A Comparison of the Relative Efficacy of Methyltestosterone by the Gastric and Oral Transmucosal Routes

Abstract

An attempt has been made to compare the relative efficacy of two methods of medication with methyltestosterone, namely by absorption through the oral mucosa from slowly soluble tablets and by ingestion.The method of comparison adopted was to estimate the extent to which menstruation was postponed after giving 25 mg methyltestosterone twice daily for 30 days from the onset of bleeding. The effectiveness of the two routes of administration was compared in the same individual.The results indicate that buccal absorption is slightly more effective than ingestion.Biskind & Mark [1939] found that, when pellets of testosterone propionate and oestrone were implanted respectively into the spleens of castrate male and female rats, the hormones did not exert their characteristic effect. They did so, however, when the spleens containing the pellets were transplanted subcutaneously and the splenic artery and vein ligated. These findings were taken to mean that the two hormones were inactivated during transport through the liver via the portal circula¬ tion, but the experiment did not exclude the possibility that the spleen

The Influence of Androgen Treatment on Ultimate Height in Males

“…), and mean ultimate height after fusion of the epiphyses was nearly 2 inches below that predicted (Table 2). Even with continuous large doses of androgens two of these cases of hypogonadism have become fertile (Foss, 1962).…”

“…Theoretically absorption through the mucosa of the mouth should increase its efficacy, as some of it by-passes the portal circulation and is not detoxicated by the liver. It was shown that the ratio of effectiveness of transmucosal to orally ingested methyl testosterone in women was 1-38: 1 (Foss, 1956). The doses of methyl testosterone that they used for these young children were much too high, and produced virilization, and in some, given 40 mg./day, treatment was withdrawn after two and a half to three months.…”

Benefits of Testosterone Replacement and Methods of Substitution

“…17α-methyl-testosterone was introduced in 1939 by Foss and became extensively used for its androgenic and protein anabolic effects. It can be ingested orally or administered via trans buccal route [20]. After several decades of use however, it was found to cause cholestatic jaundice, reversible hepatotoxicity, and some cases of death, ending its use in the 1980s [21].…”