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Prohormone / Prosteroid FAQ - Everything You Need to Know!


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Old 02-09-2004, 12:44 PM   #1
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Lightbulb Prohormone / Prosteroid FAQ - Everything You Need to KNow!

Prohormone / Prosteroid FAQ
By pogue


Included here are some of the most common questions asked about prohormones. This has been compiled into information based on some scientific studies, but mostly from user feedback after years of success using prohormones. Please keep in mind that this document might have some errors and you will need to do much more reading before you decide whether or not use prohormones.


1. What are prohormones?

Prohormones are synthetically manufactured compounds which convert to anabolic hormones via enzymes in the liver; hormone precursors. They are commonly abbreviated as PHs.


2. What are they used for?

Prohormones are used by athletes looking to increase size, strength, endurance, reduce recovery time or add lean body mass. They are most often used for increasing muscle mass or reducing bodyfat levels. Life extension groups are also increasingly using prohormones as a means of hormone replacement therapy, as an alternative to prescription drug use.


3. Do they have side effects?

Yes. Prohormones can have the same side effects as anabolic steroids, and are dependant upon the user as to which side effects one might experience. Some side effects are acne, hair loss, breast tissue enlargement, and prostate swelling. The potential for these side effects does exist, but it can be reduced if one uses proper precautionary measures (see below). Generally, if a person is genetically predisposed to a side effect it will occur (i.e.: if someone has a history of male pattern baldness in the family, it could be assumed that this could be a side effect experienced if certain prohormones are used)


4. Which prohormones convert to which compounds?
  • Here is a list:
    4 androstenediol (4AD or 4diol) converts to testosterone
    19 nor-4-androstenediol (Nordiol or nordiol) converts to nortestosterone or nandrolone
    1 androstenediol (1AD) converts to 1-testosterone (dihydroboldenone)
    1,4 androstenedione and 1,4 androstenediol (1,4andro or Boldione) converts to boldenone and slightly converts to estrogen (the diol version does not convert to estrogen)
    5 alpha androstenediol (5AA) converts to DHT
    3 beta androstenediol (3 beta) converts to DHT
    3 alpha androstenediol (3 alpha) converts to DHT
    4 hydroxy androstenedione converts to 4 hydroxy testosterone which is an aromatize inhibitor (blocks formation of estrogen)
    7-KETO-DHEA does not convert to any active anabolic compounds
    1-testosterone (1-test) is already an active compound and does not need to undergo conversion

Compounds you want to avoid:

5 androstenediol (5AD or 5diol) converts to testosterone at a very low rate and is an estrogen agonist
4 androstenedione (andro) converts to testosterone and estrone (estrogen)
19 nor-4-androstenedione (norandro) converts to nortestosterone and estrogen
DHEA converts to androstenedione and can be converted to all other hormones
Pregnenolone converts to progesterone and can be converted to all other hormones


5. How do prohormones work?

Basically, when they are administered into the system, they are broken down in the liver and converted to their target hormone via certain enzymes. There have been a number of quotes describing how much of the hormone is converted, but there is no definitive answer as to how much of the prohormone is converted into its target active. Once a certain amount is created, the enzymes used for conversion become saturated and no more can be converted. This is true with all the compounds, except for 1-testosterone which really isn’t a prohormone.


6. What do the target hormones do?

Each hormone works in different ways once it is converted, but essentially it attaches to an androgen receptor in the cells of your body. This in turn increases nitrogen retention and protein synthesis, meaning that your body is in a constant anabolic state (assuming you are continuously supplying your body with the hormone). Here is a brief description of each hormone and what it does.

Testosterone is the primary male hormone responsible for development of the sex organs and muscle growth. Testosterone is both anabolic and androgenic—anabolic meaning it causes muscle growth and androgenic meaning that it causes development of secondary sex characteristics. Testosterone converts to both DHT and estrogen in its parent form. Testosterone is often the primary hormone used on a cycle of steroids. It is a mass builder, and will often help with unwanted androgenic side effects of other steroids. Although conversion to estrogen can cause many unwanted side effects on its own, testosterone should generally be the base to any cycle.

Nandrolone is an anabolic hormone, with not as much androgenic potential. It attaches to the androgen receptor with greater affinity than testosterone, but can cause a loss of libido and generally stays active in the system much longer than does testosterone. This is the “safest” choice for users who want to avoid most common side effects.

DHT (dihydrotestosterone) is the primary androgenic hormone in the body. It is responsible for increases in strength, as well as most of the unwanted side effects common with steroids. DHT is converted from testosterone via the 5 alpha reductase enzyme. DHT receptors are high in the scale, skin and prostate; high DTH levels are the most common cause of prostate swelling, acne, and male pattern baldness.

Boldenone is a veterinary hormone, which is commercially sold as Equipoise. Equipoise is known as an alternative to nandrolone when using steroids. It provides an increase in appetite, with some fat burning potential. Boldenone converts to estrogen at about half the rate of testosterone. Those who are looking to avoid some of the stronger androgenic side effects also commonly use it. 1-testosterone is the 5 alpha reduced version of Boldenone.


7. How do I take prohormones?

There are three common routes of administration for prohormones. These are usually based on their efficacy (i.e. how much is absorbed). Since the liver and stomach lining breaks down prohormones rather efficiently, taking them orally is the poorest route of administration. Most users prefer transdermal (topical) administration. When taken this way, you apply it to your skin and it will continue being absorbed over a period of 12 hours or so. Cyclodextrins or sublingual methods are also commonly used, which is where the prohormones are dissolved under the tongue. This also has a high level of absorption and works well. There are also some products on the market which are sold as “intraoral” or “intranasal”. These are meant to be sprayed into the nostril prior to your workout, and are generally only meant as preworkout boosts, not for a cycle of prohormones.

Some manufactures have started selling prohormones in oral form with an ester attached. This, in theory, will allow it to be slowly absorbed for many hours similar to the other methods, but to my knowledge, there have been no studies demonstrating that this method increases bioavailability.


8. What is a cycle? What does stacking mean?

A cycle is generally used to describe a length of time and common dosage when taking prohormones. Stacking means taking more than one prohormone at a time to increase gains or reduce side effects. Common cycle lengths are 2 weeks, 4 weeks, 6 weeks, and 8 weeks. I recommend 4 week cycles, which seem to give the most gains with fewer sides. I would not recommend going beyond 8 weeks.

Common stacks are 4AD and Nordiol, 1AD and 4AD, 1-test and 4AD, etc. You will notice most everything is stacked with 4AD. This is because testosterone gives you a bit more leverage, providing good gains and overall anabolism, with reduced androgenic side effects. Each of the prohormones can be taken alone, or taken together. The choice is yours and should be made from reading this text, and all the user feedback from this board and others. Research, research, research!


9. What is post cycle therapy?

Post cycle therapy is a tried and true method of helping to solidify your gains by raising natural testosterone levels and lowering estrogen levels once your cycle is over. When you add external hormones to your body, your own natural production becomes suppressed. Your body attempts to compensate your endocrine system by stabilizing the other hormones, which results in an increase in estrogen. Once you quit supplying your body with external hormones, your natural testosterone will be low and estrogen will be high. Therefore, anti-estrogens are taken to halt the manufacture of estrogen in the body. This will result in higher testosterone levels, hence making it easier to keep your gains. Post cycle therapy should begin the next day after the prohormones have stopped being taken. Common post cycle therapy drugs are listed below with dosages:

6OXO
6oxo is an aromatize inhibitor sold by Ergopharm. It is the best over the counter anti-estrogen available for post cycle use.
Week 1 – 600mg daily in two divided doses, morning and night
Week 2-3 – 400mg daily
Week 4 – 300mg daily

Formasin/Formastat/Aromazap
Note: 4 hydroxy androstenedione acts as a weak androgen and can cause further suppression of natural testosterone, but can be used post cycle.
Dosages should be 250mg a day for the first two weeks, followed by anywhere from 50-250mg a day for the next two.

