Albuterol and asthma medications being Anabolic

[latinking24]

ALBUTEROL


Background for the use of albuterol in treating DMD

Although gene therapeutic approaches offer the most promise for an ultimate cure for DMD, gene therapeutics are not expected to be available for several years or longer so that many patients diagnosed at the present time are not likely to benefit from gene therapy. Our goal at the DMDRC-UCLA and specifically in the clinical trial of albuterol is to identify pharmacological approaches to reduce the loss of muscle mass and strength in DMD boys, so that they may be able to take advantage of gene therapy treatments when they become available in the future. Albuterol, a beta-agonist, is a promising agent for this type of pharmacological approach. Beta-agonists are a class of drug that have been shown to improve the quality and functional properties of muscle, both in healthy and sick individuals. This drug already has FDA approval for the treatment of asthma, and could be readily available to patients if promising results ensue from this study. It is a drug with minimal side effects and is safe for a pediatric population. However, when albuterol is administered as an inhaled aerosol in the treatment of asthma, it has no effect on skeletal muscle. Albuterol effects on skeletal muscle require long-term release of the albuterol into the circulatory system, which can occur when the drug is taken as a slowly releasing tablet.

Rationale for the expected beneficial effects of albuterol administration to DMD boys
A substantial body of scientific and clinical research shows that albuterol is an effective drug for increasing muscle mass and strength. First, several animal studies have shown increases in lean muscle mass following administration of beta-agonists [1-13]. Collectively, these studies show that beta-agonist treatment of healthy animals can increase muscle protein content, muscle mass and muscle strength and that these increases can occur after only a few weeks of treatment.

Human studies have also shown increases in muscle mass following a regimen of beta-agonist treatment [14-16]. Healthy males treated with slow release albuterol for 14 days (16 mg/day) improved their quadriceps strength by 12% [14]. The increase in strength remained 7 days following treatment. In the same study, the strength of the hamstring muscles increased by 22% after 21 days of treatment. Caruso et al. [17] also documented increases in strength following 16 mg/day of albuterol treatment of healthy individuals. Unhealthy patients have been shown to experience even greater benefits from beta-agonist treatment than healthy patients. For example, orthopedic patients demonstrated a more rapid recovery following beta-agonist administration [16]. Thus, all current evidence supports the view that albuterol can be administered safely to humans to improve muscle strength and mass.

Beta-agonists improvemuscle mass and strength in mdx mice
Several investigations have provided the most compelling evidence of the efficacy of beta-agonist administration for the treatment of muscle pathology attributable to the absence of dystrophin [18-23]. Six separate investigations using the mdx mousemodel of DMD, have shown that treatment with clenbuterol (another ß agonist) increases muscle mass and strength [18-23]. In these investigations, mdx mice were treated with clenbuterol for 15 weeks [21, 22], 2 months [18], 4 months [23] or 1 year [18], and in all cases the treatment was beneficial in reducing the wasting normally associated with the disease process.

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Albuterol, like its closely related chemical cousin clenbuterol, is an asthma medication that has been adopted by athletes and bodybuilders as an ergogenic aid. Like clenbuterol, albuterol binds to the so called beta 2 adrenergic receptors found on cells throughout the body. The beta 2 receptors on fat cells activate an enzyme called hormone sensitive lipase. This breaks up stored fat into free fatty acids that are able to then leave the fat cell and serve as a fuel source in other tissues. In athletes the primary target of these fatty acids is working muscle. This is the familiar process we know as lipolysis. Albuterol, like clen, is a potent lipolytic agent. But simply freeing up fat is not enough. Unless the body can burn the extra FFA they will simply be reincorporated into fat. Albuterol has the ability to elevate a person's metabolic rate so these FFA can be utilized for fuel. Numerous animal studies have shown that clenbuterol increases both muscle size and strength; data supporting these effects in humans are sparse. Albuterol on the the other hand has been shown to significantly increase both strength and endurance in humans (1,2). As an added benfit, albuterol lowers LDL and total cholesterol, while at the same time elevating HDL, the "good cholesterol": "Significant alterations (P < or = .02) were observed in total cholesterol ([TC] -9.1% +/- 2.5%), low-density lipoprotein cholesterol ([LDL-C] - 15.0% +/- 2.9%), and high-density lipoprotein cholesterol ([HDL-C] +10.4% +/- 3.2%) concentrations, as well as the TC/HDL-C (-17.4% +/- 2.6%) and LDL-C/HDL-C (-22.9% +/- 2.4%) ratios." (3) 4 mg of albuterol taken approximately 1 to 2 hours before a workout allows for peak plasma levels to be reached during the training session. Additionally the much shorter half life of albuterol compared to clenbuterol allows one to benefit from its ergogenic effects during a training session but not suffer the sleeplessness that many clenbuterol users experience. Moreover, the short half life leads to much less beta 2 receptor downregulation than with clenbuterol, allowing one to use the drug daily for longer periods of time. On the other hand, if one is primarily interested in fat loss rather than performance enhancement, one could take 3 or 4 multiple doses of albuterol throughout the day, always of course cutting back if clenbuterol-like side effects are felt. 1 Bottle Of CEM Laboratories Liquid USP Albuterol Sulfate is 30 ML at 4 MG/ML. (1) Med Sci Sports Exerc. 2000 Jul;32(7):1300-6. Effect of salbutamol on muscle strength and endurance performance in nonasthmatic men. van Baak MA, Mayer LH, Kempinski RE, Hartgens F. (2) Aviat Space Environ Med. 2004 Jun;75(6):505-11 Albuterol helps resistance exercise attenuate unloading-induced knee extensor losses. Caruso JF, Hamill JL, Yamauchi M, Mercado DR, Cook TD, Keller CP, Montgomery AG, Elias J. (3) Metabolism. 1996 Jun;45(6):712-7 Effects of oral albuterol on serum lipids and carbohydrate metabolism in healthy men. Maki KC, Skorodin MS, Jessen JH, Laghi F.

