Oxymetholone (aka Anadrol, Anadrol-50)
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Chemical Name |
17-β-hydroxy-2-hydroxymethylene-17-methyl-5α-androstan-3-one |
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Molecular Weight |
332.48 g/mol |
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Formula |
C21H32O3 |
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Original Manufacturer |
Syntex |
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Half Life |
8 - 9 hours |
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Detection Time |
2 months |
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Anabolic Rating |
320 |
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Androgenic Rating |
45 |
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History and Overview of Anadrol
Anadrol is known as one of the most powerful (and sometimes infamous) oral anabolic steroids on the market.
It competes closely with Dianabol (methandrostenolone), and there has always been a debate in steroid-using bodybuilding circles as to which of the two is more powerful.
Anadrol is the brand and trade name of an anabolic steroid more formally known as oxymetholone.
This is not to be confused with oxandrolone, which is known as Anavar.
Oxymetholone is anadrol.
Details of Anadrol were first published in 1959[1].
Almost immediately, the pharmaceutical company Syntex marketed oxymetholone under the name Anadrol-50, while Parke Davis & Co. also manufactured it under the trade name Androyd.
After first hitting the prescription market, Anadrol was quickly prescribed and used for a variety of medical conditions, from senile atrophy to fighting infections.
However, its most famous and popular use as a drug was to treat anemia.
Anadrol was prescribed to increase red blood cell counts and hemoglobin levels in anemic patients.
This was due to anadrol's ability to stimulate red blood cell production at a very rapid rate.
While all anabolic steroids have this ability, the ability of anadrol to stimulate red blood cell production is far greater than any other anabolic steroid.
In such cases, anadrol has been shown in studies to increase red blood cell production by 5 times[2].
As far as its general effectiveness as an anabolic steroid for muscle-building purposes is concerned, studies have shown that it exerted a notable anabolic effect on muscle-wasting AIDS patients, actually causing them to gain 8 kg of weight, while patients given a placebo not only lost weight but also experienced an increased mortality rate[3].
For this reason, anadrol tends to be prescribed almost exclusively to AIDS patients and muscle wasting conditions today.
Chemical Properties of Anadrol
Anadrol is derived from dihydrotestosterone (DHT) and belongs to the dihydrotestosterone (DHT)-derived anabolic steroid family.
This means that anadrol is basically dihydrotestosterone transformed into dihydrotestosterone.
Other compounds that belong to this 'DHT family' of anabolic steroids include Winstrol, Primobolan, Masteron, Anavar, and several other compounds that are derivatives of the parent anabolic steroid DHT.
What all of these DHT derivatives have in common is that they are all modified forms of DHT in some way, so DHT can be considered the "parent" hormone of these anabolic steroids.
Anadrol differs from its parent hormone, DHT, in that it has a methyl group attached as well as a 2-hydroxymethylene group attached to the carbon in the first cycloalkane ring of the steroid structure.
This modification allows anadrol to remain active in muscle tissue where dihydrotestosterone is reduced to other metabolites and rendered inactive once it enters muscle tissue.
The enzyme that does this to dihydrotestosterone, which is present in large amounts in muscle tissue, is 3-hydroxysteroid dehydrogenase.
Due to the chemical modification mentioned, this enzyme does not interact with Anadrol.
This allows Anadrol to be very active in muscle tissue and exert very potent effects.
Anadrol has an anabolic rating of 320 (a little over 3 times the strength of testosterone, which has an anabolic rating of 100).
Anadrol has also been found to have a lower androgenic strength compared to testosterone, with anadrol having an androgenic rating of 45 (compared to testosterone's androgenic rating of 100).
One of the unique and mysterious features of anadrol is that although it is a derivative of DHT, it has a very high level of estrogenic activity.
It is generally believed that DHT derivative anabolic steroids should not have estrogenic effects as they cannot be converted to estrogen via the aromatase enzyme, but Anadrol is very different.
Anadrol is well known to cause water retention, bloating, gynecomastia, and other estrogenic effects on the body even though it does not convert to estrogen.
It is believed that anadrol itself acts as an estrogen in certain tissues.
This will be expanded upon and discussed further later, but it is important for potential users to understand that, first and foremost, Anadrol is a DHT derivative, but they will not experience the lean hard gains commonly seen with DHT derivatives.
