Myagen (bolasterone) oral anabolic steroid structurally related methyltestosterone

akn

Musclechemistry Member
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[FONT=&quot]Bolasterone is an oral anabolic steroid structurally related to[/FONT]

[FONT=&quot]methyltestosterone. It differs only by the addition of a methyl[/FONT]
[FONT=&quot]group at c-7, which accounts for its given chemical name,[/FONT]
[FONT=&quot]7,17-dimethyltestosterone. The added c-7 methyl group[/FONT]
[FONT=&quot]makes the activity of this steroid far removed from[/FONT]
[FONT=&quot]methyltestosterone, however, such that any direct comparison[/FONT]
[FONT=&quot]is difficult to justify. For starters, bolasterone is a fairly[/FONT]
[FONT=&quot]potent steroid, measured in human subjects to have[/FONT]
[FONT=&quot]approximately twice the anabolic effect of[/FONT]
[FONT=&quot]methandrostenolone.544 This is in contrast to[/FONT]
[FONT=&quot]methyltestosterone, which is considerably less potent than[/FONT]
[FONT=&quot] [/FONT]
[FONT=&quot]methandrostenolone. Despite being a testosterone derivative,[/FONT]
[FONT=&quot]bolasterone is also much more anabolic than androgenic in[/FONT]
[FONT=&quot]nature. At a given therapeutic level, it is much less likely to[/FONT]
[FONT=&quot]cause androgenic/virilizing side effects. It does have one[/FONT]
[FONT=&quot]strong similarity to methyltestosterone, however, which lies[/FONT]
[FONT=&quot]in the fact that bolasterone too is quite estrogenic. Both[/FONT]
[FONT=&quot]agents are, therefore, most appropriately used during bulking[/FONT]
[FONT=&quot]phases or training.[/FONT]
[FONT=&quot]History:[/FONT]
[FONT=&quot]Bolasterone was first described in 1959.545 It was closely[/FONT]
[FONT=&quot]evaluated for anabolic and androgenic effect approximately 3[/FONT]
[FONT=&quot]years later.546 The drug was developed by Upjohn, and sold[/FONT]
[FONT=&quot]in the U.S. during the 1960’s under the Myagen brand name.[/FONT]
[FONT=&quot]It was mainly indicated for the treatment of advanced breast[/FONT]
[FONT=&quot]cancer in women, although the agent was also investigated[/FONT]
[FONT=&quot]for its stimulatory effect on blood cells and its general[/FONT]
[FONT=&quot]anabolic (lean-tissue sparing) activity. Bolasterone was[/FONT]
[FONT=&quot]ultimately a short-lived drug, disappearing from the U.S.[/FONT]
[FONT=&quot]market shortly after its release. By the 1980’s, bolasterone[/FONT]
[FONT=&quot]had been out of commerce for so long that it was all but[/FONT]
[FONT=&quot]forgotten among athletes. Although bolasterone is no longer[/FONT]
[FONT=&quot]produced, the drug remains listed in the U.S. Pharmacopeias,[/FONT]
[FONT=&quot]suggesting it would not be impossible to see this agent for[/FONT]
[FONT=&quot]sale (legally) in the U.S. again, perhaps under order by a[/FONT]
[FONT=&quot]private compounding pharmacy. The reemergence of an[/FONT]
[FONT=&quot] actual commercial bolasterone compound, however, remains[/FONT]
[FONT=&quot]very unlikely.[/FONT]
[FONT=&quot]How Supplied:[/FONT]
[FONT=&quot]Bolasterone is no longer available as a prescription drug[/FONT]
[FONT=&quot]product.[/FONT]
[FONT=&quot]Structural Characteristics:[/FONT]
[FONT=&quot]Bolasterone is a modified form of testosterone. It differs by:[/FONT]
[FONT=&quot]1) the addition of a methyl group at carbon 17-alpha, which[/FONT]
[FONT=&quot]helps protect the hormone during oral administration, and 2)[/FONT]
[FONT=&quot]the introduction of a methyl group at carbon 7 (alpha), which[/FONT]
[FONT=&quot]inhibits 5-alpha reduction and shifts the anabolic to[/FONT]
[FONT=&quot]androgenic ratio in favor of the former. 7,17-dimethylated[/FONT]
