydroepiandrosterone DHEA)
Testosterone
1
2
1.2.1
2 PHARMACOLOGY
2.1
Routes of administrations
The human androgen receptor bound to testosterone[10] The protein is shown as a ribbon diagram in red, green, and blue, with
the steroid shown in white.
2.3
not penetrate the fatty cell membrane and only indirectly aect the nucleus of target cells through their interaction with the cells surface receptors. However, as
fat-soluble hormones, anabolic steroids are membranepermeable and inuence the nucleus of cells by direct action. The pharmacodynamic action of anabolic steroids
begin when the exogenous hormone penetrates the membrane of the target cell and binds to an androgen receptor located in the cytoplasm of that cell. From there, the
compound hormone-receptor diuses into the nucleus,
where it either alters the expression of genes[11] or activates processes that send signals to other parts of the
cell.[12] Dierent types of anabolic steroids bind to the
androgen receptor with dierent anities, depending on
their chemical structure.[5] Some anabolic steroids such as
methandrostenolone bind weakly to this receptor in vitro,
but still exhibit androgenic eects in vivo. The reason for
this discrepancy is not known.[13]
3
creased libido, suppression of natural sex hormones, and
impaired production of sperm.[20] Eects on women include deepening of the voice, facial hair growth, and possibly a decrease in breast size. Men may develop an enlargement of breast tissue, known as gynecomastia, testicular atrophy, and a reduced sperm count.[21]
The androgenic:anabolic ratio of an AAS is an important factor when determining the clinical application of these compounds. Compounds with a high ratio of androgenic to an anabolic eects are the drug of
choice in androgen-replacement therapy (e.g., treating
hypogonadism in males), whereas compounds with a reduced androgenic:anabolic ratio are preferred for anemia and osteoporosis, and to reverse protein loss following trauma, surgery, or prolonged immobilization. Determination of androgenic:anabolic ratio is typically performed in animal studies, which has led to the marketing of some compounds claimed to have anabolic activity
The eect of anabolic steroids on muscle mass is caused with weak androgenic eects. This disassociation is less
in at least two ways:[14] rst, they increase the production marked in humans, where all anabolic steroids have sigof proteins; second, they reduce recovery time by block- nicant androgenic eects.[7]
ing the eects of stress hormone cortisol on muscle tissue, A commonly used protocol for determining the
so that catabolism of muscle is greatly reduced. It has androgenic:anabolic ratio, dating back to the 1950s, uses
been hypothesized that this reduction in muscle break- the relative weights of ventral prostate (VP) and levator
down may occur through anabolic steroids inhibiting the ani muscle (LA) of male rats. The VP weight is an indiaction of other steroid hormones called glucocorticoids cator of the androgenic eect, while the LA weight is an
that promote the breakdown of muscles.[15] Anabolic indicator of the anabolic eect. Two or more batches of
steroids also aect the number of cells that develop into rats are castrated and given no treatment and respectively
fat-storage cells, by favouring cellular dierentiation into some AAS of interest. The LA/VP ratio for an AAS is
muscle cells instead.[16] Anabolic steroids can also decalculated as the ratio of LA/VP weight gains produced
crease fat by increasing basal metabolic rate (BMR), since by the treatment with that compound using castrated
an increase in muscle mass increases BMR.
but untreated rats as baseline: (LA , LA )/(VP , VP ).
The LA/VP weight gain ratio from rat experiments
is not unitary for testosterone (typically 0.30.4), but
2.3 Anabolic and androgenic eects
it is normalized for presentation purposes, and used
as basis of comparison for other AAS, which have
As the name suggests, anabolic-androgenic steroids have their androgenic:anabolic ratios scaled accordingly (as
two dierent, but overlapping, types of eects: anabolic, shown in the table above).[13][22] In the early 2000s, this
meaning that they promote anabolism (cell growth), and procedure was standardized and generalized throughout
androgenic (or virilising), meaning that they aect the de- OECD in what is now known as the Hershberger assay.
velopment and maintenance of masculine characteristics.
