Category: Blog

As can be surmised by the commonly used term anti-estrogen, the primary goal of therapy with an estrogen maintenance drug is to block the side effects associated with this hormone from becoming apparent during steroid use (though often they are also used at the conclusion of a cycle to help restore the release of endogenous testosterone). For the purpose of combating estrogen a number of substances have been used successfully over the years, and more have recently become available due to advances in the field of breast cancer research (treatment of breast cancer is the primary clinical use for most of these agents).
Likewise the athlete now has several pharmaceutical options to select from when shopping, which can make the choice of what drug may be best for any particular case a confusing one. Since a number of issues including cost, availability, potential side effects and efficacy may factor into this decision, I thought a closer look at both the old and newer agents might be in order.
Aromatization is the technical term for it. It is a natural process in which an androgen (male sex hormone) such as testosterone can be converted to an estrogen (female sex hormone) in the human body. In normal situations of course the male body will produce estrogens only in very small amounts, though they still do play an important role metabolically (including visceral/organ fat disposition, bone growth/maturity and blood lipid regulation). Athletes however may find that estrogen can become an extremely dramatic problem with the administration of anabolic/androgenic steroids. With the natural process of aromatization in place, and extremely heightened androgen level can result in a troubling buildup of estrogens. This may cause the onset of estrogen related side effects such as
noticeable fat and water retention, as well as the buildup of female breast tissue (gynecomastia). Gynecomastia is a particularly upsetting occurrence for the steroid-using male athlete, as the characteristic unsightly buildup of tissue mass is usually permanent. Although many synthetic anabolic agents are resistant or not open to the process of aromatization at all, our standard bulking drugs such as testosterone and Dianabol are still readily aromatized. This has prompted the athletic community to seek the benefit of estrogen maintenance drugs when taking such steroids, a class of medications that are now considered standard remedies in the athletes’ drug arsenal.

Nolvadex and Clomid

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 anti-estrogen 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. 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. 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 (though admittedly Nolvadex may be slightly more potent in both regards).

Aromatase Inhibitors

Aromatase inhibitors are another, perhaps more direct, way of dealing with estrogen in the body. Instead of blocking estrogen at its receptor, these agents have the more direct task of targeting the enzyme responsible (aromatase) for the biosynthesis of estrogen. By inhibiting this enzyme, circulating levels of estrogen can be efficiently and significantly reduced. Athletes will likewise find that the more recently developed aromatase inhibitors are the most potent remedies available for the prevention of related side effects. Before detailing the various inhibitors of aromatase it is important to discuss further the potential drawbacks to this type of therapy. The most prominent being a negative impact on cholesterol profiles. Although steroid use is of course expected to negatively effect cholesterol levels, we find that when aromatization is inhibited this harmful tendency is greatly enhanced.
Alternately choosing an antiestrogen such as Nolvadex however does not offer us a 100% guarantee that lipid values will not worsen over using no estrogen maintenance drug at all. In studies combining tamoxifen with estrogen replacement therapy for instance, it was shown that this compound could interfere with the beneficial effects of estrogen-based drugs on lipid values, though not completely diminish them. Since the effects of Nolvadex during treatment with a steroid such as testosterone have not been fully investigated (admittedly it is a small and not legitimately supported corner of use for tamoxifen), it remains to be seen whether or not it is truly beneficial in terms of lipid values when given with an aromatizable steroid. For now however, should an estrogen maintenance drug be
indicated, we can still consider it to be a safer alternative to any of the following aromatase inhibitors.

Proviron (mesterolone)

Proviron is not technically classified as an anti-aromatase, but is an oral androgenic steroid. Specifically it contains a derivative of the potent steroid dihydrotestosterone, differing only by the addition of 1 methylation (the same alteration used to increase the oral efficacy of Primobolan). Its use as an antiaromatase stems from studies showing a nonaromatizing androgen such as dihydrotestosterone may interfere with this enzyme reaction. It is believed to interfere with aromatase by competing with an aromatizable steroid such as testosterone for binding to the enzyme site. With dihydrotestosterone (or Proviron) interacting with this enzyme, yet producing no reaction, the enzyme is temporally prevented from altering other hormones, and an anti-estrogenic effect is achieved.
Overall however, Proviron is much less reliable than any one of the mentioned antiestrogens or aromatase inhibitors. Though it may add some benefit when taken concurrently with a drug such as tamoxifen (though in such a case tamoxifen would be doing most of the work), I don’t think that it is potent enough as an aromatase inhibitor to recommend using along during strong cycles.

Arimidex (anastrozole)

Anastrozole is a much more recently developed, selective, non-steroidal aromatase inhibitor. It represents quite an advance in breast cancer treatments, as it can efficiently block aromatase activity without affecting enzymes involved in the biosynthesis of other adrenal steroids (hence the term selective). Its activity is therefore much more specific than aminoglutethimide, a trait that also makes it more tolerable for the patient. Numerous studies also support the superiority of this inhibitor over previously prescribed treatments, including many in which patients responded favorably to anastrozole (as a second-line therapy) after ceasing to respond to tamoxifen. In fact of all the aromatase inhibitors discussed in this article, Arimidex is shown to be the most effective and reliable.
The recommended dosage for anastrozole clinically is a single 1mg tablet daily. This is the lowest dose shown to produce maximum suppression of estrogen levels, and to spite expectations of greater results, doses of up to 10mg daily were not shown to appreciably increase the long-term response rate. In many cases the 1mg dose will produce estrogen suppression near 100%, so there seems to be little need for the athlete to venture higher.