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Albuterol is a direct-acting sympathomimetic agent with a relatively selective action on beta-2 adrenoceptors. Its main clinical use is obviously to treat asthma. Inhalers would NOT yield the potential anabolic effects that pill form would (overall systemic).

From T-MAG--

“I thought albuterol was almost not effective at all but it seems I was wrong:

There's pretty compelling evidence that shows albuterol is just about as effective as clenbuterol at increasing anabolism, with one exception: Albuterol is effective at "clinically safe" doses (in man), and clenbuterol is not. In other words, in order to achieve an anabolic effect from clenbuterol, you need to exceed its safety limits (which is not necessarily dangerous or undesirable for us healthy bodybuilder types).

On the other hand, albuterol, at clinically safe doses, increases whole-body protein content in rats by 20% in just three weeks! So it really does increase protein synthesis.

Furthermore, there are several studies that show albuterol is effective at significantly increasing power output and muscular endurance in man. Additionally, albuterol is heart healthy, prevents muscle catabolism, and is a pretty darn good asthma medicine to boot.

By all indications, albuterol should be effective for at least three to four weeks at increasing muscle mass before you need a week off from use. And from a personal experience, this bears out as well. I've had reasonably good success with albuterol, and I suggest anyone who has access to the drug to give it a try.

I recommend 16 mg a day, taken in either two doses spaced 8-10 hours apart, or four doses spaced about four hours apart. Go on cycles of 3-4 weeks on, one week off.

Be careful about stacking other adrenergic agonists, like ephedra, with albuterol. If you can tolerate the combination, go for it, but test it out first. The half-life of albuterol is about five hours, so if the doses are too frequent, there's a cumulative effect that could get the better of you, sending your heart into an arrhythmia that rivals the tempo of a hummingbird's wings.

Just be aware that there are enormous tolerance differences between people. So start out slowly with minimal doses until you get a handle on how your body reacts to these compounds.

And regarding aspirin, bag the idea of using it for anything other than pain control. Stacking it with stimulants is out of date and actually counterproductive.”

By the way...Salmeterol is just anther type of Beta-2 agonist like Albuterol. They are both generics. Albuterol is the generic form of Proventil and Ventolin. Salemeterol is the generic form of Serevent. Clenbuterol is the generic name of Spirovent. The way generic vs trade name works.......a pharmaceutical company has a "patent" for 10 years on any med they invent. They can name it anything they want and sell it for whatever they want, but they figure out a market price or else noone will buy it. But the drug still has a generic name. This is the way they recoup their millions of dollars on research. After 10 years other drug companies copy the drug and prices come down because of competition.
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A newer drug for Americans is Salbutamol. Salbutamol is chemically very similar to clenbuterol and is heavily used in the European circuit. The good news for some is that Salbutamol is readily available here in the United States. In America, Salbutamol is known as albuterol. It comes in tablet, inhaler and parenteral (injectable) forms.

Although many respectable steroid experts have pooh-poohed albuterol, in a recent head to head study (albuterol versus clenbuterol), albuterol was able to enhance muscle size regardless of age. (So did clen, but not by that much better of a margin.)

The use of steroids (in high doses) may be associated with an unfavorable risk for heart disease; the same isn’t true for our friend albuterol. In fact, one recent study demonstrated that daily ingestion of albuterol improved cardiac disease risk profile (lower cholesterol, LDL, triglycerides, while raising HDLs, the good cholesterol). In this particular study a daily dose of 16 milligrams was employed (8 mg twice daily).

