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.[4][8][9][10] It is used mostly in the United States.[4][11] In addition to its medical use, oxymetholone is used to improve physique and performance.[4] The drug is a controlled substance in many countries and so non-medical use is generally illicit.[4]
Medical uses
The primary clinical applications of oxymetholone include treatment of anemia and osteoporosis, as well as stimulating muscle growth in malnourished or underdeveloped patients.[4] However, in the United States, the only remaining FDATooltip Food and Drug Administration-approved indication is the treatment of anemia.[4][12]
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.[4][13] Similarly, there is a risk of side effects.[14][15] Oxymetholone is highly effective in promoting extensive gains in body mass, mostly by greatly improving protein synthesis.[4] For this reason, it is often used by bodybuilders and athletes.[4]
As a DHT derivative, oxymetholone is not a substrate for aromatase and hence cannot be aromatized into estrogenicmetabolites.[4] 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.[4][16][17][18] It has been suggested that this may be due to direct binding to and activation of the estrogen receptor by oxymetholone.[4] Oxymetholone does not possess any significant progestogenic activity.[4]
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 syntheticandrostanesteroid and a 17α-alkylatedderivative of DHT.[19][20][4]
Oxymetholone is the generic name of the drug and its INNTooltip International Nonproprietary Name, USANTooltip United States Adopted Name, USPTooltip United States Pharmacopeia, BANTooltip British Approved Name, and JANTooltip Japanese Accepted Name, while oxymétholone is its DCFTooltip Dénomination Commune Française.[19][20][24][11]
Brand names
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.[19][20][11][4][25]
^ abcdeSaartok T, Dahlberg E, Gustafsson JA (June 1984). "Relative binding affinity of anabolic-androgenic steroids: comparison of the binding to the androgen receptors in skeletal muscle and in prostate, as well as to sex hormone-binding globulin". Endocrinology. 114 (6): 2100–6. doi:10.1210/endo-114-6-2100. PMID6539197.
^Cortesgallegos V, Castaneda G, Alonso R, Perezpasten E, Reyeslugo V, Barron C, Mondragon L, Villalpando S (January 1982). "Spontaneous and Oxymetholone-Induced Gynecomastia". Journal of Andrology. C/O Allen Press, Inc Po Box 368, Lawrence, Ks 66044: Amer Soc Andrology, Inc. 3 (1): 33.
^Villalpando S, Mondragon L, Barron C, Reyeslugo U, Perezpasten E, Alonso R, Castaneda G, Gallegos V (January 1982). "5-Alpha Reductase Blockade May Be Responsible for Spontaneous and Oxymetholone-Induced Gynecomastia". Archivos de Investigacion Medica. Social Apdo Postal 73-032, Mexico Df 03020, Mexico: Inst Mexicano Seguro. 13 (2): s13.
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