Drug profile from Big Cat...................
Characteristics:
Mesterolone is an orally active, 1-methylated DHT. Like Masteron, but then actually delivered in an oral fashion. DHT is the conversion product of testosterone at the 5-alpha-reductase enzyme, the result being a hormone that is 3 to 4 times as androgenic and is structurally incapable of forming estrogen. One would imagine then that mesterolone would be a perfect drug to enhance strength and add small but completely lean gains to the frame. Unfortunately there is a control mechanism for DHT in the human body. When levels get too high, the 3alpha hydroxysteroid dehydrogenase enzyme converts it to a mostly inactive compound known as 3-alpha (5-alpha-androstan-3alpha,17beta-diol), a prohormone if you will. It can equally convert back to DHT by way of the same enzyme when low levels of DHT are detected. But it means that unless one uses ridiculously high amounts, most of what is administered is quite useless at the height of the androgen receptor in muscle tissue and thus mesterolone is not particularly suited, if at all, to promote muscle hypertrophy.
Proviron has four distinct uses in the world of bodybuilding. The first being the result of its structure. It is 5-alpha reduced and not capable of forming estrogen, yet it nonetheless has a much higher affinity for the aromatase enzyme (which converts testosterone to estrogen) than testosterone does. That means in administering it with testosterone or another aromatizable compound, it prevents estrogen build-up because it binds to the aromatase enzyme very strongly, thereby preventing these steroids from interacting with it and forming estrogen. So Mesterolone use has the extreme benefit of reducing estrogenic side-effects and water retention noted with other steroids, and as such still help to provide mostly lean gains. Its also been suggested that it may actually downgrade the actual estrogen receptor making it doubly effective at reducing circulating estrogen levels.
The second use is in enhancing the potency of testosterone. Testosterone in the body at normal physiological levels is mostly inactive. As much as 97 or 98 percent of testosterone in that amount is bound to sex hormone binding globulin (SHBG) and albumin, two proteins. In such a form testosterone is mostly inactive. But as with the aromatase enzyme, DHT has a higher affinity for these proteins than testosterone does, so when administered simultaneously the mesterolone will attach to the SHBG and albumin, leaving larger amounts of free testosterone to mediate anabolic activities such as protein synthesis. Another way in which it helps to increase gains. Its also another part of the equation that makes it ineffective on its own, as binding to these proteins too, would render it a non-issue at the androgen receptor.
Thirdly, mesterolone is added in pre-contest phases to increase a distinct hardness and muscle density. Probably due to its reduction in circulating estrogen, perhaps due to the downregulating of the estrogen receptor in muscle tissue, it decreases the total water build-up of the body giving its user a much leaner look, and a visual effect of possessing "harder" muscles with more cuts and striations. Proviron is often used as a last-minute secret by a lot of bodybuilders and both actors and models have used it time and again to deliver top shape day in day out, when needed. Like the other methylated DHT compound, drostanolone, mesterolone is particularly potent in achieving this feat.
Lastly Proviron is used during a cycle of certain hormones such as nandrolone, with a distinct lack of androgenic nature, or perhaps 5-alpha reduced hormones that don't have the same affinities as DHT does. Such compounds, thinking of trenbolone, nandrolone and such in particular, have been known to decrease libido. Limiting the athlete to perform sexually being the logical result. DHT plays a key role in this process and is therefore administered in conjunction with such steroids to ease or relieve this annoying side-effect. Proviron is also commonly prescribed by doctors to people with low levels of testosterone, or patients with chronic impotence. Its not perceived as a powerful anabolic, but it gets the job done equally well if not better than other anabolic steroids making it a favorite in medical practices due to its lower chance of abuse.