Clomid
Clomid is a prescription fertility drug, but is highly available and highly effective at blocking estrogen and increasing LH output.
Day 1 – 300mg
Day 2-11 100mg
Day 11-21 50mg
OR
150mg daily for 2 weeks
100mg daily for 2 weeks

Nolvadex
Nolvadex is also a prescription, which is highly available and blocks estrogen at the receptor.
Week 1-2 – 40mg daily
Week 2-4 – 20mg daily


There are other prescription anti-estrogens available, but these two will be fine unless side effects arise, so we won’t discuss the other options in this FAQ.

Other common post cycle favorites including high doses of flax oil, ZMA, tribulus and an ECA stack coupled with reduced training volume and increased calories (500 or so above maintenance). But, it is very important to use an anti-estrogen for post cycle. I would never recommend not using one unless the cycle length is 2 weeks or less.


10. What dosages should I use?

Dosages are different for the different routes of administration and for the different hormones taken. Here is a basic outline of each prohormone along with general cycles used, based on user feedback. For your first cycle, I recommend sticking to a lighter dosing schedule for 2-4 weeks. Note: This is a general guideline. Dosages for any cycle can be higher or lower, and some products may incorporate one or more of these compounds so that the below amount might not be able to be achieved. This is just a basic outline and is far from completely accurate.


1AD

1AD is by far the most popular prohormone. It is considered to be the most effective taken orally, and has resounding user feedback. It is best stacked with 4AD to reduce side effects, the most common of which include lethargy and reduced libido. 1AD should not be used transdermally, and could be used sublingually, although there are few products with this delivery system used. 1AD is commonly stacked with 4AD and shouldn’t be stacked with nordiol, or the DHT precursors.

4-6 week cycles are best taken at anywhere from 300-900mg daily. Take in divided doses throughout the day to keep blood levels elevated.


4AD

4AD is the next best. It is almost always used with other hormones due also to its resounding user feedback and adding large amounts of mass from increases in testosterone and estrogen. 4AD can be taken orally, transdermally, or sublingually.
2-6 week cycles are generally used. 4AD can be stacked with just about anything.

Oral:
300-1500mg daily. Oral is probably the worst way to take this, but if you are simply looking to reduce sides of 1AD, etc – it works. Take in divided doses to ensure elevated blood levels.

Transdermal:
400-600mg daily with two applications in morning at night.

Sublingual:
Probably 15-50mg at a time, 3 times or more daily in divided doses.


Nordiol

Nordiol is the best prohormone for use by people who want to avoid the common androgenic sides associated with the other hormones. Can be taken orally, transdermally or sublingually. 2-4 week cycles recommended. Heavily suppressive, despite what literature says. Nordiol is commonly stacked with 4ad for mass, or 1,4andro for cutting or users wanting reduced sides effects.

Oral:
500-800mg daily in divided doses

Transdermal:
500-800mg daily in split doses morning and night

Sublingual:
15-50mg in divided doses


1,4andro

1,4andro is renowned for causing appetite stimulation. It’s low in estrogenic sides and good for cutting or bulking. Some people claim that transdermal administration works well, but the feedback I’ve seen has been poor. Oral seems to be the route of administration, and the dione version appears to work better than the diol. 1,4andro can be stacked with just about anything. Taking 1,4andro for less than 4 weeks is generally a waste because it takes quite a while for the effects to kick in.

Oral:
300-600mg daily in divided doses.

Transdermal:
N/A

Sublingual:
N/A


1-Testosterone

1-test is the active form of 1AD and is best taken transdermally or sublingually, although oral products suspended in oil with an ether attached also have very good feedback. 1-test is best stacked with 4AD for mass or 1,4andro for cutting.

Oral:
150-300mg when taken in ethergel product in divided doses

Transdermal:
200-500mg daily or more in split doses

Sublingual:
Not sure


5AA/3 beta/3 alpha

These all convert to DHT at different rates and have slightly different properties. I’m a little hazy on all of them, except that 5 alpha can compete with estrogen for receptor activity when converted to DHT. Some people have used 5AA in an oral product as a preworkout boost, while others have used 3 alpha for a “hardening” agent.


(Thanks to roobear for the below info on DHT precursors)


3-Alpha/Beta
3-alpha/beta will illicit exactly the same anabolic/androgenic responses, differing only in their conversion rates - 3-alpha 43% / 3-beta 9% respectively. The bioavailability of 3-alpha/beta is purported to be relatively low (by Bill himself) and thus would serve well to be administered transdermally. These compounds are best used in conjunction with other compounds, preferably of an anabolic nature (ie Nordiol, 1,4 Andro and 4-AD) - inducing drastic increases in strength, vascularity and muscle hardness.

3-Alpha
Oral:
100-300mg (lower dosage being more of a "stacking" quantity)

Transdermal:
50-150mg (lower dosage being more of a "stacking" quantity)

3-Beta
Oral:
Outdated - use 3-alpha

Transdermal:
200-500mg(lower dosage being more of a "stacking" quantity)


7-Keto-DHEA

This is slightly out of the scope of this FAQ, but is generally used for cutting. This has been shown to increase thyroid output and lower cortisol levels, without converting to target hormones. Used for cutting stacked with other thermogenic compounds for 4-6 weeks.

Oral:
200mg in two divided doses

Transdermal:
100mg daily


11. Are prohormones legal?

Yes, currently they are legal in the US and some other countries. Please visit www.usfa.biz and write your politicians to ensure they stay that way. Prohormones are not tested for in job drug tests, but they are probably banned and can potentially show up on a drug test for athletics. Check your local laws for specific information.


12. Who should use prohormones?

Mature adults above the age of 21 looking for increases in lean muscle mass or decreases in bodyfat levels. Most veterans will advise using prohormones after several years of training, to ensure you have a good feel for proper diet, nutrition and supplementation. Using prohormones under the age of 18 is a very bad idea; it can result in the closure of growth plates, thus resulting in permanently stunted growth; it can also result in potentially serious endocrine system problems. Those with potential for or already enlarged prostate or those susceptible to male pattern baldness should not use prohormones; nor should prohormones be used by people with heart conditions, who currently have gynocomastia, or have liver or kidney problems. If you have any doubts, see a doctor before using these compounds.


13. Can I take prohormones along with steroids?

This is a hotly debated subject. Yes, you can – but why? If you have access to steroids, why would you bother with prohormones? Anabolic steroids are already hormones in their current form and require no conversion – hence, they are more powerful, albeit illegal.
The only compound I would say that you could take with any other steroid would be
1-testosterone, which would be an equivalent of Primobolan or Equipose. The only other thing I can think of would be taking 4AD with Fina to reduce side effects. There is more information about this on boards like Anabolicminds or Animal’s board.


14. How can I avoid some of the potential side effects associated with prohormones?

There are certain ancillary compounds available to treat potential side effects of prohormones. Below is a list I compiled which is pretty basic and should help clarify some of the issues of side effects.


Prostate Issues

The prostate is an organ at the neck of the bladder where it joins the urethra. It is responsible for controlling urination and ejaculation. Common symptoms of prostate problems are frequent or difficult urination, dribbling when urinating, erection difficulty, and pain in that general area. Either a rise in estrogen or DHT levels from increased testosterone, etc., probably causes this. If you have ongoing prostate issues, it’s best not to use prohormones, though potentially the use of nordiol might be acceptable.

Herbal treatments:
Saw Palmetto Extract – Usual dosage is 160mg several times daily
Beta sisterol or plant phytosterols – 300mg several times daily
Flax seed oil – anywhere from 5-20 tblspoons daily

Prescription Treatments:
Proscar/Propecia – blocks the conversion of testosterone to DHT. Ineffective with DHT derived hormones (1-test, 1ad, 5aa, etc)
Spironolactone – an anti androgen. Best not used for this, but used topically (more below)


Acne

Acne is very common on prohormone cycles, and can range from mild to moderate. It will go away once post cycle treatment concludes, or within a few weeks of cession of the product. The best way to treat acne is with the soaps available at your local grocery store or pharmacy. Just pick up some Neutrogena or whatever and scrub your face twice a day or use the body wash.


