Oral Steroids

The topic of oral steroids is probably the most popular one, especially among beginners and prospective anabolic steroid users.

For first-time anabolic steroid users, there is nothing more appealing than the convenience of anabolic steroids in pill or capsule form, which are easy to swallow.

Before we get into the basics of what oral anabolic steroids are, how they work, what they do, and how they differ from other formulations (such as injectables), it's very important to first clarify a few misconceptions about oral anabolic steroids that are widespread among the uneducated general public.

Those misconceptions are

Myth #1: Oral steroids are safer than injectables.

Myth #2: Oral steroids are less effective/stronger or more effective/stronger than injectables.

Myth #3: Oral steroids are easier to obtain.

Myth #4: Oral steroids are cheaper.

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Myth #1: Oral steroids are safer than injectables.

This is the biggest misconception about oral anabolic steroids, and probably the second biggest misconception about anabolic steroids in general (the biggest being that anabolic steroids can make you bulk up without effort, training, or diet).

The real truth is that both injectable and oral steroids contain a variety of dangerous compounds in each category.

There are oral steroids that pose a higher risk of causing various risks to the body, while there are injectable steroids that pose a higher risk.

The bottom line is that oral steroids are harsher on the body's lower systems than most injectables, and while there are one or two 'milder' and 'safer' oral steroids, most oral steroids have far greater issues with hepatotoxicity (liver toxicity) and negative cholesterol changes than most injectables.

This is not an issue with most injectables, with one or two exceptions, because most injectable compounds are well tolerated by the body.

We'll get into the specifics of why that is shortly in this article.

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Myth 2: Oral steroids are less effective/stronger than injectables.

Oral steroids are neither stronger nor weaker than injectables.

The anabolic strength ratings (a measure of how effective an anabolic steroid is in terms of promoting muscle growth) of various oral anabolic steroids actually match or exceed the anabolic strength ratings of many injectables, and some oral anabolic steroids even fall short when compared to their injectable counterparts.

Myth #3: Oral steroids are easy to obtain.

Simply put, this is not true.

While there are popular anabolic steroids in both categories that are very easy to obtain, the most popular anabolic steroid of all time is an oral steroid (Dianabol, aka Methandrostenolone).

In addition to this, the two most popular anabolic steroids of all time are both injectable: Nandrolone (Deca Durabolin) and Winstrol (Stanozolol).

All anabolic steroid suppliers and sellers are required to stock and sell all types of oral and injectable steroids in equal amounts.

Myth #4: Oral steroids are cheaper.

This is also not true.

There are both more expensive and cheaper compounds in both categories (oral and injectable), and it all has to do with factors such as the popularity of the compound, ease of manufacture, accessibility, etc.

The overall price of an anabolic steroid cycle is also generally the same, as anabolic steroid cycles should ideally be planned in advance and all costs and dosages calculated before purchase.

In the end, the overall cost of the oral steroids to be administered in a given cycle is often about the same price as other injectables, with the exception of the various expensive compounds mentioned earlier.

However, when compared to many injectable compounds, a simple cycle of testosterone in injectable form, for example, is much more cost effective than a cycle of oral steroids.

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Oral Steroids: What They Are and How They Work

It is absolutely essential to understand that there are only three oral steroids that are bioavailable orally without chemical modification: andriol, primobolan, and proviron.

Other than these three, all oral anabolic steroids must undergo some sort of transformation before they can be orally bioavailable.

When testosterone (or any other anabolic steroid) is ingested orally, the amount that enters the bloodstream is very small, too small to actually have a significant effect on the body.

This is because any ingested substance that is swallowed and processed through the gastrointestinal tract always has to go through what is known as the first pass through the liver before it finally enters the bloodstream.

Unfortunately, almost all anabolic steroids are so easily metabolized and broken down by the liver that only a very small percentage actually survive liver metabolism.

Figure 1: Basic image of a basic steroid structure showing numbered carbon positions.

It was then realized that modifying the chemical structure by adding a methyl group (also known as an alkyl group) to the 17th carbon (also known as carbon 17-alpha) of the steroid structure could make the anabolic steroid more resistant to liver metabolism. The chemical attachment of a methyl group to the 17th carbon is known as C17-alpha alkylation.

As mentioned earlier, when an anabolic steroid is C17-alpha alkylated, it becomes more orally active and bioavailable; without this process, the anabolic steroid will not survive liver metabolism.

However, the negative downside of this is increased hepatotoxicity (increased liver toxicity).

C17-alpha alkylation makes anabolic steroids more resistant to hepatic degradation, and compounds that are more resistant to hepatic degradation are always accompanied by greater hepatotoxicity for a variety of reasons.

Figure 2: A methyl group with a central carbon atom bonded to three hydrogen atoms, with one hole available for binding to a steroid molecule.