Gaining muscle mass! Now this goal depends highly on how advanced one already is as a trainer and/or steroid user. Someone who is already 40 lb. more muscular than he could achieve naturally, and who wishes to add still more for the purposes of competitive bodybuilding, will simply find no use from a recommendation to use 500 mg/week of Sustanon. At best such a dose might allow him to maintain what he has, instead of slowly losing muscle while off drugs. Such an athlete will probably not achieve his goals with less than a gram per week of injectables, stacked with at least 50 mg/day of orals. And he may need more than this. He is already far beyond what he could attain naturally, and more yet will not come easily. What of the person who, after several years of hard, quality training, is probably fairly close to his genetic limit under natural conditions? He would probably achieve excellent results with this same 500 mg/week dose of Sustanon, and undoubtedly would do so with some Dianabol added as well. Another person may not even be close to his natural genetic limit in the first place, due to inconsistent or poor training, or novice status. Such a person can make excellent gains without anabolic/androgenic steroids (AAS) at all, and while AAS can increase the rate of gains, one cannot say that any particular drug regimen is necessary or advisable. Yet another person, who simply wishes to have an attractive physique and appearance by conventional standards, and highly values the condition of his skin and hair, would be poorly served by the advice to use Sustanon or Dianabol at any dose. The likely worsening of his skin and possible acceleration of hair loss would not be worth it. He would be better served with a milder drug, which would allow him to achieve his goals with minimal cosmetic or health risk.

If this is your first use, then reconstitute the vial with bacteriostatic water or load and prime the auto-injector device.

Do not shake or tap the growth hormone medication forcefully because it will be inactivated.

Here is an easy step-by-step guide to the injection process:
* Select an injection site and disinfect it with alcohol wipes/swabs.
* If your product is in a vial, then replace the needle for reconstitution with another sterile one for subcutaneous injections. Then pinch your skin with the fingertips of your non-dominant hand and stick the whole needle with your dominant hand under 45°.
* If you are using a pen, then attach a sterile needle to the device and stick it under 90°.
* Press the button/stopper and hold it with the needle inside for a few seconds.
* After you pull the needle out, put sterile gauze and a bandage on top. Do not press or massage the injection site.
* Discard the used needle and the syringe in the container for sharp materials without recapping. Throwing sharp materials in regular waste puts the health of people who handle that waste at risk. Always use new sterile needles for the next injections.

Now let’s clear up the preparatory part of the injection process. First of all, you check if the medication is suitable for use. After reconstitution, growth hormone should be a clear and colorless liquid.

Besides, you should make sure that the injection site you have chosen is clear too. Switch to another one if there is reddening, swelling, pain, wounds, rashes, or signs of inflammation in the area.

When starting therapy you should be able to choose from several different HGH preparations including:

Vials containing powder
Preloaded and prefilled pens
Chambers for use in auto-injector devices

No matter which preparation you will use, growth hormone should be injected into the fat tissue under your skin (subcutaneous). This type of injection provides the best bioavailability and rate of absorption for HGH.

If you use growth hormone in a vial, then the powder should be first reconstituted into a liquid using a regular needle and syringe. Then the injection is performed using the lifted skinfold technique.

The method requires you to pinch your skin and insert the needle (a new needle suitable for subcutaneous injections) at a 45° angle.

When using an auto-injector device such as an HGH pen, there is no need to pinch and lift the skin. All you have to do is inject at a 90° angle (holding the pen perpendicular to your skin).

The best results of HGH therapy can be achieved by injecting the medication at the same time every day and creating a habit.

The best time for you will depend on your personal routine. Yet, small studies suggest that injecting before sleep may lead to a slightly better physiological pattern of growth hormone release in the body.

Once you begin to prepare to inject the medication, you will need the following items:

Alcohol wipes/swabs
Sterile gauze
Bandage
Container for sharp materials
Injector pen with suitable needles

If you will inject growth hormone from a regular vial that requires reconstitution, then instead of an auto-injector device you will need:

Vial with HGH
Vial with diluent (bacteriostatic water)
Sterile syringe
Sterile needle for withdrawal
Sterile needle for subcutaneous injections

Subcutaneous injections typically can be administered at several areas:

The abdominal area around the belly button
Outer upper arms
Front outer thighs
Lower loins

The best place to inject HGH is in the abdominal area. Also, it’s much more convenient than other injection sites. Furthermore, studies report that injecting in that area causes less pain.

Another method to reduce the sensation of pain during an injection is to ensure that the growth hormone solution is not too cold (if it was stored in the fridge). Therefore, you should leave HGH vials, pens, or cartridges at room temperature for 30 minutes before injection.

