NUBAIN (NALBUPHINE HCI)

Reported Characteristics
Drug Class: Narcotic/Analgesic (For injection)
Average Reported Dosage: 2.5-10.0 MG (0.25-1.0 ML) every 3 hours.
Noted Comments: HIGHLY ADDICTIVE

The first thing the reader should consider when reading this drug profile is “what is a narcotic drug doing in a book about bodybuilding chemistry? ” And in no way, assume any good did or could come from its use. Nubain is an injectable pain-killer similar to morphine in action and effect. In fact, the activity is about the same, as is its addictive potential, milligram for milligram. This is because Nubain is a synthetic opiate agonist/antagonist. The only positive aspect of Nubain is the fact that the drug is self-leveling (agonist/antagonist) which mostly prevents potential over-dosing. Dan Duchaine (the original steroid guru) has been credited with introducing Nubain to the athletic world, though its use in sports pre-dates Dan’s commentary. Dan speculated that Nubain maybe a viable anti-cortisol/anticatabolic drug with Lipolytic (fat burning) qualities. Dan was a genius when it came to thinking outside the box. But he missed on this one. (And should not be totally blamed by those addicted to it) Bodybuilders used Nubain (the crazy ones) as an intended thermogenic, anti-catabolic, and as a means of suppressing the pain of injuries from years of balls-out training.

This may have some validity since the drug does reduce an individual’s perception of stress, and is a powerful appetite suppressant. And like any opiate, the drug allowed some reported users to train well beyond the pain barrier threshold resulting in greater muscle fiber stimulation. So a lower perception of stress would slightly reduce total cortisol production. And an appetite fall-off would reduce total calorie intake while increased training intensity would increase calorie expenditure. But the fact is that the drug is no more thermogenic or anti-catabolic than any narcotic…just far more addictive. Some have speculated that Nubain will be replaced by heroin. Don’t laugh, Nubain is scheduled for manufacturer’s discontinuance. If the reader has seen Nubain users during withdrawal, the facts speak unwell for the future.

Dan Duchaine was a very resourceful individual and, though an ass at times, supplied an answer to an urgent request for help to those he cared for. In this case, a client who suffered two prior attempts at kicking Nubain, and was ready for another try out of necessity. Dan’s answer was a drug called Ultram, which is in the same drug class as Nubain but more like the clinical answer to heroin is Methadone. The client had a bit of an attitude but suffered no diarrhea no anxiety, no fever, or coughing, or sneezing. And he stated little or no Nubain craving resulted. He is Ultram/Nubain free still.

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PROSCAR (FINASTERIDE)

Proscar is a DHT inhibitor. An inhibitor usually prevents something from being
manufactured or converted, rather than simply blocking its receptor-sites. In the case of
Proscar, the drug inhibits 5-alfa reductase enzyme which is the enzyme responsible for
testosterone (nortestosterone converts to NOR-DHT) conversion to DHT
(dihydrotestosterone). As you know by now, DHT is one of the hormones associated with
accelerated balding and prostate enlargement. It is also responsible for many of the
virilizing effects from androgenic steroids. (Like it also hardens musculature)
Proscar is a prescription drug utilized for preventing hair loss. About 83% of users
reported a halt to hair loss. Unfortunately, some also report a reduced libido too. (Most
sport wooded if the wind blew during AAS cycles). Since Proscar inhibits, or atleast
reduces, the conversion of testosterones to DHT, theoretically there would be a greater
anabolic effect possible during AAS cycles. But there was an obvious loss of hardness to
the physique reported as well.

Bodybuilders who were chemically assisted did not have to be concerned with the libido
issue.
TRADE NAME
PROSCAR 1-5-MG TABS MERCK U.S.

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CATAPRES (CLONIDINE HYDROCHLORIDE)

This is a drug used to treat high blood pressure (antihypertensive). Bodybuilders
and other athletes using AAS often experience this problem due to increased water
retention and elevated blood counts. The reason this drug is included here is simple: It
raises serum levels of GROWTH HORMONE (GH) by stimulating production from the
pituitary gland. Some athletes reported taking 0.3 mg -0.15 MG on an empty stomach
both when going to bed and upon waking with a total of 0.18 mg per day, maximum.
Personally I disliked the drug due to its many negative side effects such as potency
problems, laziness, vertigo, and a few others. The use of antihypertensive drugs without a
doctor’s guidance is dangerous. Those prone to low blood pressure could die, those with
high blood pressure could miss the safe dosage and do the same.

