XSteroids.com

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.