Primobolan~methenolone acetate

Primobolan

Androgenic:44-57
Anabolic: 88
Standard: Testosterone
Chemical names:17beta-Hydroxy-l-methyl-5alpha-androst-l-en-3-one l-methyl-l (5-alpha)-androsten-3-one-17b-ol
Estrogenic Activity: None
Progestational Activity: Very Low

(methenolone acetate)

Overview
Primobolan Depot is an injectable version of the steroid methenolone. This is the same constituent in Primobolan® orals (methenolone acetate), although here an enanthate ester is used to slow the steroid's release from a site of injection. Methenolone enanthate offers a similar pattern of steroid release as testosterone enanthate, with blood hormone levels remaining markedly elevated for approximately 2 weeks. Methenolone itself is a moderately strong anabolic steroid with very low androgenic properties. Its anabolic effect is considered to be slightly less than Deca-Durabolin® (nandrolone decanoate) on a milligram for milligram basis. Methenolone enanthate is most commonly used during cutting cycles, when lean mass gain, not a raw mass increase, is the main objective. It´s easy to see why many people have tried to use less...and have been disappointed with their results. On the other hand, many competitive bodybuilders consider Primobolan indespensible to their pre-contest drug routine, and wouldn´t consider dieting without it. Anyway...I think the comparison to Masteron (another great precontest drug) is the best one we can make, with reference to expected gains and results.

Structural Characteristics:
Methenolone is a derivative of dihydrotestosterone. It contains one additional double bond between carbons 1 and 2, which helps to stabilize the 3-keto group and increase the steroid's anabolic properties, and an additional 1-methyl group, which gives the steroid some protection against hepatic metabolism. Primobolan Depot makes use of methenolone with a carboxylic acid ester (enanthoic acid) attached to the 17-beta hydroxyl group. Esterified steroids are less polar than free steroids, and are absorbed more slowly from the area of injection. Once in the bloodstream, the ester is removed to yield free (active) methenolone. Esterified steroids are designed to prolong the window of therapeutic effect following administration, allowing for a less frequent injection schedule compared to injections of free (unesterified) steroid.

Administration (Men):
The prescribing guidelines for recommend a maximum dosage of 200 mg at the onset of therapy, and a continuing dosage of 100 mg every week. Prolonged administration protocols generally call for a 100 mg dosage every 1-2 weeks, or 200 mg every 2-3 weeks. The usual administration protocols among male athletes call for a 200-400 mg per week dosage, which is taken for 6 to 12 weeks, which is sufficient to promote very noticeable increases in lean muscle tissue. It is, however, not unusual to see the drug taken in doses as high as 600 mg per week or more, although such amounts are likely to highlight a more androgenic side of methenolone, as well Primobolan as exacerbate its negative effects on serum lipids. Methenolone enanthate is often stacked with other (typically stronger) steroids in order to obtain a faster and more enhanced effect. During a dieting or cutting phase, a non-aromatizing androgen like halotestin or trenbolone can be added. The stronger androgenic component here should help to bring about an added density and hardness to the muscles. On the other hand, one might add another mild anabolic steroid such as stanozolol. The result of such a combination should again be a notable increase in muscle mass and hardness, which still should not be accompanied by greatly increased side effects. Methenolone enanthate is also used effectively during bulking phases of training. In such a scenario, the addition of testosterone or boldenone would prove quite effective for adding new muscle mass without presenting any notable hepatotoxicity to the user.

Reference:
Llewellyn’s W. (2009). Anabolics (9th ed), Primobolan (p. 362-364): Jupiter, FL: Molecular Nutrition

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Anabolic Pharmacology By Seth Roberts

Primobolan

Pharmacology is the study of drugs and their effects. Anabolic pharmacology is the study of drugs that have a growth-promoting effect in muscle. This column will explore anabolic pharmacology by profiling a different anabolic drug and its effects each month. The focus of discussion this month will be the anabolic-androgenic steroid, Primobolan.

Methenolone is a synthetic derivative of dihydrotestosterone that is more commonly known by the trade name, Primobolan. The acetate ester version is taken orally, although there was once an injectable version of this ester. A highly-overlooked steroid, many people do not consider Primobolan to be very effective and coupled with its high price, do not consider it to be worthwhile. The oral form of methenolone is relatively weak due to the fact that methenolone is not 17-alpha alkylated. Instead, the 1-methyl group seems to offer some protection from metabolism to 1- and 2-hydroxy metabolites. Even so, the acetate does not have great oral bioavailability and a pretty high dose is needed to see significant effects.