Hair Loss

Hair loss is caused by increased levels of DHT. Since DHT receptors are heavy on the top of the scalp, some people will notice a lot of shedding or a receding hairline on some cycles. There are various treatments for this; the most common is topical Spironolactone available from Nizoralman or Dr. Lee. The 2% will work as a preventative measure, while the 5% will attempt to help grow some hair back. There are also other methods, such as azelaic acid or Nizoral shampoo, but they are not proven to be effective as spiro is.
If you are concerned you are losing your hair and are currently taking something to help prevent it, prohormones are probably not the best idea. If still interested in using prohormones, Nordiol might be the best option available to you.


Gyno

Gynocomastia, or development of the breast tissue, is sometimes common among aromatizing (converting to estrogen) prohormones. The first symptoms are puffy and itchy or swollen nipples. If you start to notice this while on a cycle, you need to start taking Nolvadex or Tamoxifen immediately!Formasin/Aromazap/Formastat might work, but 6oxo is not going to help this in most cases, so Nolvadex should ALWAYS be on hand for this situation. It is highly available, not very expensive, and not illegal to posses, so there is no reason not to have it. Don’t wait and order some when you start to get the first signs of gyno, because Nolvadex needs to be taken as soon as symptoms of gyno appear. Start taking 40mg a day until the symptoms subside, and you may want to continue to take 10mg the rest of your cycle as precaution.


Liver/Kidney

Prohormones have to pass through your liver in order to convert, no matter what the route of administration, so higher levels of liver enzymes in the blood is common during a cycle. Many steroid users take Milk Thistle and ALA at high doses to combat this, and if you are concerned it would be a good idea to take one or both of these to help that. Problems with kidneys have not been an issue to my knowledge, but steroid users will often also take cranberry juice extract to help with that.


Depression

Some people report mild or moderate depression, especially post cycle when using 6oxo. This can be cured with prescription drugs such as Zoloft, Prozac, Paxil, etc. It can also be fought with herbal supplements such as St Johns Wort, 5-HTP or Sam-E. If you go with the herbal route, St Johns Wort should be 300mg 2-3 times daily, 5-HTP at 100mg several times daily, or 100-200mg of Sam-E once daily. You can combine all three if depression is extreme, otherwise my pick would be St. Johns Wort.

Testicular Atrophy

Many users report testicular shrinkage during a cycle. The testes will come back to full size once you start post cycle. If they do not, then it’s recommended you take Clomid and possibly even HCG to help restore them.


Sleeplessness

Some people report having trouble falling asleep or staying asleep on a cycle. My recommendation is to take 1mg to 3mg of melatonin 30 minutes before bed time. Some other options are Valerian root, GABA, Tylenol PM or Kava Kava (potentially stressful on the liver).


15. What kind of training should I use when using prohormones?

Everyone has their own opinion on this, and you should use whatever works for use. Most people put an emphasis on higher volume while using prohormones, and you can add more isolation sets and workout more frequently due to increased recovery time. But don’t overtrain. Just because you’re using prohormones doesn’t mean you need to train daily or twice daily. Also, doing cardio on prohormones is fine. I recommend 2-3 times weekly of 20 minutes, if at all.


16. How should I eat when on prohormones?

Try and eat 1-2g of protein per pound of body weight. Try and eat 500-1000 calories above maintenance, or more if bulking. Generally, standard nutrition guidelines should be followed. If cutting, try and eat 10-12 calories per pound of bodyweight, while keeping protein high.


17. Should I take any other supplements while using prohormones?

Take whatever you normally take. If you take creatine, it’s fine to continue taking it while using prohormones. Some people prefer to save it for post cycle to help retain some of the water weight. Otherwise, the usual stuff like a multivitamin, a good protein powder and flax seed oil should be standard issue for any athlete.


18. What are some good manufacturers of prohormone products?

My personal picks would be Molecular Nutrition, Ergopharm, Avant Labs, BDC Nutrition, San, Syntrax or 1fast400. These are stand up companies that generally pump out quality products.


19. Can I make my own prohormone transdermal/oral/sublingual?

Yes, there are several companies that offer prohormone powders in bulk such as Kilosports, Beyond a Century and 1fast400. You can buy powders from them and make your own capsules, cyclodextrins or transdermals easily. Visit Anabolicminds or Avant Labs message boards for a wealth of how-to information.


20. Can I inject prohormones?

This is out of the scope of this FAQ, but yes you can. The results have been mixed, there have been some questions of products purity used in injectables, and there is a question of whether or not using them for this purpose is legal.


21. Is there anything I should know about transdermal delivery?

Transdermals should be applied twelve hours apart. It is a good idea to apply them after showering and to rotate application spots daily. Apply lotion to application spots not in use. This is a good way to avoid a rash from the topical, which is a common side effect reported by users. Some prefer to scrub themselves with a luffa or sponge before applying them to remove the first layer of dead skin cells for optimal delivery. It is also a good idea to wear latex gloves when applying, and wash your hands when you are finished to avoid getting the solution into your eyes or other sensitive areas. Keep in mind that high amounts of sweating or getting the area wet too soon after application will wash it off, so it might have to be reapplied if this occurs.


22. Is there anything I should know about oral/liquid delivery?

There are many products on the market with liquid delivery systems. You will need to drink these, and most of them taste badly. Just try and get them down as quickly as possible, or mix with another flavored liquid to help the taste. Also keep in mind that liquid and oral delivery methods are generally less effective. Even if the product is esterfied, it is still a good idea to take it several times daily in small divided doses to ensure saturated blood levels at all times.


23. Is there anything I should know about sublingual delivery?

Try and let the product dissolve under your tongue and do not eat or drink anything for around 10-20 minutes after you take the product. As with orals, you will need to take it several times daily to maintain blood levels.


24. Which prohormones are best used in a bulking cycle and what kind of gains can I expect?

Most people prefer the combination of 1-test and 4ad. This is a tried and true stack combination and most people seem to gain the best from it. Adding 1,4andro is also common to increase appetite and may help gains. How much one will gain off a cycle depends on your diet and training but gaining 10lbs in 4 weeks is quite common.


25. Which prohormones are best for a cutting cycle?

Most commonly, people will use non-aromatizing hormones such as 1-test or DHT precursors to act as an anti-catabolic and increase hardness. However, low doses of 4ad may help, and adding 1,4andro can also be beneficial.


26. Is it okay to drink alcohol while taking prohormones?

No, it is a really poor idea to drink while doing bodybuilding/weight lifting in general, but taking them while using prohormones is even worse. Taking large amounts of prohormones, especially orally, can cause increased liver stress. When you add alcohol into the equation it is a potential for disaster. If you have to drink, try to do it moderately and take milk thistle and/or ALA to help combat potential problems. Although, it would be best to avoid it completely.


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Old 02-09-2004, 12:52 PM   #2
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Transdermal Prohormone FAQ

Transdermal Prohormone FAQ
By David Tolson

Contents

1. Transdermal basics
Q: What is transdermal delivery?
Q: Why is transdermal administration of prohormones superior to oral administration?
Q: What are the advantages and disadvantages of transdermal administration of prohormones when compared to sublingual/nasal administration?
Q: If I apply a transdermal hormone to a certain muscle group, does it increase strength in that particular muscle group?
Q: Should transdermal prohormones be cycled differently than oral prohormones?
Q: What are the dosages for transdermally administered hormones?

2. Application tips
Q: When, where and how should transdermals be applied?
Q: After applying the transdermal, should I wait before working out, showering, or swimming?
Q: Should I avoid contact with other people in the area of application?
Q: My transdermal product is resulting in rash/skin irritation. Is this normal? How do I avoid this?

3. Homebrewing
Q: Can I add more prohormones to a transdermal prohormone product?
Q: How do I make my own transdermal prohormone?
Q: I am using the Dermabolics carrier. Can adding DMSO increase the efficacy of my transdermal prohormone?

4. Miscellaneous
Q: Can transdermal prohormones be dosed more often than two times daily?
Q: Is it acceptable to use transdermal prohormones in conjunction with topical fat loss products?
Q: Can transdermal prohormones be used along with oral prohormones?
Q: What is the shelf life of transdermal prohormones?