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AVANDIA (ROSIGLITAZONE MALEATE TABS)

Reported Characteristics
Drug Class: Thiazolidinedione (Oral)
Average Reported Dosage: 2-8 MG 1-2 times daily
Water Retention: Moderate (Similar to low dose insulin use in some individuals)
High Blood Pressure: Rare

Avandia is a prescription antidiabetic drug similar in action to Glucophage (Metformin HCI) and belongs to a fairly new class of drugs called thiazolidinediones (Thigh-a-zoe-lid-een-die-owns). Medical use for Avandia is confined to treating type II diabetes. What the drug actually does is increase cell insulin receptor-site number and sensitivity. This in turn allows the body to better utilize insulin and therefore feed cells nutrients they require for repair and growth. The need for drugs such as thiazolidinediones is due to the tendency of cell insulin receptor-site number and sensitivity down-regulation realized by long term diabetic treatments. This means diabetics become resistant to insulin and their cells begin to deteriorate. In fact, insulin resistance is an underlying cause of type II diabetes. Clinical treatment for diabetes has finally begun to address drug / hormone synergy. The most elite bodybuilders polled realized that drug/hormone synergy/activity was the key to maximum growth rates.

And in the case of drugs such as Avandia, the methodology for application was multifaceted. Insulin is probably the most anabolic hormone there is. It was also noted to be highly synergistic with GH, IGF-1, PGF-2, Anabolic/Androgenic steroids, and several other growth inducing chemicals. However, maximum growth also required maximum receptor-site stimulation. (Which obviously is strongly dependant upon receptor-site number and sensitivity) There were several athletes who had hit growth plateaus due to insulin insensitivity. Sometimes this was due to over abuse of exogenous insulin during cycles and protocols. But it was more often due to either an athletes predisposition toward being a border-line diabetic or genetic limitations the endocrine system has placed upon growth. In either case, most of the elite group realized significant growth progress again by utilizing drugs like Avandia. *5-10 pounds of additional mass gain were common during a normal seasons period. Avandia is manufactured by Smith Kline Beech Pharmaceuticals and is provided as 2 MG, 4 MG, or 8 MG tablets. Athletes generally used Avandia in 12 week cycles with a progressive dosage:

Week 1-3 : 2 MG 2 times daily
Week 4-6 : 4 MG 2 times daily
Week 7-9 : 6 MG 2 times daily
Week 10-12 : 8 MG 2 times daily

According to available literature 12 weeks of continuous administration are required for Avandia to reach full effects in most individuals. A note of interest is that theoretically Avandia improved the results realized from IGF-1 use as well as insulin. This is due to the cross over stimulatory effect each of these hormones has upon the opposite receptor-sites. This may have had some positive effects upon GH use since GH converts to, and triggers IGF-1 release. Noted Comments *When athletes administered Avandia, hypoglycemia (Low blood sugar) occurred unless additional carbohydrates were ingested.

The usual ratio of carbohydrates to insulin athletes used was 10 grams of carbohydrates for each I.U. of insulin administered. However, when athletes layered Avandia (or Glucophage) into a protocol that contained insulin or pancreatic stimulators (such as Glipizide) the ratio often increased to 12-15 grams of carbohydrates for every I.U. of insulin. (*See Insulin for more information) *Failure to ingest adequate amounts of carbohydrates resulted in sweating, blurred vision, tremors, headaches, and confusion. Smarter athletes monitored their blood sugar (glucose) levels with test strips or metes.

Liver enzyme values should be checked regularly before, during and after the use of Avandia (or Glucophage) *It should be noted that additional negative side effects factually exist: Black outs, comas, and death to name a few. Insulin drugs were the most dangerous drugs utilized by athletes. FACT! Since growth induced by Insulin and IGF-1/GH use was dependent upon the hormone’s molecules merging with cell receptor-sites, it should seem apparent why Avandia was reported as quite effective for long term progress. Additionally, improved insulin sensitivity translates into an improved muscle to fat ratio body composition.