Since it is a DHT derivative, methenolone does not aromatize nor does it have much progestational activity. In fact, being a DHT derivative, Primobolan likely acts as an aromatase inhibitor to some degree, which probably contributes to its reputation as a 'dry gainer' with less suppressive effects. Since it is already 5-alpha reduced, it does not get metabolized by 5-alpha reductase. Methenolone still undergoes metabolism by 3-alpha hydroxysteroid dehydrogenase in skeletal muscle, but less so than DHT.1 This results in a molecule that is somewhat less potent but still has a decent anabolic-to-androgenic ratio. Furthermore, it binds only moderately to sex hormone-binding globulin (SHBG), and there is no evidence that methenolone interacts to any degree with the glucocorticoid or progesterone receptors.2

Primobolan does not bring on massive weight gain, but this is due to the fact that there is very little water and fat accumulated. Primobolan is used for adding quality mass with little to no side effects, but the injectable version is much preferred over the oral version. Low doses of Primobolan have been used by women, with minimal side effects. Some have argued that Primobolan can be used without shutting down natural testosterone production. While suppression will be reduced with this steroid because it does not convert to estrogen, there will still be some reduction in testosterone production that will become worse as higher doses are used. A little-known fact about methenolone is that it has been shown to have similar levels of efficacy as oxymetholone for elevating red blood cell count.3 Methenolone the tablets or the injectable has never been as available as most of the other 'standbys,' and is often expensive when it is found. There are only a few pharmaceutical preparations available, and these items are often scarce— even from black-market sources.

Methenolone enanthate is the injectable form of this steroid, referred to as Primobolan Depot, its original trade name. The enanthate ester provides for a relatively slow release from the injection site and could be injected as infrequently as every 10 to 14 days, though most users will inject it weekly or even twice weekly. The injectable version of methenolone is much more effective than the oral version, since you do not have the effect of first-pass metabolism to contend with. Once the ester is stripped off, you have just the parent methenolone molecule.

The injectable version of methenolone with the enanthate ester is a potent steroid. It is usually injected on a weekly or sometimes shorter basis in doses of 400 to 600 milligrams for men and 50 to 100 milligrams for women. Women actually do better with a longer injection period of 10 to 12 days, to avoid a buildup in androgen levels. Methenolone is considered to be one of the safest steroids. Although methenolone is not C-17 alpha-alkylated, the 1-methyl group can cause some elevations in liver enzymes (even with the injectable)— but less so than the C-17 alkyl derivatives such as methandrostenolone. This is definitely not an 'instant gratification' drug, because it does not cause large amounts of water retention, and is less potent than other commonly-used injectables like nandrolone or even testosterone. Some people still prefer methenolone because even though it does not result in immediate gains, it generally doesn't produce as many side effects as other drugs.

Seth Roberts is a former pharmaceutical research scientist with over 10 years of pharmacological research in the discovery and development of novel therapeutics. If you want to learn more about Anabolic Steroids, pick up Seth's new book, Anabolic Pharmacology at Ergogens - UnderConstruction. [© Seth Roberts, 2009. All rights reserved. For informational purposes only, not to be considered as medical advice or an endorsement of the use of illegal substances.]

References:

1. Schanzer W: Metabolism of anabolic androgenic steroids. Clin Chem, Jul;42(7):1001-20, 1996.
2. Saartok T, Dahlberg E, Gustafsson JA: Relative binding affinity of anabolic-androgenic steroids: comparison of the binding to the androgen receptors in skeletal muscle and in prostate, as well as to sex hormone-binding globulin. Endocrinology, Jun;114(6):2100-6, 1984.
3. Gorshein D, Murphy S, Gardner FH. Comparative study on the erythropoietic effects of androgens and their mode of action. J Appl Physiol, 35(3):276-8, 1973.