[FONT=&quot]steroids also tend to be very resistant to metabolism and[/FONT]
[FONT=&quot]serum-binding proteins, greatly enhancing their relative[/FONT]
[FONT=&quot]biological activity.[/FONT]
[FONT=&quot]Side Effects (Estrogenic):[/FONT]
[FONT=&quot]Bolasterone is aromatized by the body, and is considered a[/FONT]
[FONT=&quot]highly estrogenic steroid due to its conversion to 7,17-[/FONT]
[FONT=&quot]dimethylestradiol (an estrogen with high biological activity).[/FONT]
[FONT=&quot]Gynecomastia may be a concern during treatment, especially[/FONT]
[FONT=&quot]when higher than normal therapeutic doses are used. At the[/FONT]
[FONT=&quot] same time water retention can become a problem, causing a[/FONT]
[FONT=&quot]notable loss of muscle definition as both subcutaneous water[/FONT]
[FONT=&quot]retention and fat levels build. To avoid strong estrogenic[/FONT]
[FONT=&quot]side effects, it may be necessary to use an anti-estrogen such[/FONT]
[FONT=&quot]as Nolvadex®. One may alternately use an aromatase[/FONT]
[FONT=&quot]inhibitor like Arimidex® (anastrozole), which is a more[/FONT]
[FONT=&quot]effective remedy for estrogen control. Aromatase inhibitors,[/FONT]
[FONT=&quot]however, can be quite expensive in comparison to standard[/FONT]
[FONT=&quot]estrogen maintenance therapies, and may also have negative[/FONT]
[FONT=&quot]effects on blood lipids.[/FONT]
[FONT=&quot]Side Effects (Androgenic):[/FONT]
[FONT=&quot]Although bolasterone is classified as an anabolic steroid,[/FONT]
[FONT=&quot]androgenic side effects are still possible with this substance.[/FONT]
[FONT=&quot]These may include bouts of oily skin, acne, and body/facial[/FONT]
[FONT=&quot]hair growth. Higher doses are more likely to cause such side[/FONT]
[FONT=&quot]effects. Anabolic/androgenic steroids may also aggravate[/FONT]
[FONT=&quot]male pattern hair loss. Women are additionally warned of the[/FONT]
[FONT=&quot]potential virilizing effects of anabolic/androgenic steroids.[/FONT]
[FONT=&quot]These may include a deepening of the voice, menstrual[/FONT]
[FONT=&quot]irregularities, changes in skin texture, facial hair growth, and[/FONT]
[FONT=&quot]clitoral enlargement. Bolasterone is unaffected by the 5-[/FONT]
[FONT=&quot]alpha reductase enzyme, so its relative androgenicity is not[/FONT]
[FONT=&quot]affected by the concurrent use of finasteride or dutasteride.[/FONT]
[FONT=&quot]Note that studies administering 1mg and 2mg of bolasterone[/FONT]
[FONT=&quot]per day have shown no outward androgenic side effects in[/FONT]
[FONT=&quot] [/FONT]
[FONT=&quot]children and hypogonadotrophic males, as would be[/FONT]
[FONT=&quot]characterized by public hair growth, genital changes, voice[/FONT]
[FONT=&quot]changes, and acne. Higher doses remain likely to induce[/FONT]
[FONT=&quot]androgenic effects. Bolasterone is considered to have a[/FONT]
[FONT=&quot]comparable ratio of anabolic to androgenic effect as[/FONT]
[FONT=&quot]oxymetholone and methandrostenolone.[/FONT]
[FONT=&quot]Side Effects (Hepatotoxicity):[/FONT]
[FONT=&quot]Bolasterone is a c17-alpha alkylated compound. This[/FONT]
[FONT=&quot]alteration protects the drug from deactivation by the liver,[/FONT]
[FONT=&quot]allowing a very high percentage of the drug entry into the[/FONT]
[FONT=&quot]bloodstream following oral administration. C17-alpha[/FONT]
[FONT=&quot]alkylated anabolic/androgenic steroids can be hepatotoxic.[/FONT]
[FONT=&quot]Prolonged or high exposure may result in liver damage. In[/FONT]
[FONT=&quot]rare instances life-threatening dysfunction may develop. It is[/FONT]