Some other benefits observed with albuterol are improved blood ammonia levels during exercise, enhanced leg strength (and overall strength gains when combined with weight training), and elevated resting energy expenditure. Also of interest is that albuterol has been shown to help improve aerobic (running) performance as well as anaerobic metabolism (which is used in weight training). One other "side effect" of Salbutamol/albuterol ingestion is that it can enhance thyroid hormones, especially the active thyroid hormone, T3.

Of interest to athletes who undergo drug testing is that Salbutamol/albuterol isn’t on any banned list, thus it’s considered acceptable for athletes to use (remember it’s traditionally used for treatment of asthma). The dose most commonly used (tablet/capsular form) for both athletic performance enhancement and fat loss is 16 mg per day. The dose is typically divided into 4 mg. taken four times per day. It can also be taken twice daily, often started at half dose and slowly increased as tolerated.

-From T-Mag.


Beta agonist rage – the anabolic properties of asthma drugs

By Jerry Brainum

Clenbuterol has acquired a near-legendary status among some power athletes. This reputation is is based on the drug's alleged anabolic and fat-burning properties. Although never approved for sale in the United States, clenbuterol is available in other countries under various trade names, including Clenasma, Monores, Norvegan. Prontovent and Spirovent. The drug is sold either in tablet form or as a solution in various concentrations.
Clenbuterol is often mistakenly identified in the popular media as a "steroid". In fact, it is classified as a beta-2 agonist because of its interactions with adrenergic cell receptors, especially beta-2 adrenergic receptors. Since these receptors are involved in bronchodilatation (expansion of the bronchial air passages), the drug is prescribed to help control asthmatic symptoms.
Clenbuterol and similar beta-2 agonists, such as cimatero) and fenoterol, differ from other common beta-2 agonist drugs in that they remain active in the body longer. For example, clenbuterol has a half-life of 27 hours, taking about five days to dear from the body. In contrast the longest-acting beta-2 agonist sold in the United States, salmeterol lasts only about 12 hours.
However, most researchers believe that the longer a drug takes to clear from the body, the higher the risk of side effects. This explains why beta-2 agonists such as clenbuterol have never been approved for sale in the United States. In addition, from the standpoint of asthmatic therapy, the longer-acting beta-2 agonists show no significant therapeutic benefit over existing asthma drugs, so the profit motive for drug companies is also lacking.

CRITTERS ON CLENBUTEROL
Long-acting beta-2 agonists are attractive to athletes for the drugs' putative muscle-building and fat-burning effects. Animal research using various species (e.g., horses, sheep,chickens and cattle) demonstrates that clenbuterol acts as a "repartitioning agent" That is clenbuterol seems to increase the density of type-II muscle fibers (the type most prone to growth in humans) and concomitantly favors bodyfat losses. One study found a 20% gain in muscle coupled with a 20% loss of fat when clenbuterol was given for just eight to 14 days.
Extrapolated to humans, the doses provided in animal research far exceed what any human could safely tolerate. For instance, the average dose range of clenbuterol needed to provide an effective repartitioning response in animals was between 0.33 and two milligrams per kilogram (a kilogram equals 2.2 pounds). The suggested therapeutic dosage to treat asthmatic symptoms in humans is much less. Doses equivalent to those given to the research animals would most likely kill a human.

THE MYSTERY OF CLENBUTEROL
It's uncertain how clenbuterol and similar long-acting beta-2 agonists work to provide anabolic effects. Animals experience a rapid upgrade in muscle-protein synthesis that lasts for only about five days. After that protein synthesis induced by the drug diminishes: then comes decreased muscle-protein degradation, an anticatabolic effect.
A similar scenario occurs with anabolic steroids — an initial increase in muscle-protein synthesis, followed by an extended anticatabolic effect. Both the protein-synthesizing actions and anticatabolic effects of anabolic steroids are known, but how clenbuterol exerts similar activity (in mega-doses) isn't as clearly established.
No formal clinical studies using clenbuterol as an ergogenic agent in humans exist, probably because of the relatively gargantuan dosages needed to produce anabolic effects in test animals. From an anecdotal point of view, most athletes who've taken the drug use it more for its "thermogenic" or fat-burning properties than for its anabolic effects.
However, the beta-cell receptors that clenbuterol interacts with are exquisitely sensitive and are known to "down-regulate" or close up if exposed to concentrated doses of beta-agonist drugs. Athletes often attempt to circumvent this biological limitation by using a "two-days-on, two-days-off" dosing schedule. Even so, the drug usually stops exerting thermogenic effects in as little as two weeks.