1. Transdermal basics


Q: What is transdermal delivery?

Transdermal delivery is a method of delivering active drugs through the skin barrier, and is in many cases superior to other forms of delivery (oral, sublingual, etc). It involves applying active substances (such as prohormones) dissolved in a carrier (a substance or blend of substances designed to promote delivery of the active ingredient past the skin barrier).


Q: Why is transdermal administration of prohormones superior to oral administration?

There are numerous reasons why transdermal delivery can be preferable. The first is that transdermal delivery allows prohormones to avoid first pass metabolism in the liver. Most prohormones are readily destroyed in the digestive tract and liver, often making the dosages required (and money spent) much higher compared to transdermal delivery. It is estimated that transdermal prohormones have a 30-40% absorption rate, compared to 5-15% for oral prohormones. Also, certain hormonal substances may be toxic to the liver, and transdermal delivery significantly lessens this. Secondly, orally delivered prohormones have very short half-lives and must be taken 3-4 times daily. Not only is this inconvenient, but it means that during certain periods (such as sleep) blood levels of the hormone will be very low. Transdermal delivery effectively leads to a steady release over 12 or more hours, solving both of these problems.


Q: What are the advantages and disadvantages of transdermal administration of prohormones when compared to sublingual/nasal administration?

Sublingual (absorption in the mouth, like a lozenge) and nasal delivery is limited by the amount that can be absorbed by the mucous membranes. The maximum amount of hormone that can be delivered is around 25 mg, and blood levels are elevated for 2-3 hours, compared to ~12 for transdermal. Therefore, sublingual and nasal prohormones must be dosed at least 5 times a day to be effective. However, sublingual/nasal delivery delivers 80-90% of the actives to the bloodstream, making it a very efficient carrier. A combination of transdermal application (for steady blood levels) and sublingual/nasal application (to spike blood levels, particularly pre-workout) could be effective.


Q: If I apply a transdermal hormone to a certain muscle group, does it increase strength in that particular muscle group?

Transdermal prohormones are delivered systemically, so applying them to a particular area will not cause disproportionate strength gain in that area. The exception is products that are geared toward local delivery, such as Sytenhance.


Q: Should transdermal prohormones be cycled differently than oral prohormones?

Cycles with transdermal prohormones should be the same length as one would use with oral prohormones, and post-cycle recovery should remain the same. The primary differences are how often you will administer the prohormone (two times daily as opposed to three or four) and the dose used.


Q: What are the dosages for transdermally administered hormones?

First off, it should be noted that the listed dosage and duration on product labels is often conservative. Also, dosage will vary on stacking, level of experience, and many other factors.

Here are some general guidelines:
  • 1-testosterone: 200-500 mg
    19-norandrostenediol: 400-800 mg
    4-androstenediol: 400-600 mg
    3-alpha androstenediol: 50-150 mg
    3-beta androstenediol: 200-500 mg
    4-hydroxyandrostenedione (formestane): 50-200 mg
    androstenetrione (6-OXO): 150-500 mg
    7-OXO-DHEA (7-Keto): 100 mg

Note: Much of the dosage information comes from the prohormone FAQ, by pogue.


Q: What are the differences between the Dermabolics carrier and other carriers?

The Dermabolics carrier is identical to the carrier developed by Avant Labs except it does not contain carbomer, a thickening agent (due to the fact that it is a spray instead of a lotion). For a discussion of the science behind this carrier as well as comparison to some other products, see Battle of the Transdermal Prohormones by Par Deus.


2. Application tips


Q: When, where and how should transdermals be applied?

Transdermals should be applied as close to twelve hours apart as possible. An ideal time to apply is after showering or bathing. Scrubbing with a luffa, wash cloth, or sponge beforehand improves delivery, as does shaving the area of application. Ideal areas of application are those with thin skin, such as wrists, top of feet, upper arms, chest, back, or legs. Larger amounts will require larger application areas. If possible, latex gloves should be worn during application. These can be purchased at most pharmacies. It is also a good idea to shake the bottle before application to mix the ingredients. Spray or pump the lotion onto the hand and then rub into the application area. Afterwards, wash your hands with soap. Five minutes should be allowed for the transdermal to dry after contact with clothes or other objects.


Q: After applying the transdermal, should I wait before working out, showering, or swimming?

Yes. Water can wash off the transdermals making them less effective. You should wait at least half an hour before any of these activities, and ideally 1-2 hours. Also if you shower after application it is best not to scrub the area of application.


Q: Should I avoid contact with other people in the area of application?

Most definitely, especially females and children. This applies primarily if you are using a prohormone or steroid. Contact with the area may result in delivery of active hormone to the person contacted. If you think it will become a problem, it is best to keep the area covered (saran wrap over the area of application will work), or only use areas that will be covered with clothing as application spots. Also, certain application areas (such as the back of the legs) are less likely to be contacted.


Q: My transdermal product is resulting in rash/skin irritation. Is this normal? How do I avoid this?

Some people experience skin irritation or rashes from transdermals, especially those containing certain active ingredients. 1-testosterone is particularly caustic, and latex gloves are a must when applying this substance (even after washing hands thoroughly small amounts can remain that may get in the eyes or other sensitive areas, and it is quite painful). If latex gloves are not available, you can at least use a sandwich bag. The best way to avoid irritation regardless of the source is to rotate the area of application – one day apply to the feet, another to the upper arms, and so on. You can also apply lotion to areas of application not in use.



3. Homebrewing

Q: Can I add more prohormones to a transdermal prohormone product?

Yes, but it will become saturated at a certain point. Also, increasing the concentration may reduce the relative effectiveness. If you want a concentration or blend of ingredients that is not available pre-made it is usually better to make your own using a carrier product such as the transport matrix.


Q: How do I make my own transdermal prohormone?

Simply add the hormone powder to the carrier and then shake. If you accidentally put in too much hormone powder heating lightly and shaking vigorously may help. To heat a solution, boil a pot of water and let it cool to just below boiling. Place the prohormone bottle in the water for a few minutes, remove, then shake.


Q: I am using the Dermabolics carrier. Can adding DMSO increase the efficacy of my transdermal prohormone?

This carrier is quite effective as it is. In theory, adding 5-10% DMSO may increase absorption. However, one will have to put up with the side effects of DMSO (increased irritation, bad breath, etc).



4. Miscellaneous


Q: Can transdermal prohormones be dosed more often than two times daily?
If desired, a smaller dose can be used three times daily (every eight hours), but this does not have a clear benefit.


Q: Is it acceptable to use transdermal prohormones in conjunction with topical fat loss products?

Yes, just avoid applying them both in the same area.


Q: Can transdermal prohormones be used along with oral prohormones?

Yes, although if one is doing an intraday cycle (oral prohormones during the day, transdermal overnight) trying to compare oral and transdermal doses can often be difficult. Stacking one prohormone transdermally and another orally is not uncommon.


Q: What is the shelf life of transdermal prohormones?

This depends on the substance; in general the shelf life is 1-2 years. This can be increased by freezing and/or vacuum sealing. If you are planning on stocking up you are better off buying bulk prohormone powders and then mixing them in a carrier before use.


By David Tolson - Special thanks to fuzz and the members of the Avant Labs forums for helping with this FAQ
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Old 02-09-2004, 12:54 PM   #3
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Methyl-1-Testosterone

Methyl-1-Testosterone (aka M1T)
By David Tolson

http://www.bulknutrition.com/?ingredients_id=38


Methyl 1-testosterone, or 17aa-1-testosterone, is the methylated version of the steroid 1-testosterone. This structural modification makes steroids much more orally bioavailable by inhibiting breakdown in the liver. Although it has only been widely available for a short period of time, feedback on this compound indicates that it may be the most effective legal prohormone/steroid product on the market regardless of delivery method, and it is hands down the most effective oral product. On the other hand, most users report a wealth of side effects, and this compound is not to be taken lightly. It does not have a long history of use or a well-established safety profile, and proper precautions should be taken.