Shown above is testosterone without methylation (C17-alpha alkylation) and next to it is an image of methyltestosterone, which is testosterone that has been C17-alpha alkylated to make it more orally bioavailable and survive liver metabolism.

The added methyl group is shown as a broken red line forming an arrow-shaped dot at the 17th carbon position, indicating that the methyl group is located behind the visible orientation of the shown molecule (a solid line forming an arrow-shaped dot indicates that the methyl group is located in front of the visible orientation of the molecule).

The C17-alpha alkylation of anabolic steroids therefore imposes some restrictions on how they can be utilized, how long they can be used, and how oral steroids can be administered.

These restrictions are related to their hepatotoxic effects on the liver and their detrimental effects on cholesterol levels in the body.

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The following is a list of the most popular and most common C17-alpha alkylated oral steroids

- Dianabol (Methandrostenolone)

- Winstrol (stanozolol)

- Anavar (Oxandrolone)

- Anadrol (Oxymetholone)

- Turinabol (chlorodihydromethyltestosterone)

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Oral steroids and hepatotoxicity (liver toxicity)

It is important to understand that not all C17-alpha alkylated oral steroids exhibit the same amount or level of hepatotoxicity.

There are some oral steroids that are known to be quite hepatotoxic (e.g. Anadrol, aka Oxymetholone), while others are known to be fairly mildly hepatotoxic (e.g. Anavar, aka Oxandrolone).

While the determinants of which oral steroids are more hepatotoxic than others are controversial and not known with 100% certainty, it is understood that various anabolic steroids are naturally more resistant to hepatic metabolism prior to undergoing methylation and more resistant to hepatic metabolism after methylation.

A perfect example of this is Trenbolone, an injectable anabolic steroid that does not undergo C17-alpha alkylation and does not exhibit notable hepatotoxicity on its own.

However, it is known to be fairly resistant to hepatic metabolism on its own.

When it undergoes C17-alpha alkylation to produce methyltrienolone, it exhibits the most extreme level of liver toxicity ever reported and is virtually unusable.

The resistance to hepatic metabolism is so great that in a study conducted in 1966, it was found to be the most hepatotoxic oral steroid ever recorded and was classified as "extremely hepatotoxic" [1].

All C17-alpha alkylated oral steroids have shown at least some degree of hepatotoxicity in studies, and it is important to note that the doses used in many of these studies were medical therapeutic prescription doses, which are typically much lower than the doses of oral steroids needed for athletic performance and physique enhancement.

Dianabol, the most popular oral anabolic steroid, is undoubtedly a perfect example.

Studies have shown that bromosulfalane levels (a marker of increased liver burden) are elevated when Dianabol is taken at doses of 15mg or more per day, while liver burden is minimized when Dianabol is taken at doses of 10mg or less per day [2].

This means that the hepatotoxicity of Dianabol will always increase in proportion to the dose used, which is the case with all oral steroids that are C17-alpha alkylated.

Looking at how the doses in the aforementioned studies correlate to actual bodybuilding doses, it's easy to see how liver toxicity could potentially be a problem, considering that the minimum beginner dosage for bodybuilding purposes for anabolic steroids like Dianabol averages over 25mg per day.

The most common form of hepatotoxicity caused by excessive oral anabolic steroid use is a condition known as cholestasis [3].

Cholestasis is a condition in which the flow of bile from the liver is completely stopped or at least interrupted.

This can be caused by a physical blockage or a chemical blockage (as in the case of anabolic steroid-induced hepatic cholestasis).

What happens here is that the blockage or chemical disorder causes a buildup of bile salts and bilirubin in the liver and bloodstream.

If they build up in sufficiently large amounts, they can become toxic to the liver cells and kill them.

The severity of this condition can range from very mild and uncomfortable to life-threatening.

Mild cases can recover within a few weeks, but severe cases can require months or more of recovery time.

Overuse of oral steroid doses and oral steroid cycles can, and has in the past, caused very serious liver problems that can be life-threatening.

Many people have developed liver cysts, hepatocellular necrotic lesions (scarring of the liver tissue due to the death of liver cells), and in rare cases, hepatic angiocarcinoma and hepatocellular carcinoma (liver cancer).

These symptoms have been found in two bodybuilders who took high doses of oral anabolic steroids [4], and one death has been reported [5].

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Oral Steroids and Negative Cholesterol Changes

It is a well-known fact that anabolic steroids can cause negative cholesterol changes in the body, with different anabolic steroids exhibiting these changes to a lesser or greater degree, and some anabolic steroids even exhibiting the ability to change cholesterol levels in a positive way (although this is very rare).

For oral steroids, the negative effects on cholesterol levels are actually the most severe of all types of anabolic steroids.

These changes include a decrease in HDL (good cholesterol) and an increase in LDL (bad cholesterol).

The result of these changes is an increased risk of atherosclerosis, and the degree of these changes is generally dose dependent (the higher the dose, the greater the negative changes and risk).

