Oxymetholone

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. It is also used to treat osteoporosis, HIV/AIDS wasting syndrome, and to promote weight gain and muscle growth in certain situations. It is taken by mouth.

Oxymetholone, also known by its brand name Anadrol, is an anabolic steroid that is derived from dihydrotestosterone (DHT). It is primarily used in the medical field to treat conditions such as anemia and muscle wasting diseases. However, it has also gained popularity among bodybuilders and athletes for its potential to enhance muscle mass and strength.

Side effects of oxymetholone include increased sexual desire as well as symptoms of masculinization like acne, increased hair growth, and voice changes. It can also cause liver damage. 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). It has strong anabolic effects and weak androgenic effects.

Oxymetholone was first prescribed in 1959 and was introduced for medical use but shortly after was discontinued due its high lipid toxicity in the year 1961. It is used mostly in the United States. [3][10] In addition to its medical use, oxymetholone is used to improve physique and performance.

 

 

 

The primary clinical applications of oxymetholone include treatment of anemia and osteoporosis, as well as stimulating muscle growth in malnourished or underdeveloped patients. However, in the United States, the only remaining FDA-approved indication is the treatment of anemia.

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. The drug remained available despite this and eventually found a new use in treating HIV/AIDS wasting syndrome.

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. Similarly, there is a risk of side effects. Oxymetholone is highly effective in promoting extensive gains in body mass, mostly by greatly improving protein synthesis. For this reason, it is often used by bodybuilders and athletes.

Oxymetholone is used for physique- and performance-enhancing purposes by competitive athletes, bodybuilders, and powerlifters.

Muscle Mass and Strength: Oxymetholone is highly anabolic, meaning it promotes muscle growth and increases protein synthesis. It is known for its ability to rapidly increase muscle mass and strength, making it popular in the bodybuilding community.

Red Blood Cell Production: Oxymetholone stimulates red blood cell production, which can improve oxygen transportation in the body. This can enhance endurance and performance during intense physical activities.

 

 

Like other AAS, oxymetholone is an agonist of the androgen receptor (AR). 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.

As a DHT derivative, oxymetholone is not a substrate for aromatase and hence cannot be aromatized into estrogenic metabolites. 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. It has been suggested that this may be due to direct binding to and activation of the estrogen receptor by oxymetholone. Oxymetholone does not possess any significant progestogenic activity.

 

 

There is limited information available on the pharmacokinetics of oxymetholone. It appears to be well-absorbed with oral administration. 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. The C2 hydroxymethylene group of oxymetholone can be cleaved to form mestanolone (17α-methyl-DHT), which may contribute to the effects of oxymetholone. The elimination half-life of oxymetholone is unknown. Oxymetholone and its metabolites are eliminated in the urine.

 

 

1) CAS: 434-07-1
2) Trade names: Anadrol, Anapolon
3) PubChem CID: 5281034
4) Molecular Formula: C₂₁H₃₂O₃
5) Molecular Weight: 332.484g/mol

 

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