Introduction to Prohormones

By David Tolson

Prohormones are substances that are enzymatically converted to anabolic hormones in the body. They are differentiated from anabolic steroids in that enzyme conversion is a rate limiting factor in how strong of a response they illicit. In terms of effect, the results of prohormones are similar to those of steroids – increased muscle mass and strength. Depending on which substance is used, prohormones also have the capability to decrease body fat, increase sex drive, and increase concentration, among many other things. This article will discuss how to use prohormones and briefly review how they work. Future articles will focus on the specifics of certain prohormones.

It is important to emphasize that prohormones are not completely safe or free of side effects, and the decision to use prohormones should not be taken lightly and should be followed by caution and adequate research. This may help reduce or prevent some of the more common side effects such as gynocomastia (bitch tits), prostate enlargement, hair loss, acne, and lethargy and also reduce the chance of serious side effects. However, one should not expect any amount of prohormone use to be side effect free.

Target hormones

Once ingested, prohormones are converted to their active counterparts via either 17-hydroxysteroid dehydrogenase (17HSD) or 3-beta-hydroxysteroid dehydrogenase (3HSD). These are some of the anabolic hormones that prohormones convert to:

* Testosterone: Testosterone is the most well known anabolic hormone. It is very effective but also associated with many side effects, primarily because it converts to both DHT and estradiol. With the increased estrogen comes a risk of gynocomastia, female pattern fat distribution, and increased adipose (fat) mass. Despite the fact that high estrogen levels are not aesthetically pleasing, estrogen can have some anabolic benefits as well (such as increased water retention). Androstenedione and 4-androstenediol (4AD) both convert to testosterone. 4AD is generally considered to be far superior because it has a significantly higher conversion rate and does not directly convert to estrone and DHT as androstenedione does.

* Dihydrotestosterone (DHT): DHT is considered to be a highly androgenic compound, meaning it is associated with the development of secondary sex characteristics. It is not found in high quantities in skeletal muscle but is found in the prostate, skin, sex organs, and brain. High levels of DHT are implicated in acne, hair loss, and prostate enlargement. However, DHT may have a lot to do with the positive effects testosterone has on the central nervous system (such as increased concentration during exercise) and sex drive, and it also protects against excessive estrogen. Users of DHT prohormones commonly report increased muscle hardness. 3 alpha androstenediol (3 alpha), 3 beta androstenediol (3 beta), and 5 alpha androstenediol (5AA) all convert to DHT. 3 alpha is generally the prohormone of choice because 5AA is an estrogen agonist and the conversion rate of 3 alpha is significantly higher than that of 3-beta (although, when price is figured in they come out about even).

* Nandrolone: Nandrolone is generally considered to be the safest and most side effect free steroid. It does not convert to DHT, which makes prostate enlargement, acne, and hair loss all much less likely, but it does have some estrogenic side effects. The primary side effect noted with nandrolone is a temporary loss of libido. 19-norandrostenedione and 19-nor-4-androstenediol (norandrodiol) both convert to nandrolone, and norandrodiol is considered to be the better of the two because it is more potent and does not directly convert to estrogen.

* Boldenone: Boldenone is reputed as an effective steroid for "lean mass gains." It has some conversion to both estrogen and DHT, but less so than testosterone. It is also known to be an appetite stimulant. The prohormone 1,4-androstadiene-3,17-dione (1,4 andro) converts to boldenone.

* 1-testosterone: 1-testosterone (1-test) is considered by many to be top of the line for strength and size gains. It is often quoted as being over 700% more anabolic than testosterone and does not convert to estrogen at all. Users of 1-test report immediate and significant increases in strength and size, improved recovery, and decreased body fat. The downside to 1-test is that it is also highly androgenic, making acne and hair loss more likely. 1-androstene-3beta, 17beta-diol (1AD) is an effective 1-testosterone precursor, and 1-testosterone itself is also available.

Cycling and recovery

Administering an exogenous hormone or hormone precursor can lead to a variety of negative feedback mechanisms in the body. The most well known is inhibition of the hypothalamic/pituitary/testicular axis (HPTA). Essentially, when the body is receiving hormones from another source it shuts down natural production. This is the reason for some of the more common side effects from prohormone and steroid use such as testicular shrinkage. For this reason, it is essentialy to "cycle" prohormones (only use them for a specific period of time) and then follow it with a recovery period to allow natural hormone production to return to normal. A prohormone cycle is usually 2-8 weeks depending on substance, dosage and goals, and it is followed by a recovery period of equal or greater length. During this period calories are often increased and intensity or duration of training decreased to facilitate recovery.