Mesterolone is generally well liked nonetheless as it delivers very few side-effects in men. In high doses it can cause some virilization symptoms in women. But because of the high level of deactivation and pre-destination in the system (albumin, SHBG, 3bHSD, aromatase) quite a lot of it, if not all simply never reaches the androgen receptor where it would cause anabolic effects, but also side-effects. So its relatively safe. Doses between 25 and 250 mg per day are used with no adverse effects. 50 mg per day is usually sufficient to be effective in each of the four cases we mentioned up above, so going higher really isn't necessary. Unlike what some suggest or believe, its not advised that Proviron be used when not used in conjunction with another steroid, as it too is quite suppressive of natural testosterone, leading to all sorts of future complications upon discontinuation. Ranging from loss of libido or erectile dysfunction all the way up to infertility. One would not be aware of such dangers because Proviron fulfills most of the functions of normal levels of testosterone.
Stacking and Use:
Mesterolone is an oral alkylated steroid. If used primarily as an anti-aromatase drug, using it throughout a longer cycle (10-12 weeks) of injectables may elevate liver values a little bit, though much, much less than one would expect with a 17-alpha-alkylated steroid. Eventhough instead of inhibiting gains, mesterolone may actually contribute to gains. So that's a bit of a shame. Its not quite as toxic since its not alkylated in the same fashion, but at the 1 position, which reduces hepatic breakdown, but not like 17-alpha alkylation. The reason for the change of position I assume, is because alkylating at the 17-alpha position has been shown to reduce affinity for sex hormone binding proteins. This would in turn decrease its ability to free testosterone. Nonetheless the delivery rate is quite good. Its taken daily in 50-100 mg doses.
The best thing to stack it with is testosterone of course. Its most easily bound to SHBG and albumin, and deactivated for up to 98%. Since the DHT can compete for these structures with higher affinity it would naturally lead to a higher yield of whatever testosterone product you stacked it with. Since DHT levels are notably higher now there is also more stimulation of the androgen receptor causing more strength gains, and because of its affinity for aromatase the overall estrogen level decreases as well. This has as a result that gains are leaner, and once again the overall testosterone yield is increased as less I converted at the aromatase enzyme.
It's of course used in other stacks with products such as methandrostenolone, boldenone and nandrolone to reduce estrogenic activity and increase muscle hardness. The addition of proviron makes boldenone a dead lock for a cutting stack and for some may even make it possible to use nandrolone while cutting, although the use of Winstrol or a receptor antagonist in conjunction is wishful as well. The benefit of adding it to a nandrolone stack is that it may also help you reduce the decrease in libido suffered from nandrolone, since the latter is mostly deactivated by 5-alpha reductase, an enzyme that makes other hormones more androgenic.
Proviron is an anti-aromatase, so obviously anti-estrogens would be futile and redundant. Blood pressure medication for those prone to hypertension may be wise, as this DHT can increase the blood pressure.
[font=Verdana, Arial, Helvetica, sans-serif]Active Life: 8-12 hours (effects last about 24 hours)
Drug Class: Androgenic Steroid/Anti- Aromatization (Oral)
Average Dose: Men 25-100 mg/day.....Women 25-50 mg/day
Acne: Rare
Water Retention: No
High Blood Pressure: Rare
Liver Toxic: Low
Aromatization: None
DHT Conversion: No, it is a derivative of DHT
Decrease HPTA function: No
Proviron® is the Schering brand name for the oral androgen mesterolone (1 methyl-dihydrotestosterone). Just as with DHT, the activity of this steroid is that of a strong androgen which does not aromatize into estrogen. In clinical situations Proviron is generally used to treat various types of sexual dysfunction, which often result from a low endogenous testosterone level. It can usually reverse problems of sexual disinterest and impotency, and is sometimes used to increase the sperm count. The drug does not stimulate the body to produce testosterone, but is simply an oral androgen substitute that is used to compensate for a lack of the natural male androgen.
