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#Post#: 89--------------------------------------------------
Oxymetholone
By: Road2HardCoreIron Date: April 26, 2018, 9:33 pm
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Oxymetholone
Clinical data
Trade names
Anadrol, Anapolon, others
Synonyms
CI-406; NSC-26198;
2-Hydroxymethylene-17α-methyl-4,5α-dihydrotestosterone
;
2-Hydroxymethylene-17α-methyl-
Oxymetholone, sold under the brand names Anadrol and Anapolon
among others, is an androgen and anabolic steroid (AAS)
medication which is used primarily in the treatment of
anemia.[3][4] It is also used to treat osteoporosis, HIV/AIDS
wasting syndrome, and to promote weight gain and muscle growth
in certain situations.[3] It is taken by mouth.[3][4]
Side effects of oxymetholone include symptoms of masculinization
like acne, increased hair growth, voice changes, and increased
sexual desire.[3] It can also cause liver damage.[3][4] The drug
is a synthetic androgen and anabolic steroid and hence is an
agonist of the androgen receptor (AR), the biological target of
androgens like testosterone and dihydrotestosterone (DHT).[3][5]
It has strong anabolic effects and weak androgenic effects.[3]
Oxymetholone was first described in 1959 and was introduced for
medical use by 1961.[3][6][7][8] It is used mostly in the United
States.[3][9] In addition to its medical use, oxymetholone is
used to improve physique and performance.[3] The drug is a
controlled substance in many countries and so non-medical use is
generally illicit.[3]
.Medical uses[edit]
The primary clinical applications of oxymetholone include
treatment of anemia and osteoporosis, as well as stimulating
muscle growth in malnourished or underdeveloped patients.[3]
However, in the United States, the only remaining FDA-approved
indication is the treatment of anemia.[3][10]
Following the introduction of oxymetholone, nonsteroidal drugs
such as epoetin alfa were developed and shown to be more
effective as a treatment for anemia and osteoporosis without the
side effects of oxymetholone.[3] The drug remained available
despite this and eventually found a new use in treating HIV/AIDS
wasting syndrome.[3]
Presented most commonly as a 50 mg tablet, oxymetholone has been
said to be one of the "strongest" and "most powerful" AAS
available for medical use.[3][11] Similarly, there is a risk of
side effects.[12][13] Oxymetholone is highly effective in
promoting extensive gains in body mass, mostly by greatly
improving protein synthesis.[3] For this reason, it is often
used by bodybuilders and athletes.[3]
Non-medical uses[edit]
Oxymetholone is used for physique- and performance-enhancing
purposes by competitive athletes, bodybuilders, and
powerlifters.[3]
Side effects[edit]
See also: Anabolic steroid § Adverse effects
The common side effects of oxymetholone include depression,
lethargy, headache, swelling, rapid weight gain, priapism,
changes in skin color, urination problems, nausea, vomiting,
stomach pain (if taken on an empty stomach), loss of appetite,
jaundice, breast swelling in men, feeling restless or excited,
insomnia, and diarrhea.[12] In women, side effects also include
acne, changes in menstrual periods, voice deepening, hair growth
on the chin or chest, pattern hair loss, enlarged clitoris, and
changes in libido.[3][12] Because of its 17α-alkylated
structure, oxymetholone is hepatotoxic.[3] Long term use of the
drug can cause a variety of serious ailments, including
hepatitis, liver cancer, and cirrhosis; therefore periodic liver
function tests are recommended for those taking
oxymetholone.[13]
Pharmacology[edit]
Pharmacodynamics[edit]
Like other AAS, oxymetholone is an agonist of the androgen
receptor (AR).[3] It is not a substrate for 5α-reductase
(as it is already 5α-reduced) and is a poor substrate for
3α-hydroxysteroid dehydrogenase (3α-HSD), and
therefore shows a high ratio of anabolic to androgenic
activity.[3]
As a DHT derivative, oxymetholone is not a substrate for
aromatase and hence cannot be aromatized into estrogenic
metabolites.[3] However, uniquely among DHT derivatives,
oxymetholone is nonetheless associated with relatively high
estrogenicity, and is known to have the potential to produce
estrogenic side effects such as gynecomastia (rarely) and water
retention.[3][14][15][16] It has been suggested that this may be
due to direct binding to and activation of the estrogen receptor
by oxymetholone.[3] Oxymetholone does not possess any
significant progestogenic activity.[3]
Pharmacokinetics[edit]
There is limited information available on the pharmacokinetics
of oxymetholone.[4] It appears to be well-absorbed with oral
administration.[4] Oxymetholone has very low affinity for human
serum sex hormone-binding globulin (SHBG), less than 5% of that
of testosterone and less than 1% of that of DHT.[1] The drug is
metabolized in the liver by oxidation at the C2 position,
reduction at the C3 position, hydroxylation at the C17 position,
and conjugation.[4][2] The C2 hydroxymethylene group of
oxymetholone can be cleaved to form mestanolone
(17α-methyl-DHT), which may contribute to the effects of
oxymetholone.[3] The elimination half-life of oxymetholone is
unknown.[2] Oxymetholone and its metabolites are eliminated in
the urine.[1][2]
Chemistry[edit]
See also: List of androgens/anabolic steroids
Oxymetholone, also known as
2-hydroxymethylene-17α-methyl-4,5α-dihydrotestosterone
(2-hydroxymethylene-17α-methyl-DHT) or as
2-hydroxymethylene-17α-methyl-5α-androstan-17β-ol
-3-one,
is a synthetic androstane steroid and a 17α-alkylated
derivative of DHT.[17][18][3]
History[edit]
Oxymetholone was first described in a 1959 paper by scientists
from Syntex.[3][6] It was introduced for medical use by Syntex
and Imperial Chemical Industries in the United Kingdom under the
brand name Anapolon by 1961.[7][8] Oxymetholone was also
introduced under the brand names Adroyd (Parke-Davis) by 1961
and Anadrol (Syntex) by 1962.[19][20][21] The drug was marketed
in the United States in the early 1960s.[3]
Society and culture[edit]
Generic names[edit]
Oxymetholone is the generic name of the drug and its INN, USAN,
USP, BAN, and JAN, while oxymétholone is its DCF.[17][18][22][9]
Brand names[edit]
Oxymetholone has been marketed under a variety of brand names
including Anadrol, Anadroyd, Anapolon, Anasterona, Anasteronal,
Anasterone, Androlic, Androyd, Hemogenin, Nastenon, Oxitoland,
Oxitosona, Oxyanabolic, Oxybolone, Protanabol, Roboral,
Synasterobe, Synasteron, and Zenalosyn.[17][18][9][3][23]
Availability[edit]
United States[edit]
See also: List of androgens/anabolic steroids available in the
United States
Oxymetholone is one of the few AAS that remains available for
medical use in the United States.[24] The others (as of November
2017) are testosterone, testosterone cypionate, testosterone
enanthate, testosterone undecanoate, methyltestosterone,
fluoxymesterone, nandrolone decanoate, and oxandrolone.[24]
Other countries[edit]
The availability of oxymetholone is fairly limited and seems to
be scattered into isolated markets in Europe, Asia, and North
and South America.[3] It is known to be available in Turkey,
Greece, Moldova, Iran, Thailand, Brazil, and Paraguay.[3][9] At
least historically, it has also been available in Canada, the
United Kingdom, Belgium, the Netherlands, Spain, Poland, Israel,
Hong Kong, and India.[18]
Legal status[edit]
Oxymetholone, along with other
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