[FONT=&quot]advisable to visit a physician periodically during each cycle[/FONT]
[FONT=&quot]to monitor liver function and overall health. Intake of c17-[/FONT]
[FONT=&quot]alpha alkylated steroids is commonly limited to 6-8 weeks,[/FONT]
[FONT=&quot]in an effort to avoid escalating liver strain. Studies[/FONT]
[FONT=&quot]administering 1mg and 2mg of bolasterone daily for 6 weeks[/FONT]
[FONT=&quot]to 27 patients have demonstrated a trend toward increases in[/FONT]
[FONT=&quot]serum alkaline phosphatase (a marker of liver stress),[/FONT]
[FONT=&quot]although no significant untoward effects on the liver were[/FONT]
[FONT=&quot]documented.[/FONT]
[FONT=&quot]The use of a liver detoxification supplement such as Liver[/FONT]
[FONT=&quot]Stabil, Liv-52, or Essentiale Forte is advised while taking[/FONT]
[FONT=&quot]any hepatotoxic anabolic/androgenic steroids.[/FONT]
[FONT=&quot]Side Effects (Cardiovascular):[/FONT]
[FONT=&quot]Anabolic/androgenic steroids can have deleterious effects on[/FONT]
[FONT=&quot]serum cholesterol. This includes a tendency to reduce HDL[/FONT]
[FONT=&quot](good) cholesterol values and increase LDL (bad)[/FONT]
[FONT=&quot]cholesterol values, which may shift the HDL to LDL balance[/FONT]
[FONT=&quot]in a direction that favors greater risk of arteriosclerosis. The[/FONT]
[FONT=&quot]relative impact of an anabolic/androgenic steroid on serum[/FONT]
[FONT=&quot]lipids is dependant on the dose, route of administration (oral[/FONT]
[FONT=&quot]vs. injectable), type of steroid (aromatizable or nonaromatizable),[/FONT]
[FONT=&quot]and level of resistance to hepatic metabolism.[/FONT]
[FONT=&quot]Bolasterone has a strong effect on the hepatic management of[/FONT]
[FONT=&quot]cholesterol due to its structural resistance to liver breakdown[/FONT]
[FONT=&quot]and route of administration. Anabolic/androgenic steroids[/FONT]
[FONT=&quot]may also adversely affect blood pressure and triglycerides,[/FONT]
[FONT=&quot]reduce endothelial relaxation, and support left ventricular[/FONT]
[FONT=&quot]hypertrophy, all potentially increasing the risk of[/FONT]
[FONT=&quot]cardiovascular disease and myocardial infarction. Studies[/FONT]
[FONT=&quot]administering 1mg and 2mg of bolasterone daily for 6 weeks[/FONT]
[FONT=&quot]to 27 patients have demonstrated a trend toward increased[/FONT]
[FONT=&quot]serum cholesterol. Although no HDL and LDL breakdown[/FONT]
[FONT=&quot]was provided, it can be assumed based on the structure and[/FONT]
[FONT=&quot]route of administration that bolasterone significantly shifted[/FONT]
[FONT=&quot]the ratio of these two fractions of cholesterol further apart[/FONT]
[FONT=&quot] [/FONT]
[FONT=&quot] measurably increasing atherogenic risk.[/FONT]
[FONT=&quot]To help reduce cardiovascular strain it is advised to[/FONT]
[FONT=&quot]maintain an active cardiovascular exercise program and[/FONT]
[FONT=&quot]minimize the intake of saturated fats, cholesterol, and simple[/FONT]
[FONT=&quot]carbohydrates at all times during active AAS administration.[/FONT]
[FONT=&quot]Supplementing with fish oils (4 grams per day) and a natural[/FONT]
[FONT=&quot]cholesterol/antioxidant formula such as Lipid Stabil or a[/FONT]
[FONT=&quot]product with comparable ingredients is also recommended.[/FONT]
[FONT=&quot]Side Effects (Testosterone Suppression):[/FONT]
[FONT=&quot]All anabolic/androgenic steroids when taken in doses[/FONT]
[FONT=&quot]sufficient to promote muscle gain are expected to suppress[/FONT]
[FONT=&quot]endogenous testosterone production. Without the intervention[/FONT]
[FONT=&quot]of testosterone-stimulating substances, testosterone levels[/FONT]
