WHAT AN ESTER IS, AND HOW IT WORKS

I'm sure that if you have taken an interest in anabolic steroids you have noticed the similarities on the labeling of many drugs. Let's look at testosterone for example. One can find compounds like testosterone cypionate, enanthate, propionate, heptylate; caproate, phenylpropionate, isocaproate, decanoate, acetate, the list goes on and on. In all such cases the parent hormone is testosterone, which had been modified by adding an ester (enanthate, propionate etc.) to its structure. The following question arises: What is the difference between the various esterified versions of testosterone in regards to their use in bodybuilding?

An ester is a chain composed primarily of carbon and hydrogen atoms. This chain is typically attached to the parent steroid hormone at the 17th carbon position (beta orientation), although some compounds do carry esters at position 3 (for the purposes of this article it is not crucial to understand the exact position of the ester).

Esterification of an injectable anabolic/androgenic steroid basically accomplishes one thing, it slows the release of the parent steroid from the site of injection. This happens because the ester will notably lower the water solubility of the steroid, and increase its lipid (fat) solubility. This will cause the drug to form a deposit in the muscle tissue, from which it will slowly enter into circulation as it is picked up in small quantities by the blood. Generally, the longer the ester chain, the lower the water solubility of the compound, and the longer it will take to for the full dosage to reach general circulation.

Slowing the release of the parent steroid is a great benefit in steroid medicine, as free testosterone (or other steroid hormones) previously would remain active in the body for a very short period of time (typically hours). This would necessitate an unpleasant daily injection schedule if one wished to maintain a continuous elevation of testosterone (the goal of testosterone replacement therapy). By adding an ester, the patient can visit the doctor as infrequently as once per month for his injection, instead of having to constantly re-administer the drug to achieve a therapeutic effect. Clearly without the use of an ester, therapy with an injectable anabolic/androgen would be much more difficult.

Esterification temporarily deactivates the steroid molecule. With a chain blocking the 17th beta position, binding to the androgen receptor is not possible (it can exert no activity in the body).

In order for the compound to become active the ester must therefore first be removed. This automatically occurs once the compound has filtered into blood circulation, where esterase enzymes quickly cleave off (hydrolyze) the ester chain. This will restore the necessary hydroxyl (OH) group at the 17th beta position, enabling the drug to attach to the appropriate receptor. Now and only now will the steroid be able to have an effect on skeletal muscle tissue. You can start to see why considering testosterone cypionate much more potent than enanthate makes little sense, as your muscles are seeing only free testosterone no matter what ester was used to deploy it.

Cedric McMillan - 2013 Fibo Power Germany Contest Winner

It was the third professional win of McMillan’s career. The 2009 NPC Nationals Overall winner, McMillan has now won at least one contest in each of his first three years in the IFBB.
Defending champion Johnnie Jackson placed second. It was the third straight top-five finish for Jackson, who was coming off a career-best fourth place at the Arnold Classic. Ed Nunn (3rd), Robert Piotrkiwocz (4th) and Ronny Rockel (5th) rounded out the top five. Only three points separated Nunn, Piotrkiwicz and Rockel on the scoresheets.
In Fitness, Bethany Cisternino won the second contest of her pro career. Cisternino’s first win came at the 2010 Europa Super Show. Since then she has been a consistent top-five finisher. Cisternino, who was coming off a career-best third at the Fitness International, placed in the top five of four contests in 2012.
It doesn’t get any closer than it did in the battle for second between Ryall Graber-Vasani and Regiane DaSilva. Each finished with 36 total points on the final scoresheets, with Vasani winning the tiebreaker to earn the runner-up spot. DaSilva, the 2011 FIBO Fitness champ, placed third. Whitney Jones (4th) and Kizzy Vaines (5th) rounded out the top five.

General Guidelines to HIT BRIEF, HARD work done INFREQUENTLY.

When you're in the gym you want to focus your energies on only performing work that is productive, i.e., growth producing. In good form, you push yourself as far as you can go on every set. Now, by training this way you simply CANNOT do the marathon 2-3 hour workouts the "champs" say they do in the muscle mags.
HIT can be summed up in the following GENERAL guidelines. These guidelines - or ones very similar - have formed the basis of strength training programs for years:

1. TRAIN WITH A HIGH LEVEL OF INTENSITY.
Intensity is defined as "a percentage of momentary ability". In other words, intensity relates to the degree of "inroad" or muscular fatigue, made into muscle at any given instant. Research, going back almost 100 years now to studies done by German scientists, has conclusively shown that intensity is the SINGLE MOST IMPORTANT FACTOR in obtaining results from strength training.
It has been shown that the HARDER that you train (intensity), the GREATER the adaptive response. A high level of intensity is characterized by performing an exercise to the point of concentric (positive) MUSCULAR FAILURE, i.e., you've exhausted your muscles to the extent that the weight cannot be moved for any more repetitions. Failure to reach a desirable level of intensity - or muscular fatigue - will result in little or no gains in functional strength or muscular size as low intensity workouts do very little or nothing in the way of stimulating muscle size/strength.
Evidence for this "threshold" is suggested in the literature by the OVERLOAD PRINCIPLE (Enoka, 1988; Fox and Mathews, 1981; Hochschuler, Cotler and Guyer, 1993; Jones, 1988; Wilmore 1982).
Essentially this principle states that in order to increase muscular size and strength, a muscle must be stressed - or "overloaded" with a workload that is beyond its present capacity. Your intensity of effort must be great enough to exceed this threshold level so that a sufficient amount of muscular fatigue is produced.

2. FOLLOW THE "DOUBLE PROGRESSION" TECHNIQUE IN REGARDS TO REPETITIONS AND WEIGHT.
For a muscle to increase in size and strength it must be forced to do PROGRESSIVELY HARDER WORK. Your muscles must be overloaded with a workload that is increased steadily and systematically throughout the course of your program. This is often referred to as PROGRESSIVE OVERLOAD. Therefore every time you work out you should attempt to increase either the weight you use or the repetitions you perform relative to your previous workout. This can be viewed as a "double progressive" technique (resistance and repetitions). Challenging your muscles in this manner will force them to adapt to the imposed demands (or stress).

3. PERFORM 1 TO 3 SETS OF EACH EXERCISE.
In order for a muscle to increase in size/strength it must be fatigued or OVERLOADED in order for an adaptive response to occur. It really doesn't matter whether you fatigue your muscles in one set or several sets - as long as your muscles experience a certain level of exhaustion. When performing multiple sets, the cumulative effect of each successive set makes deeper inroads into your muscle thereby creating muscular fatigue; when performing a single set to failure, the cumulative effect of each successive repetition makes deeper inroads into your muscle thereby creating muscular fatigue. Numerous research studies have shown that there are NO significant differences when performing either one, two or three sets of an exercise, provided, of course, that one is done with an appropriate level of intensity (i.e. to the point of concentric muscular
failure).

4. REACH CONCENTRIC MUSCULAR FAILURE WITHIN A PRESCRIBED NUMBER OF REPETITIONS.
As stated above, research shows that our level of intensity is the most important factor in determining your results from strength training - the HARDER you train, the BETTER your response.
As muscle hypertrophy is an adaptive response by the body to stress, you should always strive to go as far as you can go on that "impossible" rep. Every centimeter matters. Your "impossible" rep should last between 10-15 seconds. One could even call this an "isometric rep". If concentric muscular failure occurs before you reach the lower level of the repetition range, the weight is too heavy and should be reduced for your next workout. If the upper level of the repetition range is exceeded before you experience muscular exhaustion, the weight is too light and should be increased for your next workout by five percent or less.
The GENERAL recommendation is 8-12 repetitions But this can vary from individual to individual, and from body part to body part. In many cases people have been known to benefit from higher reps for their lower body (12-15), while lower reps for the upper body (6-8). The most important thing to remember here is that it the *number* of repetitions isn't the key factor - TIME is. One can perform a set of 10 reps in as low as 10-15 seconds, or a set of only 1 rep in 60 seconds. So how many seconds per repetition? The general guideline is a 6 second repetition consisting of a 2 second lifting (concentric) phase, followed by a 4 second lowering (eccentric) phase. The emphasis
is placed on the lowering, or NEGATIVE, as research has shown this to be the most productive part of the rep.

The lowering of the weight should also be emphasized because it makes the exercise more efficient: the same muscles that are used to raise the weight concentrically are also used to lower it eccentrically. The only difference is that when you raise a weight, your muscles are shortening against tension and when you lower a weight, your muscles are lengthening against tension. So, by emphasizing the lowering of the weight, each repetition becomes more efficient and each set becomes more productive. Because a muscle under tension lengthens as you lower it, lowering the weight in a controlled manner also ensures that the exercised muscle is being stretched properly and safely. Thus in a 8-12 rep scheme with the above guidelines, each set should take you between 48-72 seconds until you reach concentric muscular failure.