Other factors that influence these negative cholesterol changes include duration of use and route of administration.

It is for this reason that oral anabolic steroids have a negative reputation for having a much worse effect on cholesterol than injectable anabolic steroids.

This is because the liver acts as the body's cholesterol processing center, and the increased liver toxicity associated with anabolic steroids exacerbates the negative changes in cholesterol.

Anabolic steroids have a strong effect on increasing an enzyme called hepatic lipase, which is an enzyme that actively metabolizes and breaks down 'good' HDL cholesterol in the liver [6].

As a result, there is less HDL cholesterol circulating in the body during anabolic steroid use.

To get the "big picture" and properly represent what's going on, we need to compare the differences in the effects of injectable and oral steroids on cholesterol changes.

First, we will examine injectable steroids and their effects on cholesterol levels.

Testosterone cypionate, an injectable non-alkylated anabolic steroid, was shown to reduce cholesterol levels by 21% in a study at a dose of 300 mg per week [7], and increasing to 600 mg per week did not result in any further reduction in HDL.

This data suggests that the effects of injectable testosterone on cholesterol changes are not very pronounced, and that there is a very low upper limit to how much negative change in HDL will occur.

Oral steroids such as Winstrol (stanozolol), an anabolic steroid that is generally considered to be much "milder" than testosterone, do not seem to be as "mild" in the realm of negative cholesterol changes.

For example, in one study, oral Winstrol at the extremely low dose of 6 mg daily for six weeks was associated with an average decrease in HDL cholesterol levels of 33-71% and an increase in 'bad' LDL cholesterol of 29%.

In the same study, 200 mg of testosterone enanthate resulted in only a 9% reduction in HDL cholesterol and a 16% reduction in LDL cholesterol [8].

It is very clear that the negative effects of oral steroids on cholesterol are significant enough to be of concern.

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Limitations of Oral Steroids

Due to the prominent issues of hepatotoxicity and negative cholesterol changes, it is a very wise decision to only take oral steroids for no more than 6-8 weeks in a cycle, and in fact, this is what medical organizations recommend in their prescribing guidelines for oral steroid use.

This is to ensure healthy liver function and to allow for proper liver recovery after administration.

Various oral steroids, which are known to be more hepatotoxic than others, are recommended to be used in the 4-6 week range, while others can be used in the 6-8 week range and some can be used slightly longer (up to 10 weeks).

Due diligence should always be performed in terms of proper liver function and liver health when using oral anabolic steroids.

Due to the risk of hepatotoxicity, the primary function of oral steroids in any cycle is to act as an ancillary or secondary starting compound to the solid injectable base.

Oral steroids should never be used on their own.

Testosterone in any form, above TRT (testosterone replacement therapy) doses, should always be administered in conjunction with oral steroids.

Oral steroids, like other anabolic steroids, severely suppress endogenous testosterone production, even oral steroids such as Anavar, which is considered a 'mild' compound [9].

Therefore, testosterone must always be used in some form, every cycle, to maintain normal physiological functioning of the body's hypothalamic-pituitary-testicular axis (HPTA) and during periods when exogenous hormones that suppress and/or block endogenous testosterone production are used.

All individuals (especially beginners) should understand the following very important guidelines regarding the use of anabolic steroids:

Under no circumstances should a cycle be composed solely of oral anabolic steroids.

The decision to run a cycle consisting of only one anabolic steroid without the use of injectable compounds is usually the first decision made by beginners or prospective users who want to start using anabolic steroids.

This is usually due to a fear of needles, but this is something that must be overcome, and once overcome, it becomes much easier from there on out.

Oral anabolic steroids are not designed to be used alone (by themselves), instead they act as ancillary compounds to a solid base cycle that should always include injectable compounds, of which the essential injectable compound is testosterone (for every cycle).

The injectable compound is the base compound for every cycle.

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For those of you who insist and stick to oral-only cycles, we'll outline a few examples at the end of this article.

Kickstarting

'Kickstarting' is a method that should be used when a beginner has gained enough cycle experience to stack oral anabolic steroids with other compounds.

It is a technique in which the user includes oral anabolic steroids in their cycle for the first few weeks (usually in conjunction with injectable anabolic steroids that are taken over a longer period of time due to the long kick-in period).

The kick-in period for most injectables (especially long esters) is several weeks in a cycle, so you typically won't experience any positive effects until then.

Using oral anabolic steroids for the first few weeks will allow you to experience the positive anabolic effects of oral while the effects of injectable compounds slowly increase.

By the time you discontinue the oral compound (or near the end of its use), the anabolic effects of the injectable compound will be in full force and the transition will be almost seamless.

Dianabol is one anabolic steroid that is commonly utilized as a kickstart compound for this effect due to its significant anabolic strength.

Example of an Oral Steroid Cycle

(as a kickstart to a supplemental ingredient or injectable compound base)

Oral Steroid Cycle Example #1