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hCG (Human Chorionic Gonadotropin)

Description:

Human Chorionic Gonadotropin (hCG) is a prescription medication containing chorionic gonadotropin obtained from a natural (human) origin. Chorionic gonadotropin is a polypeptide hormone normally found in the female body during the early months of pregnancy.It is synthesized in syncytiotrophoblast cells of the plecenta, and is responsible for increasing the production of progesterone, a pregnancy-sustaining hormone. Chorionic gonadotropin is present in significant amounts during pregnancy, and is used as an indicator of pregnancy by standard over-the-counter pregnancy test kits. Blood levels of chorionic gonadotropin become noticeable as early as seven days after ovulation, and rise evenly to a peak at approximately two to three months into gestation. After this point, the hormone level will drop gradually until the point of birth.

Although it possesses minor FSH-like (Follicle Stimulating Hormone) activity, the physiological actions of chorionic gonadotropin mainly mimic those of the gonadotropin luteinizing hormone (LH). As a clinical drug, hCG is used as an exogenous form of LH. It is typically applied to support ovulation and pregnancy in women, most specifically those suffering from infertility due to low concentrations of gonadotropins and an inability to ovulate. Due to the ability of LH to stimulate the Leydig’s cells in the testes to manufacture testosterone, hCG is also used with men to treat hypogonadotropic hypogonadism a disorder characterized by low testosterone levels and insufficient LH output. The drug is also used in the treatment of perpubertal cryptochidism, a condition in which one or both of the testicles have failed to descend into the scrotum. HCG is used by male athletes for its ability to increase endogenous testosterone production, generally during, or at the conclusion of, a steroid cycle, when natural hormone production has been interrupted.

Structural Characteristics:

Chorionic gonadotropin is an oligosaccharide glycoprotein composed of 244 amino acids. It has an alpha subunit that is 92 amino acids long and identical to that of luteinizing hormone (LH), follicle-stimulating hormone (FSH), and thyroid-stimulating hormone (TSH). It has a beta subunit that is unique to hCG.

Administration (Men):

When used to treat hypogonadotropin hypogonadism, current FDA-approved protocols recommend either a short 6-week program, or a long-term program lasting up to 1 year, depending on the individual needs of the patient. Prescribing guidelines for short-term use recommend 500 to 1000 units to be given given 3 times a week for 3 weeks, followed by the same dose twice a week for 3 weeks. The long-term recommendations call for 4,000 units to be administered 3 times weekly for 6 to 9 months, after which point the dosage is reduced to 2,000 USP units 3 times weekly for an additional 3 months. Bodybuilders and athletes use hCG either on cycle, in an effort to maintain testicular integrity during steroid administration, or after a cycle, to help restore hormonal homeostasis more quickly. Both types of use are deemed effective when properly applied.

Post-Cycle:

Human Chorionic Gonadotropin is often used with other medications as part of an in-depth Post Cycle Therapy (PCT) program focused on restoring endogenous testosterone production more rapidly at the end of a steroid cycle. Restoring endogenous testosterone production is a special concern at the conclusion of each cycle, a time when subnormal androgen levels (due to steroid induced suppression) could be very costly to the physique. The main concern is the action of cortisol, which in many ways is balanced out by the effect of androgens. Cortisol send the opposite message to the muscles than testosterone, or to breakdown protein in the cell. Left unchecked by a low level of testosterone, cortisol can quickly strip much of your new muscle mass away. Protocols for the post-cycle use of hCG generally call for the administration of 1500 – 4000 Units every 4th or 5th day, taken for no longer than 2 or 3 weeks. If used for too long or at too high a dose, the drug may actually function to desensitize the Leydig’s cells to luteinizing hormone, further hindering a return to homeostatis.

On-Cycle:

Bodybuilders and athletes may also administer Human Chorionic Gonadotropin throughout a steroid cycle, in an effort to avoid testicular atrophy and the resulting reduced ability to respond to LH stimulus. In effect, this practice is used to avoid the problem of testicular atrophy, instead of trying to correct it later on when the cycle is over. It is important to remember that the dosage needs to be carefully monitored with this type of use, as high levels of hCG may cause increased testicular aromatase expression (raising estrogen levels), and also desensitize the testes to LH. As such, the drug may actually induce primary hypogonadism when misused, greatly prolonging, not improving, the recovery window. Current protocol for the use of hCG in this manner involve administering 250IU subsutaneously twice per week (every 3rd or 4th day) throughout the length of the steroid cycle. Higher doses may be necessary for some individuals, but at no point should exceed 500iu per injection.

