Steroid Side Effects and How to Stop them - Part 1
This chapter, along with the chapter on the proper use of ancillary medications, are two of the most important chapters in this book. Why? Because AAS have side effects, and long-term use of AAS can have a profound effect on longevity and overall quality of life in later years if preventative measures are not taken. Having used steroids myself for over 10 years now, I have suffered through virtually ever side effect listed in this chapter, and have consequently educated myself on how to avoid them.
Regardless of your age, it’s important to always bear in mind that the use of AAS for the purposes of gaining an edge in sport can be an inherently unhealthy endeavor. There is a distinct difference between the doses of hormones or drugs that are used in slowing the aging process through hormone replacement therapy (hereafter referred to as HRT, please see the chapter on HRT by Dr. Ramon Scruggs for further clarification) and those that are used to enhance performance. If one is to properly use performance enhancing drugs, it is vital that they know the potential side effects of drugs they are using, know how to combat these side effects, and most importantly, actually implement the knowledge they have. Time and time again I’ve seen a bodybuilder develop gynecomastia (commonly referred to as “bitch tits” in the bodybuilding vernacular) despite the fact that the individual in question knew this was a possibility and also knew the preventative measures to take. One should not engage in the use of AAS or any other performance enhancing drug if the maintenance of proper health is not of primary concern.
Compounding the problem of treating the side effects of AAS is the hysteria surrounding their use in the first place. Many bodybuilders that use steroids find themselves to be social pariahs, muscular misfits if you will, and end up finding comfort in the company of others that engage in steroid use as well. Because a bodybuilder wears his sport, he’s branded a steroid user by many regardless of whether that’s the case or not. Often times, the shame one feels regarding their steroid use will cause them to suffer through the side effects associated with their use, rather than seeking competent medical help. Truth be told, it’s very difficult to find competent medical help to treat the side effects of steroids, as most doctors simply have no idea how to properly do so. More often than not, the physicians I worked with for most of my years on steroids were completely clueless as to how one might ameliorate the negative side effects of these drugs, and would simply tell me to “get off the steroids”. I say this not to dissuade those of you reading this from seeking out the advice of a doctor regarding the side effects of steroid use, just to prepare you for a probable response.
Most of the side effects related to steroids are cosmetic and will disappear when one discontinues their use. But those that aren’t are the most important to understand and treat as necessary. Most of these cannot be seen or felt, and all are related to issues of cardiovascular health. Steroids can adversely affect cholesterol levels, triglyceride levels, and hypertension, which over time can and will lead to an increase in heart disease. Always monitor your resting hear rate and blood pressure on a weekly basis when taking steroids and have your cholesterol and triglycerides checked every six months if you are using steroid consistently. These are not problems you can live with, ignore them and you may very well die much earlier than you would have otherwise. Ask yourself this question: “How much is every year of my life worth to me?” If you ignore the potential for an increased risk of heart disease when using anabolic steroids, you are essentially answering the question with, “Very little indeed.”
Before we begin a look at the actual side effects themselves and how to treat them, it’s important to note that not all AAS are created equal!! At times, for the sake of brevity, I will lump all AAS together, but the fact remains that some steroids will cause more negative side effects than others. One of the points of this book is to allow you to make that distinction, and walk away with the knowledge of how to use them as safely as possible. Below is a list of steroids most commonly associated with the side effects listed in this chapter:
Anadrol-50 (Oxymetholone)
Dianabol (Methandrostenolone)
Halotestin (Fluoxymesterone)
Testosterone and its various esters
Unfortunately for us, these also happen to be most of THE most effective AAS (with the exception of Halotestin) for building LBM. Generally, the maxim that the more effective a steroid is the more side effects it has holds true.
Finally, before we begin, readers will notice that I do not advocate the use of estrogen blockers such as Nolvadex, Clomid (I do post cycle, but not for the purposes of estrogen suppression), or Proviron. With anti-aromatases like arimidex (anastrazole), femara (letrozole), and to a lesser extent Cytadren (aminoglutethiamide) becoming cheaper and more readily available, use of estrogen blockers should be relegated to the bodybuilding archives. For a complete explanation as to why, read the chapter Proper Use of Ancillary Medications Both On and Off Cycle.
AAS Side Effects
Acne: One of the primary indicators of steroid use is acne, and I’m sure many of you reading this have either experienced acne caused by steroids or have seen someone who has. Like all steroid side effects, the degree to which someone will suffer from acne varies from individual to individual. The more androgenic a compound is, the more profound effect it will have on increasing oil production in the skin via stimulation of the sebaceous glands. Having said that, I’ve seen individuals use incredibly androgenic stacks and never have a hint or a pimple or blemish, and I’ve seen athletes (especially women) use very mild anabolics and suffer from horrible acne.
Treating acne is very important, both for physical and psychological reasons. Untreated acne can cause permanent scarring of the skin if it becomes severe enough, resulting in a pockmarked area that can only be smoothed through expensive plastic surgery. And acne can have a very powerful negative psychological effect on someone suffering from it, branding someone a steroid user and further isolating them from “normal” society. Severe acne can and will detract from the most aesthetic of physiques, and take away from ones overall presentation.
Depending on the severity, there are several options for the treatment of acne. Since acne is generally caused by the more androgenic steroids, there is always the option of switching to steroids that have few androgenic properties, such as nandrolone, oxandrolone, or primobolan. Light cases can commonly be controlled through frequent washings of the effected area (to remove excess dirt and oil before pores become clogged and infected) and the use of over the counter topical treatments. Moderate cases will generally respond to the use of Retin-A coupled with use of an antibiotic (such as tetracycline) which kills the bacteria which feeds off the oil created by the sebaceous gland. Severe cases of acne should be treated with Accutane, a prescription drug manufactured by Roche that is very effective at permanently eliminating acne. Accutane has a host of unpleasant side effects itself, and treatments are both lengthy and costly (health insurance is a must), but its use is much better than the possibility of permanent scarring from cystic acne. Fortunately, while acne is one of the most commonly seen side effects, it’s also the easiest to treat, as competent Dermatologists can easily be found.
It should also be noted that acne commonly become an issue for bodybuilders that do not cycle off steroids correctly, which will often cause a severe imbalance between levels of androgens and estrogens. Preparation for your off cycle period is equally important as the time spent on steroids, so use of an anti-aromatase both on and immediately following a cycle containing AAS that can convert to estrogen is a must.
Aggression: Men, due to their higher natural production of testosterone, are generally more aggressive than women. AAS, especially those that are extremely androgenic, will further increase aggression in both males and females. This can be beneficial as long as the individual in question can focus the aggression appropriately, such as the lifting of heavier weights during training. There often seems to be a direct correlation between ones ability to control aggression and ones intelligence.
There is nothing worse than an out of control steroid user who is unable or unwilling to control their aggression. Before beginning a cycle of AAS, especially one containing strong androgens, you must prepare yourself mentally for the fact that you are in all likelihood going to be more aggressive than normal, and consequently take the time to assess the nature of your reactions while using them.
Wednesday, May 30, 2007
Friday, May 25, 2007
Steroids charges evidence disputed
ALBANY -- A criminal case against an Orlando pharmacy accused of running a nationwide steroids distribution network is being hampered as defense attorneys in Florida ask an appellate court to seal critical wiretap evidence, while the pharmacists' New York attorneys demand its disclosure.
Meanwhile, defense attorneys for Signature Pharmacy contend Albany prosecutors may have violated Florida laws when they showed certain evidence -- hundreds of pages of sealed wiretap transcripts taken by an Orlando task force -- to an Albany County grand jury that handed up indictments against numerous pharmacists, doctors and so-called "wellness center" operators.
The wiretap transcripts were under seal at the time.
But Anne Wedge-McMillan, an attorney with Florida's Office of Statewide Prosecution, argued in a Kissimmee court last Friday that her office was "fully and legally entitled" to share the wiretaps with Albany prosecutors for use in the grand jury proceedings. She called the conflicting motions by Signature's attorneys "mind-boggling."
She told a Florida judge the legal tug-of-war is calculated with the hopes that an Albany judge "will get frustrated and dismiss the Albany case."
Still, defense attorneys say the multi-jurisdictional case is in jeopardy and that Albany County prosecutors may have made serious missteps.
"This was a classic case of the consequences of a rush to judgment," said E. Stewart Jones, a Troy attorney whose firm represents two executives at Signature Pharmacy in Orlando. "That office had material that they shouldn't have had and they unsealed it before a grand jury when they had no authority."
Albany prosecutors dispute that opinion and are suggesting the pharmacy's attorneys may be plotting to scuttle their case on technical grounds by making conflicting arguments in separate states.
"The defense is basically trying to hide the ball until the clock runs out. I think the courts will see through that," said Albany County Assistant District Attorney Christopher Baynes. "Either they're not communicating or some of these arguments are being made in bad faith."
Defense attorneys in the case have countered that the interests of the pharmacy and its executives, who face criminal charges individually, are separate and that there has been no collusion on their part.
The face-off is unfolding in an Orlando-area court. The issue appeared to be resolved last Friday when a Florida judge ruled that Albany County prosecutors may have unfettered access to the wiretap transcripts, including turning them over to defense attorneys here.