Although this steroid is strongly androgenic, the anabolic effect of it is considered too weak for muscle building purposes. This is due to the fact that Proviron is rapidly reduced to inactive metabolites in muscle tissue, a trait also characteristic of dihydrotestosterone. The belief that the weak anabolic nature of this compound indicated a tendency to block the androgen receptor in muscle tissue, thereby reducing the gains of other more potent muscle building steroids, should likewise not be taken seriously. In fact due to its extremely high affinity for plasma binding proteins such as SHBG, Proviron may actually work to increase the activity of other steroids by displacing a higher percentage into a free, unbound state. Among athletes Proviron is primarily used as an anti-estrogen. It is believed to act as an anti-aromatase in the body, preventing or slowing the conversion of steroids into estrogen. The result is somewhat comparable to Arimidex (though less profound), the drug acting to prevent the buildup of estrogen in the body. This is in direct contrast to Nolvadex, which only blocks the ability of estrogen to bind and activate receptors in certain tissues. The anti-aromatization effect is preferred, as it is a more direct and efficient means of dealing with the problem of estrogenic side effects. Another disadvantage of Nolvadex is that if discontinued too early, a rebound effect may occur as high serum estrogen levels are again free to take action. This of course could mean a rapid onset of side effects such as gynecomastia. Most actually prefer to use both Proviron and Nolvadex, especially during strongly estrogenic cycles. With each item attacking estrogen at a different angle, side effects are often greatly reduced.
The anti-estrogenic properties of Proviron are not unique to this compound. A number of steroids have in fact demonstrated similar activity. Dihydrotestosterone and Masteron (2methyl-dihydrotestosterone) for example have been successfully used as therapies for gynecomastia and breast cancer due to their strong anti-estrogenic effect. It has been suggested that nandrolone may even lower aromatase activity in peripheral tissues where it is more resistant to estrogen conversion (the most active site of nandrolone aromatization seems to be the liver). The anti-estrogenic effect of all of these compounds is presumably caused by their ability to compete with other substrates for binding to the aromatase enzyme. With the aromatase enzyme bound to the steroid, yet being unable to alter it, and inhibiting effect is achieved as it is temporarily blocked from interacting with other hormones.
This drug is also favored by many during contest preparations, when a lower estrogen/high androgen level is particularly sought after. This is especially beneficial when anabolics like Winstrol, oxandrolone and Primobolan are being used alone, as the androgenic content of these drugs is relatively low. Proviron can supplement a well needed androgen, and bring about an increase in the hardness and density of the muscles. Women in particular find a single 25mg tablet will efficiently shift the androgen/estrogen ratio, and can have a great impact on the physique. Since this is such a strong androgen however, extreme caution should be taken with administration. Higher dosages clearly have the potential to cause virilization symptoms quite readily. For this reason females will rarely take more than one tablet per day, and limit the length of intake to no longer than four or five weeks. One tablet used in conjunction with 10 or 20mg of Nolvadex can be even more efficient for muscle hardening, creating an environment where the body is much more inclined to burn off extra body fat (especially in female trouble areas like the hips and thighs).
The typical dosage for men is one to four 25 mg per tablets per day. This is a sufficient amount to prevent gynecomastia, the drug is often used throughout the entire cycle. As mentioned earlier, it is often combined with Nolvadex (tamoxifen citrate) or Clomid (clomiphene citrate) when heavily estrogenic steroids are being taken (Dianabol, testosterone etc.). Administering 50mg of Proviron and 20mg Nolvadex daily has proven extremely effective in such instances, and it is quite uncommon for higher dosages to be required. And just as we discussed for women, the androgenic nature of this compound is greatly welcome during contest preparation. Here again Proviron should noticeably benefit the hardness and density of the muscle, while at the same time increasing the tendency to burn off a greater amount of body fat. Proviron is usually well tolerated and side effects (men) are rare with dosages under 100 mg per day. Above this, one may develop an excessively high androgen level and encounter some problems. Typical androgenic side effects include oily skin, acne, body/facial hair growth and exacerbation of a male pattern baldness condition, and may occur even with the use of a moderate dosage. With the strong effect DHT has on the reproductive system, androgenic actions may also include an extreme heightening of male libido. And as discussed earlier, Women should be careful around Proviron. It is an androgen, and as such has the potential to produce virilization symptoms quite readily. This includes, of course, a deepening of the voice, menstrual irregularities, changes in skin texture and clitoral enlargement.