These on-cycle hCG protocols were developed by Dr.John Crisler, a well-known figure in the anti-aging and hormone-replacement field, for use with this testosterone replacement therapy (TRT) patients. Although TRT is often administered on a long-term basis, testicular atrophy is a common cosmetic complaint of patients irrespective of the maintenance of normal androgen levels. Dr. Crisler’s hCG program is designed to alleviate this concern in a manner that is acceptable for longer-term use. For those interested in precisely timing their hCG shots in relation to a prescribed testosterone replacement program, Dr. Crisler recommends the following in his paper, “An Update to the Crisler hCG Protocol,” “mmy test cyp TRT patients now take their hCG at 250IU two days before, as well as the immediately previous to, their IM shot. All administer their hCG subcutaneously, and dosage may be adjusted as necessary (I have yet to see more than 350IU per dose required)… Those TRT patients who prefer a transdermal testosterone, or even testosterone pellets (although I am not in favor of them), take their hcg every third day.”

Administration (Women):

When used to induce ovulation and pregnancy in anovulatory infertile woman, a dose of 5,000 to 10,000 units is administered one day following the last dose of menotropins. The timing is specific so that the hormone is given precisely at the right moment in the ovulation cycle. Human Chrionic Gonadotropin is not used by women for physique- or performance-enhancing purposes. We recommend you to read our steroid profiles before buying any drug from us or elsewhere.

Proscar (Finasteride)

Finasteride is a specific inhibitor of 5a-reductase, which is the enzyme responsible for converting testosterone into DHT (dihydrotestosterone). This drug can efficiently reduce the serum concentration of DHT, therefore minimizing the unwanted androgenic effects that results from its presence. The effect of this drugs is quite rapid, suppressing serum DHT concentrations as much as 65% within 24 hours after taking a single 1mg tablet. Medically, this drug has been marketed to treat two specific conditions. The first release of finasteride in the U.S. was under the brand name of Proscar, made for use by patients with benign prostate hyperplasia (prostate enlargement). Finasteride was approved for use as an anti-balding medication. We now have the additional brand name Propecia, which is the same drug but the tablet contains only 1/5th of the Proscar dosage. Scientists have long believed that DHT was the main culprit in many cases of male hair loss (along with genetic factors), so there was little doubt after the release of Proscar that finasteride would eventually be used for this purpose. It has provided what many feel is a breakthrough for men with hair-loss problems.

Due to the very specific nature of finasteride, it has little effect on the other hormones in the body. It has no affinity for the androgen receptor, and does not exhibit any androgenic, anti-androgenic, estrogenic or anti-estrogenic properties. It should have no impact on circulating levels of cortisol, thyroid-stimulating hormone, or thyroxine, nor should it alter HDL/LDL cholesterol levels. Changes in luteinizing hormone (LH) or follicle-stimulating hormone (FSH) are also not notable, and it is not shown to have an effect on the hypothalamic-pituitary-testicular axis. In a small percentage of cases the decreased DHT level did produce symptoms of sexual disinterest/dysfunction. Although this is not a common complaint, this problem can usually be resolved quickly by discontinuing the drug. It is also interesting that finasteride has been shown to increase circulating levels of testosterone by roughly 15%, since a greater amount of the androgen is being left unaltered by the reductase enzyme.

Proscar/Propecia shows great potential for the steroid using athlete. And as you know, the dihydrotestosterone (DHT) metabolite is responsible for many of the unwanted androgenic side effects associated with testosterone use. The high levels of DHT that form in certain tissues produce oily skin, acne, facial/body hair growth and accelerated male pattern baldness. By minimizing the production of DHT, we should greatly reduce many of these harsh side effects and make our testosterone cycles more comfortable. In many instances, Proscar/Propecia can allow the athlete the use of steroid compounds (testosterone esters such as cypionate, enanthate, sustanon etc.), Halotestin and methyltestosterone with much less androgenic side activity. Of course we must not forget that all steroids activate the androgen receptor, so while this item offers help by means of reduced androgenic activity, no drug exists that can completely block androgenic side effects from appearing with steroid use.

One other to note is that finasteride specifically blocks the Type II 5a reductase enzyme. There are actually two “isozymes” in the human body, labeled as Type I and Type II. Type I 5a-reductase is predominant in the sebaceous glands of most regions of skin. The Type II 5a-reductase isozyme is primarily found in prostate and hair follicles (among others). So although the Type II enzyme is responsible for about two-thirds of the circulating DHT, a small amount of DHT may still be produced in the body by the Type I enzyme. Finasteride may therefore have a more pronounced effect when preventing hair loss, and be somewhat of a lesser benefit when dealing with acne and body/facial hair growth (tissues where the Type I enzyme is still active).Of course the drop down in serum DHT will still have some beneficial effect on all related side effects. This is not a major concern in any event, as hair loss is really the primary worry amongst most male steroid users who would use this drug. A little oily skin or new hair growth on the back/shoulders can be dealt with by other means or simply endured. The user knows these problems will only be temporary. But the advancement of balding condition can be very difficult, if not impossible to reverse. We must also so remember that testosterone, halotestin and methyltestosterone are really the only hormones that converts to stronger steroids via 5-alpha reductase. Boldenone and methandrostenolone do also I guess, but to such a low degree that one would think Proscar would be of little significance. Perhaps we will come to find that some other steroids are broken down into stronger metabolites via 5a-reductase, but needles to say for now the uses of this drug are not great in number.