The profile of methyl 1-test is similar to that of 1-test – it does not convert to estrogen, and it is highly anabolic and moderately androgenic (less than 1-test). When compared to orally administered methyltestosterone, methyl 1-test is 910-1600% as anabolic and 100-220% as androgenic.

The side effects reported by users of methyl 1-test are many and individual reactions vary considerably. The most commonly reported side effect is lethargy, which can range from mild to severe. Other common side effects include increased blood pressure, bloating, joint pains, cramps, mild headaches, insomnia, aggressiveness, and irritability. Many users also find that methyl 1-test decreases appetite, which can be harmful or beneficial depending on one's goals. These side effects can be reduced by lowering dosage or taking smaller doses more frequently. Combining it with another androgen (such as 4-AD) may also help, but feedback on this is limited.

Another concern with methyl 1-test (and methylated steroids in general) is hepatotoxicity. Although this tends to be exaggerated, it is still prudent to take certain precautions. First and foremost, other substances that are toxic to the liver (such as alcohol) should be avoided to avoid placing extra stress on the liver. If methyl 1-test is stacked, it would be best to stack it with something other than an oral steroid/prohormone, such as a transdermal. Milk thistle, alpha lipoic acid, and N-acetyl-cysteine are commonly recommended to help protect the liver. For further information on 17aa steroids and hepatotoxicity, see the following article:

Hepatotoxicity: Fact or Fiction, by Roy Harper

When taking methyl 1-test, it is best to start out with at least a week at a dose of 5-10 mg to see how one reacts. Many users find this range to be effective, while others feel the ideal amount is 20-40 mg. It comes down to the experience, goals, and individual reaction. Many find a lower dose to be just as effective as a higher one, but with less side effects. With a compound such as this, it is generally best to err on the side of caution, especially for those that are less experienced with steroids. Most seem to find their ideal dose to be in the 10-30 mg range. Cycle length should be kept short, in the range of 1-4 weeks. Finally, it is especially important to take adequate time off after each cycle with this substance to allow the body to recover.
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Old 02-09-2004, 12:55 PM   #4
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1-Testosterone/1-AD Explained

1-Testosterone/1-AD Explained
By David Tolson

http://www.bulknutrition.com/?ingredients_id=25


1-Testosterone (17beta-hydroxy-5alpha-androst-1-en-3-one) and 1-AD (1-androstenediol, 1-androstene-3beta, 17beta-diol) are probably the two most effective muscle building supplements presently on the market. 1-testosterone is a steroid that is closely chemically related to testosterone; it has a double bond at the 1 position whereas testosterone has a double bond at the 4 position. 1-AD is a 1-testosterone prohormone that is converted to 1-testosterone by the enzyme 17beta-hydroxysteroid dehydrogenase. Unlike most other prohormones which are readily deactivated in the liver, 1-AD has significant oral activity.

The strong anabolic properties of 1-testosterone have been established in the literature. Research conducted in the 60's found that 1-testosterone had a myotrophic (anabolic) potency of 200 as compared to 26 for testosterone, making it over 7 times as anabolic. This was done using the rat levator ani assay, which is commonly used to test the anabolic potency of steroids. In addition to this, 1-testosterone and 1-AD are both unable to aromatize to estrogen. Hence these substances cause very significant increases in muscle size and strength with about the androgenic potential of testosterone and almost no estrogenic side effects (water retention, fat gain, gynecomastia).

However, 1-testosterone use is not without side effects. The side effects that can be primarily expected from 1-testosterone are androgenic, similar to the side effects of DHT prohormones but not as severe. These include hair loss, acne, and an increased risk of benign prostate hypertrophy (BPH) (although there is much debate concerning the latter subject). Finasteride (propecia, proscar) cannot be expected to reduce these side effects, as 1-testosterone converts to DHT through a pathway other than 5alpha-reduction. 1-testosterone causes prostate growth in castrated rats equal to that of testosterone; unfortunately this is not a good model for BPH. Those wishing to avoid androgenic side effects should steer clear of 1-AD and 1-testosterone and instead opt for a 19-nor prohormone.

1-AD is used orally, with a low dose being 200-300 mg daily and 600-900 mg daily being commonly utilized (women, should they choose to use 1-AD, should not use a dose higher than 100 mg daily). Dosages as high as 1200-1500 mg daily are not unheard of. 1-testosterone is not considered to be very effective when orally administered, and is most commonly used transdermally at 200-400 mg daily with some going as high as 600 mg. Cycle length for both of these substances is usually 4-8 weeks, although some see good results from 2 week cycles of 1-testosterone. They are most commonly stacked with 4-AD, which can reduce or reverse common side effects such as lethargy and reduced libido. This stack is especially ideal during bulking; during cutting periods, lower doses of 4-AD should be utilized if this stack is chosen. 1-testosterone and 1,4-androstenedione can also be stacked during cutting periods. It is not a good idea to stack these products with DHT precursors (to avoid excessive androgenic side effects) or 19-nor prohormones (as this would cause a significant reduction in libido).
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Old 02-09-2004, 12:56 PM   #5
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4-AD Technical Information

4-AD Technical Information
By David Tolson

http://www.bulknutrition.com/?ingredients_id=49


4-androstenediol (4-AD) is an effective prohormone to testosterone. Naturally found in several tissues of the body, 4-AD is converted to testosterone via the enzyme 3beta-HSD. 4-AD converts to testosterone at a significantly higher rate than other commercially available prohormones (such as androstenedione), and also does not have the weakness of conversion to estrogen and/or DHT prior to conversion to testosterone. This makes 4-AD the best testosterone prohormone on the market.

Since testosterone is the target hormone, the effects of 4-AD supplementation will be consistent with an increase in testosterone levels. Since testosterone converts to both estrogen and DHT, both androgenic and estrogenic side effects can be expected. Although not commonly used as a standalone because of these side effects, 4-AD is used in most prohormone stacks. Since exogenous steroids shut down natural production of testosterone via negative feedback, 4-AD can help reduce the side effects of low testosterone and low estrogen experienced with many substances (such as loss of libido) while also providing additional anabolic benefit. 19-nordiol and 4-AD and 1-AD or 1-test and 4-AD are both common stacks. 4-AD is also recommended to counteract some of the side effects of methyl-1-test.

4-AD is best used as a transdermal, as it has low oral bioavailability. 300-600 mg is the commonly used transdermal dosage when stacking, while higher doses (700-1000 mg) are used as a standalone. Oral 4-AD doses, even when stacking, may go up to as much as 1.5 g daily, although most use 600-900 mg. This is generally spread out over 3-4 doses. Sublingual 4-AD can also be used as a preworkout stimulant.
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Old 02-09-2004, 12:56 PM   #6
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1,4-Andro Information

1,4-Andro Information
By David Tolson

http://www.bulknutrition.com/?ingredients_id=34


1,4-andro (1,4-androstadienedione) and 1,4-androdiol (1,4-androstadienediol) are both prohormones to the steroid boldenone. 1,4-andro is well known as the most orally active prohormone, with a recovery rate as high as 50%. This is because its chemical structure renders it resistant to first pass metabolism in the liver. However, unlike many other steroidal compounds, the chance of liver toxicity from oral administration is very low.

Boldenone (1,4-androstadiene-3-one,17b-ol) is an injectable veterinary steroid most commonly found as Equipoise (used for horses). It is structurally related to testosterone and methyl-testosterone, and a small amount (10-20%) may metabolize into testosterone. It is very popular among bodybuilders and other athletes because of its unique characteristics. It is highly anabolic, while having only low-moderate androgenic effects and low estrogenic effects. This is because it is a poor substrate for 5-alpha reductase and has low aromatization to estrogen. Boldenone is commonly stacked with other steroids, and it has the reputation of leading to smaller, more consistent, and easier to keep gains as opposed to rapid muscle gains which are difficult to maintain off cycle. Other reputed effects of boldenone include increased pumps and muscle hardness and increased appetite.

