Oral Anabolic Steroids History & Overview
Oral steroids are among the most popular of all types of anabolic steroids, and it is perhaps the most popular subject within the topic of steroids. This is because of the perceived convenience of them and their use, as well as their method of administration. This is usually the case for first time users, as they are deeply attracted to the convenience of oral steroids upon first reading and researching the subject prior to their journey into their first cycle(s). This is because the perception is that all of the benefits of anabolic steroid use lies in a convenient and easy to swallow capsule or pill. This article will discuss and describe the basics of what oral steroids are and how oral steroids work, and the difference between oral steroids and other formats (such as injectable). However, there are some misconceptions that need to be addressed first, especially where the general public and masses are concerned, often due to their lack of knowledge and/or education on the subject at hand.
The first and most common misconception is the following: oral steroids are safer than injectables. Quite plainly and simply put, this is wrong. This is by far the most commonly believed and propagated misconception about steroids in general, next to the misconception that anabolic steroids in general can provide massive and rapid gains without the need to train hard in the gym or devote oneself to a strict diet and nutrition regimen. While both injectable and oral steroids are composed of a subcategory of various compounds that can be equally as harmful, oral steroids are more harmful in general. The fact is that there does exist a couple of oral steroid compounds that are considered ‘safer’ or ‘milder’ than others, but in general, oral steroids pose a far higher risk of liver toxicity and damage (known as hepatotoxicity). Other risks that oral steroids pose above and beyond injectables are their considerable negative effect on blood lipid profile values (also known as blood cholesterol levels) whereby they tend to alter the ratio of HDL:LDL cholesterol levels towards higher levels of LDL (the so called ‘bad’ cholesterol). Although all steroids – both injectable and oral – do have this negative effect on cholesterol levels, oral steroids have a far greater negative impact here in this area. The technical details of how and why these issues are the case with oral steroids will be expanded upon further in this article very shortly.
The second most common oral steroid misconception is: oral steroids are stronger or weaker than injectables. Once again, this is wrong. Oral steroids are not stronger than injectable steroids, and neither are they weaker either. All anabolic steroids are given a strength rating based on how anabolic they are/were on tissues in in-vitro laboratory tests. This strength rating is indeed a measurement of how effective a given steroid is in the area of muscle anabolism, and while some oral steroids do have anabolic ratings that meet or exceed various injectables, some also have lower ratings too. Their strengths and weaknesses vary among each other, and even each anabolic steroid’s given anabolic or androgenic strength rating must be taken with a grain of salt, as these numbers were determined in in-vitro lab tests. These results might differ in a real world in-vivo setting in a real person (and differences may continue to manifest when we examine anabolic effects of an anabolic steroid in different animals versus humans, etc. However, these anabolic strength ratings are good baseline figures to start with in terms of general knowledge of how strong a compound might be, but they cannot and should not be taken completely at face value.
The third frequent oral steroid misconception is: oral steroids are easier to get. This is also untrue. Although some of the most popular anabolic steroids ever conceived and used are oral compounds by nature, there are other anabolic steroids that are injectables that are equally as popular that are just as easy to obtain. For example, the most popular anabolic steroid ever used is indeed an oral steroid – the anabolic steroid known as Dianabol (Methandrostenolone) – but there are other extremely popular compounds that are just as easy to obtain, such as Winstrol (Stanozolol) or Nandrolone (Deca-Durabolin). At the end of the day, anabolic steroid use is so prolific in today’s day and age that any anabolic steroid vendor, supplier, dealer, or point-of-sale should be able to offer all types of steroid compounds that are commonly used.
The fourth misconception is as follows: oral steroids are cheaper. Again, this is wrong. Much like the previous misconception, this is not necessarily the case. Oral anabolic steroids contain at least a dozen different commonly used compounds that all vary in price, some of which are actually quite more expensive than some injectables. On the other side of the same coin, there are injectable steroids that are cheaper than oral steroids on a milligram for milligram basis, and there are also those that are more expensive as well. When planning an anabolic steroid cycle, one should always be aware of the total costs involved with everything included, and that most cycles of a specific or certain nature (mass gaining / bulking cycles, cutting cycles, etc.) most often generally cost around the same amount. At the end of the day, it does turn out, however, that various injectable steroids (such as the various forms of Testosterone, for example) do end up being cheaper overall than oral steroids, especially when one is tempted to do an oral-only steroid cycle (which is not recommended in any case).