There is no research to site on exactly what dosage would be the most appropriate for a steroid user. Logic would dictate that the typically prescribed amount of Propecia, a single 1mg tablet per day, would most likely be sufficient. In clinical trials the effect of just a single tablet is clearly dramatic. But if after a while the androgenic content of the cycle is still perceived as too high, increasing the number of tablets per day may be necessary. Proscar/Propecia is also a relatively expensive compound, so it can become quite costly as the dosage increases. It is probably best to keep the dosage at the lowest effective amount. Cost may not be the only basis for such a decision, as DHT is believed to affect the nervous & reproductive system in many beneficial ways. By minimizing this conversion we not only face the possibility of interference with sexual functioning, but might also be inadvertently lessening the level of strength gained during testosterone therapy (this being tied to the action of DHT on the neuromuscular system). A “use only when necessary” position should likewise be taken in regard to this drug.

It is also important to note that while women may receive some small benefit from the drug (although testosterone is really not a steroid for females), they must be very careful with it. Those who are, or might become pregnant, should never take or even handle a finasteride tablet. The DHT blocking action can cause severe developmental problems to an unborn fetus, even in very small amounts. Since the drug can be absorbed through the skin, handling a broken tablet may be all that is needed for such an occurrence. Since women generally stay away from testosterone, and the design of Proscar/Propecia has been strictly for men, as of yet there is little to report on the effectiveness of this compound for combating virilization symptoms.

Clenbuterol (Clenbuterol Hydrochloride)

Clenbuterol is a widely used bronchodilator in many parts of the world. The drug is most often prepared in 20mcg tablets, but it is also available in syrup and injectable form. Clenbuterol belongs to a broad group of drugs known as sympahtomimetics. These drugs affect that sympathetic nervous system in a wide number of ways, largely medicated by the distribution of andrenoceptors. There are actually nine different types of these receptors in the body, which are classified as either alpha or beta and further sub categorized by type number. Depending on the specific affinities of these drugs for the various receptors, they can potentially be used int he treatment of conditions such as asthma, hypertension, cardiovascular shock. The text Goodman and Gillman’s The Pharmacological Basis of Therapeutics 9th Edition does a good job of describing the diverse nature in which these drugs affect the body:

“Most of the actions of catecholamines and sympathomimetic agents can be classified into seven broad types: (1) peripheral excitatory action on certain types of smooth muscles such as those in blood vessels supplying the skin, kidney, and mucous membranes, and on the gland cells, such as those of the salivary and sweat glands; (2) a peripheral inhibitory action on certain other types of smooth muscle, such as those in the wall of the gut, in the bronchial tree, and in blood vessels supplying skeletal muscle; (3) a cardiac excitatory action, responsible for an increase in heart rate and force of contraction; (4) metabolic actions, such as an increase in the rate of glycogenolysis in liver and muscle and liberation of free fatty acids from adipose tissue; (5) endocrine actions, such as modulation of the secretion of insulin, rennin, and pituitary hormones; (6) CNS actions, such as respiratory stimulation and, with some of the drugs, an increase in wakefulness and psychomotor activity and a reduction in appetite; and (7) presynaptic actions that result in either inhibition or facilation of the release of the neurotransmitters such as norepinephrine and acetylcholine.”

The drug clenbuterol is specifically a selective beta-2 sympathomimetic, primarily affecting only one of the three subsets of beta-receptors. Of particular interest is the fact that this drug has little beta-1 stimulating activity. Since beta-1 receptors are closely tied to the cardiac effects of these agents, this allows clenbuterol to reduce reversible airway obstruction (and effect of beta-2 stimulation) with much less cardiovascular side effects compared to non-selective beta agonists. Clinical studies with this drug show it is extremely effective as a bronchodilator, with a low level of user complaints and high patient compliance.

Clenbuterol also exhibits and extremely long half-life in the body, which is measured to be approximately 34 hours long. This makes steady blood levels easy to achieve, requiring only a single or twice daily dosing schedule at most. This of course makes it much easier for the patient to use, and may tie in to its high compliance rate. Despite that clenbuterol is available in a wide number of other countries however; this compound has never been approved for use in the United States. The fact that there are a number of similar, effective asthma medications already available in this country may have something to do with this, as a prospective drug firm would likely not find it a profitable enough product to warrant undergoing the expense of the FDA approval process.

In animal studies clenbuterol is shown to exhibit anabolic activity, obviously an attractive trait to the athlete. The compound is additionally a known thermogenic, with beta-2 agonists like clenbuterol shown to directly stimulate fat cells and accelerate the breakdown of triglycerides to form free fatty acids. Its efficacy in this area makes clenbuterol a very attractive, and today almost mandatory, pre-contest drug. Those interested in this drug are most often hoping it will impart a little of both benefits, promoting the loss of body fat while imparting strength and muscle mass increases. But as was well pointed out by a review published in the August 1995 issue of Medicine and Science in Sports and Exercise, the possible anabolic activities in humans are very questionable, and based only on animal data using much larger doses than would be required for bronchodilation. With such reports there has been a lot of debate lately as to whether or not clenbuterol is really anabolic at all. Some seem to swear by the fact that it builds muscles regardless, firmly sticking by “clen” as a great off-season or adjunct anabolic. To others such reports are confirmation that athletes have wasted valuable time and money on drugs that do not work as they are intended to by the user.