A low dose of 1,4-andro falls in the range of 300-600 mg daily, with a medium dose being in the range of 600-1000 mg. It is good for both cutting or bulking, and can be stacked with most compounds depending on the situation. Cycle length is usually on the longer side, around 4-12 weeks, because it usually takes around 3 weeks for most users to notice an effect. This is because boldenone has a long half-life, so the effects build up over time. The difference between the dione and diol versions is that the dione version converts to estrogen (at about half the rate that testosterone does), while the diol version does not.
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Old 02-09-2004, 12:59 PM   #7
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ErgoPharm Conquers Estrogen

ErgoPharm Conquers Estrogen with 6-OXO

http://www.bulknutrition.com/?products_id=378

For athletes familiar with prohormones and steroids, the female hormone estrogen is undoubtedly a familiar enemy. While most of us understand that estrogen is not necessarily always a harmful and worthless substance to men (in the right amounts it is necessary and beneficial), we still are aware that it must be kept under control or some pretty undesirable conditions may arise in the body.


The Evils of Estrogen
In males, higher than normal estrogen levels (or estrogen levels that are out of balance with androgen levels) can lead to several physiological disturbances. The most well known estrogen induced malady is, of course, gynecomastia (aka gyno or bitch tits). Gyno, simply put, is the growth of breast tissue in men. Usually gyno is a benign growth that is little more than a cosmetic nuisance, however it occasionally (rarely) can become malignant and lead to male breast cancer. Either way, it is something than definitely is anathema to any guy that takes pride in his physical appearance and musculature. Rock hard pecs topped off with puffy cone shaped girlie lumps are simply not for showing off - at least not in my neighborhood.

High estrogen can also promote excessive water and sodium retention, resulting in a bloated, puffy, and smooth appearance. Steroids that aromatize heavily (such as testosterone and Anadrol) are renowned for putting on lots of bodyweight. However, that body weight usually is in large part estrogen induced water retention, and certainly not all muscle.

If all this is not enough then there is the potent inhibitory effect of estrogen on the hypothalamus, resulting in a shutdown of testicular testosterone production. Science has demonstrated that perhaps the most important regulator of testosterone production in males is estrogen - produced by the conversion of testosterone (and other androgens) to estrogen in the body and the brain. Estrogen sends a signal to the hypothalamus to shut down production of a substance known as GnRH. GnRH is a hormone that stimulates the pituitary to produce luteinizing hormone (LH) which is the signal that tells the testicles to produce testosterone. Therefore, men with elevated estrogen levels will have suppressed testosterone levels and perhaps even atrophied testes. Not a pretty picture, eh?

Controlling estrogen in males
Bodybuilders who use steroids caught on years ago to drugs that control estrogen in the body. The first drugs to be utilized were estrogen receptor antagonists such as tamoxifen and clomiphene. These drugs worked by binding to the estrogen receptor like estrogens do, but unlike estrogens they are unable to translocate to the nucleus and activate estrogen responsive genes. While these drugs are somewhat effective in countering gynecomastia and testicular shut down, they still retain some estrogenic activity in certain tissues such as the liver. The result of this residual estrogenic activity can be a reduction in IGF-1 production and an increase in sex hormone binding globulin (SHBG) production. These are both undesirable side effects.

Later on, bodybuilders discovered aromatase inhibitors. These drugs work by blocking the production of estrogens in the body through binding to the enzyme aromatase. Aromatase catalyzes the transformation of aromatizable androgens (i.e. androstenedione, testosterone) into estrogens such as estrone and estradiol. By actually blocking the production of estrogens altogether, aromatase inhibitors do not share the undesirable estrogen agonist activity of estrogen receptor blockers. Instead they function as true anti-estrogens, and because of this have arisen as the most preferred compounds for combating estrogen.

6-OXO™, the first effective all natural aromatase inhibitor
Before I go into detail about 6-OXO™, I would like to give a very brief review and commentary on the current variety of estrogen blocking supplements.

The first estrogen blocking supplement to be introduced, and perhaps the most popular one to date is the isoflavone chrysin. Yes, chrysin has some good in-vitro (“test tube”) research on it that demonstrates it blocks aromatase. However, for years many experts including myself have contended that it suffers from very poor bioavailability, and therefore is ineffective in-vivo. Recently, an article has been published in a very reputable journal that substantiates this suspicion. [1] So chrysin, as promising as it once seemed, unfortunately appears to be a total bust.

After chrysin there was Indole-3-carbinol and Di-indoylmethane . These related compounds work by shifting the metabolism of estrogens away from strong estrogen compounds (16-hydroxylated) and towards weaker estrogens (2-hydroxylated). This can have benefits for women prone to breast cancer as 16-hydroxylated estrogens are quite notorious for promoting estrogen dependent breast cancer. However, there has never been any benefit demonstrated in men for reducing estrogen related effects or for increasing androgen levels. In fact, these compounds may actually REDUCE androgen levels. [2] So for males looking to reduce estrogen and raise testosterone, I-3-C and DIM are poor choices.

In addition to these aforementioned compounds there have been a slew of other compounds sold for estrogen control purposes. These include bioflavonoids such as quercitin, herbs such as Vitex Agnus Castus, and phytochemicals such as resveratrol (3,5,4’-trihydroxystilbene). None of these has ever been substantiated by any research to reduce estrogen levels or to increase testosterone levels.

6-OXO™
After years of research into natural estrogen blockers I finally discovered a compound that really truly works, in males, to both reduce estrogen and increase testosterone. Its called 6-OXO™, which is short for 3,6,17-androstenetrione.


6-OXO™ is what is known as a suicide inhibitor of aromatase. This means that 6-OXO™ binds to the aromatase enzyme in a permanent and irreversible manner, rendering it inactive. The result of this is an eventual diminishment of aromatase enzyme in the body and a concomitant reduction in estrogen levels. [3] [4] [5] [6] [7] A corresponding increase in testosterone production is usually experienced as well.[8]

It is important to note here that this deactivation of aromatase enzymes by 6-OXO™ does not mean that your body becomes permanently deficient in the ability to synthesize estrogen. Your body will react to the deficiency of enzyme by producing more enzyme to replace that which has been deactivated. Therefore, when you stop taking 6-OXO™ your aromatase enzyme level will quickly catch up to normal and full estrogen production will resume.

6-OXO™ is all natural as it is known to be an androgen metabolite formed in the adrenal [9] and placenta [10]

When and how you should use 6-OXO™
There are two main situations where 6-OXO™ can come in useful. The first situation is in combating estrogen elevation while taking aromatizable prohormones or steroids. Aromatizable prohormones/steroids include testosterone, testosterone precursors (4-androstenedione, 4-androstenediol), nortestosterone, nortestosterone precursors (19-nor-4-androstenedione, 19-nor-4-androstenediol), and synthetic anabolic steroids such as oxymetholone (Anadrol) and methandrostenolone (Dianabol).

The second situation where 6-OXO™ stands very useful is in restoring full endogenous testosterone production after a cycle of prohormones or steroids. Prohormones and steroids act as replacements for natural testosterone, and as a consequence, prolonged usage of these substances results in the body resetting the level of its own natural testosterone production. Your body does this by adjusting the activity of the hypothalamic pituitary testicular axis, or HPTA. The HPTA acts like a thermostat that constantly adjusts the body’s production of testosterone to maintain a certain level in the blood. The hypothalamus is the primary sensor in this system, and it responds to both androgens (i.e. testosterone, DHT) and estrogens (derived from aromatization of androgens). The hypothalamus is so sensitive to estrogens in fact that administration of an estrogen blocker can often result in a very substantial surge in testosterone production. This is why steroid using bodybuilders take products such as Clomiphene (an estrogen receptor antagonist) and Anastrazole (an aromatase inhibitor) after cycles to jump-start their suppressed testicular testosterone production. Now, with the introduction of 6-OXO™, there is a natural - over the counter alternative available to these prescription only drugs.

