Methenolone was first described in 1960. Squibb would introduce the drug (as methenolone acetate) to the United States in 1962. This agent was sold for a very short time as a 20 mg tablet, under the brand name of Nibal. Schering in West Germany (now Bayer) would be granted rights to the drug that same year, and would sell it under the Primobolan name. Nibal was soon removed from the U.S. market, never to return as a commercial product. Schering now had exclusive patent rights to produce methenolone acetate, and would continue to sell the drug uninterrupted since 1962, and consumers had naturally come to identify methenolone acetate as a product of Schering.
Primobolan has always been identified as a European steroid, and during the 1960’s and ’70’s was being offered for sale in such countries as Germany, Austria, Belgium, France, the Netherlands, and Finland. At one time Schering also manufactured a 20 mg/ml oil-based injectable of methenolone acetate in limited markets (called Primobolan Acetate), but it has been out of manufacture since 1993. Injectable methenolone acetate proved to be very popular for pre-contest cutting use, and was gravely missed among European competitors when discontinued. Although we still have the acetate in oral form, it is a close, but not equal, substitute (injection is a much more efficient form of delivery for this steroid).
Primobolan is prescribed as a lean tissue building anabolic agent, often used in cases where body wasting has occurred secondary to major surgery, infection, wasting disease, aggressive corticosteroid administration, or malnutrition. (Some clinicians also prescribe this agent for treating osteoporosis and sarcopenia, or the natural loss of muscle mass with aging). This steroid has also been used to promote weight gain in underweight premature infants and children in clinical studies, and was able to do so effectively and without signs of toxicity or undesirable effects. Athletes have long favored the combined strong anabolic, weak androgenic, and non-estrogenic nature of this drug, which makes it very desirable for building lean muscularity without side effects.
Although Primobolan demonstrated a good record of clinical safety, Schering had withdrawn this drug from most markets by the early 2000s. No 50 mg versions are still in manufacture, and at most a select couple of products containing 5 mg or 25 mg may still be in circulation. The only confirmed sources for oral brand name Primobolan in recent years were in Japan and South Africa, and these were sold under the Schering name. It is unknown if any such products have been brought over to the new Bayer label. Aside from this, a very small number of pharmaceutical preparations containing methenolone acetate may still be in production.
How is Primobolan Supplied
All forms of Schering Primobolan contain 5 mg, 25 mg, or 50 mg (no longer available) of methenolone acetate per tablet. Composition and dosage of other brands may vary by country and manufacturer.
Structural Characteristics of Primobolan
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 protects the steroid against hepatic metabolism. Primobolan makes use of methenolone with a carboxylic acid ester (acetic acid) attached to the 17-beta hydroxyl group to further help protect it from oxidation during oral administration. Studies have demonstrated the methenolone is an effective oral anabolic agent in both the acetate and unesterified forms.
Primobolan Side Effects (Estrogenic)
Methenolone is not aromatized by the body, and is not measurably estrogenic. Estrogenlinked side effects should not be seen when administering this steroid. Sensitive individuals need not worry about developing gynecomastia, nor should they be noticing any appreciable water retention with this drug. The increase seen with methenolone should be quality muscle mass, not the smooth bulk that often accompanies steroids open to aromatization. During a cycle, the user should additionally not notice strong elevations in blood pressure, as this effect is also related (generally) to estrogen and water retention. Methenolone is a steroid most favored during cutting phases of training, when water and fat retention are major concerns, and sheer mass not the central objective.
Primobolan Side Effects (Androgenic)
Although classified as an anabolic steroid, androgenic side effects are still possible 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 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. Methenolone is still a very mild steroid, however, and strong androgenic side effects are typically related to higher doses. Women often find this preparation an acceptable choice, observing it to be a very comfortable and effective anabolic.
Primobolan Side Effects (Hepatotoxicity)
Methenolone is not considered a hepatotoxic steroid; liver toxicity is unlikely. Studies have failed to produce appreciable changes in markers of hepatic stress when the drug was given in therapeutic levels. This steroid does have some resistance to hepatic breakdown, however, and liver toxicity, failure, and death was reported in one elderly patient receiving oral methenolone acetate. Although unlikely, hepatotoxicity cannot be completely excluded, especially with very high oral doses.