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Primobolan (methenolone acetate)
Primobolan by Anthony Roberts

(methenolone acetate)

Primobolan is one of those anabolic steroids which has a cult following not unlike the old original version of Masteron. Actually, as you can easily see from its anabolic:androgenic ratio below in the profile, its a pretty weak steroid but actually stronger than Masteron in both regards. I dont know anyone who has run both compounds at the same dose. We are probably justified in speculating that youd probably get similar results from either of them, when you consider the fact that you are getting quite a bit less actual drug and more ester when you choose injectable Primobolan (which has the very long Enanthate ester attached to it) over Masteron (which has the very short propionate ester attached to it). In truth, I think part of the reason many Primobolan users have been disappointed is that they failed to use enough of it, for long enough. From its chemical structure and anabolic:androgenic rating, we can assume it is at least as effective as Masteron, on an equal Mg for mg basis. However, due to its ester (in the injectable version), it needs to be run for at least 12 weeks to see the full benefits from it. When you consider a measly dose of 400mgs of this stuff for 12 weeks will probably cost you around $500.

Its easy to see why many people have tried to use less...and have been disappointed with their results. On the other hand, many competitive bodybuilders consider Primobolan indespensible to their pre-contest drud routine, and wouldnt consider dieting without it. Anyway...I think the comparison to Masteron (another great precontest drug) is the best one we can make, with reference to expected gains and results.

I happen to be one of the few people who have used Drostanolone Enanthate (Masteron with the Enanthate ester attached) as well as Methenolone Enanthate (injectable Primobolan). I can tell you that the results from these two compounds, when ester and mg potency are the same, are in fact very similar.

Effects of Primobolan

Lets flesh out some of the various general effects of Primobolan, before we get into the differences between the oral and injectable versions... One study performed on sheep involved administering 100mgs of Methenolone, and electronically stimulating their lats (electronic stimulation was used because they kept falling off the chin-up bars). Anyway, when compared with the lat muscles of sheep who didnt receive Methenolone, the receiving group gained significantly more muscle mass as well as strength (1)(2). Its also has a relatively high affinity for binding to the AR, actually binding better than testosterone (3). This ability to strongly bind to the AR may be why Primobolan is such a good "fat burner." Strong AR binding has been positively correlated with lypolysis (fat-burning) (8).

In addition, as this steroid can actually aid in reducing breast tumors, no ancillary products need be considered for use with Primobolan, and in fact, it may actually be a useful ancillary agent in its own right, similar to Masteron. Also, just like Masteron, Primobolan has no propensity to aromatize (convert to estrogen). Since it doesnt aromatize, alot of the side effects commonly associated with estrogen will not be of concern. This means water retention, acne, and gyno will be non-existent more or less. this lack of water retention combined with the slow and steady gains provided by Primo may help to explain why it has earned a reputation for creating quality muscle gains. This also helps to explain why it is so expensive. Although estrogenic sides are not a concern, hair loss still, remains a very real concern with Primobolan, as with many DHT-Derived steroids. Many primobolan fans always include Finasteride and Ketoconazole (shampoo) in cycles containing Primobolan.

Although nobody would ever suggest to use Primobolan as a bulking agent, its been studied as an agent to halt wasting and possibly reverse many of the adverse effects of anemia. It is a shocking failure in both areas, according to some of the case studies Ive read, (5)(6) and this should come to no surprise to anyone. Anadrol reigns supreme in this area, and nobody in the athletic community would ever compare those two drugs. However, Michael Mooney and many other respected doctors who work with AIDS patients have found sufficient evidence to claim that Primobolan is an immune enhancer and as such is very useful for AIDS patients (not that the FDA cares...Primobolan is still not approved for sale in the United States). AIDS patients arent really in need of Bulking Drugs, so an immune enhancer like Primo which will add small, quality gains in muscle is perfect for them. And since we arent even going to vaguely consider the use of Primobolan as a bulking agent, clearly this leaves us with considering it primarily for use in gaining and maintaining lean tissue. Its a great choice for this purpose, and many competitors have used it very successfully to retain muscle while on a calorie reduced diet. The reason Primo is so useful for this purpose is that one of its primary functions is to help your body retain nitrogen (7) at a greatly enhanced rate. The greater your nitrogen retention is, the more muscle you will build. In the case of using primo as a pre-contest drug, this nitrogen retention will help you retain muscle and ensure that your dieting preferentially favors fat loss over muscle loss.