Some examples of the anabolic eects 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. Through a number of
mechanisms anabolic steroids stimulate the formation of
muscle cells and hence cause an increase in the size of
skeletal muscles, leading to increased strength.[17][18][19]
The androgenic eects of AAS are numerous. Depending on the length of use, the side eects of the steroid
can be irreversible. Processes aected include pubertal growth, sebaceous gland oil production, and sexuality (especially in fetal development). Some examples of
virilizing eects are growth of the clitoris in females and
the penis in male children (the adult penis size does not The upper region of the body (thorax, neck, shoulders,
change due to steroids ), increased vocal cord size, in- and upper arm) seems to be more susceptible for AAS
than other body regions because of predominance of androgen receptors in the upper body. The largest dierence in muscle ber size between AAS users and nonusers was observed in type I muscle bers of the vastus
lateralis and the trapezius muscle as a result of long-term
AAS self-administration. After drug withdrawal, the effects fade away slowly, but may persist for more than 612
weeks after cessation of AAS use.[5]
Strength improvements in the range of 520% of baseline strength, depending largely on the drugs and dose
used as well as the administration period. Overall, the
exercise where the most signicant improvements were
observed is the bench press.[5] For almost two decades, it
was assumed that AAS exerted signicant eects only in
experienced strength athletes.[23][24] A randomized controlled trial demonstrated, however, that even in novice
athletes a 10-week strength training program accompanied by testosterone enanthate at 600 mg/week may improve strength more than training alone does.[5][25] This
dose is sucient to signicantly improve lean muscle
mass relative to placebo even in subjects that did not exercise at all.[25] The anabolic eects of testosterone enanthate were highly dose dependent.[5][26]
3.1
Medical uses
growth failure.[28] However, the availability of synthetic growth hormone, which has fewer side eects,
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.[29][30]
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.[31]
Male contraception, in the form of testosterone
enanthate; potential for use in the nearfuture as a safe, reliable, and reversible male
contraceptive.[32][33]
Stimulation of lean body mass and prevention
of bone loss in elderly men, as some studies indicate.[34][35][36] However, a 2006 placebocontrolled trial of low-dose testosterone supplementation in elderly men with low levels of testosterone
found no benet on body composition, physical performance, insulin sensitivity, or quality of life.[37]
Hormone replacement for men with low levels of
testosterone; also eective in improving libido for
elderly males.[38][39][40][41]
Gender dysphoria, 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 trans
man patients,[42] among other people designated female at birth or who develop female secondary sexual characteristics but desire to rather be read as
male or look more ambiguous, such as a number of
non-binary transgender people,[43][44][45][46][47] both
intersex and dyadic, and dysphoric non-transgender
intersex men.[48][49]
Increased Maximum Inspiratory Pressure: A study
in Research in Sports Medicine has found that
the combination of resistance training and anabolic
steroid administration produce a signicant increase
in MIP in a cohort of long-term AAS users.[50]
5
that long term AAS users were more likely to have symptoms of muscle dysmorphia and also showed stronger
endorsement of more conventional male roles.[59] A recent study in the Journal of Health Psychology showed
that many users believed that steroids used in moderation
were safe.[60]
men with a median age of about 25 who are noncompetitive bodybuilders and non-athletes and use the drugs for
cosmetic purposes.[53] Among 12- to 17-year-old boys,
use of steroids and similar drugs jumped 25 percent from
1999 to 2000, with 20 percent saying they use them for
looks rather than sports, a study by insurer Blue Cross
Blue Shield found."(Eisenhauer) Another study found
that non-medical use of AAS among college students
was at or less than 1%.[54] 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,[55] though a 2007
study found that sharing of needles was extremely uncommon among individuals using anabolic steroids for nonmedical purposes, less than 1%.[8] Another 2007 study
found that 74% of non-medical anabolic steroid users had
secondary college degrees and more had completed college and fewer had failed to complete high school than is
expected from the general populace.[8] The same study
found that individuals using anabolic steroids for nonmedical purposes had a higher employment rate and a
higher household income than the general population.[8]
Anabolic steroid users tend to research the drugs they are
taking more than other controlled-substance users; however, the major sources consulted by steroid users include
friends, non-medical handbooks, internet-based forums,
blogs, and tness magazines, which can provide questionable or inaccurate information.[56]
4 Adverse eects
Anabolic steroid use can cause many adverse eects.
4.1 Neuropsychiatric
A 2005 review in CNS Drugs determined that signicant
psychiatric symptoms including aggression and violence,
mania, and less frequently psychosis and suicide have
been associated with steroid abuse. Long-term steroid
abusers may develop symptoms of dependence and
withdrawal on discontinuation of AAS.[62] High concentrations of AAS, comparable to those likely sustained by
many recreational AAS users, produce apoptotic eects
on neurons, raising the specter of possibly irreversible
neuropsychiatric toxicity. Recreational AAS use appears
to be associated with a range of potentially prolonged psychiatric eects, including dependence syndromes, mood
disorders, and progression to other forms of substance
abuse, but the prevalence and severity of these various
eects remains poorly understood.[63] There is no evidence that steroid dependence develops from therapeutic use of anabolic steroids to treat medical disorders, but
instances of AAS dependence have been reported among
weightlifters and bodybuilders who chronically administered supraphysiologic doses.[64] Mood disturbances (e.g.