Anadrol is notorious for its estrogenic effects which cannot be fought with aromatase inhibitors as it cannot convert to estrogen.
Anadrol is an orally active anabolic steroid, which means that it has been C17 alpha alkylated to allow the anabolic steroid to first pass through the liver without being destroyed through liver metabolism.
However, anadrol is well known for its very harsh liver toxicity, which we will discuss in more detail shortly.
The chemical modifications and chemical structure of anadrol (including the C17 alpha alkylation) make it very resistant to hepatic breakdown (hepatic metabolism).
The more resistant a substance is to hepatic breakdown, the more toxic and taxing it can be on the liver, and anadrol is notorious for its liver toxicity and is considered perhaps the most hepatotoxic of the commonly available oral anabolic steroids.
Anadrol Side Effects
Anadrol is an orally active C-17 alpha alkylated anabolic steroid and therefore exhibits hepatotoxicity and negative effects related to the liver.
In fact, anadrol is the most hepatotoxic of all anabolic steroids on the market.
It is very likely that this is exaggerated in the bodybuilding community, but it should be taken very seriously nonetheless.
Interestingly, anadrol actually has a chemical modification that reduces its hepatotoxicity[4].
However, the reality is that Anadrol still increases liver enzyme markers during use[5] [6], as demonstrated in studies with HIV and AIDS patients.
Therefore, it is highly recommended to limit the cycle of Anadrol use to no more than 4-6 weeks and to supplement with proven liver support compounds.
When examining other side effects, things get weirder with the use of anadrol.
It is well known that anadrol is a DHT (dihydrotestosterone) derivative and therefore does not convert to estrogen.
However, estrogenic side effects are notoriously known to cause side effects such as bloating and water retention (often reported to be extreme) along with increased blood pressure, and the development of gynecomastia. While SERMs (such as Nolvadex) can alleviate gynecomastia, they do not address the issue of water retention (and resulting blood pressure).
Aromatase inhibitors cannot be used with anadrol because they have no interaction with the aromatase enzyme to begin with.
It has been speculated that anadrol may act as a progestin causing these side effects, but research has shown that anadrol does not have progestogenic properties [7].
The most likely (yet unconfirmed) explanation is that anadrol interacts directly with estrogen receptors, or that metabolites of anadrol may also have this action.
The evidence for strange metabolites of anadrol becomes even stronger when examining other anadrol side effects.
For example, androgenic side effects tend to be significantly reduced in comparison to testosterone.
However, anadrol does not convert to DHT, but is instead metabolized to 17-alpha-methyldihydrotestosterone (mestanolone)[8].
Mestanolone is a more potent androgen, so some degree of androgenic side effects (such as oily skin, acne, androgenic alopecia, benign prostatic hyperplasia, etc.
Finally, like all oral anabolic steroids, anadrol tends to have an extremely negative effect on the cardiovascular system, causing significant changes in blood cholesterol profile (both LDL and HDL)[9].
Anadrol Cycles and Uses
Cycles that include oxymetholone are generally of the type for bulking, strength gains, and general overall mass.
Anadrol cycles are not suitable for cutting, fat loss, pre-contest, or similar purposes.
Anadrol can indeed be used to aid and accelerate fat loss, but its estrogenic effects, specifically water retention and bloating, make it a poor choice.
This side effect makes the physique appear overall soft and smooth, blurring and obscuring definition, making fat loss difficult to measure visually.
This is exacerbated by the fact that anadrol does not convert to estrogen, so it imposes this effect on the user through other, as yet unidentified means.
Therefore, in this case, aromatase inhibitors are not effective in reducing the bloating effect.
An anadrol cycle usually consists of using anadrol as a starting compound for the first 4-6 weeks, supplementing it with other injectable base compounds used for similar purposes, such as testosterone enanthate, deca durabolin (nandrolone decanoate), trenbolone enanthate, etc.
It can also be used in the middle of a cycle to get over a hump or plateau in your training progress.
It is also used by some users at the end of a cycle to act as a 'finisher' compound to round out the cycle and achieve very impressive strength and size gains as they move into the post cycle therapy (PCT) phase.
Anadrol cycles should not be extended beyond 4-6 weeks due to hepatotoxicity concerns.