This debate continues today, with many still using clenbuterol as a potential anabolic. With this in mind athletes will tailor their dosage and cycling of this product individually depending on which of the two “possible” results are most desired, and how much side effects are to be tolerated. The possible side effects of clenbuterol include those of other CNS stimulants, and include such occurrences as shaky hands, insomnia, sweating, increased blood pressure and nausea. These side effects will generally subside after a week or so of use however, once the user becomes accustomed to the drug. One would typically start a cycle by gradually increasing the dosage each day until a desired range is established. This process will minimize the unwanted side effects seen from the drug; which otherwise might be dramatic if a large dose is administered from the onset. Men generally end up in the range of 2 – 8 tablets per day (40mcg – 160mcg), although some people do claim to tolerate even higher dosages. Women get by on less generally 2 – 4 tablets daily (40mcg – 80mcg). Very quickly, the drug will elevate the body temperature. The rise is not usually dramatic, perhaps a half of a degree or so, sometimes a little more. This elevation is due to your body burning excess energy (largely from fat) and is usually not comfortable.

Now that it is working, the number of consecutive days clenbuterol can be used is believed to be dependent on the goal of the individual. To be clear, the athletic benefits of this drug will only last for a limited time and then diminish, largely due to beta-receptor down regulation. When using it for fat loss, the primary effect of the drug, it seems to work well for approximately 4 – 6 weeks. During this peroid, users will want to constantly monitor their body temperature elevation. Once the temperature drops back to normal, clenbuterol is no longer exhibiting a thermogenic effect. At this point increasing the dosage would not be very effective, and a break for at least a few weeks should be taken before it is used again effectively. If one is looking for strength gains, clenbuterol appears to be effective for a much shorter period of time, around 3 – 4 weeks. This may be due to an absence of real anabolic effect, with the strength gain seen with clenbuterol possibly due only to the stimulant properties of the drug. Again however, this is still debated.

Many competitors also find the fat burning effect of clenbuterol can be further enhanced by additional substances. When combined with thyroid hormones, specifically Cytomel, the thermogenic effect can become extremely dramatic. This can be to a point that the athlete could shred exceptional amounts of extra far during contest preparations, without a dramatic restriction in calories. Such a mix can be further used during a steroid cycle, eliciting a much harder look from the anabolics. These cutting agents can often greatly inhibit extra fat storage during the cycle, even when using strong aromatizing androgens. A clenbuterol/thyroid mix is also common when using growth hormone, further enhancing the thermogenic and anabolic effect of this therapy. Ketotifen has also been extremely popular adjunct to clenbuterol therapy as of late, which is an anthistamine that exhibits the peculiar and extremely welcome side affect of upregulating beta-2 receptor density. It seems capable of not only increasing the potency of each dose of clenbuterol, but also preventing the rapid drop in thermogenic effect that is attributed to receptor down regulation.

Zaditen (Ketotifen Fumarate)

Ketotifen is an antihistamine, which is, oddly enough, used for the treatment of asthma in addition to allergy symptoms (the main focus of antihistamine use). It is sold in a number of countries around the world including Canada white it is available in both its brand name and generic forms. The drug is an ophthalmic anti-allergy solution (Zaditor), and not as an oral allergy/asthma medication. When used for asthma it is not effective in treating an immediate attack (it is not an immediate bronchodilator), but does seem to reduce the frequency and severity of problems overall when taken on a daily basis, as well as increase the efficacy of other asthma medications. This drug seems to have proven itself in the marketplace as a very safe, and effective, treatment option for persistent asthma or allergy symptoms.

Ketotifen works works to alleviate allergy symptoms by blocking histamine H1 receptors. But it is through its second, extremely unique, mode of action that this agent helps with asthma: Ketotifen is a potent upregulator of beta-adrenergic receptors, especially beta-2 receptors. This also makes it an extremely valuable compound when it comes to fat loss, at least in the bodybuilding world. Perhaps maybe not this drug directly, but when taken with a beta-2 agonist thermogenic like clenbuterol, the benefits are both obvious and dramatic. You see, clenbuterol has a limited scope of usefulness because beta-2-adrenergic receptors down regulate very quickly. Soon after you start using the drug, its benefits begin to diminish. Within several weeks, the drug is usually discontinued because it is no longer working very effectively as a fat loss agent. Zaditen changes all that. A dosage of 2 – 3mg per day (two or three 1mg tablets) seems more than sufficient to prevent the normal receptor down regulation with clenbuterol, allowing you to run long cycles instead of brief intermittent ones. Some are finding the combination of clen and ketotifen to be effective for 12-week cycles or longer, something nobody would have dreamed possible before Zaditen.