What Oral Steroids Are and How Oral Steroids Work
All oral steroids are chemically modified in order to specifically survive what is known as the first pass through the liver. There are only 3 oral steroids that are known to survive the first pass through the liver without this modification, and they are: Proviron (which is not really anabolic by nature), Andriol (an oral and highly fat-soluble version of Testosterone), and Primobolan. Aside from the three that have just been mentioned, all other oral steroids have undergone a chemical modification known as C17 Alpha Alkylation (also known as C17 Methylation). This chemical modification allows the anabolic steroid to survive the first pass through the liver after ingestion, and make its way into the bloodstream in a high(er) percentage. Without this modification, studies have deemed the absorption rate to be almost negligible, as the majority of the compound ends up passing through the liver, broken down and metabolized by various enzymes in the liver, and excreted through the urinary system.
Historically, scientists in the mid-late 1950s discovered that by adding a methyl group to the 17th carbon on the steroid molecule, liver enzymes responsible for metabolization and breakdown of the compound would not recognize the compound, and thus a higher and very significant percentage of the compound would make its way to the bloodstream. This is what was previously mentioned as C17 Alpha Alkylation, because, as mentioned, the 17th carbon on the molecule would be alkylated (or also known as methylated). Although some percentage of a C17 alkylated oral steroid will still succumb to metabolic breakdown in the liver, the chemical modification allows it to be more resistant to this process in the body.
A perfect example of this would be the very first experiments conducted in the late 1940s with Testosterone. While drinking a vial of injectable Testosterone would result in no measurable effects, modifying Testosterone by way of C17 methylation to result in the compound known as Methyltestosterone resulted in a significant amount of it surviving liver metabolism. Although this modification might at first seem like an extremely convenient miracle in the administration and delivery of anabolic steroids in science, there are some limitations and downsides to this that need to be heeded. Some of these limitations include: how the oral steroid can be effectively used, for how long it can be used, and how these oral steroids are to be dosed. As previously mentioned in the introduction to this article, there are significant negative effects that oral steroids have on the body in the way of liver toxicity and negative cholesterol changes – both of which are a direct result of this C17 alpha alkylation modification we have just discussed.
Some of the most popular C17 Alpha Alkylated oral steroids are: Dianabol (Methandrostenolone), Winstrol (Stanozolol), Anavar (Oxandrolone), Anadrol (Oxymetholone), and Turinabol (Chlorodehydromethyltestosterone). Although there are indeed other oral steroids that could be listed alongside those, these are some of the most popular and most frequently used and discussed.
Hepatotoxicity (Liver Toxicity) From Oral Steroids
Although C17 Methylation is what is responsible for the liver toxic effects of oral steroids, not all oral steroids are equal in their potential liver toxicity. Some are well known for being quite significantly liver toxic, such as Anadrol (Oxymetholone), and some are actually quite minimal in their liver toxic effects, like Anavar (Oxandrolone), for example. Science does not know exactly how or why some oral steroids are more or less liver toxic than others, but there are some pretty strong ideas and theories which are points of discussion on the matter. The fact is that some C17AA oral steroids are more resistant to liver metabolism than others by their very nature even before they were methylated, and so their methylation makes them even more resistant to liver metabolism (and therefore this is why some of the strongest oral steroids are also the most liver toxic on a milligram for milligram basis). Thus, there seems to be a direct correlation between the anabolic strength of an oral steroid and its degree of liver toxicity.
For example, Trenbolone is an injectable anabolic steroid that is not C17 alpha alkylated, but it is known as being quite resistant to liver metabolism. Trenbolone, like most other anabolic steroids, can be modified via C17 alpha alkylation / methylation, thus turning it into Methyltrienolone (also known as Methyltrenbolone). This results in Methyltrienolone becoming so incredibly anabolic that its anabolic rating is thought to be in the tens of thousands (believed to be no less than a rating of 12,000) compared to its parent (Trenbolone) rating of 500. However, part in parcel of this strength is its almost as equally monstrous liver toxicity, which is thought to be so extreme that in 1966, lab tests lead researchers to conclude that it is the most liver toxic oral steroid ever recorded. Shortly after basic laboratory tests, Methyltrienolone was deemed as completely un-useable simply due to how dangerous it is in terms of its devastating effects on liver tissue. Its existence was then ended at the stage of very early rudimentary testing, and it was never even considered for use as a medicine / drug even for animal use, much less for humans.