But attorneys for Signature Pharmacy, which is owned by husband-and-wife pharmacists Stan and Naomi Loomis, filed an emergency appeal on Monday seeking to undo the Florida judge's ruling.
Their appeal was filed as Albany County Judge Stephen W. Herrick has ordered that Albany prosecutors turn over the wiretap transcripts to defense attorneys here. Herrick's order called for the materials to be turned over by last week. It's not clear what the delay could mean to the criminal cases here, although Herrick has the power to dismiss the indictments.
Meanwhile, defense attorneys for Signature Pharmacy contend Albany prosecutors may have violated Florida laws when they showed certain evidence -- hundreds of pages of sealed wiretap transcripts taken by an Orlando task force -- to an Albany County grand jury that handed up indictments against numerous pharmacists, doctors and so-called "wellness center" operators.
The wiretap transcripts were under seal at the time.
But Anne Wedge-McMillan, an attorney with Florida's Office of Statewide Prosecution, argued in a Kissimmee court last Friday that her office was "fully and legally entitled" to share the wiretaps with Albany prosecutors for use in the grand jury proceedings. She called the conflicting motions by Signature's attorneys "mind-boggling."
She told a Florida judge the legal tug-of-war is calculated with the hopes that an Albany judge "will get frustrated and dismiss the Albany case."
Still, defense attorneys say the multi-jurisdictional case is in jeopardy and that Albany County prosecutors may have made serious missteps.
"This was a classic case of the consequences of a rush to judgment," said E. Stewart Jones, a Troy attorney whose firm represents two executives at Signature Pharmacy in Orlando. "That office had material that they shouldn't have had and they unsealed it before a grand jury when they had no authority."
Albany prosecutors dispute that opinion and are suggesting the pharmacy's attorneys may be plotting to scuttle their case on technical grounds by making conflicting arguments in separate states.
"The defense is basically trying to hide the ball until the clock runs out. I think the courts will see through that," said Albany County Assistant District Attorney Christopher Baynes. "Either they're not communicating or some of these arguments are being made in bad faith."
Defense attorneys in the case have countered that the interests of the pharmacy and its executives, who face criminal charges individually, are separate and that there has been no collusion on their part.
The face-off is unfolding in an Orlando-area court. The issue appeared to be resolved last Friday when a Florida judge ruled that Albany County prosecutors may have unfettered access to the wiretap transcripts, including turning them over to defense attorneys here.
But attorneys for Signature Pharmacy, which is owned by husband-and-wife pharmacists Stan and Naomi Loomis, filed an emergency appeal on Monday seeking to undo the Florida judge's ruling.
Their appeal was filed as Albany County Judge Stephen W. Herrick has ordered that Albany prosecutors turn over the wiretap transcripts to defense attorneys here. Herrick's order called for the materials to be turned over by last week. It's not clear what the delay could mean to the criminal cases here, although Herrick has the power to dismiss the indictments.
Tuesday, May 22, 2007
Nolva vs. Clomid for PCT
Nolva vs. Clomid for PCT
It seems like everyday questions concerning PCT pop up, and weather one should use either Clomid or nolva or a combo of both. I hope that this article written by BigCat may help to clear up some misconceptions.
While practically similar compounds in structure, few people ever really consider Clomid and nolva to be similar. Its not just a common myth in steroid circles, but even in the medical community. This misconception originates from their completely different uses. Nolvadex is most commonly used for the treatment of breast cancer in women, while Clomid is generally considered a fertility aid. In bodybuilding circles, from day one, Clomid has generally been used as post-cycle therapy and Nolvadex as an anti-estrogen.
But as I intend to demonstrate this is in essence the same. I believe the myth to have originated because nolva is clearly a more powerful anti-estrogen, and the people selling Clomid needed another angle to sell the stuff, so it was mostly used as a post-cycle aid. But few users really understand how Clomid (and also Nolvadex, logically) works to bring back natural testosterone in the body after the conclusion of a cycle of androgenic anabolic steroids. After a cycle is over, the level of androgens in the body drop drastically. The body compensates with an overproduction of estrogen to keep steroid levels up. Estrogen as well inhibits the production of natural testosterone, and in the period between the return of natural testosterone and the end of a cycle, a lot of mass is lost. So its in everybody's best interest to bring back natural test as soon as humanly possible. Clomid and Nolvadex will reduce the post-cycle estrogen, so that a steroid deficiency is constated and the hypothalamus is stimulated to regenerate natural testosterone production in the body. That's basically how the mechanism works, nothing more, nothing less.
Both compounds are structurally alike, classified as triphenylethylenes. Nolvadex is clearly the stronger component of the two as it can achieve better results in decreasing overall estrogen with 20-40 mg a day, than Clomid can in doses of 100-150 mg a day. A noteworthy difference. Triphenylethylenes are very mild estrogens that do not exert a lot, if any activity at the estrogen receptor, but are still highly attracted to it. As such they will occupy the receptor and keep it from binding estrogens. This means they do not actively work to reduce estrogen in the body like Proviron, Viratase or arimidex would (by competing for the aromatase enzyme), but that it blocks the receptor so that any estrogen in the body is basically inert, because it has no receptor to bind to.
This has advantages and disadvantages. The disadvantage is that when use is discontinued, the estrogen level is still the same and new problems will develop much sooner. The advantage is that it works much faster and has results sooner than with an aromatase blocker like Proviron or arimidex. Therefor, when problems such as gynocomastia occur during a cycle of steroids one will usually start 20 mg/day of nolva or 100 mg/day of Clomid straight away, in conjunction with some Proviron or arimidex. The proviron or arimidex will actively reduce estrogen while the Clomid or Nolvadex will solve your ongoing problem straight away. This way, when use is discontinued there is no immediate rebound.
So which one should you use? Well personally, I'd have to say Nolvadex. Both as an on-cycle anti-estrogen and a post-cycle therapy. As an anti-estrogen its simply much stronger, demonstrated by the fact that better results are obtained with 20-40 mg than with 100-150 mg of Clomid. For post-cycle, this plays a key role as well. It deactivates rebound estrogen much faster and more effective. But most importantly, Nolvadex has a direct influence on bringing back natural testosterone, where as Clomid may actually have a slight negative influence. The reason being that tamoxifen (as in Nolvadex) seems to increase the responsiveness of LH (luteinizing hormone) to GnRH (gonadtropin releasing hormone), whereas Clomid seems to decrease the responsiveness a bit1.
Another noteworthy fact about Nolvadex is that it acts more potently as an estrogen in the liver. As you remember, I mentioned that clomiphene and tamoxifen are basically weak estrogens. Well, tamoxifen is apparently still quite potent in the liver. This offers us the positive benefits of this hormone in the liver, while avoiding its negative effects elsewhere in the body. As such Nolvadex can have a very positive impact on negative cholesterol levels2 in the body, and therefore too should be considered a better choice than Clomid. It will not solve the problem of bad cholesterol levels during Steroid use, but will help to contain the problem to a larger degree.
Another reason why I promote the use of Nolvadex over Clomid post-cycle (as if being 3-4 times stronger and having more of a direct effect on restoring natural test wasn't enough) is because it's a lot safer. Not just because it improves lipid profiles, but also because it simply doesn't have the intrinsic side-effects that Clomid has. Clomid causes more acne for sure, but that's mainly because you need to use a 3-4 times higher dose. But Clomid seems to also affect the eyesight. Long-term Clomid therapy causes irreversible changes in eyesight3 in users. Irreversible. For me that alone is reason enough to prefer Nolvadex.
Lastly, one should be aware that use of these compounds can reduce the gains made on steroids. Nolvadex more so than Clomid, simply because it is stronger. Estrogen is responsible for a number of anabolic factors such as increasing growth hormone output, upgrading the androgen receptor and improving glucose utilization. This is why aromatizing steroids like testosterone are still best suited for maximum muscle gain. When reducing the estrogen levels, we therefore reduce the potential gains being made. For this reason one may opt to try Clomid during a cycle instead of Nolvadex. Although I would imagine that the problem that needed solved would be of more concern, in which case nolva remains the weapon of choice. It's a plain fact that there is a high correlation between gains and side-effects. Either you go for maximum gains and tolerate the side-effects, or you reduce the side-effects, and with it the gains. That's life, nothing is free.
Stacking and Use:
If problems of Gynocomastia or other estrogen related symptoms tend to pop up during a cycle the use of 20-30 mg of Nolvadex or 100 mg of Clomid daily should easily contain the problem, and be used until a few days after the problem subsides. For best results and the least amount of problems upon cessation it is best stacked with proviron (50 mg) or arimidex (0.5 mg) for this duration as well. Its not advised that these products be ran concomitantly with the steroid for the entire duration of the stack, as this will reduce your gains. Instead cease the usage of anti-estrogens once the problem is contained, and should the problem resurface, simply recommence the use of the products in the same manner as described above.