Auto-injector pens require thinner and smaller needles which also helps minimize pain. Your sensation also depends on the total volume injected – lower than 0.8ml is tolerated the most amongst patients.

Here are several extra tips from our medical specialists on how to reduce pain and discomfort during a growth hormone injection:

Apply pain-numbing cream or ice to your skin before the injection
Relax your muscles in the injection area to pinch your skin more easily
When injecting at a 45° angle, turn the bevel of the needle up to prevent skin tearing.
Pierce through your skin with a single swift motion
Don’t change the direction of the needle while going in or out of your skin
Push the plunger of the syringe slowly

According to research, local skin reactions are common after HGH injections and involve transitory complaints such as redness, short-term bleeding, pain, discomfort, and swelling. They resolve spontaneously without treatment.

Make sure to keep a list of the sites where you inject and rotate these sites frequently. Scientists warn that injecting repeatedly on the same spot can lead to the formation of a dent in the area due to lipoatrophy (localized fat loss).

Subcutaneous injections are the easiest method to self-inject a substance at home. The method provides a lower risk of pain, infection, or complications.

In the case of inappropriate technique, there is a risk of injecting the medication within the layers of the skin or in a blood vessel instead of subcutaneously.

This may significantly diminish the effectiveness of the medication but without a higher risk of adverse reactions.

Injecting an air bubble subcutaneously is also not dangerous since the gases can get absorbed from the tissues.

Concerning side-effects include allergic reactions, continuous bleeding, and numbness in the limb.

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.

There are many different esters that are used with anabolic/androgenic steroids, but again, they all do basically the same thing. Esters vary only in their ability to reduce a steroid’s water solubility. An ester like propionate for example will slow the release of a steroid for a few days, while the duration will be weeks with a decanoate ester. Esters have no effect on the tendency for the parent steroid to convert to estrogen or DHT (dihydrotestosterone: a more potent
metabolite) nor will it effect the overall muscle-building potency of the compound. Any differences in results and side effects that may be noted by bodybuilders who have used various esterified versions of the same base steroid are just issues of timing. Testosterone enanthate causes estrogen related problems more readily than Sustanon, simply because with enanthate testosterone levels will peak and trough much sooner (1-2 week release duration as opposed to 3 or 4).

Propionate:
Also referred to as Carboxyethane; hydroacrylic acid; Propionic Acid. Propionate esters will slow the release of a steroid for several days. To keep blood levels from fluctuating greatly, propionate compounds are usually injected two to three times weekly. Testosterone propionate and methandriol dipropionate (two separate propionate esters attached to the parent steroid methandriol) are popular items.

Phenylpropionate:
Also referred to as Propionic Acid Phenyl Ester. Phenylpropionate will extend the release of active steroid a few days longer than propionate. To keep blood levels even, injections are given at least twice weekly. Durabolin is the drug most commonly seen with a phenylpropionate ester (nandrolone phenylpropionate), although it is also used with testosterone in Sustanon and Omnadren.

Isocarpoate:
Also referred to as Isocaproic Acid; isohexanoate; Isocaproate begins to near enanthate in terms of release. The duration is still shorter, with a notable hormone level being sustained for approximately one week. This ester is used with testosterone in the blended
products Sustanon and Omnadren.

Enanthate:
Also referred to as heptanoic acid; enanthic acid; enanthylic acid. Enanthate is one of the most prominent esters used in steroid manufacture (most commonly seen with testosterone but is also used in other compounds like Primobolan Depot). Enanthate will release a steady (yet fluctuating as all esters are) level of hormone for approximately 10-14 days. Although in medicine enanthate compounds are often injected on a bi-weekly or monthly basis, athletes will inject at least weekly to help maintain a uniform blood level.

Cypionate:
Also referred to as Cyclopentylpropionic acid, cyclopentylpropionate. Cypionate is a very popular ester. Its release duration is almost identical to enanthate (10-14 days), and the two are likewise thought to be interchangeable. Athletes commonly hold the belief than cypionate is more powerful than enanthate, although realistically there is little difference between the two. The enanthate ester is in fact slightly smaller than cypionate, and it therefore releases a small (perhaps a few milligrams) amount of steroid more in comparison.

Decanoate:
Also referred to as decanoic acid; capric acid; Nonanecarboxylic acid. The Decanoate ester is most commonly used with the hormone nandrolone (as in Deca-Durabolin) and is found in virtually all corners of the world. Testosterone decanoate is also the longest acting constituent in Sustanon, greatly extending its release duration. The release time with Decanoate compounds is listed to be as long as one month, although most recently we are finding that levels seem to drop significantly after two weeks. To keep blood levels more uniform, athletes will follow a weekly injection schedule.

Undecylenate:
Also referred to as Undecylenic acid; Hendecenoic acid. This ester is very similar to decanoate, containing only one carbon atom more. Its release duration is likewise very similar (approximately 2-3 weeks), perhaps extending a day or so past that seen with decanoate. Undecylenate seems to be exclusive to the veterinary preparation Equipoise (boldenone undecylenate), although there is no reason it would not work well in human-use preparations
(Equipoise certainly works fine for athletes). Again, weekly injections are most common.