Okay, am I saying that one has to be a prohormone or steroid user to find 6-OXO™ useful? Certainly not! Even if you never touch prohormones/steroids you can obtain a very substantial and beneficial increase in natural testosterone production by taking nothing but 6-OXO™. For those that are wary of hormonal supplements and their effects on the bodies endocrine balance, yet still want to obtain the benefits of increased testosterone levels, 6-OXO™ offers a very safe and effective alternative.

So how does one use 6-OXO™? If you are using it to combat estrogen during a cycle of aromatizable steroids then you can take it every day of your cycle, once a day (preferably with your evening meal) at a dosage of 200-600 mg. If you are using it to jump-start your testosterone production after a cycle of prohormones (or just to increase your own natural production in a clean state) then you would also take 200-600mg of 6-OXO™ once a day, for a period of 3-6 weeks.

If you are a prohormone user, or even a steroid user, I doubt I have to entice you anymore than I have to give this stuff a try. The research is solid, and the product is affordable. This is the first new product that Ergopharm has introduced in over a year, and I am sure you will soon discover for yourselves that 6-OXO™ is a product well worth the wait!!



[1] Saarinen N et.al., “No evidence for the in vivo activity of aromatase-inhibiting flavonoids.” J Steroid Biochem Mol Biol. 2001 Sep;78(3):231-9.
[2] Wilson, V.S., et al., “Alteration in sexually dimorphic testosterone biotransformation profiles as a biomarker of chemically induced androgen disruption in mice.” Environ Health Perspect, 1999. 107(5):377-384.
[3] Covey DF, Hood WF, “Enzyme-generated intermediates derived from 4-androstene-3,6,17-trione and 1,4,6-androstatriene-3,17-dione cause a time-dependent decrease in human placental aromatase activity” Endocrinology. 1981 Apr;108(4):1597-9.
[4] Numazawa M, Mutsumi A, Tachibana M, “Mechanism for aromatase inactivation by a suicide substrate, androst-4-ene-3,6,17-trione. The 4 beta, 5 beta-epoxy-19-oxo derivative as a reactive electrophile irreversibly binding to the active site” Biochem Pharmacol. 1996 Oct 25;52(8):1253-9.
[5] Numazawa M, Midzuhashi K, Nagaoka M, “Metabolic aspects of the 1 beta-proton and the 19-methyl group of androst-4-ene-3,6,17-trione during aromatization by placental microsomes and inactivation of aromatase” Biochem Pharmacol. 1994 Feb 11;47(4):717-26.
[6] Numazawa M, Tsuji M, Mutsumi A, “Studies on aromatase inhibition with 4-androstene-3,6,17-trione: its 3 beta-reduction and time-dependent irreversible binding to aromatase with human placental microsomes”.J Steroid Biochem. 1987 Sep;28(3):337-44.
[7] Marsh DA, Brodie HJ, Garrett W, Tsai-Morris CH, Brodie AM, “Aromatase inhibitors. Synthesis and biological activity of androstenedione derivatives” J Med Chem. 1985 Jun;28(6):788-95.
[8] Booth JE “Effects of the aromatization inhibitor androst-4-ene-3,6,17-trione on sexual differentiation induced by testosterone in the neonatally castrated rat” J Endocrinol. 1978 Oct;79(1):69-76.
[9] Levy H et.al, “The inhibition by metopirone of 11beta and 19-hydroxylations of androst-4-ene-3,17-dione in bovine adrenal perfusion” Steroids. 1965; 5:479-493
[10] Tan L et al., “De novo biosynthesis of 6 beta-hydroperoxyandrostenedione in human placental microsomes.” Biochem Biophys Res Commun. 1984 Feb 14;118(3):805-13.
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Old 02-09-2004, 02:10 PM   #8
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Methyl 1-Test (aka M1T)

Methyl 1-Test is 1-testosterone with an alteration to the molecule that allows it to pass through the liver more freely without degredation. When a compound is methylated it changes the physical structure of the compound and it tends to act differently in the body. In the case of methyl 1-test, it seems to be a much stronger anabolic without particularly androgenic sides. Methyl 1-test is being sold in 5mg and 10mg tablets, as well as in powder and solutions. Common doses are10-30mg once daily. The side effects seem to be harsher the more you use. Some of the more common side effects reported are lethargy, decreased appetite, very painful pumps as well as high blood pressure.
Methyl 1-test is a very powerful compound and is not recommended for beginners. Methyl 1-test can be stacked with 4AD to help counteract some of these sides and give you the benefits of testosterone supplementation. I would not recommend a cycle of methyl 1-test longer than 4 weeks.

Methyl 4/ad
This hormone will directly convert to methyltestosterone, which is a very poor compound. Methyltestosterone will aromatize to methyl-estradiol and convert to methyl-DHT. Dosages recommended are 10-40mg daily. Again, you would not want to use this for more than 4 weeks. Although it looks poor on paper, I have seen some good feedback and positive results from this product.

Methyl 1,4AD Diol
Converts to D-bol. This is a methylated version of the boldenone precursor, 1,4diol. In this version, the methylated version of the diol prohormone has been used instead of the dione. This will allow the hormone only direct conversion to its parent hormone, methylboldenone (Methandrostenolone) better known as Dianabol. Expect the same effects of it such as bloating, water retention and the high possibily of gyno. This is due to the fact that boldenone can aromatize into estrogen, here we would have a more powerful methylated estrogen, Methyl-estradiol. This would obviously be a very good mass builder, imparting gains in size and strength in a very short peroid of time. Obviously, quite a bit of it will be water though. Just as you would run Dianabol, you would want to stack it around 4AD/testosterone. You would want to have a good anti-estrogen on hand such as Nolvadex or Tamoxifen.


Methyl 5aa
Methyl 5AA should be a similar to Proviron or Masteron. This compound will make a conversion to Methyl-DHT in the liver through the 3bHSD enzyme. It should be very well suited as a preworkout stimulant, as well as reducing the effects of estrogen. Since DHT acts as an aromatize inhibitor, it can help reduce circulating estrogen on a cycle in place of typical anti-estrogens such as Nolvadex or 6OXO.
A concern for its users is the strong androgenic effets of DHT. This would obviously be a concern with individuals with potential prostate issues. It would be particularly beneficial preworkout, where it would impart some of the positive benefits on neural activity, giving the user added aggression, energy and strength to have a better workout. Doses are 5-30mg a day.


METHYLDIENOLONE
Methyldienolone is the trademarked name for the prosteroid 17a-methyl-17b-hydroxyestra-4,9(10)dien-3-one. Methyldienolone is similar to the effects of Methyl-1-Testosterone with far fewer side effects. Additionally, because it is not a "1-ene" compound, the typical lethargy and mild depression found in users of Methyl-1-Testosterone and other 1-testosterone products is not present with Methyldienolone use. Methyldienolone is a very close chemical cousin to methyltrenbolone (aka methyltrienolone). Common doses are 1-3mg per day. I think this will eventually replace M 1-Test.

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Old 02-10-2004, 12:34 PM   #9
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Coming Off A Cycle

Coming Off A Cycle
by Marcus Haidam

http://www.avantlabs.com/main.php?issueID=1&pageID=38


Introduction

A few minor inconveniences aside, the only really bad thing about steroids is that you have to come off of them. Technically, of course, you don't HAVE to, but this article isn't intended for those who fall into that category. Nor is it intended for the athlete who uses a gram per week for long periods and then typically uses insulin, DNP, prostaglandins, and other such compounds if they ever do actually come off (That topic, though quite fun to fantasize about, has nothing to do with most athletes). The recommendations in this article will do very little for maintaining the unnatural degree of muscularity attained with such methods. It's instead intended primarily for the moderate user, whom I'll (arbitrarily) define for our purposes as someone using 400-600 mg/week of steroids -- or very high doses of prohormones (1g/day of a topical, 100+mg/day intranasal). I don't recommend continuous lower intakes as suppression will still occur without the concomitant dramatic increases in LBM.

To start, we should mention a little bit about the "on" part of the cycle. We'd like to maximize gains and, at the same time, put ourselves in an optimal position to keep them once the cycle is stopped. What to do during the cycle could be an entire article itself, so I'll merely cover the areas where what we do has a direct influence on the recommendations while coming off.