Once a cycle of steroids is concluded one should always initiate a post-cycle therapy to help bring back natural testosterone as soon as possible. This will help you to retain the mass you gained. How this is done depends highly on the type of steroid used. If only orals were used, therapy should start immediately, even the last day of the stack. If short-acting esters or water-based injectables were used, therapy should commence within 4-7 days after last injection, and if long-acting esters were used then it should commence 1.5 to 2 weeks after the last injection was given. The length of the therapy will vary as well, from 3-5 weeks. The longer acting the product was, the longer therapy should be continued to make sure all suppressive factors are cleared before use of Clomid/Nolvadex is discontinued.
The questions you will hear from athletes over and over is if they can get legal steroids clomid and nolvadex, is it possible?well I say yes you just have to look.
For best results, it is best stacked with HCG (Human Chorionic gonadotrophin), which functions as an LH analog and can help bring testicle size back up. HCG use starts the last week of a cycle, and on from there every 5-6 days (usually 1500-3000 IU) and discontinued 1.5 to weeks prior to the cessation of Nolvadex/clomid. The reason being that HCG itself is also suppressive of natural testosterone and should be out of the body before therapy is over, or it will inhibit natural testicle function. But I can not stress enough that HCG possibly plays a more important role in post-cycle therapy than clomid/Nolvadex. For Clomid and Nolvadex, doses are usually tapered down. Its best to start with 40-50 mg of Nolvadex or 150 mg of Clomid for the first week or the first two weeks, and then finish the program with 20-25 mg of Nolvadex or 100 mg of Clomid for an additional two weeks.
References
1 Vermeulen A., Comhaire F., Hormonal effects of an anti-estrogen, tamoxifen, in normal and oligospermic men, Fertil. Ster. 29 (1978) 320-27
2 Bruning PF, Bronfer JMG, Hart AAM, Jong-Bakker M, tamoxifen, serum lipoproteins and cardiovascular risk, Br. J. Cancer 1988 Oct, 58 (4) 497-9
Thursday, May 17, 2007
How to Make Anabolic Steroids Orally-Active?
The subject of androgenic / anabolic steroids, and the different ways that have been found to make them orally active, has been tossed around lately on the internet mags. This is an interesting topic to the science minded out there, but beyond that, it also has potential utility to the prohormone supplements. The following is my take on the subject, including scientific references and conjecture on my part.
The problem with natural androgens
Testosterone is the primary androgen in the human, and is the golden standard by which all other steroids are compared. Unfortunately, testosterone has very poor activity when taken orally. This necessitates that testosterone be administered by extra-oral means such by injection, subcutaneous pellet implant, and transdermal gel or patch.
17alpha alkylated steroids
Scientists have developed several synthetic testosterone derivatives that have increased oral bioavailability. The first synthetic alteration that scientists utilized is known as 17 alpha alkylation. 17a alkylation involves the addition of an alkyl group (methyl or ethyl) to the alpha position of the 17 carbon of the steroid backbone. The alkylation at this position prevents the major route of androgen deactivaton – oxidation to a 17-keto steroid - from taking place. This allows a large part of the steroid to avoid liver first pass metabolic degradation. Examples of 17a alkylated steroids are methyltestosterone and Norethandrolone (Nilevar)
While 17a alkylation is a very effective means of rendering steroids orally active, it suffers from a serious drawback. These steroids are all to some extent toxic to the liver. Some are more toxic than others, but they all have been associated with this problem. Jaundice is not completely uncommon with the usage of this stuff, although this condition is generally confined to individuals who are predisposed to liver problems. Several cases of liver cancer have supposedly been linked to 17a alkylated steroids, however, nothing definitive has been established in this regard. On the other hand, it is somewhat common to observe increases in blood test indicators of liver stress such as BSP retention, and intrahepatic cholestasis (a condition where bile clogs up and stops flowing from the liver).
While the dangers of 17a alkylated steroids are not trivial, they still comprise some of the most potent anabolic agents available, and therefore their use continues. Most smart bodybuilders are aware of the potential toxicities of these steroids, and therefore they are judicious with their use of them.
Lipophilic steroid derivatives
After ingestion, most steroids make their way to the intestines where they are absorbed into the portal circulation. The portal circulation carries the steroid directly to the liver, which is the workhouse of destructive metabolism and inactivation of drugs. As a result, if the steroid is not protected in some way, very little will make it through the liver and into the rest of the body where it can do its magic.
In addition to the portal route, there is another route through which substances can be absorbed into the body from the intestine. If a substance is lipophilic (fat like) enough it will be absorbed in the same manner that dietary fat is. Dietary fat is incorportated into chylomicra, which are small fat globules composed of protein and fat. These chylomicra are absorbed into the lymphatic circulation, which by passes the liver. If you make a steroid lipophilic enough by altering its structure, then it too will incorportate into chylomicra and absorb into the lymphatic system. Once in the lymphatic system it can cross over into the general blood circulation, making it there without being subjected to the massive metabolic breakdown in the liver.
Scientists have found that by adding lipophilic side chains to steroids, they will to some extent be absorbed into the lymphatic system. If the side chain is linked on in such a way that it can hydrolyze (break apart) easily after being absorbed, the steroid is essentially rendered orally active. Two side chains that have been utilized to increase the oral bioavailability of steroids through increased lymphatic absorption are long chain alkyl ester groups, such as is seen with testosterone undecanoate (andriol), and enyl ether groups, such as is seen with quinbolone (anabolicum vaster).
The term "orally active" is of course a relative term. Lipophilically modified steroids are more orally active than the free parent steroids, however, they are no where near as active as the 17alpha-alkylated steroids. Testosterone undecanoate (TU) is probably the most commonly known lipophilically modified androgen, and it is not considered a very potent compound (its recommended daily dosage is about 240mg). In fact, one study found the oral administration of testosterone undecanoate led only to an absolute testosterone bioavailability of 6.83 +/- 3.32%. That is very slight, especially considering the fact that in the same study they found the bioavailability of straight testosterone to be 3.56 +/- 2.45% (Eur J Drug Metab Pharmacokinet 1986 Apr-Jun;11(2):145-9). That means TU is just a little less than twice as orally active as free testosterone, which is unimpressive to say the least.
The other problem with lipophilic steroid preparations is the high variability in absorption from one person to another. In other words, one guy might absorb the stuff very well while the other guy might absorb very little. There is also high variation within individuals themselves, depending on their gastrointestinal condition when they take the stuff. In another study, ten post-menopausal women were given 40 mg of TU and their peak blood values were recorded. The values varied widely - more than ten fold (range: 5.8-64.0 nmol/L) - amongst the subjects (J Clin Endocrinol Metab 1998 Nov;83(11): 3920-4).
There is no specific data I can find on the bioavailabilty of enyl ether compounds, but since their mode of action is identical to long chain alkyl ester compounds like TU, it is a fair assumption that they too are not outstandingly high in oral bioavailability, or in consistency of absorption. What I do know is that the one and only enyl ether oral steroid on the market today (quinbolone) is generally regarded by european bodybuilders / athletes as too weak to even bother taking.
Ring A modified steroids
There is one more class of anabolic / androgenic steroids that are orally active. These have unique structural modifications in the steroid A ring. What these modifications do is help preserve the steroids 17beta hydroxyl group, and minimize oxidation to the inactive 17-keto form.
Androgens such as testosterone exist in the body in an equilibrium between their active 17beta hydroxyl form and the inactive 17-keto form.
Normally, the equilibrium lies pretty far to the right (formation of inactive 17 keto steroid), however some steroids have certain modifications made in the A ring that alter this equilibrium by shifting it heavily to the left (towards the formation of active 17beta hydroxyl steroid).
The most common A-ring modifications that shift the 17beta hydroxyl / 17-keto equilibrium to the left are methylation at the 1alpha position, and unsaturation (double bond) in the 1(2) position (Acta Endocr, 41, (1962) 494). Examples of orally active steroids that contain one or more these modifications include methenolone (Primobolan), mesterolone (Proviron), and 1-testosterone.
You probably have heard of mesterolone and methenolone, but it is doubtful you have ever heard of 1-testosterone. 1-testosterone is a very interesting compound, not just because it is orally active but also because it is very anabolic. It has been reported to be over 7 times as anabolic as testosterone in a study funded by the pharmaceutical giant Searle (J Org Chem, 27 (1962) 248). Furthermore, being a 5alpha reduced steroid, it should not aromatize to estrogens.
The problem with natural androgens
Testosterone is the primary androgen in the human, and is the golden standard by which all other steroids are compared. Unfortunately, testosterone has very poor activity when taken orally. This necessitates that testosterone be administered by extra-oral means such by injection, subcutaneous pellet implant, and transdermal gel or patch.