The ability of ketotifen to potentiate the effects of beta-adrenergic agents is not just theory. This fact has been demonstrated in a number of placebo-controlled human medical studies. For example, one study published back in 1990 demonstrated that when ketotifen and clenbuterol were taken together, there was a clear increase in beta-adrenergic receptor density compared to the use of clenbuterol alone. Other studies with salbutamol show that the down regulation that had been caused by long-term use of these beta-adrenergic agent, was rapidly reversed with as little as 2mg of Ketotifen per day. All this just solidifies what almost everyone who uses the drug will tell you: it works, and it works well. There is little questioning how much of a breakthrough this agent is in the world of bodybuilding drugs.

The drug does tend to produce some side effects that you should be aware of. This may include dry mouth, appetite stimulation, weight gain, or the drowsiness often associated with strong antihistamine compounds. But then again, this compound does seem to have a very good record when it comes to patient compliance and comfort, with users rarely reporting much trouble. Provided the drowsiness doesn’t get to you (this side effect seems to be most noticeable with higher doses like 6 – 10mg per day), this drug can make a night and day difference on your next fat loss cycle, at least if your planning to include a beta-agonist such as clenbuterol.

Cytomel (Liothyronine Sodium)

Cytomel is the popularly recognized brand name for the drug liothyronine sodium. This is not an anabolic steroid but a thyroid hormone. It is used medically to treat cases of thyroid insufficiency, obesity, certain metabolic disorders and fatigue. Specifically this drug is a pharmaceutical preparation of the natural thyroid hormone triiodothyronine (T-3). When administered, Cytomel increases the patient’s metabolism. The result is an increased rate of cellular activity (noted by a more rapid utilization of carbohydrates, fats and proteins). Bodybuilders are particularly attracted to this drug for its ability to burn of excess body fat. Most often utilized during contest preparation, on can greatly decrease the amount of stored fat without being forced to severely restrict calories. To this end Cytomel is commonly used in conjunction with clenbuterol and can produce extremely dramatic results. This combination has become very popular in recent years, no doubt responsible for many “ripped” on-stage physiques. It is also noted by many that when thyroid hormones are taken in conjunction with steroids, an increased anabolic effect can be seen (noticeably greater than if the steroids are used alone). This is likely due to faster utilization of proteins by the body, increasing the rate for new muscle accumulation.

One should take caution if considering using this drug. Cytomel comes with an extensive lists of warnings and precautions which are not to be ignored. Side effects include, but are not limited to, heart palpitations, agitation, shortness of breath, irregular heartbeat, sweating, nausea, headaches, and psychic/metabolic disorders. It is a powerful hormone, and one that could potentially alter the normal functioning of the body if misused. When administering Cytomel, one must remember to increase the dosage slowly. Generally one 25mcg tablet is taken on the first day, and the dosage is thereafter increased by one tablet every three or four days for a maximum dosage of 100mcg. This will help the body adjust to the increased thyroid hormone, hopefully avoiding any sudden “shock” to the system. The daily dose is also to be split evenly throughout the day, in an effort to keep blood levels steadier. Women are more sensitive to the side effects of Cytomel than men, and usually opt to take no more than 50mcg daily.

It is important to stress that a cycle should last no longer than 6 weeks and it should never be halted abruptly. As slowly as the dosage was built up it should also be lowered, one tablet every 3 – 4 days. Taking Cytomel for too long and/or at too high a dosage can result in a permanent thyroid deficiency. After doing such, one might need to be treated with a drug like Cytomel for life. It is also a good idea to first consult your physician and have your thyroid function tested. An undiagnosed hyperfunction would not mix well with the added hormone. An athlete should also be sure never to purchase an injectable form of this drug. It is generally an emergency room product, much too powerful for athletic use. Since T-3 is the most powerful thyroid hormone athletes are using, this is generally not the starting point for a beginner. Before using such a powerful item, it is a good idea to become familar with a weaker substance. Synthroid (synthetic T-4), still weaker in action than Cytomel. Once the user is ready however, the fat burning effect of this hormone can be extremely dramatic.

Synthroid (Levothyroxine Sodium)

Synthroid is a popularly referenced brand name (U.S.) for the drug levothyroxine sodium. Specifically this is a synthetically manufactured thyroid hormone, with the effect of the endogenous hormone thyroxine (T-4). Thyroid hormones are primarily responsible for regulating the body’s metabolic rate, and play an important role in determining one’s physical disposition. When thyroid preparations are administered, the metabolism is markedly stimulated. This is noted for the faster conversion of carbohydrates, proteins and fats, as the body utilizes more calories throughout the day. These hormones are used medically to treat cases of both thyroid dysfunction and obesity (due to a related deficiency).