Proviron is also not a c17 alpha alkylated compound, an alteration commonly used with oral anabolic/androgenic steroids. Not using this structure in the case of Proviron removes the notable risk of liver toxicity we normally associate with oral drugs. It is therefore considered a "safe" oral, the user having no need to worry about serious complications with use. This steroid in fact utilizes the same 1-methylation we see present on Primobolan (methenolone), another well tolerated orally active compound. Alkylation at the one position also slows metabolism of the steroid during the first pass, although much less profoundly than 17 alpha alkylation. Likewise Proviron and Primobolan are resistant enough to breakdown to allow therapeutically beneficial blood levels to be achieved, although the overall bioavailability of these compounds is still much lower than methylated oral steroids.
The popularity of Proviron amongst bodybuilders has been increasing in recent years. Many experienced bodybuilders have in fact come to swear by it, incorporating it effectively in most markedly estrogenic cycles. Due to high demand Proviron is now very easy to obtain on the black market. Most versions will be manufactured by Schering, and should cost about $1-$2 per 25 mg tab. This drug is packaged in both push-through strips and small glass vials, so do not let this alarm you. There is currently no need to worry about authenticity with this drug, as no counterfeits are known to exist. If money and availability does not prevent it, Arimidex, Femara, or Aromasin ares actually a much better choice than Proviron though. These drugs were designed specifically as an anti-aromatase, and works much more effectively than anything else we have available.
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Active Life: 8-12 hours (effects last about 24 hours)
Drug Class: Androgenic Steroid/Anti- Aromatization (Oral)
Average Dose: Men 25-100 mg/day.....Women 25-50 mg/day
Acne: Rare
Water Retention: No
High Blood Pressure: Rare
Liver Toxic: Low
Aromatization: None
DHT Conversion: No, it is a derivative of DHT
Decrease HPTA function: No
Proviron® is the Schering brand name for the oral androgen mesterolone (1 methyl-dihydrotestosterone). Just as with DHT, the activity of this steroid is that of a strong androgen which does not aromatize into estrogen. In clinical situations Proviron is generally used to treat various types of sexual dysfunction, which often result from a low endogenous testosterone level. It can usually reverse problems of sexual disinterest and impotency, and is sometimes used to increase the sperm count. The drug does not stimulate the body to produce testosterone, but is simply an oral androgen substitute that is used to compensate for a lack of the natural male androgen.
Although this steroid is strongly androgenic, the anabolic effect of it is considered too weak for muscle building purposes. This is due to the fact that Proviron is rapidly reduced to inactive metabolites in muscle tissue, a trait also characteristic of dihydrotestosterone. The belief that the weak anabolic nature of this compound indicated a tendency to block the androgen receptor in muscle tissue, thereby reducing the gains of other more potent muscle building steroids, should likewise not be taken seriously. In fact due to its extremely high affinity for plasma binding proteins such as SHBG, Proviron may actually work to increase the activity of other steroids by displacing a higher percentage into a free, unbound state. Among athletes Proviron is primarily used as an anti-estrogen. It is believed to act as an anti-aromatase in the body, preventing or slowing the conversion of steroids into estrogen. The result is somewhat comparable to Arimidex (though less profound), the drug acting to prevent the buildup of estrogen in the body. This is in direct contrast to Nolvadex, which only blocks the ability of estrogen to bind and activate receptors in certain tissues. The anti-aromatization effect is preferred, as it is a more direct and efficient means of dealing with the problem of estrogenic side effects. Another disadvantage of Nolvadex is that if discontinued too early, a rebound effect may occur as high serum estrogen levels are again free to take action. This of course could mean a rapid onset of side effects such as gynecomastia. Most actually prefer to use both Proviron and Nolvadex, especially during strongly estrogenic cycles. With each item attacking estrogen at a different angle, side effects are often greatly reduced.