Primobolan 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. Methenolone should have a stronger negative effect on the hepatic management of cholesterol than testosterone or nandrolone due to its non-aromatizable nature, but a much weaker impact than c-17 alpha alkylated steroids. Due to the route of delivery, oral methenolone will have a slightly stronger negative effect on lipids compared to methenolone enanthate injections. 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.
Primobolan 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. Primobolan is generally described as having a low impact on endogenous testosterone production. While this may be true in small clinical doses (20-25 mg daily), this may not be a major distinction when used for physique- or performance-enhancing purposes. In one study, more than half of the patients receiving only 30-45 mg per day noticed a 15-65% suppression of gonadotropin levels. While this is far from having no hormonal impact, the suppression caused by methenolone acetate may still be less pronounced than with many other agents. If Primobolan is used at moderate doses for less than 8 weeks, hormonal recovery should not be a protracted experience.
Primobolan Administration (General)
Studies have shown that taking an oral anabolic steroid with food may decrease its bioavailability. This is caused by the fat-soluble nature of steroid hormones, which can allow some of the drug to dissolve with undigested dietary fat, reducing its absorption from the gastrointestinal tract. For maximum utilization, this steroid should be taken on an empty stomach.
Primobolan Administration (Men)
The prescribing guidelines for Primobolan recommend a maximum daily dosage of 100- 150 mg per day. The usual administration protocols for physique- or performance-enhancing purposes call for 75-150 mg daily, which is taken for 6 to 8 weeks. This level is sufficient to impart a measurable anabolic effect, although one usually doesn’t expect to achieve great gains in muscle mass with this drug. Instead, Primobolan is utilized when the athlete has a specific need for a mild anabolic agent, most notably in cutting phases of training.
Due to its mild nature, Primobolan is often used in conjunction with other steroids for a stronger effect. In such cases, a slightly lower dose is often used (50-100 mg per day). During a dieting or cutting phase, thought to be its primary application, a non-aromatizing androgen like Halotestin or trenbolone is often added. Such combinations would enhance the physique without water retention, and help bring out a harder and more defined look of muscularity. Non-aromatizing androgen/anabolic stacks like this are very popular among competing bodybuilders, and prove quite reliable for rapidly improving the contest form. This compound is also occasionally used with more potent androgens during bulking phases of training. The addition of testosterone, Dianabol or Anadrol 50 is common, although the gains are often accompanied by some level of smoothness due to the added estrogenic component, as well as hepatotoxicity in the case of the latter two agents.
Primobolan Administration (Women)
The prescribing guidelines for Primobolan do not offer separate dosing recommendations for women, although it is indicated that women who are pregnant, or may become pregnant, should not use the drug. Female athletes generally respond well to 50-75 mg daily, with no signs of virilization symptoms. One would not expect a tremendous amount of muscle mass with this drug, and instead find a slow and steady (quality) increase. Some women choose to further add-in other anabolics such as Winstrol or oxandrolone, in an effort to increase the muscle-building effectiveness of a cycle. While both of these compounds are quite tolerable, one must be sure not to use too high an accumulated dosage. Taken at too high a dosage, these weak anabolics can quickly cause masculinizing side effects.
Pharmaceutical preparations containing methenolone acetate remain scarce. The drug has been unavailable in western nations for many years now, and the bulk of the supply presently comes from underground steroid manufacturers. In reviewing some of the remaining products and changes in the global pharmaceutical market, we have made the following observations.
Balkan Pharmaceuticals produces Primobol in Moldova. It comes in 50 mg tablets, with 20 sealed in each foil and plastic strip.
Primobolan Tabs is produced by Swiss Remedies and available across Europe. Due to numerous fakes of this product, Swiss Remedies offers a convenient online product checker.
Magnus Pharmaceuticals makes the product Primobolan Tabs primarily for the EU and UK markets. Due to fake products appearing on the market, Magnus offers an online checker that lets steroid users verify their product originality.
Primobolan tablets are a moderately anabolic and low androgenic oral steroid that was reported as limited in use by most bodybuilders. This was likely simply because alone and when it was administered in listed dosages the drug was not very effective. However, gains were made in muscle mass and strength were consistently reported to be of a very high quality and were mostly retained post-cycle. Acetates are "said" to aid in fat burning, so this drug was mostly used in a stack pre-contest.
