Oral testosterone, by the simple fact that it’s taken by swallowing a little pill it has a very strong appeal. Unfortunately, most oral testosterone is extremely toxic and cannot be used safely in most situations. Methyltestosterone is the first oral testosterone to ever be created; in fact, it is one of the very first testosterone preparations. When testosterone was first synthesized it was in the form of injectable Testosterone Suspension. This was a raw testosterone product, there was no ester attached. Testosterone Suspension is very fast acting due to there being no ester; in fact, it often needs to be injected at a minimum of every other day to even daily. Once Testosterone Suspension was created, it wasn’t long after that Testosterone Propionate would hit the market. The Propionate version would represent the very first commercially available injectable testosterone. However, in between Testosterone Suspension and Testosterone Propionate was Methyltestosterone, which would appear in 1936.
The most well-known brand of Methyltestosterone is without question Ciba’s Metandren. However, it has been pulled from the market in recent years with the only pharmaceutical brand name left being Teston out of Greece. However, there are plenty of generic brands. In fact, while rarely prescribed in the U.S., for reasons that are largely unknown, the supply of the compound in the U.S. remains extremely high.
Over the years Methyltestosterone has enjoyed a fair amount of success. It has been used in andropausal men, as well as in treating cryptorchidism. The compound has also been used with enormous success in women who are suffering from libido issues due to menopause; however, this has in recent years fallen out of popularity in lieu of various creams and gels. Many women now enjoy creams that are a mix of low dose testosterone and progesterone.
Methyltestosterone represents one of the most controversial testosterone medications to ever exist; this is largely due to its high level of hepatotoxicity. Other forms of testosterone do not carry a toxic nature. Further, like all testosterone medications, it is estrogenic, but it tends to be far more so than other testosterone forms.
Beyond Methyltestosterone, there is another oral testosterone we must take a look at in Andriol. Andriol is an oral testosterone gel cap that was released by Organon in the late 1980’s and was redesigned in 2003 and released as Andriol Testocaps. Originally Andriol had to be kept refrigerated and had a shelf-life of only three months, but the new Testocaps can be kept at room temperature with a shelf-life of three years. More importantly, both forms, the original and the newer Testocaps, neither version is toxic to the liver. For this reason, Andriol Testocaps (old Andriol is rarely used anymore) has been used very successfully and quite commonly in low testosterone treatment across the globe except in the U.S. The U.S. FDA has never approved Andriol nor made an attempt to examine it or consider it.
Functions & Traits:
Methyltestosterone: This is a testosterone hormone that is designed to survive oral ingestion due to an added methyl group being attached to the hormone. Officially, it is classified as a C17-alpha alkylated (C17-aa) anabolic androgenic steroid. This label refers to the structural change, the added methyl group at the 17th carbon position. This is precisely what makes the compound hepatotoxic.
Andriol: This is an oral capsule that contains testosterone attached to an ester, specifically Testosterone Undecanoate. Unlike Methyltestosterone, Andriol is not hepatotoxic; it is the only oral testosterone that is not C17-aa. At first glance, one would assume it would be largely destroyed by the liver due to the lacking added methyl group, but it is designed to absorb (in part) through the lymphatic system along with dietary fat.
Regardless of the form of oral testosterone, Methyltestosterone or Andriol, both are simply testosterone. The hormone does not change from one to the next; in fact, the hormone does not change from one form of testosterone to another in any type of testosterone. What changes is the hormone’s function based on timing, toxicity, half-lives and administration as well as efficiency. Based on efficiency, the most important aspect, oral testosterone does not carry a high bioavailability. It will require large doses of either form to reap a reward, and as Andriol is the one you’d want to use due to it carrying no hepatic nature, unfortunately, it is very expensive.
Based on hepatotoxicity, although appealing on the basis of administration, Methyltestosterone cannot be recommended for the treatment of low testosterone. There are too many options available that are far safer. As for Andriol, while its bioavailability is rather low, with a proper dose it will work tremendously well and can easily be recommended. Unfortunately, those in the U.S. will not have access to the medication in either form, Andriol or Andriol Testocaps.