The anti-estrogenic properties of Proviron are not unique to this compound. A number of steroids have in fact demonstrated similar activity. Dihydrotestosterone and Masteron (2methyl-dihydrotestosterone) for example have been successfully used as therapies for gynecomastia and breast cancer due to their strong anti-estrogenic effect. It has been suggested that nandrolone may even lower aromatase activity in peripheral tissues where it is more resistant to estrogen conversion (the most active site of nandrolone aromatization seems to be the liver). The anti-estrogenic effect of all of these compounds is presumably caused by their ability to compete with other substrates for binding to the aromatase enzyme. With the aromatase enzyme bound to the steroid, yet being unable to alter it, and inhibiting effect is achieved as it is temporarily blocked from interacting with other hormones.
This drug is also favored by many during contest preparations, when a lower estrogen/high androgen level is particularly sought after. This is especially beneficial when anabolics like Winstrol, oxandrolone and Primobolan are being used alone, as the androgenic content of these drugs is relatively low. Proviron can supplement a well needed androgen, and bring about an increase in the hardness and density of the muscles. Women in particular find a single 25mg tablet will efficiently shift the androgen/estrogen ratio, and can have a great impact on the physique. Since this is such a strong androgen however, extreme caution should be taken with administration. Higher dosages clearly have the potential to cause virilization symptoms quite readily. For this reason females will rarely take more than one tablet per day, and limit the length of intake to no longer than four or five weeks. One tablet used in conjunction with 10 or 20mg of Nolvadex can be even more efficient for muscle hardening, creating an environment where the body is much more inclined to burn off extra body fat (especially in female trouble areas like the hips and thighs).
The typical dosage for men is one to four 25 mg per tablets per day. This is a sufficient amount to prevent gynecomastia, the drug is often used throughout the entire cycle. As mentioned earlier, it is often combined with Nolvadex (tamoxifen citrate) or Clomid (clomiphene citrate) when heavily estrogenic steroids are being taken (Dianabol, testosterone etc.). Administering 50mg of Proviron and 20mg Nolvadex daily has proven extremely effective in such instances, and it is quite uncommon for higher dosages to be required. And just as we discussed for women, the androgenic nature of this compound is greatly welcome during contest preparation. Here again Proviron should noticeably benefit the hardness and density of the muscle, while at the same time increasing the tendency to burn off a greater amount of body fat. Proviron is usually well tolerated and side effects (men) are rare with dosages under 100 mg per day. Above this, one may develop an excessively high androgen level and encounter some problems. Typical androgenic side effects include oily skin, acne, body/facial hair growth and exacerbation of a male pattern baldness condition, and may occur even with the use of a moderate dosage. With the strong effect DHT has on the reproductive system, androgenic actions may also include an extreme heightening of male libido. And as discussed earlier, Women should be careful around Proviron. It is an androgen, and as such has the potential to produce virilization symptoms quite readily. This includes, of course, a deepening of the voice, menstrual irregularities, changes in skin texture and clitoral enlargement.
Proviron is also not a c17 alpha alkylated compound, an alteration commonly used with oral anabolic/androgenic steroids. Not using this structure in the case of Proviron removes the notable risk of liver toxicity we normally associate with oral drugs. It is therefore considered a "safe" oral, the user having no need to worry about serious complications with use. This steroid in fact utilizes the same 1-methylation we see present on Primobolan (methenolone), another well tolerated orally active compound. Alkylation at the one position also slows metabolism of the steroid during the first pass, although much less profoundly than 17 alpha alkylation. Likewise Proviron and Primobolan are resistant enough to breakdown to allow therapeutically beneficial blood levels to be achieved, although the overall bioavailability of these compounds is still much lower than methylated oral steroids.
The popularity of Proviron amongst bodybuilders has been increasing in recent years. Many experienced bodybuilders have in fact come to swear by it, incorporating it effectively in most markedly estrogenic cycles. Due to high demand Proviron is now very easy to obtain on the black market. Most versions will be manufactured by Schering, and should cost about $1-$2 per 25 mg tab. This drug is packaged in both push-through strips and small glass vials, so do not let this alarm you. There is currently no need to worry about authenticity with this drug, as no counterfeits are known to exist. If money and availability does not prevent it, Arimidex, Femara, or Aromasin ares actually a much better choice than Proviron though. These drugs were designed specifically as an anti-aromatase, and works much more effectively than anything else we have available.
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