The problem in effectiveness lies in the fact that PRIMOBOLAN ACETATE is not a c17-ALFA-ALKYLATED steroid and is therefore mostly deactivated during the first pass through the liver. As the reader is aware, oral AAS are commonly altered to decrease liver deactivation. The most common alteration is called a c-17 alfa-alkylated drug. This alteration makes the liver work over-time to deactivate it and is therefore said to be highly liver toxic. (But so are most oral birth control drugs) But another alteration in structure allows Primobolan orals to be somewhat resistant to liver deactivation. It is referred to as unsaturation in the 1-position.This alteration allows the compound to resist metabolic deactivation by significantly shifting the 17-Keto redox potential toward creation of active 17-beta hydroxyl AAS. The result is an active oral AAS that is not liver toxic except in very high dosages.
Some have recalled the injectable form of Primobolan acetate with great fondness for its supposed fat burning/lean mass building qualities. The vials contained only 20-mg of METHENOLONE ACETATE (MA) yet it was reported far more effective than 150- mg of the oral. A commonly reported method to obtain greater blood circulatory levels of the oral form was to mix 20-25-mg of the ground tables with either DMSO gel or a 50/50 solution of DMSO and water. Users then simply applied the mixture to their skin (especially in areas of stubborn fat deposits). 10-20% absorbed and passed directly into the blood stream thus avoiding first pass liver deactivation. This was done 1-5 times daily.
DMSO is a solvent that carries smaller molecule structures mixed with it directly through the skin. It is said to be found at some health food stores and chemical supply warehouses.
Another reported method was mixing ground Primobolan tabs with Vitamin-E oil. The users then ingested it orally. This caused a great deal of the active steroid to be absorbed through the lymph system like Andriol and therefore avoid first pass deactivation.
There is a great deal of research under way in the OTC supplement industry that employs a similar pharmacological solution to liver destruction of micronutrients.
Back to reported tablet use...
Primobolan tabs were reportedly used most by women and steroid novices because they do not aromatize or cause water retention. Women who utilized 50-100mg daily of this drug seldom noted virilizing side effects. Most report a distinct harder look and a 3-4 LB muscle mass gain in 6-8 weeks. Obviously many females also stacked Primobolan tabs with other drugs to heighten results. Males normally ingested 100-200 mg daily in 2-4 divided doses (due to short half-life 4-6 daily divided dosages were more effective at maintaining plasma concentrations of the active drug) and report fair gains. Stacked with more androgenic steroids such as testosterone, Parabolan, or even moderate androgenics such as Deca Durabolin or Equipoise, males made high quality muscle mass and strength gains with safer low side effect results.
Anabolic Steroid Guide reference
Primobolan is an almost pure anabolic with an extremely low an-drogenic component. The ratio of the anabolic to the androgenic effect is indeed very favorable but, since the overall anabolic effect is only moderately strong, Primobolan tablets have only a limited effect in building up muscle mass and strength. With Primobolan nei-ther fast weight gains nor explosive strength gains occur. Primobolan is therefore mostly taken over a prolonged period since it gives only a slow but also a high-quality muscle gain which mostly remains after use of the compound is discontinued. An effective daily dose observed in athletes is in the range of 50- 150 mg so that the 25 mg tablets are preferred to the 5 mg tablets. As for the recommended dose, the athlete obtains interesting information from the German package insert by Schering AG for their compound Primobolan S: "Unless otherwise prescribed the following guidelines apply: The dosage should be I - 1,5 mg per pound of body weight/day, that is 4-6 tablets for 100 pound of bodyweight." A bodybuilder weighing 100 kg should therefore take 200-300 mg daily which would corre-spond to a dosage of eight to twelve 25 mg tablets per day. We believe that this dosage is too high; however, this example shows that a fairly large dosage of the oral acetate form is necessary. The reason is that the Primobolan acetate tablets are not I 7-alpha alky-lated and, during the first pass in the liver, a large part of the substance is destroyed and thus deactivated leaving only a much smaller quantity of the substance to get into the blood.
If Primobolan is the only steroid that is taken, then with respect to strength and muscle buildup, it will usually lead to success in women and steroid novices. This, however, changes greatly when Primobolan is combined with steroids that are moderately too highly androgenic but which themselves do not aromatize or retain water. In such an environment the anabolic effect of Primobolan can develop to its optimum. Masteron, Parabolan, Equipoise, and Winstrol, are par-ticularly suitable. The effect can be optimized by the additional in-take of Oxandrolone. Steroid novices and the less advanced achieve a good strength and muscle gain by taking 50- 100 mg Primobolan S/day and 150 mg Winstrol Depot/week, without retaining water. Even competing athletes report good quality gains with continu-ously "harder" muscles when taking 150 mg Primobolan S/day and 50 mg Winstrol Depot every two days, as well as 76 mg of Parabolan every two days.