depression, [hypo-]mania, psychotic features) are likely
to be dose- and drug-dependent, but AAS dependence or
withdrawal eects seem to occur only in a small number
of AAS users.[5]
Anabolic steroid users tend to be disillusioned by the portrayal of anabolic steroids as deadly in the media and
in politics.[57] According to one study, AAS users also
distrust their physicians and in the sample 56% had not
disclosed their AAS use to their physicians.[58] Another
2007 study had similar ndings, 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 communitys knowledge of nonmedical anabolic steroid use was lacking, and 99% felt Large-scale long-term studies of psychiatric eects on
that the public has an exaggerated view of the side-eects AAS users are not currently available.[63] In 2003, the rst
of anabolic steroid use.[8] A recent study has also shown naturalistic long-term study on ten users, seven of which
DSM assertion
ADVERSE EFFECTS
4.2
Physiological
4.2
7
AAS use can cause harmful changes in cholesterol levels:
Some steroids cause an increase in LDL bad cholesterol
and a decrease in HDL good cholesterol.[97] In addition,
steroids provoke a rapid increase in body weight and an
accompanying rise in blood pressure, both of which leave
users more vulnerable to a cardiovascular event.[98]
Physiological
AAS ABUSE
tures in the female fetus and female features in the male 5.1.1 DSM
fetus.[103]
For DSM-IV, anabolic-androgenic steroid dependency is
found in the other substance-related disorder (include
4.2.6 Kidney problems
inhalants, anabolic steroids, medications) section and can
be coded, depending on which diagnostic criteria are
Kidney tests revealed that nine of the ten steroid users de- met.[110]
veloped a condition called focal segmental glomerulosclerosis, a type of scarring within the kidneys. The kidney
damage in the bodybuilders has similarities to that seen 5.1.2 ICD
in morbidly obese patients, but appears to be even more
ICD10 criteria for dependence include experience of at
severe.[104]
least three of the following during the past year:[67]
4.2.7
Liver problems
AAS abuse
Anabolic steroids are not psychoactive and cannot be detected by stimuli devices like a pupilometer which makes
them hard to spot as a source of neuropsychological imbalaces in some AAS users.
Research data indicates that steroids aect the serotonin and dopamine neurotransmitter systems of the
brain.[105] In an animal study, male rats developed
a conditioned place preference to testosterone injections into the nucleus accumbens, an eect blocked by
dopamine antagonists, which suggests that androgen reinforcement is mediated by the brain. Moreover, testosterone appears to act through the mesolimbic dopamine
system, a common substrate for drugs of abuse. Nonetheless, androgen reinforcement is not comparable to that of
cocaine, nicotine, or heroin. Instead, testosterone resembles other mild reinforcers, such as caeine, or benzodiazepines. The potential for androgen addiction remains
to be determined.[106] However, abuse of steroids is rivalling heroin use in Britain.[107]
5.1
Abuse potential
5.4
they do with other addictive drugs. People may persist in abusing steroids despite physical problems and
negative eects on social relationships, reecting these
drugs addictive potential. Also, steroid abusers typically spend large amounts of time and money obtaining
the drug; another indication of addiction. Individuals
who abuse steroids can experience withdrawal symptoms
when they stop taking them, including mood swings, fatigue, restlessness, loss of appetite, insomnia, reduced sex
drive, and steroid cravings, all of which may contribute
to continued abuse. One of the most dangerous withdrawal symptoms is depression. When depression is persistent, it can sometimes lead to suicidal thoughts. Research has found that some steroid abusers turn to other
drugs such as opioid to counteract the negative eects of
steroids.[112]
9
stated that Anabolic steroid abuse by police ocers is a
serious problem that merits greater awareness by departments across the country.[118] It is also believed that police ocers across the United Kingdom are using criminals to buy steroids and abuse their power for sexual gratication which he claims to be a top risk factor for police
corruption.[119]
5.3.3 Sports
Professional wrestling Main article: WWE Wellness Program
5.3
5.3.1
Anabolic steroid use has been associated with an antisocial lifestyle involving various types of criminality.[116]
5.3.2
Governments
Law enforcement Steroid abuse among law enforcement is considered a problem by some. Its a big problem, and from the number of cases, its something we
shouldn't ignore. Its not that we set out to target cops,
but when we're in the middle of an active investigation into steroids, there have been quite a few cases that
have led back to police ocers, says Lawrence Payne,
a spokesman for the United States Drug Enforcement
Administration.[117] The FBI Law Enforcement Bulletin
10
6.1
Legal status
Steroid pills intercepted by the US Drug Enforcement Administration during the Operation raw deal bust in September 2007.