 

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TRIACANA (TIRATRICOL)

Reported Characteristics
Drug Class: Thyroid Hormone Metabolite. (Oral)
Average Reported Dosage: 1 MG per 50 LBS of bodyweight daily.
Noted Comments: Significant stimulator of thyroid activity / suppression of thyroid
function during use.

Triacana is a trade or brand name for the thyroid drug Tiratricol. The body naturally (endogenously) produces T-4/L-thyroxine, T-3/L-triiodothyronine, and T-2 /Ldiiodothyronine. Triacana is simply a synthetic form of these three thyroid hormones natural metabolite product, Triiodothyroacetic acid, or tiratricol for short. This means the body naturally produces Triacana as a metabolic by-product of other thyroid hormones. Triacana is sold in Europe as a prescription synthetic thyroid drug intended to restore natural metabolic rate. And of course it did not take long before bodybuilders began importing the drug with anabolic/androgenic steroids into Canada and the United States. This lead to custom agents adding Triacana to drug alert list and confiscation. Interesting since the chemical itself is not a controlled substance in most of the U.S. at this time. Have no fear though, the FDA and DEA are actively pursuing reclassifying Triacana /Tiratricol/Triiodothyroacetic acid as a controlled substance there. Triacana reaches maximum effects at a daily dosage of about 1 MG per 50 LBS of bodyweight. (Daily, meaning “total”) Since the chemical possesses a 6 hour half-life, this “daily dosage” was reported to be divided into 4 equal dosages. So a 200 pound athlete required 1 MG 4 times daily. Beyond this dosage no subsequent increase in metabolic rate occurs. What many, including the FDA, fail to realize is that Triacana administration will not induce a true replacement metabolic rate like other thyroid hormones. This means any polled athlete was able to increase their metabolic rate only equivalent to the upper range considered normal and acceptable through administration. So an individual whom employed this chemical realized a metabolic rate about equal to a so-called ectomorph only. Which is, in truth, a very significant increase and considered highly effective by all but a few users. This would make Triacana one of the safer thyroid drugs. *I have not found post administration thyroid function suppression from Triacana as of yet. But it is possible if use were prolonged. Obviously someone, somewhere, will somehow find a way to be the one exception who sues and does T.V. talk shows decrying the evils of this drug. No doubt while smoking cigarettes and drinking alcohol. (Another case of a day without the lifeguard monitoring the gene pool)

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T-2 (L-diiodothyronine or 3, 5-diiodo-L-thyronine)

Drug Class: Thyroid Hormone. (Oral)
Average Reported Dosage: 150-600 MCG daily.
*Minor noted suppression of thyroid function during lower dosage short term (30-35
days) administration.

There are two well known synthetic thyroid hormones commonly administered by bodybuilders known as T-4 and T-3. (*See “Synthroid” and “Cytomel” for more info) However, some have not yet heard of another natural thyroid hormone called T-2 or Ldiiodothyronine. The good new is that it is highly active and naturally occurring in some foods such as beef products. It is also non-prescription in many countries…so far. The bad news is that since it works quite well and offers individuals freedom of choice, it probably will not be legal for long.

So far, T-2 seems to be slightly more effective for fat oxidation (burning) than either T-4 or T-3 alone while offering an improved protein sparing-like result. This may be true. T-2 stimulates cellular mitochondria (cellular energy producers) more so than the cell nucleus. This means, unlike T-4 and T-3, T-2 is less likely to activate other cellular functions and more likely to focus upon increased metabolic rate or energy expenditure. Personal experience had shown an excellent synergistic effect between T-2, Norephedrine, and ephedrine plus caffeine. This is due to an interesting interplay between the substances.

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SYNTHROID (T-4/L-THYROXINE)

Reported Characteristics
Drug Class: Synthetic Thyroid Hormone. (Oral)
Average Reported Dosage: 100-400 MCG daily.

