Oxymetholone is an anabolic steroid used for the treatment of types of anemia, such as acquired aplastic anemia, congenital aplastic anemia, myelofibrosis, and the hypoplastic anemias.
Oxymetholone is a synthetic anabolic steroid marketed under the brand name Anapolon by Hoffmann La Roche Limitedand used in the treatment of osteoporosis, anaemia, and as an agent to stimulate muscle growth in malnourished or underdeveloped patients. Anabolic-androgenic steroids (AAS), such as oxymetholone, have been abused by bodybuilders and athletes.
The uncontrolled misuse of oxymetholone can lead to a large variety of detrimental effects, the most often reported of which are cardiovascular events. In 2009, no producers of oxymetholone were identified worldwide (SRI 2009), but it was available from 14 suppliers, including 8 U.S. suppliers (ChemSources 2009).
Indicated in the treatment of anemias caused by deficient red cell production. Acquired aplastic anemia, congenital aplastic anemia, myelofibrosis and the hypoplastic anemias due to the administration of myelotoxic drugs often respond. Oxymetholone should not replace other supportive measures such as transfusion, correction of iron, folic acid, vitamin B12 or pyridoxine deficiency, antibacterial therapy and the appropriate use of corticosteroids.
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.
Oxymetholone is used for physique- and performance-enhancing purposes by competitive athletes, bodybuilders, and powerlifters.
Metabolism: 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. 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.
Absorption: Well absorbed following parenteral administration.
Route of elimination: Oxymetholone and its metabolites are eliminated in the urine.
Half life: The elimination half-life of oxymetholone is unknown.
Oxymethalone is a 17 alpha-alkylated anabolic-androgenic steroid and a synthetic derivative of testosterone, whose anabolic effects are used to treat muscle wasting in HIV patients. The effects of testosterone in humans and other vertebrates occur by way of two main mechanisms: by activation of the androgen receptor (directly or as DHT), and by conversion to estradiol and activation of certain estrogen receptors.
Free testosterone (T) is transported into the cytoplasm of target tissue cells, where it can bind to the androgen receptor, or can be reduced to 5α-dihydrotestosterone (DHT) by the cytoplasmic enzyme 5α-reductase. DHT binds to the same androgen receptor even more strongly than T, so that its androgenic potency is about 2.5 times that of T.
The T-receptor or DHT-receptor complex undergoes a structural change that allows it to move into the cell nucleus and bind directly to specific nucleotide sequences of the chromosomal DNA. The areas of binding are called hormone response elements (HREs), and influence transcriptional activity of certain genes, producing the androgen effects.
All medicines may cause side effects, but many people have no, or minor, side effects. Some medical conditions may interact with Oxymetholone.
Tell your doctor or pharmacist if you have any medical conditions.
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. 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. Because of its 17α-alkylated structure, oxymetholone is hepatotoxic. 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.
This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider.