The action of this drug is very similar to that of the popular thyroid preparation Cytomel. Cytomel is slightly different in structure however, being a synthetic triiodothyronine (T-3) hormone. A healthy individual will actually have sufficient levels of both T-3 and T-4 thyroid hormones present in the body. In comparison, T-3 thyroid has an effect four times stronger than that of T-4 on a weight basis (most of T-4′s action actually comes from converting to T-3). This is clear when we look at the average tablet strength of both items, Cytomel produced in much smaller microgram amounts. Likewise the preparation Cytomel is much stronger than the product Synthroid, and is usually the preference should both items be available. Since Synthroid is much weaker, an athlete will generally expect to take the drug for a longer duration than Cytomel in order to achieve a similar result.

Thyroid hormones are among the most efficient cutting agents in the athlete’s drug arsenal. Administration should noticeably increase the rate in which the body breaks down fat stores, allowing more muscle definition to become visible. And since the body is utilizing more calories during the treatment, the need for drastic dieting is greatly reduced. This is an added benefit during contest time, as muscle mass is often sacrificed when nutrients are severely deprived. Thyroid use will generally allow the athlete to burn off body fat while still consuming a comfortable level of calories each day. Anabolic steroids are generally used in conjunction with these hormones, as the metabolism boosting effect may result in faster muscle gains (increased protein utilization). This leads some to use thyroids during off-season bulk cycles, looking to obtain a greater muscle mass gain while accumulating less body fat than typically expected.

The dosage of this drug, as with all thyroid medications, must be built up slowly and evenly. An athlete will generally start with a low dosage of 25 – 100mcg and slowly increase the amount 25 – 50mcg each day or two. The final dosage should not exceed 200 – 400mcg. With thyroid medications you run the risk of permanently altering your metabolic functioning when administering too high a dose or continuing treating for too long a period. Cautious individuals will be sure not to use excessive amounts nor continue treatment for longer than 6 to 8 weeks. On the same note it is important to reduce your Synthroid dosage gradually at the end of your cycle, just as the dosage was built up in the beginning. Dropping the dosage by 25 – 50mcg every second or third day should should be and acceptably gradual withdrawal. This will give your body a chance to become more adjusted to the changing hormone level and avoid the “shock” that is possible when the drug is suddenly discontinued.

There are a number of side effects associated with Synthroid that a potential user should be aware of. These include, but are not limited to, trembling, excessive sweating, diarrhea, insomnia, nausea, elevated heart rate, inner unrest and weight loss. Mild occurrences of such side effects are usually eliminated by temporarily lowering the daily dosage. If the side effects are becoming uncomfortably pronounced, the drug of course should be discontinued. Again, abruptly stopping the drug may produce more unwelcome side effects; so tapering at this point is still recommended if possible. In an effort to avoid any severe problems, many athletes opt to first visit a doctor and have thyroid functions screened before committing to use. A previously unnoticed thyroid hyperfunction can prove very troublesome to someone administering this drug.

Lasix (Furosemide)

Lasix is a brand name for the drug furosemide, a very potent diuretic. Technically it belongs to a class of drugs known as loop diuretics, which will cause the body to excrete water as well as potassium, sodium and chloride. Loop diuretics are amongest such drugs available, having an extremely dramatic effect on fluid levels in the body. Potassium levels need to be particularly watched, Lasix greatly increasing the amount excreted. The use of a prescription potassium supplement therefore is often required to keep levels in balance, otherwise serious heart complications might develop. Mistakes in potassium dosage have equally serious consequences, so Lasix is clearly a risky item to use. But when an athlete needs to shed water, it is very difficult to find something that works better.

Athletes use diuretics for a couple of specific purposes. Competitive athletes use these drugs to drop water weight, in an effort to make adjustments in their weight class standing. Since the weigh-in is most often a day or days before a competition/match, one can drop their bodyweight considerably and be back to normal within hours after dehydration. This logically seems to provide an unfair advantage, the athlete competing at a much heavier weight than believed. This advantage is only offset by the now near universal nature of this practice. Bodybuilders also rely heavily on diuretics when preparing for a contest. It can effectively lower subcutaneous water concentrations, helping to produce that super-ripped look so common on stage today. Make no mistake; a winning look is extremely difficult to obtain without some form of diuretic.

This drug is prepared as both an oral tablet (usually 20 – 40mg per tablet) or IM/IV injection solution, the injection being much more rapid in effect. The dosage and method of administration is tailored to the individual, dependent on the desired goals and condition of the athlete. Tablets are the most common form of administration. Each oral Lasix tablet becomes effective about 1 hour after ingesting and will remain active for an additional 3 or 4 hours. The athlete will usually start with a mild dose, and add to this amount accordingly later in the day. The initial dosage is usually 20 to 40mg, with the maximum amount usually not to exceed 80mg. The user will attempt to calculate the optimal dosage, and determine the best intake schedule in relation to the show or competition. In order to minimize the side effects associated with this drug, it is generally used for no longer than a few days.