17alpha alkylated steroids
Scientists have developed several synthetic testosterone derivatives that have increased oral bioavailability. The first synthetic alteration that scientists utilized is known as 17 alpha alkylation. 17a alkylation involves the addition of an alkyl group (methyl or ethyl) to the alpha position of the 17 carbon of the steroid backbone. The alkylation at this position prevents the major route of androgen deactivaton – oxidation to a 17-keto steroid - from taking place. This allows a large part of the steroid to avoid liver first pass metabolic degradation. Examples of 17a alkylated steroids are methyltestosterone and Norethandrolone (Nilevar)
While 17a alkylation is a very effective means of rendering steroids orally active, it suffers from a serious drawback. These steroids are all to some extent toxic to the liver. Some are more toxic than others, but they all have been associated with this problem. Jaundice is not completely uncommon with the usage of this stuff, although this condition is generally confined to individuals who are predisposed to liver problems. Several cases of liver cancer have supposedly been linked to 17a alkylated steroids, however, nothing definitive has been established in this regard. On the other hand, it is somewhat common to observe increases in blood test indicators of liver stress such as BSP retention, and intrahepatic cholestasis (a condition where bile clogs up and stops flowing from the liver).
While the dangers of 17a alkylated steroids are not trivial, they still comprise some of the most potent anabolic agents available, and therefore their use continues. Most smart bodybuilders are aware of the potential toxicities of these steroids, and therefore they are judicious with their use of them.
Lipophilic steroid derivatives
After ingestion, most steroids make their way to the intestines where they are absorbed into the portal circulation. The portal circulation carries the steroid directly to the liver, which is the workhouse of destructive metabolism and inactivation of drugs. As a result, if the steroid is not protected in some way, very little will make it through the liver and into the rest of the body where it can do its magic.
In addition to the portal route, there is another route through which substances can be absorbed into the body from the intestine. If a substance is lipophilic (fat like) enough it will be absorbed in the same manner that dietary fat is. Dietary fat is incorportated into chylomicra, which are small fat globules composed of protein and fat. These chylomicra are absorbed into the lymphatic circulation, which by passes the liver. If you make a steroid lipophilic enough by altering its structure, then it too will incorportate into chylomicra and absorb into the lymphatic system. Once in the lymphatic system it can cross over into the general blood circulation, making it there without being subjected to the massive metabolic breakdown in the liver.
Scientists have found that by adding lipophilic side chains to steroids, they will to some extent be absorbed into the lymphatic system. If the side chain is linked on in such a way that it can hydrolyze (break apart) easily after being absorbed, the steroid is essentially rendered orally active. Two side chains that have been utilized to increase the oral bioavailability of steroids through increased lymphatic absorption are long chain alkyl ester groups, such as is seen with testosterone undecanoate (andriol), and enyl ether groups, such as is seen with quinbolone (anabolicum vaster).
The term "orally active" is of course a relative term. Lipophilically modified steroids are more orally active than the free parent steroids, however, they are no where near as active as the 17alpha-alkylated steroids. Testosterone undecanoate (TU) is probably the most commonly known lipophilically modified androgen, and it is not considered a very potent compound (its recommended daily dosage is about 240mg). In fact, one study found the oral administration of testosterone undecanoate led only to an absolute testosterone bioavailability of 6.83 +/- 3.32%. That is very slight, especially considering the fact that in the same study they found the bioavailability of straight testosterone to be 3.56 +/- 2.45% (Eur J Drug Metab Pharmacokinet 1986 Apr-Jun;11(2):145-9). That means TU is just a little less than twice as orally active as free testosterone, which is unimpressive to say the least.
The other problem with lipophilic steroid preparations is the high variability in absorption from one person to another. In other words, one guy might absorb the stuff very well while the other guy might absorb very little. There is also high variation within individuals themselves, depending on their gastrointestinal condition when they take the stuff. In another study, ten post-menopausal women were given 40 mg of TU and their peak blood values were recorded. The values varied widely - more than ten fold (range: 5.8-64.0 nmol/L) - amongst the subjects (J Clin Endocrinol Metab 1998 Nov;83(11): 3920-4).
There is no specific data I can find on the bioavailabilty of enyl ether compounds, but since their mode of action is identical to long chain alkyl ester compounds like TU, it is a fair assumption that they too are not outstandingly high in oral bioavailability, or in consistency of absorption. What I do know is that the one and only enyl ether oral steroid on the market today (quinbolone) is generally regarded by european bodybuilders / athletes as too weak to even bother taking.
Ring A modified steroids
There is one more class of anabolic / androgenic steroids that are orally active. These have unique structural modifications in the steroid A ring. What these modifications do is help preserve the steroids 17beta hydroxyl group, and minimize oxidation to the inactive 17-keto form.
Androgens such as testosterone exist in the body in an equilibrium between their active 17beta hydroxyl form and the inactive 17-keto form.
Normally, the equilibrium lies pretty far to the right (formation of inactive 17 keto steroid), however some steroids have certain modifications made in the A ring that alter this equilibrium by shifting it heavily to the left (towards the formation of active 17beta hydroxyl steroid).
The most common A-ring modifications that shift the 17beta hydroxyl / 17-keto equilibrium to the left are methylation at the 1alpha position, and unsaturation (double bond) in the 1(2) position (Acta Endocr, 41, (1962) 494). Examples of orally active steroids that contain one or more these modifications include methenolone (Primobolan), mesterolone (Proviron), and 1-testosterone.
You probably have heard of mesterolone and methenolone, but it is doubtful you have ever heard of 1-testosterone. 1-testosterone is a very interesting compound, not just because it is orally active but also because it is very anabolic. It has been reported to be over 7 times as anabolic as testosterone in a study funded by the pharmaceutical giant Searle (J Org Chem, 27 (1962) 248). Furthermore, being a 5alpha reduced steroid, it should not aromatize to estrogens.
Sunday, May 13, 2007
Sustanon 250
Sustanon 250
(testosterone)
This product was developed by Organon as an ideal HRT (Hormone Replacement Therapy) solution, and it was thought at the time that the different esters would be able to provide a constant release of Testosterone over a months time. Sustanon is a blend of different estered testosterones (4 of them): testosterone propionate - 30 mg, testosterone phenylpropionate - 60 mg, testosterone isocaproate - 60mg, and testosterone decanoate -100 mg.
This drug was highly sought after as a "superior" version of testosterone in the late 80´s and through the mid 90´s. No doubt this is partly due to the very nice write-up Dan Duchaine gave it in his newsletters. However, lets keep in mind that this drug was designed for convenience, not athletics or bodybuilding. The advantage to this drug, according to the manufacturer, is that it can be injected once a month, and the different esters would provide different timed releases over that month, and the patient would therefore only need to visit the doctor once a month for his shot. For athletes or bodybuilders (who routinely use between half a gram and a gram of testosterone per week), this product is really no better than any other form of injectable testosterone.
Lately, it seems that this product has fallen out of favor with Steroid.com members, as many feel that the inclusion of the Propionate and phenylpropionate estered forms of testosterone in this blend would necessitate shooting every other day. This stems from the fact that testosterone propionate would be shot every other day at least, and testosterone phenylpropionate would generally be shot every third day.
Sustanon will do exactly what other forms of testosterone will do:
Testosterone will cause both muscle growth as well as fat loss. It sends a message to muscle cells to store more contractile protein (called actin and myosin), thus making your muscles grow. It also protects your muscles from catabolic (muscle wasting) glucocorticoid hormones(1). Thus it is often said that testosterone is not only anabolic, but it is strongly catabolic. Not only does it cause an increase in size of the muscle fibres (hyperfascia) but it also can change the appearance and the actual number of muscle fibres (Hyperplasia)(2). Testosterone has the ability to increase erythropoiesis (red blood cell production) in your kidneys(4), and a higher Red Blood Cell (RBC) count may improve endurance by producing more highly oxygenated blood. More RBCs can also improve recovery from strenuous physical activity. Agression levels often rise dramatically with the use of any exogenous testosterone (3). Testosterone improves muscle contraction by increasing the number of motor neutrons in muscle(5) and improves neuromuscular transmission(6). It also promotes glycogen synthesis(7)
And, since Sustanon is simply a form of (well actually 4 forms of) testosterone, we also know that administration of this compound will produce a dose respondant curve. (10)A what? Yeah...basically a "dose respondant curve" is the fancy way of saying "the more you take, the bigger you get..."
This is true of Sustanon as well as for every form of testosterone, up to a point.
Unfortunately, Sustanon will also do all of the bad things that any form of testosterone is known for:
It will convert to the female hormone estrogen (via a mechanism known as aromatization) by the (you guessed it) aromatize enzyme. Excessive estrogen can lead to unwanted side effects, such as acne, the growth of breast tissue (gynecomastia), fat gain and reduced fat breakdown, loss of sex drive, testicular shrinkage and water retention. Water retention can increase blood pressure weakening blood vessels over time. Unfortunately, this isn´t all it does& it can also interact with the 5 alpha-reductase enzyme. This interaction converts the testosterone to Dihydro-testosterone (DHT), a more androgenic form of the parent hormone. DHT has a high binding affinity to the tissues of the scalp resulting in hair loss in loss in users who suffer from male pattern baldness. DHT can affect the prostate as well, making it larger. This swelling can cause the gland to press against the bladder causing urinary problems. Drugs called 5alpha-reductase inhibitors can prevent these symptoms without blocking testosterone´s anabolic effects.(8) Higher dosages of test can also negatively impact cholesterol, lowering HDL(9). Testosterone is probably the safest steroid around, but it can´t be taken lightly, and Sustanon is no different.