Primobolan is a very unique steroid, as it is one of the few that comes in both an oral as well as an injectable version. I suppose Winstrol does also, but Primobolan actually has a different ester on the oral (acetate ) and injectable (Enanthate) versions. The oral version is one of the more interesting oral compounds Ive looked into. For starters, its one of the few compounds available to athletes and bodybuilders which is both oral as well as non-17-alpha-alkylation. This alteration is (as Im sure you remember from other stuff Ive written) what generally makes oral steroids survive their first pass through your liver, but also makes them Hepatoxic (Liver toxic). Well... oral Primo doesnt have this feature, so it is very mild on your liver (actually it basically isnt liver toxic at all), but also is largely destroyed by it, since 17 beta estrification and 1 alkylation is the method used to make this stuff orally available. Youll need to take a lot of this stuff for it to be effective... 100mgs/day of the oral version is a safe estimate for reasonable gains& for women, you could get away with less; perhaps 25mgs/day. Even though the acetate ester has a 2-3 day active life, your liver will do some damage to oral primo, so every day dosing will still be necessary.

When men were given a 30-45mg dose of the oral version of Primo, they experienced a 15-65% decrease in gonadotropin levels (9). Remember, I said 100mgs is a good dose for gains... well, youll also reduce your gonadotropin levels considerably. I have personally never understood why people recommend either oral or injectable Primobolan as a possible bridging compound for this reason... maybe at a too-low-to-do-anything dose of 10mgs it could be used as a bridge. And forget about using injectable Primo to bridge &

Hey... speaking about injectable Primo...

Ive used this stuff at 200mgs/week and wasnt very impressed with it. Generally, I think injectable primo needs to be used at a dose of at least 350mgs/week (100mgs/Every other Day), and preferably at a dose of 400-600mgs/week. I happen to like running it with testosterone propionate, but for convenience I would imagine most people would run it with Testosterone Enanthate, to keep dosing times the same (shooting it twice per week, in most cases).

Buying Primobolan

The unfortunate truth about injectable Primo is that its a very expensive chemical to obtain, and that price is reflected in the cost to the average consumer. Ten dollars per 1ml/100mg ampule is not unheard of, and Ive seen it go for more. This is, of course, absurd. As if thats not enough, this is also the most commonly counterfeited steroids on the black market. I recommend buying Primobolan (either the oral or injectable) from a respected Underground lab instead of trying to play a game of "spot the fake steroid" in Mexico or Europe. The underground versions should cost between $5-7 for 100mgs of Methenolone and I wouldnt really consider paying more for it, although I have seen the British Dragon version of this product priced up to $20/ml.

Primobolan Profile

(Methenolone)

(Oral Version is + Acetate Ester)
(Injectable Version is + Enanthate Ester)
[17beta-Hydroxy-1-methyl-5alpha-androst-1-en-3-one]
Molecular weight of base: 302.4558
Molecular weight of Acetate ester: 60.0524
Molecular weight of Enanthate ester: 130.1864
Formula: C20H30O2
Melting Point:
Manufacturer: Schering
Effective dose(oral): (Men)50-100mgs/day; (Women) 10-25mgs/day
Effective dose (injectable): (Men) 350-600mgs/week; (Women) 100mgs/week
Active Life: 10-14 days (injectable); 4-6hrs (oral)
Detection Time: 4-5 weeks
Anabolic/Androgenic Ratio (Range): 88:44-57

References:







Anabolic steroids (metenolone) improve muscle performance and hemodynamic characteristics in cardiomyoplasty. Ann Thorac Surg. 1995 Apr;59(4):961-9; discussion 969-70.
Effect of an anabolic steroid (Metenolon) on contractile performance of the chronically stimulated latissimus dorsi in sheep. Eur J Cardiothorac Surg. 1994;8(4):214-9.
Relative binding affinity of anabolic-androgenic steroids: comparison of the binding to the androgen receptors in skeletal muscle and in prostate, as well as to sex hormone-binding globulin. Endocrinology. 1984 Jun;114(6):2100-6.
[Anabolic therapy in metastatic breast cancer] Med Klin. 1981 Nov 20;76(24):689-91. German.
Partial remission and severe adverse effect caused by metenolone acetate in a male patient with aplastic anem. Eur J Haematol. 1995 Jul;55(1):57-8.
Fatal outcome of a patient with severe aplastic anemia after treatment with metenolone acetate. Ann Hematol. 1993 Jul;67(1):41-3.
Metabolic effects of anabolic steroids. Wien Med Wochenschr. 1993;143(14-15):368-75.
Biochim Biophys Acta. 1995 May 11;1244(1):117-20.
Comparative Studies about the influence of Metenolone Acetate and Mesterolone on hypophysis and male gonads. Arzneimittelforshung. 1970 20(4) 545-7


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