Since Lasix has such a strong effect on electrolyte and potassium levels, it is much safer to addition a potassium sparing agent like Aldactone (spironolactone) than it is to keep increasing the amount of Lasix used. A combination of 50mg Aldactone and 20mg Lasix would be a good starting point, having roughly the effect of a 40mg Lasix tablet without the notable potassium loss. This dosage is repeated 2 – 3 times during the day and the effect judged to determine the optimal dosage. It is important to remember that these drugs can be active for many hours. It can become difficult to control the dehydrating effect with an overlapping schedule, so one should be careful not to administer such diuretics too frequently.

The injectable is a much powerful version of the drug. It can be administered both intramuscularly and intravenously, depending on the intensity the user is looking for. The IV method is extremely fast, the strong effect of the drug felt in a matter of minutes. Since the injection is much more powerful than the oral, the dosage is to be considerably reduced in comparison. The injected dosage is usually in the range of 10 – 40mg, rarely going any higher. Drug testing for Lasix at bodybuilding competitions has increased the popularity of last minute IV diuretic use, a very dangerous practice. Instead of slowly shedding water the few days prior, the user is forced to wait until after the “piss-test.” Then in a frantic rush to remove subcutaneous water before the show, the drug is administered. The user often has little time to adjust the dosage, resulting in a number of fatal mistakes in recent years. The effect of Lasix is actually easier to control with the injectable under normal conditions. When there is room to experiment, adjustments in dosage are much easier to make (the user not having to wait very long to see an effect). And the optimal dosage is certainly less trouble to calculate for a later time as well, the user having fewer variables to worry about. But again, when used in a rush this drug can be extremely dangerous.

Lasix is no doubt one of the most dangerous drugs a competitor will use. This can be seen on occasion when severe dehydration and electrolyte imbalance take the life of an ambitious athlete. Warning signs that Lasix may be causing severe dehydration include (not limited to) dizziness, cramping, vomiting, diarrhea, fainting and circulatory disturbances. Potassium depletion can be marked well, so as discussed users often opt to take a prescription potassium supplement, also with its own set of dangers. One should use extreme caution when considering using Lasix or other diuretics; they are certainly not needed for recreational users.

Dostinex (Cabergoline)

Dostinex is the pharmacy trade name for the drug cabergoline, a selective dopamine receptor agonist. This agent is highly specific in its actions, with a strong affinity for the dopamine D2 receptor, and a low affinity for dopamine D1, A1-adrenergic, 5-HT1-serotonin, and 5-HT2-serotonin receptors. Its main clinical use is for the treatment of hyperprolactinemia, or the hypersecretion of prolactin from lactotropes in the anterior pituitary (pituitary tumor is a common cause of this disorder). Carbergoline effectively inhibits prolactin secretion, which it does by mimicking the actions of dopamine on the D2 receptor (dopamine normally serves as negative feedback for prolactin release). As a targeted agonist of the dopamine D2 receptor, cabergoline should not affect other pituitary hormones like growth hormone (GH), luteinizing hormone (LH), corticotrophin (ACTH), or thyroid stimulating hormone (TSH).

Prolactin is a somatotropic hormone, in the same family as human growth hormone (somatropin). It is a single peptide hormone, containing a chain of 199 amino acids. This makes it similar to (though slightly larger than) growth hormone, which is made of 192 amino acids. Any similarity between these two hormones, however, ends at structure. Prolactin is not an anabolic agent (at least not to skeletal muscle but a lactation hormone. Most of its physiological value is in women, and becomes apparent during pregnancy when it aids in milk production. In men, prolactin has no known therapeutic value, and high levels are associated with impotence, infertility, and sometimes even gynecomastia (whether or not it has a causative role here remains the subject of much debate).

Although this is almost never associated with males, high levels of prolactin have actually been related to lactating gynecomastia in a very small percentage of steroid-using athletes. This disorder is often characterized by small fluid discharge that becomes noticed with the squeezing of one’s gynecomastic nipple. Although the situation can become worse, the first sign of this is often enough to scare the individual away from their current regimen of steroids. Gynecomastia is not automatically (or even normally) associated with lactation, so this is a somewhat rare phenomenon. It is probably caused by an unusual imbalance of hormones (androgens, estrogens, progestins can all be involved, and play varying roles), and/or a particular personal sensitivity to the disorder. When it does occur, however, cabergoline has offered a very effective remedy for the sometimes embrassing situation.

High prolactin levels (as would be associated with the need for Dostinex) are commonly not documented in steroid-using athletes, further underscoring the relative uncommon nature of this disorder. We do know that estrogen plays a stimulatory role here, and likely is the key to increasing prolactin secretion in males. Other studies, however, show suppressive actions toward prolactin from other hormones including androgens. This is perhaps why an actual hormonal imbalance, and not necessarily high estrogen, would be the cause of lactating gynecomastia. Scanning the medical books, we find few studies even looking at prolactin levels and steroid use, and those few are relatively inconclusive. One looking at the effects of testosterone enanthate and propionate in men noted significant prolactin increase 4 days after injection. Yet another noted a 7-fold increase in estrogen (to values typical for women) in 5 power athletes self-administering testosterone and other steroids, yet no consistent effect on prolactin secretion. A third self-administration study with athletes, and a fourth clinical with nandrolone, failed to show an increase in prolactin levels.