The principal drawback to Sustanon is it´s cost. It can cost between $5 an ampule and $12 an ampule. Compared with Omnadren, Testoviron, or even Sten (other testosterone products featuring various blends of Testosterone), the cost makes it prohibitive. An equal amount of an of the aforementioned products can be had for less than half the average cost of an amp of Sustanon. Sustanon, therefore, is no better or worse than any other form of testosterone... if the price is right.
17b-hydroxy-4-androsten-3-one
Testosterone base + 4 different esters
Propionate, Phenylpropionate, Isocaproate, Decanoate
Formula (base): C27 H40 O3
Molecular Weight (base): 288.429
Molecular Weight, Esters:
Propionate: 362.5082
Phenylpropionate: 438.6058
Isocaproate: 404.5886
Decanoate: 460.6958
Formula (base): C19 H28 O2
Melting Point (base): 155
Manufacturer: Organon
Effective Dose (Men): 500-2000mg/ week
Effective Dose (Women): Not recommended
Active life: Up to 3 weeks
Detection Time: 3+ months
Anabolic/Androgenic ratio:100/100
References:
Human Anatomy and Physiology, 6th Edition, John W. Hole jr.
J Appl Physiol 94: 2273-2281, 2003. First published February 14, 2003; doi:10.1152
Journal of Applied Physiology, Vol 77, Issue 1 23-29,
EFFECTS OF RECOMBINANT GROWTH HORMONE ON VISCERAL FAT ACCUMULATION: PILOT STUDY IN HIV-INFECTED ADOLESCENTS. J Clin Endocrinol Metab. 2005 Apr 19; [Epub ahead of print]
Measures of submaximal aerobic performance evaluate and predict functional response to growth hormone (HGH) treatment in HGH-deficient adults. J Clin Endocrinol Metab. 1999 Dec;84(12):4570-7.
Hormonal responses to consecutive days of heavy-resistance exercise with or without nutritional supplementation. J Appl Physiol, Oct 1998; 85: 1544 - 1555.
Hormonal and growth factor responses to heavy resistance exercise protocols. J Appl Physiol, Oct 1990; 69: 1442-1450
High dose growth hormone exerts an anabolic effect at rest and during exercise in endurance-trained athletes.J Clin Endocrinol Metab. 2003 Nov;88(11):5221-6.
Christ ER, Cummings MH, Westwood NB, Sawyer BM, Pearson TC, Sonksen PH, Russell-Jones DL. The importance of growth hormone in the regulation of erythropoiesis, red cell mass, and plasma volume in adults with growth hormone deficiency., J Clin Endocrinol Metab 1997 Sep;82(9):2985-90
The Journal of Clinical Endocrinology & Metabolism Vol. 87, No.8 3573-3577
Am J Physiol Endocrinol Metab. 2002 Mar;282(3):E601-7.
Testosterone blunts feedback inhibition of growth hormone secretion by experimentally elevated insulin-like growth factor-I concentrations.J Clin Endocrinol Metab. 2005 Mar;90(3):1613-7. Epub 2004 Dec 7.
Comparison of the Metabolic Effects of Raloxifene and Oral Estrogen in Postmenopausal and Growth Hormone-Deficient Women.J Clin Endocrinol Metab. 2005 Apr 26; [Epub ahead of print]
Serum insulin-like growth factor I levels in growth hormone-deficient adults: influence of sex steroids.Horm Res. 2004;62 Suppl 1:73-6.
Growth hormone enhances effects of endurance training on oxidative muscle metabolism in elderly women. Am J Physiol Endocrinol Metab, Nov 2000; 279: 989 - 996.
J Gerontol A Biol Sci Med Sci 1998 May;53(3):M183-7
(testosterone)
This product was developed by Organon as an ideal HRT (Hormone Replacement Therapy) solution, and it was thought at the time that the different esters would be able to provide a constant release of Testosterone over a months time. Sustanon is a blend of different estered testosterones (4 of them): testosterone propionate - 30 mg, testosterone phenylpropionate - 60 mg, testosterone isocaproate - 60mg, and testosterone decanoate -100 mg.
This drug was highly sought after as a "superior" version of testosterone in the late 80´s and through the mid 90´s. No doubt this is partly due to the very nice write-up Dan Duchaine gave it in his newsletters. However, lets keep in mind that this drug was designed for convenience, not athletics or bodybuilding. The advantage to this drug, according to the manufacturer, is that it can be injected once a month, and the different esters would provide different timed releases over that month, and the patient would therefore only need to visit the doctor once a month for his shot. For athletes or bodybuilders (who routinely use between half a gram and a gram of testosterone per week), this product is really no better than any other form of injectable testosterone.
Lately, it seems that this product has fallen out of favor with Steroid.com members, as many feel that the inclusion of the Propionate and phenylpropionate estered forms of testosterone in this blend would necessitate shooting every other day. This stems from the fact that testosterone propionate would be shot every other day at least, and testosterone phenylpropionate would generally be shot every third day.
Sustanon will do exactly what other forms of testosterone will do:
Testosterone will cause both muscle growth as well as fat loss. It sends a message to muscle cells to store more contractile protein (called actin and myosin), thus making your muscles grow. It also protects your muscles from catabolic (muscle wasting) glucocorticoid hormones(1). Thus it is often said that testosterone is not only anabolic, but it is strongly catabolic. Not only does it cause an increase in size of the muscle fibres (hyperfascia) but it also can change the appearance and the actual number of muscle fibres (Hyperplasia)(2). Testosterone has the ability to increase erythropoiesis (red blood cell production) in your kidneys(4), and a higher Red Blood Cell (RBC) count may improve endurance by producing more highly oxygenated blood. More RBCs can also improve recovery from strenuous physical activity. Agression levels often rise dramatically with the use of any exogenous testosterone (3). Testosterone improves muscle contraction by increasing the number of motor neutrons in muscle(5) and improves neuromuscular transmission(6). It also promotes glycogen synthesis(7)
And, since Sustanon is simply a form of (well actually 4 forms of) testosterone, we also know that administration of this compound will produce a dose respondant curve. (10)A what? Yeah...basically a "dose respondant curve" is the fancy way of saying "the more you take, the bigger you get..."
This is true of Sustanon as well as for every form of testosterone, up to a point.
Unfortunately, Sustanon will also do all of the bad things that any form of testosterone is known for:
It will convert to the female hormone estrogen (via a mechanism known as aromatization) by the (you guessed it) aromatize enzyme. Excessive estrogen can lead to unwanted side effects, such as acne, the growth of breast tissue (gynecomastia), fat gain and reduced fat breakdown, loss of sex drive, testicular shrinkage and water retention. Water retention can increase blood pressure weakening blood vessels over time. Unfortunately, this isn´t all it does& it can also interact with the 5 alpha-reductase enzyme. This interaction converts the testosterone to Dihydro-testosterone (DHT), a more androgenic form of the parent hormone. DHT has a high binding affinity to the tissues of the scalp resulting in hair loss in loss in users who suffer from male pattern baldness. DHT can affect the prostate as well, making it larger. This swelling can cause the gland to press against the bladder causing urinary problems. Drugs called 5alpha-reductase inhibitors can prevent these symptoms without blocking testosterone´s anabolic effects.(8) Higher dosages of test can also negatively impact cholesterol, lowering HDL(9). Testosterone is probably the safest steroid around, but it can´t be taken lightly, and Sustanon is no different.
The principal drawback to Sustanon is it´s cost. It can cost between $5 an ampule and $12 an ampule. Compared with Omnadren, Testoviron, or even Sten (other testosterone products featuring various blends of Testosterone), the cost makes it prohibitive. An equal amount of an of the aforementioned products can be had for less than half the average cost of an amp of Sustanon. Sustanon, therefore, is no better or worse than any other form of testosterone... if the price is right.
17b-hydroxy-4-androsten-3-one
Testosterone base + 4 different esters
Propionate, Phenylpropionate, Isocaproate, Decanoate
Formula (base): C27 H40 O3
Molecular Weight (base): 288.429
Molecular Weight, Esters:
Propionate: 362.5082
Phenylpropionate: 438.6058
Isocaproate: 404.5886
Decanoate: 460.6958
Formula (base): C19 H28 O2
Melting Point (base): 155
Manufacturer: Organon
Effective Dose (Men): 500-2000mg/ week
Effective Dose (Women): Not recommended
Active life: Up to 3 weeks
Detection Time: 3+ months
Anabolic/Androgenic ratio:100/100
References:
Human Anatomy and Physiology, 6th Edition, John W. Hole jr.
J Appl Physiol 94: 2273-2281, 2003. First published February 14, 2003; doi:10.1152
Journal of Applied Physiology, Vol 77, Issue 1 23-29,
EFFECTS OF RECOMBINANT GROWTH HORMONE ON VISCERAL FAT ACCUMULATION: PILOT STUDY IN HIV-INFECTED ADOLESCENTS. J Clin Endocrinol Metab. 2005 Apr 19; [Epub ahead of print]
Measures of submaximal aerobic performance evaluate and predict functional response to growth hormone (HGH) treatment in HGH-deficient adults. J Clin Endocrinol Metab. 1999 Dec;84(12):4570-7.