After most cycles, certain substances are used to accelerate recovery of natural testosterone production. The most common tools used are anti-estrogens. These serve the dual purpose of decreasing estrogen levels that are commonly elevated after a cycle and signalling the body to produce more testosterone. The most commonly used are the over the counter drugs 6-OXO and formestane and the prescription drugs Clomid and Nolvadex.

Stacking and delivery methods

Most prohormones are found in different forms and can be used with mutiple delivery methods. The most commonly used methods are oral, transdermal, and sublingual. Cyclodextrins are commonly used to enhance sublingual delivery while cypionate esters are used for advanced delivery methods. Oral delivery is the easiest but is usually associated with the lowest bioavailability and a higher possibility of liver toxicity. Also, oral use necessitates dosing 3-4 times daily as it only keeps blood levels elevated for a few hours. Sublingual delivery is a more effective route, but for those seeking maximum effectiveness transdermal delivery is usually the way to go. It allows for sustained 12 hour release of a prohormone with high bioavailability. Application areas should be clean, preferably shaved, and rotated daily to avoid irritation. In theory, some prohormones may also be injected, but there is little literature on this and it should not be attempted without medical supervision.

Using more than one prohormone at a time is commonly referred to as stacking. This can have numerous advantages, as many prohormones complement each other well. Most stacks include 4AD for numerous reasons such as avoiding decreased libido, with 19-nordiol and 4AD and 1-test or 1AD and 4AD being common stacks. In some stacks, an anti-estrogen such as formestane is also included.

Side effects and prevention

* Gynocomastia: Gyno (bitch tits) is one of the most feared side effects resultant of androgen use. It is due to excessive levels of estrogen and can be exacerbated by excessive body fat and genetic factors. If gyno is a serious concern it is best not to take prohormones that aromatize or are estrogen agonists, making the best choices 1-testosterone or DHT precursors, with 1,4 andro also being on the safer side. One should also always keep a prescription anti-estrogen such as Nolvadex on hand and begin taking it at the first signs of gyno development, such as large or itchy nipples. If you notice these symptoms in the first few weeks of a cycle it is also prudent to discontinue the cycle immediately.

* Acne: In most cases this is just something you are going to have to live with if you decide to use prohormones or steroids, although some individuals are much more susceptible than others. There are a variety of OTC topical medications available and also prescription medications available from a dermatologist. There is a study that indicates that guggul may be of use in reducing acne. It should be noted (as this is a common question) that if you are prescripted Accutane (isotretinoin), do NOT use prohormones at the same time.

* Hair loss and prostate enlargement: The primary cause of hair loss as well as prostate enlargement resultant of prohormone use is increased quantities of DHT in the scalp and prostate respectively. Obviously, this makes DHT precursors an unwise decision if hair loss or prostate enlargement is a significant concern. Most prohormones with the possible exception of 19Nor have the ability to significantly increase DHT, and in this case 1,4 andro is again on the safer side. There are a variety of topical medications available for hair loss, although most nonprescription treatments won't do the trick. Effective topical medications include minoxidil, azeleic acid, Folligen, Nizoral, retinoic acid, and spironolactone. For androgen-mediated hair loss azeleic acid and spironolactone may be particularly effective. Finasteride (Propecia, Proscar) prevents the conversion of testosterone to DHT and may also aid in the prevention of hair loss and prostate enlargement, but may negate some of the systemic benefits that DHT has to offer. Saw palmetto extract also prevents DHT conversion and may decrease the risk of prostate enlargement.

* Psychological effects: Depression, fatigue, and insomnia can all become problems on a prohormone cycle. The use of a
prescription depression medication for the sole purpose of combating depression caused by prohormone use is not recommended. Insomnia can be decreased with various OTC medications such as melatonin. If depression or fatigue from prohormone use becomes serious or intolerable, it is best to try a different substance or discontinue use. One may also choose to fight it with various supplements (common choices are St. Johns Wort and 5-HTP).

* Liver/kidney problems: The issue of the degree of liver and kidney toxicity caused by prohormone use is debatable, with liver toxicity being of greater concern. Mitochondrial nutrients and antioxidants such as acetyl-l-carnitine, ALA, coenzyme Q10, and green tea should help immensely in this area, and milk thistle may also be of some benefit. One should also maintain as healthy of eating habits as possible while on a prohormone cycle.