Methyltestosterone is a synthetic analog of testosterone that possesses all of the properties of
testosterone, exhibiting stimulatory action on the development of male sex organs and secondary sex characteristics, although it is not degraded by enzymes in the gastrointestinal
tract, and therefore it can only be taken orally
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white to slightly yellowish-white crystalline
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Androgen. It has been used as an androgenic agent.
Controlled substance (anabolic steroid).
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ChEBI: A 17beta-hydroxy steroid that is testosterone bearing a methyl group at the 17alpha position.
Pharmacokinetics
The synthesis of 17α-methyltestosterone made available a compound that was orally active in
daily doses between 10 and 50 mg, which is equivalent to a 400 mg oral dose of testosterone. The
presence of a 17α alkyl group reduces susceptibility to hepatic oxidative metabolism, thereby
increasing oral bioavailability by slowing metabolism. Following oral administration,
methyltestosterone is well absorbed from the gastrointestinal tract, with a half-life of approximately 3
hours. This drug has the androgenic and anabolic activities of testosterone. Although orally active, it
is more effective when administered sublingually. The alkylated oral androgens should be viewed as
potentially hepatotoxic and should not be used.
Safety Profile
Poison by
intraperitoneal route. Moderately toxic by
ingestion. Human teratogenic effects by
ingestion: developmental abnormalities of
the urogenital system. Experimental
teratogenic and reproductive effects. Human
systemic effects: cholestatic jaundce, weight
loss or decreased weight gain. Questionable human carcinogen producing liver tumors.
A synthetic androgenic steroid. When
heated to decomposition it emits acrid
smoke and irritating fumes.
Purification Methods
This anabolic steroid is crystallised from hexane or hexane/*benzene. It has E1cm 1% 495-530 at 241nm (EtOH). The colour reaction with 2,4-dinitrophenyl hydrazine is used for assaying it. [Gornall & Macdonald J Biol Chem 201 279 1953.] In another colour reaction the sterone (1mg) in acetic acid (0.2ml) + 88% H3PO4 (2mL) is allowed to stand for 1hour when it becames fluorescent. After 1hour it is diluted with acetic acid (~3mL) and provides a strong yellow fluorescence with the intensity of 50-100 times that of estrone. [Stuart & Stuckey J Pharm Pharmacol 1 130 1949, Openauer Rec Trav Chim Pays-Bas 56 137 137, Beilstein 8 IV 1010.]