[FONT=&quot]should return to normal within 1-4 months of drug secession.[/FONT]
[FONT=&quot]Note that prolonged hypogonadotrophic hypogonadism can[/FONT]
[FONT=&quot]develop secondary to steroid abuse, necessitating medical[/FONT]
[FONT=&quot]intervention.[/FONT]
[FONT=&quot]Administration (General):[/FONT]
[FONT=&quot]Studies have shown that taking an oral anabolic steroid with[/FONT]
[FONT=&quot]food may decrease its bioavailability.547 This is caused by[/FONT]
[FONT=&quot]the fat-soluble nature of steroid hormones, which can allow[/FONT]
[FONT=&quot]some of the drug to dissolve with undigested dietary fat,[/FONT]
[FONT=&quot]reducing its absorption from the gastrointestinal tract. For[/FONT]
[FONT=&quot]maximum utilization, this steroid should be taken on an empty[/FONT]
[FONT=&quot]stomach.[/FONT]
[FONT=&quot]Administration (Men):[/FONT]
[FONT=&quot]Clinical studies have demonstrated that significant nitrogen[/FONT]
[FONT=&quot]retention and weight gain can be induced with a daily dosage[/FONT]
[FONT=&quot]of 1-2mg per day. In the athletic arena, doses of 2-5 mg daily[/FONT]
[FONT=&quot]seem to be most reasonable, taken in cycles lasting no more[/FONT]
[FONT=&quot]than 6-8 weeks in length to minimize hepatotoxicity. This[/FONT]
[FONT=&quot]level is sufficient for strong increases in muscle size and[/FONT]
[FONT=&quot]strength, although such gains will likely be accompanied by[/FONT]
[FONT=&quot]significant water retention.[/FONT]
[FONT=&quot]Administration (Women):[/FONT]
[FONT=&quot]Bolasterone was not widely used with women in clinical[/FONT]
[FONT=&quot]medicine. When applied, it was most often used as a[/FONT]
[FONT=&quot]secondary medication during inoperable breast cancer, when[/FONT]
[FONT=&quot]other therapies have failed to produce a desirable effect. The[/FONT]
[FONT=&quot]dosage used for this application would be as high as 10 mg[/FONT]
[FONT=&quot]per day, a level that has caused significant virilization among[/FONT]
[FONT=&quot]patients. Bolasterone is generally not recommended for[/FONT]
[FONT=&quot]women for physique- or performance-enhancing purposes[/FONT]
[FONT=&quot]due to its very strong nature and tendency to produce[/FONT]
[FONT=&quot]virilizing side effects.[/FONT]
[FONT=&quot]Availability:[/FONT]
[FONT=&quot]Bolasterone is no longer produced as a prescription drug,[/FONT]
[FONT=&quot]although a handful of underground laboratories have taken to[/FONT]
[FONT=&quot]selling this material.[/FONT]
[FONT=&quot] [/FONT]
[FONT=&quot]By WL[/FONT][FONT=&quot][/FONT]
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SemiHidden="false" UnhideWhenUsed="false" QFormat="true" Name="Intense Reference"/> <w:LsdException Locked="false" Priority="33" SemiHidden="false" UnhideWhenUsed="false" QFormat="true" Name="Book Title"/> <w:LsdException Locked="false" Priority="37" Name="Bibliography"/> <w:LsdException Locked="false" Priority="39" QFormat="true" Name="TOC Heading"/> </w:LatentStyles> </xml><![endif]--><!--[if gte mso 10]> <style> /* Style Definitions */ table.MsoNormalTable {mso-style-name:"Table Normal"; mso-tstyle-rowband-size:0; mso-tstyle-colband-size:0; mso-style-noshow:yes; mso-style-priority:99; mso-style-qformat:yes; mso-style-parent:""; mso-padding-alt:0in 5.4pt 0in 5.4pt; mso-para-margin-top:0in; mso-para-margin-right:0in; mso-para-margin-bottom:10.0pt; mso-para-margin-left:0in; mso-pagination:widow-orphan; font-size:11.0pt; font-family:"Calibri","sans-serif"; mso-ascii-font-family:Calibri; mso-ascii-theme-font:minor-latin; mso-hansi-font-family:Calibri; mso-hansi-theme-font:minor-latin;} 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