General Guidelines to HIT BRIEF, HARD work done INFREQUENTLY. (part 2)

5. TRAIN FOR NO MORE THAN ONE HOUR PER WORKOUT.
If you are training with a high level of intensity, more than one hour is counterproductive as it increases the probability of overtraining due to a catabolic hormone called cortisol. Overtraining, next to injury, is your worst enemy. Avoid it like the plague. In addition, the faster you can complete your workout, given the same amount of sets performed, the BETTER CONDITIONING obtained.

6. MOVE QUICKLY BETWEEN SETS
The transition time between each set varies with your level of conditioning. You should proceed from one exercise to the next as soon as you catch your breath or feel that you can produce a maximal level of effort. After an initial period of adjustment, you should be able to recover adequately within 1 to 3 minutes. Training with a minimal amount of recovery time between exercises will elicit a metabolic conditioning effect that cannot be approached by traditional multiple set programs.

7. EXERCISE THE MAJOR MUSCLE GROUPS FIRST.
The emphasis of your exercises should be your major muscle groups (i.e. your hips, legs and upper torso). You should select any exercises that you prefer in order to train those body parts. It is recommended that lower body work be done first, as it is more taxing. This is not always the case, as a technique for bringing up a lagging body part is to work it first in your routine, but it is a general outline.

8. DO NOT SPLIT YOUR ROUTINE - DO NOT WORK YOUR BODY ON SUCCESSIVE DAYS
Many bodybuilders practice a split routine. The reasoning is that training their upper body on one day and lower body on the next day allows them additional time to work each muscle group "harder". HIT advocates fervently believe that this is NOT the case. First, split routines lead you to believe that *more* exercise is better exercise. Remember HARDER exercise is better. And if you train harder you MUST train briefer, not longer. You cannot train hard for a long period of time. Thus, out of physiologic necessity, people who use a split routine have to reduce the intensity of their exercise which leads to less growth stimulation.

9. GET AMPLE REST AFTER EACH TRAINING SESSION
Believe it or not, your muscles DON'T get stronger while you work out. Your muscles get stronger while you RECOVER from your workout. After high intensity training your muscle tissue is broken down (although that's a very basic way of describing it) and the recovery process allows your muscle time to rebuild itself.

10. AS YOU GET STRONGER DECREASE THE FREQUENCY OF WORKOUTS AND/OR AMOUNT OF SETS
Exercise physiologists have found that your strength increases disproportionately to your recovery ability. Thus the stronger you get the LESS high intensity exercise you can tolerate. Some authorities, such as Dr. Ellington Darden, mention a "300/50%" ratio of strength to recovery ability potential. Thus in theory, the average trainee has the potential to increase his untrained strength by a factor of 4, but his recovery ability will only increase by a factor of 1.5.

What is "HIT"?

The acronym "HIT" stands for HIGH INTENSITY TRAINING. HIT simply means organizing your workouts so that they are:

1. HARD - as hard as possible IN GOOD FORM.
2. BRIEF - 1-3 sets of a few basic exercises performed in an hour or less.
3. INFREQUENT - No more than three times per week, often times two, or even one.
4. SAFE - HIT is meant to be extremely productive in terms of size/strength gains AND also has a built-in safety component. One of the fundamental goals of strength training is to act as INJURY PREVENTATIVE

HIT is a disciplined style of training which is based on the two universally known factors affecting muscular growth - OVERLOAD and PROGRESSION.

The reps should be done in a controlled fashion so tension is placed on the muscles. Some use a 2 second count for the concentric (lifting) phase while others use a 20 second count. The key is performing QUALITY repetitions to a point of volitional fatigue.

One set IS productive, although some high intensity advocates sometimes choose to perform more than one set. Some people may require additional sets. As a general rule, with of course some exceptions, one set performed in a high intensity manner will provide all the stimulation you need.

Nolvadex and Clomid (estrogen receptor antagonists)

