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Oral Agents Oral testosterone formulations are quickly absorbed by the liver and therefore require relatively large doses. Because of the risk of liver toxicity they are rarely prescribed. Do not waste your money or time using oral testosterone. Also, avoid over-the-counter supplements that claim to increase testosterone. Most do not increase testosterone for more than a few minutes and can also affect your liver and blood pressure. Oral testosterone also seems to cause larger decreases of the good cholesterol (HDL) than other forms of testosterone therapies. Chemically unbound testosterone, if taken orally, is immediately deactivated by the liver. Two chemically modified forms of testosterone are available that require several doses a day: methyl testosterone and testosterone undecanoate (not approved in the United States but popular in Canada). Methyl testosterone Methyl testosterone is one of the earliest available oral testosterones. Its chemical structure is the hormone testosterone with an added methyl group at the c-17 alpha position of the molecule to slow down its clearance by the liver. The use of oral c-17 alpha methylated testosterone causes toxicity to the liver and is not recommended for testosterone hormone therapy. Brand names around the world include “Metesto,” “Methitest,” “Testred,” “Oreton Methyl,” and “Android.” These products are responsible for many of the misconceptions that still exist about testosterone replacement due to their liver and lipid problems. The same information is applicable to fluroxymesterone, another oral formulation no longer used in the United States. Testosterone undecanoate Testosterone undecanoate is not a c-17 alpha alkylated hormone. Therefore it is considered a safer oral form of testosterone. It is designed to be absorbed through the small intestine into the lymphatic system, and has fewer negative effects on the liver. Brand names around the world for oral testosterone undecanoate include “Andriol,” “Androxon,” “Understor,” “Restandol,” and “Restinsol.” It is not available in the United States but widely used in Canada and some European countries. One disadvantage of orally administered undecanoate is that it is eliminated from the body very quickly, usually within three to four hours. Frequent administration is necessary—usually from three to six capsules a day, which makes it impractical for most men with busy lives. PERSONAL COMMENT: I've never used oral testosterones and I never will. Other formulations are so much more user-friendly.

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