NOW, YOU'RE MAKING ME MAD

Clenbuterol is similar in structure to epinephrine, and like epinephrine, clenbuterol can excessively stimulate the heart, resulting in a rapid heartbeat, or tachycardia. Other possible side effects include muscle tremors, heart-rhythm disturbances, headaches and muscle cramps. The latter problem is thought to occur because beta-2 agonist drugs affect potassium distribution in the body.
A few recent inquiries point to a possible behavioral side effect from using beta-2 agonist drugs. An increase in hostility and anger has been observed in men after a down-regulation of beta-adrenergic cell receptors. One study, published in Psychosomatic Medicine (59:481-87, 1997), found that men with decreased cellular adrenergic receptors also showed greater plasma catecholamine (epinephrine) and cortisol responses to anger provocation.
What's curious about this research is that a similar situation - the infamous 'roid rage is reported to occur in some anabolic-steroid abusers. What happens to an athlete taking clenbuterol and anabolic steroids concurrently is still unknown. Could the anger/rage effect be cumulative? And could the danger be compounded further, since investigations have linked increased anger to a higher risk of cardiovascular disease?
The research on clenbuterol isn't completely negative. A study published in Brain Research (717:44-54,1996) found that giving clenbuterol to rats and mice increased a protective brain substance called "nerve growth factor." This effect was especially evident in the hippocampus, a brain area vital to memory storage and intellectual functioning. If this work is reproducible in humans, it may prove that drugs such as clenbuterol might prevent certain types of degenerative brain diseases.

ARE ASTHMA INHALERS ANABOLIC?
Many athletes familiar with clenbuterol might wonder if using commonly available metered-dose asthma-drug inhalers would produce similar responses. It's not unreasonable to assume that such drugs would offer some ergogenic benefits, since they fall into the same beta-2 agonist category as clenbuterol.
The first thing to consider about asthma inhalers is their highly selective distribution. In essence, most of the drug is delivered to the lungs, with some slight spillover into the general blood circulation. Also, the dosage used in such sprays is usually in micrograms — not enough to promote any type of true ergogenic activity.
Despite these notable shortcomings, however, some investigations have confirmed an increase in power in non-asthmatics given asthma inhalers. For example, a 1988 study (Canadian Jouma; or Sports Science. 13:144-48) found that subjects showed improved prolonged exercise performance (lasting more than an hour) after inhaling a commonly available asthma spray drug called albuterol. Most other research has failed to confirm this effect, although a 1992 investigation did find increased power output with the same drug.
A recent report in the journal Medicine and Science in Sports and Exercise (29:1631-36.1997) looked at the effects of another asthma drug inhaler, terbutaline, on 20 elite male athletes from various sports. The drug was used during tow-temperature conditions, which often provoke exercise-induced asthma. The study, however, found no increase in exercise performance in any of the athletes who used the inhaler.
In another case, reported in the Journal of Allergy and Clinical Immunology (99:443-49,1997), a newer type of commonly available asthma inhaler called salmeterol was examined for its ability to increase power output in athletes. Salmeterol is sold commercially as Serevent inhaler and differs from other asthma inhalers because of its extended activity. It binds to beta-cell receptors with an affinity 50 times greater than that of the other most popular asthma inhaler, albuterol. As a result, it lasts twice as long as albuterol (12 hours versus six) in providing increased bronchodilatation.
Any type of beta-2 agonist drug is capable of raising muscle strength by stimulating an influx of calcium into a portion of the muscle called the sarcoplasm. This in turn, leads to an increase in the binding of muscle contractile proteins (actin and myosin), resulting in more potent muscular contraction.
Actually, this process does not usually occur. Regular exercise leads to a release of catecholamines such as epinephrine, which interact with muscle beta-adrenergic receptors. This constant exposure to epinephrine leads to a down-regulation of the muscle receptors (as occurs when drugs such as clenbuterol are used). The result is lowered muscle responsiveness to beta-2 type drugs, such as various asthma inhalers.
The study on salmeterol confirmed the lack of ergogenic or power increases in athletes inhaling this drug in standard doses (two puffs or inhalations). Based on this finding and others discussed above, most asthma inhalers are deemed legal for use in international athletic competition. In contrast, similar drugs, such as clenbuterol are banned.
The main problem with asthma drugs is the same as that typically occurring with clenbuterol — cell-receptor downgrade. Some doctors fear that with continual usage, some asthma inhalers may not work at all thus endangering asthmatics who depend on them. Salmeterol, unlike albuterol, isn't for emergency use anyway; it takes 20-180 minutes to begin opening up the lungs, while albuterol works immediately.

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	Clen

	T3

	protein

	energy

[latinking24]

Ill be doing some personal experiments with liquid and inhalation albuterol on performance and muscle growth...