The side effects of oral testosterone are the same regardless of the form and are the same as all testosterone forms with the exception of liver toxicity and lipids. The primary side effects of oral testosterone will surround testosterone’s estrogenic nature. Testosterone has the ability to convert to estrogen via the aromatase enzyme. As estrogen levels rise, this can lead to gynecomastia, water retention and even high blood pressure when water retention becomes severe. Fortunately, while these are the primary side effects of oral testosterone they are also the easiest to control. The use of an Aromatase Inhibitor (AI) can easily keep estrogen levels from going too high. This is accomplished by the AI inhibiting the aromatase process and in turn, reducing serum estrogen levels. Approximately 25-30% of all men will not need an AI; using one when not needed will drive your estrogen levels too far down, which can lead to numerous symptoms, but many men will need it and it will work each and every time.
The side effects of oral testosterone can also include those of an androgenic nature due to the testosterone hormone being metabolized by the 5-alpha reductase enzyme. This reduction will cause testosterone to convert to dihydrotestosterone (DHT), which can promote hair loss, acne and body hair growth. However, in a testosterone replacement therapy setting, such occurrences are rare; they are far more commonly associated with supraphysiological doses. This doesn’t mean such effects aren’t possible, but they are strongly tied to genetic predispositions such as a predisposition to male pattern baldness.
As with all testosterone medications, oral testosterone can reduce HDL cholesterol. Testosterone should not have a significant negative impact on lipids, but a slight reduction in HDL cholesterol is possible. However, data has shown that it can be reduced by as much as 20% with the conjoined use of an AI. In order to maintain a healthy lipid profile, with or without testosterone use, the individual’s diet should be rich in omega fatty acids and limited in saturated fats and simple sugars. Regular cardiovascular activity is also a good thing to keep in your daily routine.
The above applies to all testosterone forms regarding lipids including Andriol. However, the above does not apply to Methyltestosterone. Methyltestosterone can have a much stronger, negative impact on lipids by significantly suppressing HDL cholesterol with or without an AI and increasing LDL cholesterol by as much as 30%. This trait held by Methyltestosterone is due to it being a C17-aa medication. Extra attention to cholesterol is often needed when using this particular type of testosterone. Supplementation with a cholesterol antioxidant is often recommended.
The final side effect associated with all forms of oral testosterone is natural testosterone suppression. When exogenous testosterone is used, endogenous production comes to a halt. The body has no need to make its own testosterone when it’s being provided by an outside source. Fortunately, this is of absolutely no concern for the low testosterone patient. The low testosterone patient does not have the ability to produce enough testosterone on his own to begin with. Important note – the use of HCG will keep natural testosterone production going while using exogenous testosterone. This will give the individual an approximate 20% boost in total testosterone above what he would have received with exogenous testosterone alone. It’s also important to note that HCG will only work in this regard in men who suffer from secondary hypogonadism. It will not work for those suffering from primary hypogonadism.
The final side effect of oral testosterone is liver toxicity. This does NOT apply to Andriol Testocaps, but it does apply to Methyltestosterone and any other form of oral testosterone you might come across. The use of Methyltestosterone will see liver enzyme values go up. However, enzyme values going up is not a sign of liver damage, it is a sign of stress that could lead to liver damage. With continuous use, the individual would most certainly experience severe liver damage. However, short-term use in some cases where deemed medically necessary can be acceptable. While liver enzyme values will increase, they will return to normal shortly after use is discontinued and no damage should be done. It is abuse of this form of testosterone that will cause damage or at least greatly increase the risk.
Dosing & Administration:
Methyltestosterone: In the treatment of low testosterone, Methyltestosterone doses will normally fall in the 10-40mg per day range. In many cases, therapy begins at 40mg per day and then decreases to a comfortable maintenance dose. Methyltestosterone is not normally used for a long period of time; however, there are rare instances where it is used indefinitely. In such cases, it’s extremely important to have blood work done to measure lipid and liver health to determine if the individual should continue.
Andriol: For the treatment of low testosterone, standard Andriol doses will normally be in the 120-160mg per day range. Commonly such doses are held for 4-6 weeks and then a blood test is done to determine the necessary maintenance dose. Standard maintenance Andriol doses can fall anywhere from 40-120mg per day and will be determined on a patient-by-patient basis. Total use is indefinite. If you truly have low testosterone, it can be remedied through compounds like Andriol, but there is no permanent cure. If you have low testosterone, you will always need testosterone treatment. Failing to continue treatment will simply return you to your prior low level state.