However, other compounds used in conjunction with it, such as injectables, can be used beyond the termination period of Anadrol.
Anadrol Dosage and Administration
Anadrol prescription guidelines varied widely from the 1950s to the 1980s and depended on the medical condition being treated and the constantly changing FDA guidelines. Medical anadrol dosages ranged from 2.5mg taken three times a day to as high as 30mg per day.
Eventually, in the 1970s, the FDA issued guidelines of 1 to 2 mg per kilogram of body weight per day.
Since anadrol is most commonly manufactured in 50 mg tablets, beginners for bodybuilding and athletic purposes should take 25 to 50 mg per day.
Intermediate users are known to use 50 - 100 mg per day, and advanced users use up to 150 mg per day, although this is approaching the dangerous limit.
In general, however, most users, whether beginners, intermediate or advanced, will rarely need more than 50mg per day due to the sheer potency and strength of anadrol as an anabolic steroid.
This is especially the case when research has proven that a 100mg anadrol dosage is actually more effective than a 50mg anadrol dosage, but beyond 100mg it becomes no more effective than 100mg itself and diminishing returns begin to show[10].
Another concern with Anadrol dosage is that many users report a decrease in appetite in direct proportion to the dosage used, and studies have shown that it increases glucose intolerance and insulin resistance[11], making the body's use of nutrients less efficient.
Anadrol doses can and ideally should be split throughout the day to ensure stable and steady plasma levels of the hormone.
Anadrol exhibits a half-life of approximately 8-9 hours in the body, so a schedule that includes a morning (AM) dose and an afternoon/evening (PM) dose is best.
Latest research
December 30, 2017: Sports scientists at the University of Southern California examined the results of daily doses of placebo, 50 mg, and 100 mg of oxymetholone in healthy elderly patients.
The team published their findings in 2003, showing the positive effects of oxymetholone on muscle growth and fat loss.
The study found that men who took the compound increased their lean body mass by about 3.3 kilograms, and those who took the larger dose of 100 mg actually gained more than 4.2 kilograms.
The amount of body fat in both groups actually decreased by 2.6 kilograms and 2.5 kilograms, showing that it was able to remove fat as well as lean mass.
In fact, body scans showed that men who took 50 mg lost almost 2 kilograms of body fat in their trunk, which is their torso area.
And those who doubled up to 100 mg lost about 2.2 kilograms.
Based on the results of the study, it appears that most of the fat was lost from the trunk and torso.
These are the areas where men tend to store body fat.
The study also showed a number of negative effects, such as hepatotoxicity (liver damage) and a decrease in HDL (good cholesterol).
This is why it is often recommended that anadrol not be used continuously for more than 4-6 weeks.
Source: https://www.ncbi.nlm.nih.gov/pubmed/12388137
Anadrol Reference
[1].2-Methyl and 2-hydroxymethylene-androstane derivatives. Ringold HJ et al. J am Chem Soc 1959;81:427-32.
[2].Oxymetholone treatment of anemia due to bone marrow failure. Alexanian R, Nadell J, et al. Blood. 1972;40:353-6.
[3].Schroeder et al. Am J Physiol Endocrinol Metab 284:E 120-28
[4].Effects of various 17 alpha alkyl substitutions and structural modifications of steroids on sulfobromophthalein (BSP) retention in rabbits. Lennon HD et al. Steroids 7 (1966): 157-70.
[5].Long-term oxymetholone use in HIV patients not associated with significant hepatotoxicity. Hengge UR et al. Poster presented at the 3rd International Conference on Nutrition and HIV Injection; April 22-25, 1999; Canex, France.
[6].Clin Nutr. June 1984;114(6):2100-6.
[7].Les Hormons anabolisantes du point de vue experiment. PA Desaulles. Helb. Med. Acta 1960;479-503.
[8].Studies on anabolic steroids-8. GC/MS characterization of an unusual seco-acidic metabolite of oxymetholone in human urine. J Steroid Biochem Mol Bio 42 (1992):229-42.
[9].Effects of oral androgens on muscle and metabolism in elderly, community-dwelling men. Schroder et al. Am J Physiol Endocrinol. Metab. 284:E 120-28.
[10].J Clin Endocrinol Metab. 1981 Nov 53(5):905-8. Epilepsy Behav. April 2004.
