Dimethazine was first described in 1962. It was developed into a medicine by Ormonoterapia Richter in Milan, Italy. The firm sold it under the Roxilon brand name in ltaly and as Dostalon in Mexico. The Roxilon brand was also reportedly sold under license by Lepetit. Dimethazine has been evaluated clinically for a number of treatments, often including use with women, the elderly, and children. Such applications have included the promotion of growth in underweight children and adolescents, the retention of lean body mass with chronic pulmonary tuberculosis, the treatment of osteoporosis, and as a general anabolic in conditions necessitating the use of such an agent. In spite of a favorable record of efficacy and safety, dimethazine was ultimately a drug that saw only limited success as a prescription agent. It was discontinued many years ago, and has been unavailable worldwide for so long that few even recognize the active ingredient as a once-marketed commercial steroid.
How is Roxilon Supplied
Dimethazine is no longer sold as a prescription drug preparation.
Structural Characteristics of Roxilon
Methyldrostanolone is a modified form of dihydrotestosterone. It differs by: 1) the addition of a methyl group at carbon 17-alpha, which helps protect the hormone during oral administration, and 2) the introduction of a methyl group at carbon-2 (alpha), which considerably increases the anabolic strength of the steroid by heightening its resistance to metabolism by the 3-hydroxysteroid dehydrogenase enzyme in skeletal muscle tissue. Dimethazine consists of two methyldrostanolone molecules bonded together with an azine bridge. These molecules are metabolically separated, yielding free methyldrostanolone.
Roxilon Side Effects (Estrogenic)
Dimethazine is not aromatized by the body, and is not measurably estrogenic or progestational. An antiestrogen is not necessary when using this steroid, as gynecomastia should not be a concern even among sensitive individuals. Since estrogen is the usual culprit with water retention, this steroid instead produces a lean, quality look to the physique with no fear of excess subcutaneous fluid retention. This makes it a favorable steroid to use during cutting cycles, when water and fat retention are major concerns.
Roxilon Side Effects (Androgenic)
Although classified as an anabolic steroid, androgenic side effects are still possible with this substance, especially with higher doses. 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 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. Dimethazine is a steroid with relatively low androgenic activity relative to its tissue-building actions, making the threshold for strong androgenic side effects comparably higher than with more androgenic agents such as testosterone, methandrostenolone, or fluoxymesterone. Note that the 5-alpha reductase enzyme does not metabolize dimethazine, so its relative androgenicity is not affected by the concurrent use of finasteride or dutasteride.
Roxilon Side Effects (Hepatotoxicity)
Dimethazine 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 in studies administering 20 mg per day to patients for 45-95 days, dimethazine was shown to induce modest to moderate bilirubinemia (excess bilirubin in the blood, indicative of hepatic stress) in close to 50% of patients. Approximately 25% of the patients noticed substantial increases in serum transaminases. These results suggest this steroid has a significant level of hepatotoxicity.
Roxilon 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. Dimethazine has a strong effect on the hepatic management of cholesterol due to its non-aromatizable nature, structural resistance to liver breakdown, and route of administration. 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.
Roxilon 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.
Roxilon Administration (Men)
An effective dosage of dimethazine for physique- or performance-enhancing purposes begins in the range of 10-20 mg per day, taken for no longer than 6 or 8 weeks. At this level it seems to impart a measurable musclebuilding effect, which is usually accompanied by fat loss and increased definition. Higher doses are usually avoided due to potential hepatotoxicity.
Roxilon Administration (Women)
An effective dosage of dimethazine for physique- or performance-enhancing purposes would fall around 2.5 mg per day, taken in cycles lasting no more than 4-6 weeks to minimize the chance for virilization. As with all anabolic/androgenic steroids, virilization is still possible.
Dimethazine is no longer commercially produced, and is unavailable on the black market.
Wlliam Llewellyn (2017) - Anabolics