Mesterolone

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Template:Short description Script error: No such module "Distinguish". Template:Drugbox Mesterolone, sold under the brand name Proviron among others, is an androgen and anabolic steroid (AAS) medication which is used mainly in the treatment of low testosterone levels.[1][2] It has also been used to treat male infertility, although this use is controversial.[1][3][4] It is taken by mouth.[1]

Side effects of mesterolone include symptoms of masculinization like acne, scalp hair loss, increased body hair growth, voice changes, and increased sexual desire.[1] It has no risk of liver damage.[1][2] 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).[1][5] It has strong androgenic effects and weak anabolic effects, which make it useful for producing masculinization.[1] The drug has no estrogenic effects.[1][2]

Mesterolone was first described by 1966[6] and introduced for medical use by 1967.[7][8] In addition to its medical use, mesterolone has been used to improve physique and performance, although it is not commonly used for such purposes due to its weak anabolic effects.[1] The drug is a controlled substance in many countries and so non-medical use is generally illicit.[1][9]

Medical uses

Mesterolone is used in the treatment of androgen deficiency in male hypogonadism, anemia, and to support male fertility among other indications.[1][10][11] It has also been used to treat delayed puberty in boys.[12] Because it lacks estrogenic effects, mesterolone may be indicated for treating cases of androgen deficiency in which breast tenderness or gynecomastia is also present.[13] The drug is described as a relatively weak androgen with partial activity and is rarely used for the purpose of androgen replacement therapy, but is still widely used in medicine.[1][11][14][2]

Mesterolone is used in androgen replacement therapy at a dosage of 50 to 100 mg 2 to 3 times per day.[15]

Template:Androgen replacement therapy formulations and dosages used in men

Non-medical uses

Mesterolone has been used for physique- and performance-enhancing purposes by competitive athletes, bodybuilders, and powerlifters.[1]

Side effects

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Side effects of mesterolone include virilization among others.[1]

Pharmacology

Pharmacodynamics

Like other AAS, mesterolone is an agonist of the androgen receptor (AR).[1] Mesterolone is described as a very poor anabolic agent due to inactivation by 3α-hydroxysteroid dehydrogenase (3α-HSD) in skeletal muscle tissue, similarly to DHT and mestanolone (17α-methyl-DHT).[1] In contrast, testosterone is a very poor substrate for 3α-HSD, and so is not similarly inactivated in skeletal muscle.[1] Because of its lack of potentiation by 5α-reductase in "androgenic" tissues and its inactivation by 3α-HSD in skeletal muscle, mesterolone is relatively low in both its androgenic potency and its anabolic potency.[1] However, it does still show a greater ratio of anabolic activity to androgenic activity relative to testosterone.[1]

Mesterolone is not a substrate for 5α-reductase, as it is already 5α-reduced, and hence is not potentiated in so-called "androgenic" tissues such as the skin, hair follicles, and prostate gland.[1]

Mesterolone is not a substrate for aromatase, and so cannot be converted into an estrogen.[1] As such, it has no propensity for producing estrogenic side effects such as gynecomastia and fluid retention.[1] It also has no progestogenic activity.[1]

Because mesterolone is not 17α-alkylated, it has little or no potential for hepatotoxicity.[1] However, its risk of deleterious effects on the cardiovascular system is comparable to that of several other oral AAS.[1]

Pharmacokinetics

The C1α methyl group of mesterolone inhibits its hepatic metabolism and thereby confers significant oral activity, although its oral bioavailability is still much lower than that of 17α-alkylated AAS.[1] In any case, mesterolone is one of the few non-17α-alkylated AAS that is active with oral ingestion.[1] Uniquely among AAS, mesterolone has very high affinity for human serum sex hormone-binding globulin (SHBG), about 440% that of DHT in one study and 82% of that of DHT in another study.[16][1][17] As a result, it may displace endogenous testosterone from SHBG and thereby increase free testosterone concentrations, which may in part be involved in its effects.[1]

Chemistry

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Mesterolone, also known as 1α-methyl-4,5α-dihydrotestosterone (1α-methyl-DHT) or as 1α-methyl-5α-androstan-17β-ol-3-one, is a synthetic androstane steroid and derivative of DHT.[18][19][1] It is specifically DHT with a methyl group at the C1α position.[18][19][1] Closely related AAS include metenolone and its esters metenolone acetate and metenolone enanthate.[18][19][1] The antiandrogen rosterolone (17α-propylmesterolone) is also closely related to mesterolone.[20]

History

Mesterolone was developed in the 1960s[21] and was first described by 1966.[6][22][23][24] It was introduced for medical use by Schering under the brand name Proviron by 1967.[7][8] The well-established brand name Proviron had previously been used by Schering for testosterone propionate starting in 1936.[25] Following the introduction of mesterolone as Proviron, Schering continued to market testosterone propionate under the brand name Testoviron.[25] A number of sources incorrectly state that mesterolone was synthesized or introduced for medical use in 1934.[21][1][26][27]

Society and culture

Generic names

Mesterolone is the generic name of the drug and its Template:Abbrlink, Template:Abbrlink, Template:Abbrlink, and Template:Abbrlink, while mestérolone is its Template:Abbrlink.[18][19][28][29]

Brand names

Mesterolone is marketed mainly under the brand name Proviron.[18][19][29][1]

Availability

Mesterolone is available widely throughout the world, including in the United Kingdom, Australia, and South Africa, as well as many non-English-speaking countries.[19][29] It is not available in the United States, Canada, or New Zealand.[19][29] The drug has never been marketed in the United States.[26]

Legal status

Mesterolone, along with other AAS, is a schedule III controlled substance in the United States under the Controlled Substances Act and a schedule IV controlled substance in Canada under the Controlled Drugs and Substances Act.[9][30]

Research

In one small scale clinical trial of depressed patients, an improvement of symptoms which included anxiety, lack of drive and desire was observed.[31] In patients with dysthymia, unipolar, and bipolar depression significant improvement was observed.[31] In this series of studies, mesterolone lead to a significant decrease in luteinizing hormone and testosterone levels.[31] In another study, 100 mg mesterolone cipionate was administered twice monthly.[32] With regards to plasma testosterone levels, there was no difference between the treated versus untreated group, and baseline luteinizing hormone levels were minimally affected.[32]

References

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Further reading

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External links


Template:Androgens and antiandrogens Template:Androgen receptor modulators

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