Although foreseeing the need for an anti-prolactin is difficult, the use of Dostinex itself is relatively simply should one become apparent. The typical protocol involves not taking the drug daily, but administering it only twice per week. The user starts with a dosage of .25mg per application, or a 1/2 tablet. This is used for four weeks, at which point the dosage might be adjusted upwards to a full tablet if needed. In clinical medicine this dosage may be further increased to 1mg (2 tablets) in some cases, however the high cost of the drug (and relative low levels of prolactin compared to those produced with some tumor disorders) usually precludes such use in bodybuilders. The drug itself is usually taken for 6 months or longer in a medical setting, although athletes usually find a 4 – 6 week course of therapy (combined with an intelligent rearrangement of the offending drugs) most appropriate.

Since effects are relatively infrequent with Dostinex use, and most reported events are mild or moderate in nature. The most common complaints were headache, nausea, an vomiting, which occurred in 26%, 27%, and 2% of patients (respectively) receiving the medication during one clinical trial. Other potential side effects include (but are not limited to) constipation, dry mouth, abdominal pain, diarrhea, dizziness, vertigo, fatigue, anxiety, anorexia, malaise, depression, insomnia, hot flashes, heart palpitations, hypotension, breast pain, and acne, however their prominences tended to be much lower than those of nausea and headache. Many are dose related, further reason for starting off with the lowest possible therapeutic dose and working up. The prescribing information does not mention death as a clear consequence of an overdose, but it does list hallucinations, low blood pressure, and nasal congestion. It is also noted that overdose patients may need supportive measures to raise blood pressure.

Overall, Dostinex can be considered a relatively safe drug, with a side effect profile that is not much different than many drugs on the market. There are some risks with its use, but these do not appear to be very high, and in most cases are far outweighed by the potential benefits to the patient. Dostinex is a drug with limited use in bodybuilding, but a need does present itself from time to time. Note that this is a drug that should be employed to treat lactating gynecomastia, specifically the aspect of lactation. This expensive drug should not be employed as a general remedy for gynecomastia. It is certainly no replacement for Nolvadex, Clomid, or any one of the many aromatase inhibitors. Dostinex should logically be used only subsequent to a blood test reporting high levels of prolactin, or an obvious episode of lactation.

Parlodel (Bromocriptine Mesylate)

Bromocriptine is a dopaminomimetic ergot derivative with D2 dopamine receptor agonist and D1 dopamine receptor antagonist activities. It is used most commonly as a prolactin inhibitor in cases of hyperprolactinemia, a growth hormone suppressant in acromegaly (high doses are required), and as an adjunctive medication to levodopa in the management of Parkinson’s disease.

The most vocal proponent of bromocriptine use for fat loss is probably Lyle McDonald, author of the online e-Book “Bromocriptine: An Old Drug With New Uses.” In this McDonald describes how the drug can be used to normalize the metabolism, such that some of the normal physiological responses to dieting (which begin to slow the loss of body fat as the duration of dieting increases) are hindered. A lot focuses on leptin, a hormone looked at as sort of a fat themostat, telling your brain how much adipose tissue you have on your body and how many calories you are regularly consuming (an “anti-starvation” hormone). Dieting tends to lower leptin levels signficantly, which causes your body to respond in an appropriate way for survival (it tries to hold on to its nutrient stores as much as possible). Maintaining normal leptin stimulation could be key to keeping any diet productive, and bromocriptine may indeed allow us to do that.

The human medical date on this drug is very encouraging. In cases where it was given while dieting, bromocriptine was capable of increasing fat loss by a measurable degree, and seemed to extend the duration in which the diet was most effective. In one case, both placebo and treatment groups were noticing a good level of fat loss during the first 6 weeks of calorie restriction, however only the bromocriptine group continued to lose noticeable amounts of weight for the remaining 12 weeks of intervention. Looking over the dosing regimens of several human studies like this, McDonald is recommending that dieting bodybuilders take between 2.5 and 5mg per day. This is given in a single morning dose, due to the relatively long half-life of the drug.

Bromocriptine can produce a number of unwanted side effects, the most notable being low blood pressure, dizziness, confusion and nausea. These side effects do tend to be dose related, with the low recommended doses used in bodybuilding probably not likely to be much trouble for many. Further, initial nausea sometimes goes away after a couple of applications, once the user becomes accustomed to the drug. Obviously the strong incidence of any unwelcome side effects should warrant discontinuing therapy, especially if your blood pressure is becoming negatively affected (too low a drop). Less common adverse reactions include anxiety, dry mouth, edema, seizures, fatigue, headache, lethargy, nasal congestion, rash or changes in urinary frequency.