It is also important to keep in mind that all C17 methylated oral steroids demonstrate some degree of liver toxicity in scientific studies, and that the majority of these studies examined their use in what would be considered therapeutic dosages that are fit for medical prescriptions in the treatment of disorders and diseases. When it comes to bodybuilding dosages, they are commonly higher than those used in medicine, and users should take note of this and be very aware of the risks. For example, studies have shown that Dianabol dosages of 10-15mg/day resulted in elevated liver enzyme values to the extent that it was considered minimal liver strain. By comparison, most bodybuilding dosages are commonly in the range of 25mg per day or higher.
Oral steroid abuse can be in the form of excessive daily dosages and/or excessive lengths of use. There have been recorded incidences of serious liver damage over the years in medical records that can (and have been) life-threatening. Most oral steroid cycles should be no greater than 4 – 6 weeks in length before going on a considerable break from their use.
Cholesterol Alterations From Oral Steroids
Oral steroids are prime offenders for negative alterations in HDL-LDL values. HDL (High Density Lipoprotein) is what is known as the ‘good’ cholesterol in the body, while LDL (Low Density Lipoprotein) is what is known as the ‘bad’ cholesterol in the body. Because of the effect that oral steroids have on the liver, they have significant effects in terms of shifting the balance of HDL-LDL towards very high levels of LDL. This is because the liver is, for the most part, the body’s central processing organ for cholesterol of all types. The negative cholesterol effects of oral steroids are indeed directly linked to the liver toxicity that has been previously discussed. Anabolic steroids in general tend to increase a liver enzyme known as hepatic lipase. This enzyme is responsible for breaking down the ‘good’ cholesterol, and thus less HDL will end up circulating the bloodstream during anabolic steroid cycles. The problem here is that LDL (‘bad’ cholesterol) is lower in density and tends to be ‘gooey’ and sticks to the arterial walls, piling up over time. HDL (‘good’ cholesterol) is higher in density and is responsible for circulating the bloodstream and tends to smash and break up LDL cholesterol, thus preventing LDL from building up too much (which can result in unsafe blockage build-up, resulting in coronary problems). While injectable compounds tend to only reduce HDL levels for the most part, oral steroids not only do the exact same thing, but they also seem to generate more production of LDL cholesterol at the same time.
Oral Steroid Limitations and How To Use Oral Steroids
Oral steroids are convenient because of their ability to be ingested in a simple pill or capsule. However, due to their previously discussed downsides, there is a specific way to go about using them so as to maximize benefits and minimize negative effects. The first thing that should be mentioned is that due to their nature, risks, and effects, oral steroids should be used in a supplemental manner to compliment an anabolic steroid cycle whereby the base compounds are injectables. In no way, shape, or form should oral-only cycles ever be considered or used. This is also because of the other major limitation: most oral steroids should be used no more than 4 – 6 weeks in length, and some of the stronger and more potent oral steroids should ideally be utilized for shorter durations (such as Anadrol, for example).
Due to this nature of oral steroids, most anabolic steroid users tend to use oral steroids to ‘kickstart’ their cycles, whereby an injectable or two are used for a total cycle length of 12 weeks. Because long-acting injectable steroids (such as Testosterone Enanthate or Nandrolone Decanoate) tend to slowly ‘kick-in’ and no effects are observed until 4 or 5 weeks into use, an oral compound is used for the first 4 – 6 weeks of the cycle while the blood levels of the long-acting injectables are used. This is because, due to the shorter half-lives of oral steroids, they tend to ‘kick-in’ and users see and feel their effects in the gym far sooner than long-acting, long-estered injectable compounds. Thus, once the oral steroids are removed from the cycle around weeks 4 – 6, the long-estered injectables will have built up to optimal blood plasma levels and their effects in terms of strength and muscle gains will be seen.