Various compounds with anabolic and androgenic eects, their
relation with anabolic steroids
Substances Act following the controversy over Ben Johnsons victory at the 1988 Summer Olympics in Seoul.
During deliberations, the American Medical Association
(AMA), Drug Enforcement Administration (DEA), Food
and Drug Administration (FDA) as well as the National
Institute on Drug Abuse (NIDA) all opposed listing anabolic steroids as controlled substances, citing the fact
that use of these hormones does not 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 Steroids Control
Act of 1990.[132]
The same act also introduced more stringent controls with
higher criminal penalties for oenses involving the illegal distribution of anabolic steroids and human growth
hormone. By the early 1990s, after anabolic steroids
were scheduled in the U.S., several pharmaceutical companies stopped manufacturing or marketing the products
in the U.S., including Ciba, Searle, Syntex, and others.
In the Controlled Substances Act, anabolic steroids are
dened to be any drug or hormonal substance chemically
and pharmacologically related to testosterone (other than
estrogens, progestins, and corticosteroids) that promote
muscle growth. The act was amended by the Anabolic
Steroid Control Act of 2004, which added prohormones
to the list of controlled substances, with eect from January 20, 2005.[133]
United States
11
Part 1 drugs are subject to full import and export controls with possession being an oence without an appropriate prescription. There is no restriction on the possession when it is part of a medicinal product. Part 2 drugs
require a Home Oce licence for importation and export
unless the substance is in the form of a medicinal product
and is for self-administration by a person.[134]
this purpose. The anabolic steroids, whether of endogenous or exogenous origin, are subject to extensive hepatic biotransformation by a variety of enzymatic pathways. The primary urinary metabolites may be detectable for up to 30 days after the last use, depending
on the specic agent, dose and route of administration.
A number of the drugs have common metabolic pathways, and their excretion proles may overlap those of
the endogenous steroids, making interpretation of test6.2 Status in sports
ing results a very signicant challenge to the analytical chemist. Methods for detection of the substances or
See also: Use of performance-enhancing drugs in sport
their excretion products in urine specimens usually inAnabolic steroids are banned by all major sports bod- volve gas chromatographymass spectrometry or liquid
chromatography-mass spectrometry.[148][149][150][151]
7 Illegal trade
Main article: Illegal trade in anabolic steroids
Anabolic steroids are frequently produced in pharmaceu-
Legal status of anabolic steroids and other compounds with anabolic eects in Western countries
6.3
Detection of use
12
9 SEE ALSO
veterinarians, and physicians.[157] In addition, a signicant number of counterfeit products are sold as anabolic
steroids, in particular via mail order from websites posing as overseas pharmacies. In the U.S., black-market
importation continues from Mexico, Thailand, and other
countries where steroids are more easily available, as they
are legal.[158]
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 other amateur weight lifters.
In response to the success of Russian weightlifters, the
U.S. Olympic Team physician John Ziegler worked with
synthetic chemists to develop an anabolic steroid with reduced androgenic eects.[167] Zieglers work resulted in
the production of methandrostenolone, which Ciba Pharmaceuticals marketed as Dianabol. The new steroid was
approved for use in the U.S. by the Food and Drug Administration (FDA) in 1958. It was most commonly administered to burn victims and the elderly. The drugs olabel users were mostly bodybuilders and weight lifters.
Although Ziegler prescribed only small doses to athletes,
he soon discovered that those having abused Dianabol
suered from enlarged prostates and atrophied testes.[168]
AAS were placed on the list of banned substances of
the IOC in 1976, and a decade later the committee introduced 'out-of-competition' doping tests because many
athletes used AAS in their training period rather than during competition.[5]
8.1
History
Isolation of gonadal AAS
9 See also
Antiandrogen
Androgen insensitivity syndrome
Steroid rosacea
Steroid use in Bollywood
Bigger, Stronger, Faster*
Juiced: Wild Times, Rampant 'Roids, Smash Hits
& How Baseball Got Big
13
Selective androgen receptor modulator
10
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19
11
Further reading
12 External links
Dmoz Directory of websites on anabolic steroids
National Institute on Drug Abuse: "NIDA for Teens:
Anabolic Steroids".
20
13
13
13.1
13.2
Images
21
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13.2
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13.3
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