Hormonal responses to consecutive days of heavy-resistance exercise with or without nutritional supplementation. J Appl Physiol, Oct 1998; 85: 1544 - 1555.
Hormonal and growth factor responses to heavy resistance exercise protocols. J Appl Physiol, Oct 1990; 69: 1442-1450
High dose growth hormone exerts an anabolic effect at rest and during exercise in endurance-trained athletes.J Clin Endocrinol Metab. 2003 Nov;88(11):5221-6.
Christ ER, Cummings MH, Westwood NB, Sawyer BM, Pearson TC, Sonksen PH, Russell-Jones DL. The importance of growth hormone in the regulation of erythropoiesis, red cell mass, and plasma volume in adults with growth hormone deficiency., J Clin Endocrinol Metab 1997 Sep;82(9):2985-90
The Journal of Clinical Endocrinology & Metabolism Vol. 87, No.8 3573-3577
Am J Physiol Endocrinol Metab. 2002 Mar;282(3):E601-7.
Testosterone blunts feedback inhibition of growth hormone secretion by experimentally elevated insulin-like growth factor-I concentrations.J Clin Endocrinol Metab. 2005 Mar;90(3):1613-7. Epub 2004 Dec 7.
Comparison of the Metabolic Effects of Raloxifene and Oral Estrogen in Postmenopausal and Growth Hormone-Deficient Women.J Clin Endocrinol Metab. 2005 Apr 26; [Epub ahead of print]
Serum insulin-like growth factor I levels in growth hormone-deficient adults: influence of sex steroids.Horm Res. 2004;62 Suppl 1:73-6.
Growth hormone enhances effects of endurance training on oxidative muscle metabolism in elderly women. Am J Physiol Endocrinol Metab, Nov 2000; 279: 989 - 996.
J Gerontol A Biol Sci Med Sci 1998 May;53(3):M183-7
Saturday, May 12, 2007
HCG (Human Chorionic Gonadotropin)
HCG (Human Chorionic Gonadotropin)
Quick overview:
Active Life: 64 hours
Drug Class: Leutenizing Hormone (LH) - Gonadotropin
Average Dose: debatable
Acne: Yes
Water Retention: Yes
High Blood Pressure: Yes
Liver Toxic: No
Aromatization: No, but it will raise testosterone levels and increased aromatization may occur.
Chorionic gonadotropin is a hormone found in the female body during the early months of pregnancy (it is produced in the placenta). It is in fact the pregnancy indicator looked at by the over the counter pregnancy test kits, as due to its origin it is not found in the body at any other time. Blood levels of this hormone will become noticeable as early as seven days after ovulation. The level will rise evenly, reaching a peak at approximately two to three months into gestation. After this point, the hormone level will drop gradually until the point of birth. As a prescription drug, HCG offers us some interesting benefits. In the United States, we have the two popular brands, Pregnyl, made by Organon, and Profasi, made by Serono. These are FDA approved for the treatment of undescended testicles in young boys, hypogonadism (underproduction of testosterone) and as a fertility drug used to aid in inducing ovulation in women. When prepared as a medical item, this hormone comes from a human origin. Although there is often a fear of biological origin products, there is little research to be found regarding pathogen or sterility problems with HCG. The problems seen with human origin growth hormone are certainly not to be repeated with HCG, as this compound is obtained in a much different way.
While HCG offers the female no performance enhancing ability, it does prove very useful to the male steroid user. The obvious use of course being to stimulate the production of endogenous testosterone. The activity of HCG in the male body is due to its ability to mimic LH (luteinizing hormone), a pituitary hormone that stimulates the Leydig's cells in the testes to manufacture testosterone. Restoring endogenous testosterone production is a special concern at the end of each steroid cycle, a time when a subnormal androgen level (due to steroid induced suppression) could be very costly. The main concern is the action of cortisol, which in many ways is balanced out by the effect of androgens. Cortisol sends the opposite message to the muscles than testosterone, or to breakdown protein in the cell. Left unchecked (by an extremely low testosterone level) in the body, cortisol can quickly strip much of your new muscle mass away.
The main focus with HCG is to restore the normal ability of the testes to respond to endogenous luteinizing hormone. After a long period of inactivity, this ability may have been seriously reduced. In such a state testosterone levels may not reach a normal point, even though the release of endogenous LH has been resumed. Many who have suffered severe testicular shrinkage may be able to relate, as it is often some time before normal testicle size and feelings of virility are restored if ancillary drugs had not been used. The excessive stimulation brought forth by administration of HCG can likewise cause the testicles to rapidly return to their normal size and level of activity. We are not simply looking for it to fix the problem however, as the resulting high testosterone level can itself trigger negative feedback inhibition at the hypothalamus. Estrogen production is also heightened with the use of HCG, due to its ability to increase aromatase activity in the Leydig's cells. This is due to the main action of HCG, namely the increase of cycIicAMP (a secondary messenger that regulates cellular activity). When stimulated by HCG, the ability of the testes to aromatize androgens could potentially be heightened several times greater than normal. This also may inhibit testosterone production, so we therefore use HCG only as a quick shock to the testes.
The usual protocol is to inject 1500-3000 I.U. every 4th or 5th day, for a duration usually no longer than 2 or 3 weeks. If used for too long or at too high a dose, the drug may actually function to desensitize the Leydig's cells to luteinizing hormone, further hindering a return to homeostasis. Timing the initial dose is also very crucial. If your were coming off a cycle of Sustanon for example, testosterone levels in your blood will likely stay elevated for at least 3 to 4 weeks after your last injection. Taking HCG on the day of your last shot would therefore be useless. Instead one would want to calculate the last week in which androgen levels are likely to be above normal, and begin ancillary drug therapy at this point. In this case HCG would be started around the third or fourth week. Likewise, after ending a cycle of Dianabol (an oral) your blood levels will be sub normal after the third day. Here you may want to begin HCG therapy a few days before your last intake of tablets, giving it a few days to take effect. One would also want to give some thought to the level of suppression that the cycle might have brought about. After an 8 week cycle of Equipoise for example, 1500-2500 I.U. would likely be a sufficient initial dosage. The lower amount of hormonal suppression one associates with this drug would probably not require much more. On the other hand, 750-1000mg of Sustanon per week might incline the user to inject a much larger HCG dose, perhaps as much as 5000 I.U. for the opening application. It may thereafter also be a good idea to reduce the dosage on subsequent shots, so as to step down the intake of HCG during the two or three weeks of intake.
As discussed above, HCG acts only to mimic the action of LH. It is likewise not the perfect hormone to combat testosterone suppression, and for this reason it is used most often in conjunction with estrogen antagonists such as Clomid, Nolvadex or cyclofenil. These drugs have a different effect on the regulating system, namely inhibiting estrogen-induced suppression at the hypothalamus. This of course also helps to restore the release of testosterone, although through a much different mechanism than HCG. A combination of both drugs appears to be very synergistic, HCG providing an immediate effect on the testes (shocking them out of inactivity) while the anti-estrogen helps later to block inhibition on the hypothalamus and resume the normal release of gonadotropins from the pituitary. The typical procedure involves giving the Clomid/Nolvadex dose from the start with HCG, but continuing it alone for a few weeks once HCG has been discontinued. This practice should effectively raise testosterone levels, which will hopefully remain stable once Clomid/Nolvadex have been discontinued. While unfortunately there is no way to retain all of the muscle gains produced by anabolic steroids, using ancillaries to restore a balanced hormonal state is the best way to minimize the loss felt with ending a cycle.
Quick overview:
Active Life: 64 hours
Drug Class: Leutenizing Hormone (LH) - Gonadotropin
Average Dose: debatable
Acne: Yes
Water Retention: Yes
High Blood Pressure: Yes
Liver Toxic: No
Aromatization: No, but it will raise testosterone levels and increased aromatization may occur.
Chorionic gonadotropin is a hormone found in the female body during the early months of pregnancy (it is produced in the placenta). It is in fact the pregnancy indicator looked at by the over the counter pregnancy test kits, as due to its origin it is not found in the body at any other time. Blood levels of this hormone will become noticeable as early as seven days after ovulation. The level will rise evenly, reaching a peak at approximately two to three months into gestation. After this point, the hormone level will drop gradually until the point of birth. As a prescription drug, HCG offers us some interesting benefits. In the United States, we have the two popular brands, Pregnyl, made by Organon, and Profasi, made by Serono. These are FDA approved for the treatment of undescended testicles in young boys, hypogonadism (underproduction of testosterone) and as a fertility drug used to aid in inducing ovulation in women. When prepared as a medical item, this hormone comes from a human origin. Although there is often a fear of biological origin products, there is little research to be found regarding pathogen or sterility problems with HCG. The problems seen with human origin growth hormone are certainly not to be repeated with HCG, as this compound is obtained in a much different way.