Noted Comments: Significant suppression of thyroid function during use. Synthroid is a man-made synthetically manufactured version of T-4/L-thyroxine. The average person produces about 76 MCG/d of T-4/L-thyroxine which is then converted by the liver into the more active T-3/L-triiodothyronine. This is true of the oral T-4/L-thyroxine medications as well. The average conversion rate of T-4 to T-3 is about 30-33%/ MCG. Since the conversion of T-4 to T-3 is dependent upon adequate levels of since and selenium, athletes commonly increase daily intake of these minerals during synthetic T-4/L-thyroxine use. As is the case with all thyroid hormone drug use, most athletes were noted as wiser to begin at a lower dosage of 100 MCG/d and slowly progress to their chosen dosage. Daily dosages of T-4/L-thyroxine that exceed 400 MCG will not increase metabolic rate beyond what is realized at 400 + MCG/d. Dosages that were increased too rapidly or that were too high commonly resulted in diarrhea, excessive sweating, rapid heart beat, nausea, vomiting, insomnia and trembling. T-4 drugs suppress endogenous thyroid hormone production significantly. After discontinuance, most athletes experienced a metabolic lag period of 3-15 days before thyroid function rebound occurred. Interesting fact is that most monitored athletes experienced a 120-130 % increase in endogenous thyroid hormones at that point. And some maintain that level permanently. *See guggulsterones for other possibilities.

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GUGGULSTERONES R

Reported Characteristics

Drug Class: Thyroid hormone stimulator. (Oral) Average

Reported Dosage: 20 MG (pure extract) 3-4 times daily.

Significant stimulation of thyroid function during use. Guggulsterone are an extract of the herb Commiphora Mukul, clinically proven to restore lagging metabolic rate caused by dietary calorie deficiency such as during diet phases. Ayurvedic medicine has utilized the unprocessed herb for centuries to treat energy deficiencies related ailments. Guggulsterones Z and E seem to have the greatest effect upon stimulation of thyroid hormone, though other substrates of the herb commiphora mukul may effect different metabolic factors as well. Thus far, research suggests this is a result of guggulsterones Z & E stimulation of TSH (Thyroid-Stimulating-Hormone) production. This results in an increase in Thyroid gland T-4 production and subsequent liver conversion to the more active T-3 hormone. Guggulsterones can be very beneficial to dieting athletes. When calorie intake is decreased, the body naturally decreases metabolic rate or calorie expenditure. This is why dieters often hit a fat loss wall after 2-4 weeks. Since TSH production begins the entire thyroid hormone cascade, guggulsterones can be very helpful at restoring “normal” metabolic rate at this point. It should be noted that guggulsterones do not inhibit normal thyroid activity or induce a negative feed-back loop. It is very unlikely that the use of this extract will lead to above normal accepted TSH, T-4, T-3 reference range production. Other benefits of guggulsterone supplementation include reduced blood cholesterol and triglyceride levels, increased fat oxidation (fat burning), increased energy, and better post-training recovery during diet restriction phases. Reduced acne has been noted. Please note that other diet defiencies can lead to reduced metabolic rate including phosphates, niacin, selenium, and magnesium among others, such as Zinc. Some athletes used guggulsterones to regenerate thyroid function after discontinuance of synthetic T-3/T-4 protocols. Those who thought ahead, utilized guggulsterones ” synthetic T-3/T-4 thyroid hormone use to prevent thyroid function suppression even temporarily. This usually was initiated 10-14 days prior to synthetic thyroid administration discontinuance. Coleus Forskohlii, the amino acid tyrosine, and iodine also had a noted great deal of value for this purpose.

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COLEUS FORSKOHLII (FORSKOLIN)

Drug Class: Herbal thyroid stimulator. (Oral)

Average Reported Dosage: (Standardized for 10% forskolin) 165-250 MG 3-4 times daily.

Significant stimulation of thyroid gland and adenylate cyclase production. Why is an herbal supplement in a book intended to report upon the things hardcore athletes have done? It should be recalled that most AAS synthesis begins with a plant extract as does ephedrine, methamphetamine, and heroin. The point being that powerful things come from many places…sometimes. Coleus Forskohlii increases cyclic AMP (cAMP) in cells and up-regulates thyroid gland function. Why is cellular cAMP so cool? The active substrate in Coleus Forskohlii is a diterpene derivative called forskolin. Well, forskolin stimulates the production of an enzyme called Adenylate-Cyclase (AC) which is sort of a master enzyme in the body that positively effects many other enzymes that regulate muscle growth and fat loss. In this case, AC increases cAMP which in turn activates Protein- Kinase (PK). This event allows a PK/phosphorylation reaction resulting in the active form of Hormone-Sensitive-Lipase (HSL). Finally …HSL stimulates the release of fatty acids from adipose tissue (fat cells) so muscle cells can use them as an energy (ATP) and fuel for heat source. Remember, UCP-3’s earlier in this section? Well, forskolin stimulates thyroid gland activity similarly to Thyroid-Stimulating-Hormone (TSH). TSH is also sometimes called thyrotropin. When the thyroid gland stimulated it begins the thyroid hormone cascade by releasing T-4 and so on. Since this results in an increase in circulatory thyroids hormone levels and an increase in (yup!) UCP-3’s, more of that newly released fatty acids supply is burned off.