Training

Training during the cycle should be high volume because muscle contraction upregulates androgen receptors (AR), and with supraphysiological levels of androgens, it's in our best interest to have as many AR's as possible. It will be very difficult to overtrain while "on", assuming optimal nutrition and rest, so basically do as much volume as you can handle and still have energized workouts and muscles that are not sore. This might be as much as 2 workouts/day (of about 45 minutes), 6 days per week for the genetically gifted)

We should avoid going to failure as it will ultimately limit our volume, plus we'll want our CNS fresh when we come off the cycle. So, no HIT shit, if you please. HIT type training is primarily effective in a situation where overtraining of the endocrine system has occurred (from 2 hour a day workouts) leaving the athlete with a poor testosterone to cortisol ratio. Again, we have supraphysiological levels of androgens, so that issue goes out the window.

The eccentric portion of the exercises won't be overemphasized because steroids cause increased muscle protein breakdown/fiber damage (with an even greater increase in muscle protein synthesis), so the high degree of muscle fiber trauma inflicted by eccentric training isn't only unnecessary, but it's probably counterproductive.

The preceding training strategies will not only maximize our gains while on the cycle, but as you will see later, will leave us primed for optimal retention when we come off.


The HPTA

Our other area of focus will be the hypothalamus-pituitary-testicular axis (HPTA). An 8-10 week, 24-7 cycle will almost certainly cause full suppression despite any strategies we might undertake, so it's a mute point in that situation, but with the 2 week mini-cycles that are becoming increasingly popular, it's likely that we can still have significant testicular function when our cycle is stopped.

There are two mechanisms by which negative feedback inhibition of the HPTA occurs, estrogen binding to the estrogen receptors (ER) and androgens binding to the androgen receptors(AR), both of which occur in the hypothalamus. We could prevent binding to the AR by using a receptor antagonist, but it would also antagonize the AR in the muscle, thus defeating the purpose of taking steroids -- unless, that is, significant non-AR mediated anabolism occurs, as has been suggested by some.


Another option here is to be "on" only during the mornings, using either orals or intranasal (or possibly a fast acting topical when/if an effective one becomes available), leaving us with normal systemic androgen levels at night when LH release occurs. This has been found to avoid significant alterations of the HPTA, even with as high as 100mg d-bol/day.

The final option is to decrease estrogen binding in the hypothalamus. This can be accomplished by lowering systemic estrogen with an aromatase inhibitor (and/or choosing anabolics that do not readily convert to estrogen) such as Arimadex, Cytadren, and perhaps high delivered doses of chrysin (whose in vivo potency equals that of Cytadren, but whose oral bioavailabilty is extremely poor, making sufficient delivery by that route basically unattainable for all practical purposes). We can also block access to the ER with an antagonist such as Clomid, Proviron, or Nolvadex (which, unfortunately, also interferes with a couple of enzymes involved in steroid production in the testes, thus canceling out its benefits on the AR, making it inferior to Clomid in that regard). Or, we could use a combination of aromatase inhibition and receptor antagonism. This strategy should prevent negative feedback to some extent, perhaps leaving us with testosterone levels of 400 instead of 200 (again, being rather arbitrary).

We have done all we can during the cycle, and now we have stopped and must do all we can to preserve our gains. If steps have not been taken to reduce estrogen binding in the hypothalamus, that should begin immediately. Clomid is the preferred choice in this area at 50-100mg/day, but an aromatase inhibitor should be just as effective, but its use should begin a few days earlier as it won't do anything for estrogen that's already present. Ideally, both methods should probably be used.

We must also now decide if we want to completely stop cold or use a morning only system in an attempt to maximize anabolism for as long as possible while still allowing HPTA recovery. If we choose the latter, it would probably not be a bad idea to time workouts to occur during this period - both for CNS effects and for anabolic effects. In deciding which is the best choice, the basic questions to be answered are: Does this method even provide significant anabolic benefit?? How much, if any, does it inhibit natural testosterone production?? And most importantly, do the positives of the first outweigh the possible negatives of the second?? My guess based on the available data and anecdotal reports is that is does. I would recommend this strategy for 2-3 weeks. At that point either go off completely or start a new "on" cycle.


Nutrition

When we stop our cycle, androgen levels are going to be below normal. That is a given, even with the afore mentioned strategies. What we can do something about is whether the other anabolic hormones (insulin, IGF-l, GH, thyroid, etc.) are maximized or not. Being handicapped by the first, we want to make the second as optimal as possible (hint: DO NOT START A DIET AT THIS POINT!!). Overeating (editors note: gluttons "overeat", athletes "overfeed") has been shown in numerous studies to maximize these factors, so I recommend continuing with above maintenance calories for the first week of "off" time. This will result in a bit of extra fat gain, but I've found it (when combined with all the other strategies in this article) to allow for almost total retention of LBM gains (again this is on a "moderate" cycle). As testosterone production returns to normal, calories can be lowered to maintenance or below.


Training

During the cycle, we trained using a high volume approach. During the "off" cycle, we will change things up (which, in itself, will be helpful for growth). As much shit as HIT gets (and deservedly so), it does have its uses. This is one of them. As mentioned earlier, the primary benefit of HIT type training is its beneficial effects on the endocrine system, and that will be very helpful now, as we desperately want to maximize testosterone levels.

Long workouts lower testosterone to cortisol ratios, so we are going to keep our workouts under ½ hour, no more than 4-5 times per week. We are going to stick to heavy, basic movements such as squats, deadlifts, pullups, etc, which also tend to increase testosterone levels. We'll also make heavy use of eccentric training during this period, as it is the eccentric part of a lift that causes most of the muscle fiber damage of weight training (hence, most of the gains). I have had a good deal of success doing one set per exercise, 2 sets per bodypart of drop sets that consist of 2-3 eccentric reps at 110-120% of 1-RM, followed immediately by 2-3 eccentric reps at 90-100% 1 RM, followed immediately by 2-3 full reps at 80-85% - taking 5-6 seconds for the eccentric portion on all 3 mini-sets.


Supplements

Clearly, if you are doing the mornings only "off" cycle, then the appropriate prohormone or oral is a necessity. I think creatine and a protein powder should always be used, and glutamine or BCAA's in fairly high doses (20+g/day) might also be helpful, but other than that, I won't make any specific recommendations at this time. I have a few thoughts on a combination of supplements in conjunction with a specific training method that I think is very promising , but I think I will refrain from mentioning it until a bit of real world testing is done.

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Old 02-11-2004, 02:04 PM   #10
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4-Hydroxytestosterone

4-Hydroxytestosterone
By David Tolson

http://www.bulknutrition.com/?ingredients_id=35

4-Hydroxytestosterone (4-OHT, 4,17beta-dihydroxy-4-androstene-3-one) is a legal steroidal compound that is relatively new to the market. Unlike prohormones, 4-OHT does not require enzymatic conversion to have an anabolic effect. It was first patented by G.D. Searle & Co. in 1955, but it did not reach the commercial market, and has recently become available as a dietary supplement. Chemically, 4-OHT is testosterone with a hydroxy group at the four position, making it most similar to the steroid clostebol, which has a chloro group at the four position. These two compounds are also very similar in effect.

4-OHT has moderate anabolic, mild androgenic, and anti-estrogenic properties. All in all, it can be expected to be associated with very few side effects, but this also comes at the expense of reduced anabolic activity. In the levator ani assay, 4-OHT is .65 times as anabolic and .25 times as androgenic as testosterone propionate. The reason that this compound has such low androgenic activity is that the modification at the 4 position prevents DHT conversion. In vitro, 4-OHT is actually a weak inhibitor of 5-alpha reductase. This weak androgenic effect is ideal for those who want to avoid or minimize side effects such as baldness, acne, and BPH. 4-OHT also has the benefit of having anti-estrogenic effects, which will eliminate chances of estrogen levels increasing, which can lead to side effects such as extra water retention and gyno. 4-OHT itself is a weak inhibitor of the aromatase enzyme which converts testosterone into estrogen, and a metabolite, 4-hydroxyan