While HCG offers the female no performance enhancing ability, it does prove very useful to the male steroid user. The obvious use of course being to stimulate the production of endogenous testosterone. The activity of HCG in the male body is due to its ability to mimic LH (luteinizing hormone), a pituitary hormone that stimulates the Leydig's cells in the testes to manufacture testosterone. Restoring endogenous testosterone production is a special concern at the end of each steroid cycle, a time when a subnormal androgen level (due to steroid induced suppression) could be very costly. The main concern is the action of cortisol, which in many ways is balanced out by the effect of androgens. Cortisol sends the opposite message to the muscles than testosterone, or to breakdown protein in the cell. Left unchecked (by an extremely low testosterone level) in the body, cortisol can quickly strip much of your new muscle mass away.
The main focus with HCG is to restore the normal ability of the testes to respond to endogenous luteinizing hormone. After a long period of inactivity, this ability may have been seriously reduced. In such a state testosterone levels may not reach a normal point, even though the release of endogenous LH has been resumed. Many who have suffered severe testicular shrinkage may be able to relate, as it is often some time before normal testicle size and feelings of virility are restored if ancillary drugs had not been used. The excessive stimulation brought forth by administration of HCG can likewise cause the testicles to rapidly return to their normal size and level of activity. We are not simply looking for it to fix the problem however, as the resulting high testosterone level can itself trigger negative feedback inhibition at the hypothalamus. Estrogen production is also heightened with the use of HCG, due to its ability to increase aromatase activity in the Leydig's cells. This is due to the main action of HCG, namely the increase of cycIicAMP (a secondary messenger that regulates cellular activity). When stimulated by HCG, the ability of the testes to aromatize androgens could potentially be heightened several times greater than normal. This also may inhibit testosterone production, so we therefore use HCG only as a quick shock to the testes.
The usual protocol is to inject 1500-3000 I.U. every 4th or 5th day, for a duration usually no longer than 2 or 3 weeks. If used for too long or at too high a dose, the drug may actually function to desensitize the Leydig's cells to luteinizing hormone, further hindering a return to homeostasis. Timing the initial dose is also very crucial. If your were coming off a cycle of Sustanon for example, testosterone levels in your blood will likely stay elevated for at least 3 to 4 weeks after your last injection. Taking HCG on the day of your last shot would therefore be useless. Instead one would want to calculate the last week in which androgen levels are likely to be above normal, and begin ancillary drug therapy at this point. In this case HCG would be started around the third or fourth week. Likewise, after ending a cycle of Dianabol (an oral) your blood levels will be sub normal after the third day. Here you may want to begin HCG therapy a few days before your last intake of tablets, giving it a few days to take effect. One would also want to give some thought to the level of suppression that the cycle might have brought about. After an 8 week cycle of Equipoise for example, 1500-2500 I.U. would likely be a sufficient initial dosage. The lower amount of hormonal suppression one associates with this drug would probably not require much more. On the other hand, 750-1000mg of Sustanon per week might incline the user to inject a much larger HCG dose, perhaps as much as 5000 I.U. for the opening application. It may thereafter also be a good idea to reduce the dosage on subsequent shots, so as to step down the intake of HCG during the two or three weeks of intake.
As discussed above, HCG acts only to mimic the action of LH. It is likewise not the perfect hormone to combat testosterone suppression, and for this reason it is used most often in conjunction with estrogen antagonists such as Clomid, Nolvadex or cyclofenil. These drugs have a different effect on the regulating system, namely inhibiting estrogen-induced suppression at the hypothalamus. This of course also helps to restore the release of testosterone, although through a much different mechanism than HCG. A combination of both drugs appears to be very synergistic, HCG providing an immediate effect on the testes (shocking them out of inactivity) while the anti-estrogen helps later to block inhibition on the hypothalamus and resume the normal release of gonadotropins from the pituitary. The typical procedure involves giving the Clomid/Nolvadex dose from the start with HCG, but continuing it alone for a few weeks once HCG has been discontinued. This practice should effectively raise testosterone levels, which will hopefully remain stable once Clomid/Nolvadex have been discontinued. While unfortunately there is no way to retain all of the muscle gains produced by anabolic steroids, using ancillaries to restore a balanced hormonal state is the best way to minimize the loss felt with ending a cycle.
Sunday, May 6, 2007
Guide to rHGH use
Guide to rHGH use
Disclaimer (warning): This information is for entertainment value only. I am not a medical doctor , therefore, I am not qualified to offer any medical advice nor advise you on how to take any substances. What follow is my experience and knowledge of HGH.
According to studies in the New England Journal of Medicine GH use will:
- Shed Bodyfat- Increase Muscle Tone- Boost your Energy, Strength, and Endurance- Reduce Wrinkles - Create Tighter, Smoother Skin- Help you Sleep Better- Improve Sex Drive and Performance- Improve Immune and Heart Function, Bone Density, Healing Time and Cholesterol, Improve Brain Function, Memory and Mental Focus
Wow! Sure sounds like a wonder drug to me! Yeah right, anyway here is some real world information for bodybuilders. Somatropin (rHGH) is produced by the pituitary gland and is responsible in adolescence for growth of tissues, protein deposition, and the breakdown of sub-q fat stores. As we age, growth hormone levels decrease but still remain active in the body, releasing in cycles during the day. Synthetic growth hormone used exogenously by bodybuilders is a 191 chain sequence of amino acids that replicates the bodies natural production of growth hormone.
Growth hormone has been in use by bodybuilders since the early 1980’s, though at this time, HGH was being extracted from the pituitary glands of cadavers and had enormous side effects, most prominently Creutzfeldt Jacob disease. This is a rare and fatal brain disease, it need not be discussed here since it is not possible in synthetic forms of HGH, but if you want more info just run a search in google. rHGH stimulates growth in most body tissues which is due to an increase in cell number rather than cell size. This includes muscle tissue as well as internal organs, hence the dreaded GH gut.
Use of growth hormone by bodybuilders will cause increased muscle size, localized and overall bodyfat loss, increased protein synthesis, increased glucose output by the liver, increased insulin resistance and lowered thyroid output. Stored fats will be used as a primary fuel source, thus the body fat loss.
So is rHGH the wonder drug everyone lusts after? It certainly is beneficial but not for everyone. You must be willing to take risks to achieve maximum benefits from its use, as well as substantial financial investment. Do it right the first time or don’t do it at all! You will achieve faster and greater growth from cycles of steroids than with GH, though once you reach a plateau, not many products work better.
Ok, so now you have decided that this is the drug for you and you are ready to try it, so what next? Well here are some general guidelines to follow for maximal results from GH use:
Daily injections are a must to maintain stable blood levels as GH has a very short life span in the body. It will peak almost immediately after injection and will clear the body with a half-life of only 20-30 minutes. It is best injected first thing in the morning upon rising to raise levels that are very low from sleeping, and immediately after training. I do not recommend injecting before bed as many bodybuilders do, since that is the time of day that your body will release naturally high levels of growth hormone, and exogenous use will only block that release. If you take it in the morning when levels are low, after training when levels are depleted and then let your body release while sleeping, you are getting one extra release for free! GH is best taken long term, short cycles do not maximize the benefits of muscle cell increase, only fat loss. Here is how I take my GH for maximum benefits:
6iu ed injected sub-q, preferably in the stomach (IM for certain brands)3iu injected upon rising, 3iu injected immediately post-workout10iu insulin taken 30 minutes after HGH injection25mcg cytomel eduse of androgens such as testosterone
The timing of GH and insulin injections is critical. If insulin is injected before the GH, your pancreas will stop release of insulin monitoring due to the exogenous source. GH when injected will mobilize stored glycogen release which will turn into glucose for energy. This will cause a rapid rise in blood sugar levels that will not shut down or stop rising due to the feedback loop being momentarily cut off. You will go hyperglycemic and end up in the hospital. You must first inject your GH, then the insulin; this will cause a rise in glucose release by the GH and will be controlled and shuttled into muscle tissue for repair by the later injection of insulin.Use of cytomel or some type of T3 hormone is critical since GH use will severely lower thyroid levels. Small exogenous sources are necessary to maintain normal levels and 25 mcg ed is sufficient. This will also aid in body fat loss by maintaining proper thyroid functioning.Use of androgens is also necessary due to the promotion of anabolism by increasing muscle size that benefits the new cell number increase by the GH. Remember GH will not directly cause muscle cell size increase, just the number of cells, therefore, androgens are necessary to increase size. Testosterone or trenbolone are both highly androgenic and perfect for out stack.
One myth that needs to be cleared up: high doses of GH use and the 5 on 2 off program. First, if you find that you are not achieving results off of 4-6iu ed, than something else is the problem, not your dose. The use of high doses if primarily cause by heat damage to the protein chain causing denatured proteins. This will decrease the effect and you must use higher doses to achieve the same effect. Other reasons for high dose use are; fake gh, not using insulin, cytomel or test, poor diet, improper timing schedule and the 5 on 2 off. This program was recommended by dealers as a way to move product by offering a lower cost cycle. No doctor in the world would recommend this protocol, Peak blood concentrations are reached in 2-6 hours after injection, and therefore, multiple daily injections are necessary to achieve stable release schedule and results. If you take your last injection Friday afternoon, and then not again till Monday morning, then you have negated all effects offered by the 6 hour concentration. Yes, you will achieve results using a 5 on 2 off program, but not as well as if you inject ed. It’s your money; I can only tell you how to optimize use.