The reason the basic biochemistry was explained here is simple. First, anything that affects any of the biochemicals we briefly discussed, also effects body composition. This includes all thermalgenics, AAS, insulin, GH, and most other anabolic chemistries. Second, the basic knowledge may prevent the reader from falling for supplement ad scams by knowing why something will or will not actually have value. Most products containing Coleus Forskohlii should be (but rarely actually are) standardized for a 10% forskolin content. An effective dosage of the 10% standardized product has been 165-250 MG, 3-4 times daily. So far there is some existing research that supports the listed effects of Coleus Forskohlii. And anecdotal /personal evaluations are positive thus far. It seems finding an actual standardized source is the most difficult aspect of acquiring favorable results. A note of interest. The use of Coleus Forskohlii seems to have possible cardiovascular benefits by acting as a vasodilator (lowers blood pressure) , inhibition of platelet aggregation (reduced blood clotting), and positive inotropic activity in the heart (increased contractile force). The use of Coleus Forskohlii does not seem to inhibit endogenous TSH production. There is a synergy between this product and beta-andrenergic drugs such as Clenbuterol, ephedrine, synephrine, and norephedrine.

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LASIX (FUROSEMIDE)

Reported Characteristics
Active-Life: About 6-8 hours (Diuretic effects)
Drug Class: Loop Diuretic (Oral)
Average Reported Dosage: 40-100mg total in a 12 hour period
Acne: None
Water Retention: You must be joking!
High Blood Pressure: None
Liver Toxic: Unknown
Aromatization: Does not apply

Lasix is probably one of the most dangerous drugs some pre-contest bodybuilders used. Even the IFBB tests for diuretics, and that is saying something Lasix was used to excrete excess water during the last day or two before a show. This was said to be especially effective with subcutaneous water (under the skin) so a “ripped to the bone, dry, and hard” look was achieved. Lasix was also used by some to lose weight for weight class oriented sports. Loop diuretics work by increasing the excretion of electrolytes (sodium, chloride, potassium) which the body normally uses to maintain intra cellular and extracellular water. Monitoring of the re-absorption of potassium, sodium, and chloride ions during use should have been a must, but few did so. Lasix can and has caused death. As to dosages, it depended upon the effect achieved. Normally 20-40-mg was taken and (over a periods of 2-4 hours) the bodybuilder evaluates the results. This was followed once or twice more at 4 hour intervals if more water loss was necessary. Too much water loss makes the body appear flat with no vascularity and makes it impossible to pump-up before walking out onto the stage. The effects of Lasix begin within about an hour of administration and continue for 6-8 hours. Once “the look” was achieved, it was unnecessary to ingest more to maintain “the look”.

Lasix is very strong and was reported to cause diarrhea, dehydration, dizziness, muscle cramps, circulatory disorders, vomiting, circulatory collapse, fainting, and cardiac arrest. It was considered far more safe to start with 20-mg and repeat every 4 hours than to use higher dosages for a shorter period of tome. Over 40-mg per dosage increased side effects dramatically!

TRADE NAMES
DIUNRAL 5,10,20,40,250,500-MG TABS
DIURAPID 40/500 40,500-MG TABS
DURAFURID 40-MG TAB
FURANTHRIL 40,500-MG TAB
FUROMEX 40-MG TAB
FUROMIN 40-MG TAB
FURON 40-MG TAB
FURONET 40-MG TAB
FUROSEMIDE 20,40,80-MG TAB
FUROSIFAR 40-MG TAB
LASIX 20-MG TAB
LASIX 25MG TAB
SEMID 40-MG TAB
VESIX 40-MG TAB
“INJECTABLE SOLUTION”-LASIX 20 or 40 MG/2ML or 4ML
SEMID 20MG/2ML
TROFURIT 20-MG/2-ML
VESIX 10-MG/1-ML

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