The main uses of the Primobolan tablets, however, are in the preparation for a competition and in use by women. Since the acetate form does not aromatize into estrogens and does not cause water retention, the use of Primobolan during competitions is widespread. Acetate tablets are special in that they actively help burn fat. The Primobolan acetate tablets, however, must never be taken as the only steroid during a diet since, due to its extremely low androgenic effect, significant losses in muscle and strength can occur and there is a risk of overtraining. The above mentioned common steroid combinations are extremely effective when combined with a suitable diet during the preparation for a competition. Due to the fact that the acetate tablets burn fat but, at the same time, that in large part they are already deactivated in the liver, it would be most efficient to apply the compound locally, bringing the substance directly into the blood through the skin in the areas with undesired fat deposits. At first this seems a little adventurous, but it is possible with the DMSO compound. Dimethyl sulfoxide (DMSO) is one of few substances which are fully absorbed through the skin and distributed through the body It is included in many ointments and gels which are used to treat sport injuries, contusions, swellings, and effusions in order to transport the casing substance through the skin. ln addi-tion, DMSO makes the skin permeable to other substances.
Finely grind up one 25 mg Primobolan tablet with the grip of a knife on your kitchen board, mix it with half a teaspoon of DMSO gel and then apply a thin layer to your skin. It is important that you only apply it; do not rub it in. One or two applications is usu-ally enough. Another way to avoid the liver and consequent destruction of the substance is to grind up the Primobolan tablets in a mortar and consume them together with heated vitamin E oil. The Primobolan/vitamin E mixture reaches the blood similar to Andriol that is the absorption occurs through the lymph system and the solution does not reach the liver through the portal vessel.
Since the Primobolan tablets are not I 7-alpha alkylated but have a I 7-beta hydroxy group they are almost non-toxic to the liver. in a high dosage, however, they can influence the liver values resulting in higher biliburin, GPT, GOT, and alkaline phosphatase. Primobolan generally does not cause any significant side effects since it does not aromatize, does not cause water retention, is not I 7-alpha alkylated, and is only slightly androgenic. Blood pressure, liver values, cholesterol level, HDL and LDL values usually remain unaffected, making Primobolan well-liked by health-conscious older athletes. Primo is often an "entry drug" for novice users and, due to its rare side effects, encourages many steroid users to switch to "harder" stuff such as Dianabol, Anadrol 50, and testosterone. Since Primobolan is a precursor of dihydrotestosterone it can accelerate hair loss if such a predisposition exists.
The availability of Primobolan Acetate tablets on the black market is quite poor both in Europe and the U.S. The price for one 25 mg tablet on the black market is about $2.
Newbies Research Guide reference
This is a derivative of dihydrotestosterone, which is very popular with bodybuilders. The drug is very low androgenic compound and it is not toxic to the liver. Primobolan will not aromatise, and it is one of very few steroids, which have proven to be effective on a low calorie diet. This is why so many pre-contest bodybuilders use it, including the best in the business. While using Primobolan, a lifter can shed fat and retain muscle better than with any other steroid. It will not result in massive weight or strength gains, but some like to use it on muscle building cycles, especially women. In fact a great number of women do use this drug, and for them it is one of very few steroids they should ever experiment with. Users report fair but high quality muscle gains with Primobolan. Side effects seldom result from its use, even in high dosages. The Acetate version of this drug is the most popular. Users say it has the most “kick” of all the Primobolans. Even though this product is an oil based injectable, it is very fast in and out of the system. Therefore shots are taken every other day, at an average dosage of 20 mg per shot half that for women. This drug’s major drawback is that the shots can be extremely painful for a lot of people. It seems there are a great number of people who are allergic to acetates. Once found abundantly on the U.S. black market, Primobolan Acetate is now very hard to find. It costs around $12 per ampule.
Wlliam Llewellyn (2011) - Anabolics
L. Rea (2002) - Chemical Muscle Enhancement Bodybuilders Desk Reference
Anabolic Steroid Guide
Newbies Research Guide