Side effects of GH use include; carpal tunnel syndrome, tingling in the extremities, numbness in the hands and feet, increased organ growth, decreased insulin reception, acromegaly but only in extreme dose use, and decreased thyroid output causing fat accumulation. If you find that you are experiencing any of the above side effects, lower your dose immediately. This is especially important with carpal tunnel. If you feel like your wrists are hurting then lower the dose until pain subsides. You do not want to have that surgery, trust me.
GH is a fantastic product, beneficial for many reasons. Most people will experience thinning of the skin, increased vascularity, fat loss, permanent increases in muscle size due to the cell number increase, and overall feelings of wellness. You will probably need less sleep and feel supercharged all day long. I highly recommend HGH use, but only when you have the money to do it right. 4-6 month cycles are optimal, year round if you are over age 35.
Disclaimer (warning): This information is for entertainment value only. I am not a medical doctor , therefore, I am not qualified to offer any medical advice nor advise you on how to take any substances. What follow is my experience and knowledge of HGH.
According to studies in the New England Journal of Medicine GH use will:
- Shed Bodyfat- Increase Muscle Tone- Boost your Energy, Strength, and Endurance- Reduce Wrinkles - Create Tighter, Smoother Skin- Help you Sleep Better- Improve Sex Drive and Performance- Improve Immune and Heart Function, Bone Density, Healing Time and Cholesterol, Improve Brain Function, Memory and Mental Focus
Wow! Sure sounds like a wonder drug to me! Yeah right, anyway here is some real world information for bodybuilders. Somatropin (rHGH) is produced by the pituitary gland and is responsible in adolescence for growth of tissues, protein deposition, and the breakdown of sub-q fat stores. As we age, growth hormone levels decrease but still remain active in the body, releasing in cycles during the day. Synthetic growth hormone used exogenously by bodybuilders is a 191 chain sequence of amino acids that replicates the bodies natural production of growth hormone.
Growth hormone has been in use by bodybuilders since the early 1980’s, though at this time, HGH was being extracted from the pituitary glands of cadavers and had enormous side effects, most prominently Creutzfeldt Jacob disease. This is a rare and fatal brain disease, it need not be discussed here since it is not possible in synthetic forms of HGH, but if you want more info just run a search in google. rHGH stimulates growth in most body tissues which is due to an increase in cell number rather than cell size. This includes muscle tissue as well as internal organs, hence the dreaded GH gut.
Use of growth hormone by bodybuilders will cause increased muscle size, localized and overall bodyfat loss, increased protein synthesis, increased glucose output by the liver, increased insulin resistance and lowered thyroid output. Stored fats will be used as a primary fuel source, thus the body fat loss.
So is rHGH the wonder drug everyone lusts after? It certainly is beneficial but not for everyone. You must be willing to take risks to achieve maximum benefits from its use, as well as substantial financial investment. Do it right the first time or don’t do it at all! You will achieve faster and greater growth from cycles of steroids than with GH, though once you reach a plateau, not many products work better.
Ok, so now you have decided that this is the drug for you and you are ready to try it, so what next? Well here are some general guidelines to follow for maximal results from GH use:
Daily injections are a must to maintain stable blood levels as GH has a very short life span in the body. It will peak almost immediately after injection and will clear the body with a half-life of only 20-30 minutes. It is best injected first thing in the morning upon rising to raise levels that are very low from sleeping, and immediately after training. I do not recommend injecting before bed as many bodybuilders do, since that is the time of day that your body will release naturally high levels of growth hormone, and exogenous use will only block that release. If you take it in the morning when levels are low, after training when levels are depleted and then let your body release while sleeping, you are getting one extra release for free! GH is best taken long term, short cycles do not maximize the benefits of muscle cell increase, only fat loss. Here is how I take my GH for maximum benefits:
6iu ed injected sub-q, preferably in the stomach (IM for certain brands)3iu injected upon rising, 3iu injected immediately post-workout10iu insulin taken 30 minutes after HGH injection25mcg cytomel eduse of androgens such as testosterone
The timing of GH and insulin injections is critical. If insulin is injected before the GH, your pancreas will stop release of insulin monitoring due to the exogenous source. GH when injected will mobilize stored glycogen release which will turn into glucose for energy. This will cause a rapid rise in blood sugar levels that will not shut down or stop rising due to the feedback loop being momentarily cut off. You will go hyperglycemic and end up in the hospital. You must first inject your GH, then the insulin; this will cause a rise in glucose release by the GH and will be controlled and shuttled into muscle tissue for repair by the later injection of insulin.Use of cytomel or some type of T3 hormone is critical since GH use will severely lower thyroid levels. Small exogenous sources are necessary to maintain normal levels and 25 mcg ed is sufficient. This will also aid in body fat loss by maintaining proper thyroid functioning.Use of androgens is also necessary due to the promotion of anabolism by increasing muscle size that benefits the new cell number increase by the GH. Remember GH will not directly cause muscle cell size increase, just the number of cells, therefore, androgens are necessary to increase size. Testosterone or trenbolone are both highly androgenic and perfect for out stack.
One myth that needs to be cleared up: high doses of GH use and the 5 on 2 off program. First, if you find that you are not achieving results off of 4-6iu ed, than something else is the problem, not your dose. The use of high doses if primarily cause by heat damage to the protein chain causing denatured proteins. This will decrease the effect and you must use higher doses to achieve the same effect. Other reasons for high dose use are; fake gh, not using insulin, cytomel or test, poor diet, improper timing schedule and the 5 on 2 off. This program was recommended by dealers as a way to move product by offering a lower cost cycle. No doctor in the world would recommend this protocol, Peak blood concentrations are reached in 2-6 hours after injection, and therefore, multiple daily injections are necessary to achieve stable release schedule and results. If you take your last injection Friday afternoon, and then not again till Monday morning, then you have negated all effects offered by the 6 hour concentration. Yes, you will achieve results using a 5 on 2 off program, but not as well as if you inject ed. It’s your money; I can only tell you how to optimize use.
Side effects of GH use include; carpal tunnel syndrome, tingling in the extremities, numbness in the hands and feet, increased organ growth, decreased insulin reception, acromegaly but only in extreme dose use, and decreased thyroid output causing fat accumulation. If you find that you are experiencing any of the above side effects, lower your dose immediately. This is especially important with carpal tunnel. If you feel like your wrists are hurting then lower the dose until pain subsides. You do not want to have that surgery, trust me.
GH is a fantastic product, beneficial for many reasons. Most people will experience thinning of the skin, increased vascularity, fat loss, permanent increases in muscle size due to the cell number increase, and overall feelings of wellness. You will probably need less sleep and feel supercharged all day long. I highly recommend HGH use, but only when you have the money to do it right. 4-6 month cycles are optimal, year round if you are over age 35.
Friday, May 4, 2007
Testosterone Suspension
Testosterone Suspension
Testosterone suspension is simply testosterone crystals suspended in a sterile water solution. As such, it becomes active very quickly after injection, and agressiveness often sets in immediatel as well as a possible strength elevation. Since there is no ester, it also basically drops crystals into your muscle (painful), but it also gives you more bang for the buck than other forms of injectable testosterone.
As with all forms of testosterone, this product will convert to estrogen, cause some water
retention, possible acne and hairloss. Of course, testosterone will also build mass and strength faster than any other anabolic steroid as well, and should be the base of any cycle.
Reported Characteristics
Pharmaceutical Name:Testosterone
Chemical Name:4-androstene-3-one-17b-ol
Cutting/Bulking:Cutting
Anabolic Rating: 100
Active-Life: About one day.
Drug Class: Androgenic/Anabolic Steroid (For injection)
Average Reported Dosage: Men 150-1400mg weekly Women 25-50mg weekly
Acne: Yes, high
Water Retention: Yes, high
High blood Pressure: Often in higher dosages
Liver Toxic: Low
Aromatization: Yes, high
DHT Conversion: Yes-high
Decreases HPTA function: Yes
Average Price: $10/100mgs
Testosterone suspension is simply testosterone crystals suspended in a sterile water solution. As such, it becomes active very quickly after injection, and agressiveness often sets in immediatel as well as a possible strength elevation. Since there is no ester, it also basically drops crystals into your muscle (painful), but it also gives you more bang for the buck than other forms of injectable testosterone.
As with all forms of testosterone, this product will convert to estrogen, cause some water
retention, possible acne and hairloss. Of course, testosterone will also build mass and strength faster than any other anabolic steroid as well, and should be the base of any cycle.Reported Characteristics
Pharmaceutical Name:Testosterone
Chemical Name:4-androstene-3-one-17b-ol
Cutting/Bulking:Cutting
Anabolic Rating: 100
Active-Life: About one day.
Drug Class: Androgenic/Anabolic Steroid (For injection)
Average Reported Dosage: Men 150-1400mg weekly Women 25-50mg weekly
Acne: Yes, high
Water Retention: Yes, high
High blood Pressure: Often in higher dosages
Liver Toxic: Low
Aromatization: Yes, high
DHT Conversion: Yes-high
Decreases HPTA function: Yes
Average Price: $10/100mgs
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