Methyldienolone was first described in 1960. Eli Lilly & Co. (U.S.) developed this steroid, although the firm never released it as an actual medicine. It is of note that Lilly-also developed a 17-alpha-ethylated version (ethyldienolone) at the same time, which had an even more favorable anabolic to androgenic ratio in standard assay tests, but was not quite as potent overall. Being that methyldienolone was never sold as a prescription drug, it remained a research steroid of little interest for approximately forty years. The steroid actually came to life not as a prescription agent, but as an OTC "nutritional supplement" in 2004. Bruce Kneller, who had found the old research on methyldienolone and determined it to be a favorable agent to market with Gaspari Nutrition, was actually credited with developing the product. Gaspari sold the agent for a brief time as Methyl-D, before the 2004 amended Anabolic Steroid Control Act was passed, eliminating much of the grey area "prohormone" or "prosteroid" market in the U.S. Today, methyldienolone is again unavailable to athletes.
How is Methyl-D Supplied
Methyldienolone is not available as a commercial agent. When sold as a nutritional supplement, it contained 1 mg of steroid per tablet.
Structural Characteristics of Methyl-D
Methyldienolone is a modified form of nandrolone. It differs by: 1) the addition of a methyl group at carbon 17-alpha to protect the hormone during oral administration and 2) the introduction of a double bond at carbon 9, which increases its binding affinity and slows its metabolism. The resulting steroid is significantly more potent than its nandrolone base, and displays a much longer half-life and lower affinity for serum-binding proteins in comparison.
Methyl-D Side Effects (Estrogenic)
Methyldienolone is not aromatized by the body, and is not measurablyestrogenic. lt is of note, however, that based on its structure methyldienolone likely displays significant binding affinity for the progesterone receptor. The side effects associated with progesterone can be similar to those of estrogen, including negative feedback inhibition of testosterone production and enhanced rate of fat storage. Progestins also augment the stimulatory effect of estrogens on mammary tissue growth. There appears to be a strong synergy between these two hormones here, such that gynecomastia might even occur with the help of progestins, without excessive estrogen levels. The use of an anti-estrogen, which inhibits the estrogenic component of this disorder, is often sufficient to mitigate gynecomastia caused by progestational anabolic/androgenic steroids. Note that significant side effects are not likely unless high doses are taken, or the drug is used with other strongly aromatizable steroids.
Methyl-D Side Effects (Androgenic)
Although classified as an anabolic steroid,androgenic side effects are still common with this substance. This may include bouts of oily skin, acne, and body/facial hair growth. Anabolic/androgenic steroids may also aggravate male pattern hair loss. Women are also warned of the potential virilizing effects of anabolic/androgenic steroids. These may include a deepening of the voice, menstrual irregularities, changes in skin texture ,facial hair ' growth, and clitoral enlargement. Additionally, the 5-alpha reductase enzyme does not metabolize methyldienolone, so its relative androgenicity is not affected by finasteride or dutasteride/
Methyl-D Side Effects (Hepatotoxicity)
Methyldienolone is a cl 7-alpha alkylated compound. This alteration protects the drug from deactivation by the liver, allowing a very high percentage of the drug entry into the bloodstream following oral administration. Cl 7-alpha alkylated anabolic/androgenic steroids can be hepatotoxic. Prolonged or high exposure may result in liver damage. In rare instances life-threatening dysfunction may develop. It is advisable to visit a physician periodically during each cycle to monitor liver function and overall health. Intake of cl 7-alpha alkylated steroids is commonly limited to 6-8 weeks, in an effort to avoid escalating liver strain. Note that given its high level of potency and close structural similarity to methyltrienolone, one of the most hepatotoxic steroids known, methyldienolone is likely also very hepatotoxic; liver strain should be carefully monitored with use.
Methyl-D Side Effects (Cardiovascular)
Anabolic/androgenic steroids can have deleterious effects on serum cholesterol. This includes a tendency to reduce HDL (good) cholesterol values and increase LDL (bad) cholesterol values, which may shift the HDL to LDL balance in a direction that favors greater risk of arteriosclerosis. The relative impact of an anabolic/androgenic steroid on serum lipids is dependant on the dose, route of administration (oral vs. injectable), type of steroid (aromatizable or non-aromatizable), and level of resistance to hepatic metabolism. Although not studied in humans, the high relative potency, oral route, and non-aromatizable nature of methydienolone suggests that this agent is extremely prone to negatively altering lipid values and increasing atherogenic risk. Anabolic/androgenic steroids may also adversely affect blood pressure and triglycerides, reduce endothelial relaxation, and support left ventricular hypertrophy, all potentially increasing the risk of cardiovascular disease and myocardial infarction. To help reduce cardiovascular strain it is advised to maintain an active cardiovascular exercise program and minimize the intake of saturated fats, cholesterol, and simple carbohydrates at all times during active AAS administration. Supplementing with fish oils (4 grams per day) and a natural cholesterol/antioxidant formula such as Lipid Stabil or a product with comparable ingredients is also recommended.
Methyl-D Side Effects (Testosterone Suppression)
All anabolic/androgenic steroids when taken in doses sufficient to promote muscle gain are expected to suppress endogenous testosterone production. Without the intervention of testosterone-stimulating substances, testosterone levels should return to normal within 1-4 months of drug secession. Note that prolonged hypogonadotrophic hypogonadism can develop secondary to steroid abuse, necessitating medical intervention.
Methyl-D Administration (General)
Prescribing guidelines generally advise that oral steroids can be taken with or without meals. The difference in bioavailability is generally not regarded as substantial. However, a 2016 study on newborn infants did find the absorption of oxandrolone to be significantly improved when dissolved directly in fat (MCT oil). If the diet includes considerable fat content, taking this oral steroid with meals might be more advantageous.
Methyl-D Administration (Men)
Methyldienolone was never approved for use in humans. Prescribing guidelines are unavailable. Effective oral daily doses for physique- or performance-enhancing purposes fall in the range of 2-10 mg. At this level, one should expect measurable strength and lean tissue gains, which should be accompanied by decent fat loss and minimal side effects. In an effort to reduce liver strain, it is usually recommended to limit drug duration to no longer than 6-8 weeks, after which point a break is taken from all c-17 alkylated steroids. Users often avoid combining this drug with other liver toxic orals, and instead opt to use an injectable base when stacking. A dose of 5 mg per day of methyldienolone combined with 400 mg weekly of testosterone cypionate/enanthate or Equipoise® seems to be a common and effective lean-mass stack. Trenbolone (225 mg) or Primobolan® (300-400 mg) is often used instead for cutting purposes.
Methyl-D Administration (Women)
Methyldienolone was never approved for use in humans. Prescribing guidelines are unavailable. This agent is not recommended for women for physique- or performance-enhancing purposes due to its high level of potency and tendency to produce virilizing side effects. Note that the high anabolic to androgenic ratio of methyldienolone makes use possible without significant virilization, but would likely require measuring very small doses (well below Img per day) and respecting a very periodic use schedule (4 weeks or less).
Methyldienolone is not produced as a prescription steroid product in any part of the world. This agent was manufactured as a nutritional supplement for a brief period of time before the 2004 amendment to the Anabolic Steroid Act went into effect.
Wlliam Llewellyn (2017) - Anabolics