Estrogen receptor antagonists, more simply referred to as anti-estrogens (though this term is often loosely applied to all estrogen maintenance drugs), are drugs that block estrogens from exerting activity in the body. This is actualized by the ability of a particular substance to bind to a segment of the estrogen receptor, yet not activate it. This in turn prevents other estrogens from binding and activating the same receptor site. In a clinical setting an estrogen antagonist, most prominently the drug tamoxifen citrate (sold under the brand name Nolvadex) is typically used as the first line of defense during advanced breast cancer therapy. Its use can efficiently deprive estrogen responsive cancer cells of necessary hormone, allowing a high rate of response in patients with such forms of cancer.
Stronger agents such as aromatase inhibitors (discussed below) are usually a second choice, substituted when conventional antiestrogen therapy fails to elicit the desired response.
A drug like tamoxifen is preferred over other agents as the first course of breast cancer treatment for a number of reasons, most due to the fact that that it is both extremely effective yet does not inhibit the actual formation of estrogen in the body. Among other things, this may allow Nolvadex therapy to be somewhat more comfortable for the patient. Although many women (particularly pre-menopausal) seem to suffer menopausal-like side effects with virtually all estrogen maintenance drugs, estrogen antagonists are often somewhat more tolerable than agents that block the synthesis of estrogen. In fact the activity of tamoxifen is itself variable, such that in certain target tissues it may actually act as an agonist (activator) of the estrogen receptor. It therefore does not completely diminish the biological activity of estrogens, though it does considerably reduce it nonetheless.
It is also well understood in medicine today that estrogens play a supportive role in the cardiovascular system. For example, studies show that a rise in the estrogen level (as in post-menopausal estrogen replacement therapy) is typically linked with a reduction in LDL (bad) cholesterol, and a rise in HDL (good) cholesterol. The ability of tamoxifen to act as an estrogen agonist in the liver likewise gives it what may be its most welcome property, namely that it exhibits an estrogenic, rather than antiestrogenic, effect on blood lipid (cholesterol) values. As a 1998 study by the Department of Clinical Oncology in the Netherlands Cancer Institute shows, during long-term treatment with tamoxifen (6 months) a lowered LDL cholesterol level, and significantly elevated HDL cholesterol level and HDL-C/total-cholesterol ratio may result. This trend should reduce an important risk factor for heart disease, obviously a welcome effect during treatment.
For the steroid-using athlete already faced with negative alterations in lipid profiles, such an effect could obviously an important consideration.
Clomid (clomiphene citrate) is very similar in structure to Nolvadex, both drugs being classified as triphenylethylene compounds and used clinically for similar purposes (breast cancer as well as female infertility treatment). As well as we see with Nolvadex, Clomid is a partial agonist/antagonist of the estrogen receptor depending on the target tissue in question. Although athletes most commonly think of Clomid as a testosterone-stimulating drug only (another effect of antiestrogenic compounds), to be used at the conclusion of steroid treatment, its activity in the human body is not at all dissimilar to Nolvadex. It should likewise be thought of not as a drug with its own niche of use, but instead as another efficient remedy for gynecomastia similar to Nolvadex (with the related ability to support the release of testosterone). It could clearly replace Nolvadex as a preventative measure against gynecomastia during cycles with aromatizable steroids without noticeably altering the level of effect received, just as Nolvadex can be used effectively to increase the synthesis of testosterone in the body at the conclusion of steroid use.

Protein Supplementation

Protein-powder is a very popular supplement, and is available at most local drug and health food stores. Before proteins can be used for muscle hypertrophy in the body, they must be broken down to amino acids in the liver. In the liver, they can be resynthesized into muscle proteins, and transported to the muscles for hypertrophy.
Obviously, if the proper stimulus is given, the more amino acids responsible for muscle growth that are present in the body, the more muscle hypertrophy will occur. Simply put, the more protein in the body, the more muscle hypertrophy will occur.
Studies show that ingestion of protein with carbohydrate increases insulin and/or growth hormone level, thus assisting the process of muscle growth. The intake of protein and carbohydrate before exercise boost the efficiency of the workout and lessens recovery time, allowing the athlete to endure more vigorous training sessions. As much as 1.3 to 1.8 g of protein for every Kg of body mass, or 2.2 g at high altitudes, is recommended for weight trainers per day. It is shown that 20 calories per pound of body mass is required to sustain muscle mass, and 25 to 30 calories per pound to actually build muscle mass. Thirteen to seventeen percent of those calories should come from proteins, with twelve to sixteen percent coming from fats, and the rest obtained from carbohydrates.
Tests show that taking protein supplements along with creatine monohydrate works better than just taking protein supplements alone. The positive effects include leaner tissue mass, and increase in bench press power. Another independent study shows how a combination of protein and creatine helps boost muscle GLUT-4 (glucose transport proteins) matter and increases glucose tolerance in the athlete. Human subjects’ right leg was immobilized for the time period of two weeks, and then resistance exercises were put in place for six weeks. GLUT-4 content was decreased in creatine-taking subjects, creatine and protein-taking subjects, and placebo-taking subjects during the 2 weeks of immobilization. When the resistance exercise program was introduced, the GLUT-4 content in creatine-taking subjects were up by 24%, creatine and protein-taking subjects’ GLUT-4 content were increased by 33%, while placebo-taking subjects’ GLUT- content remained constant. Muscle glycogen content in both creaine-taking and creatine and protein-taking subjects, but not placebo-taking subjects.