Albuterol - Salbutamol Profile

Albuterol/Salbutamol Profile

Drug Classification: selective beta-2 agonist/antagonist
Active Life: approximately 3-4 hours



Albuterol is a selective beta-adrenergic agonist/antagonist. It is primarily medically prescribed for the treatment of asthma, similar to other beta-adrenergic agonists that are available for the management of airway obstruction. Selective beta-2 agonists such as albuterol are the preferred method of treating asthma due to their ability to help alleviate breathing problems in users, while minimizing the cardiovascular effects that accompanies the use of the drug.

For strength athletes, bodybuilders and others who are seeking to improve performance or their physical appearance, albuterol offers numerous benefits. For the most part, it is most often considered a “fat burner” in the bodybuilding community. This is due to the ability of the drug to stimulate fat cells, increase lypolysis, decrease appetite, increase body temperature, as well as increasing basal metabolic rate, among other things (1). All of these factors, when combined with proper diet and training, would obviously help to increase the rate of fat loss in users. However the use of albuterol is not limited to simply fat loss. There is evidence that it can help to dramatically improve athletic performance as well as helping to contribute to anabolism.

It has been demonstrated in numerous studies that the use of albuterol can help to increase muscular strength in users. These are often accompanied by increases in muscle mass. Specifically, in one such study it was noted that users of albuterol showed much greater improvements in strength when compared to a control group, after both groups had previously been training for ten weeks with no significant differences in their progress. The group given albuterol also showed larger increases in lean body mass (2). The doses for these individuals began at 4 milligrams per day, given orally, and were increased and then maintained at 16 milligrams per day for the duration of the study. Similar findings were made in another study where the subjects only trained their quadriceps muscles. Again, both gains in strength and muscle size were noted in the group that was administered albuterol during their training (3).

However the performance enhancing ability of albuterol is seemingly not limited to strength training. It was shown that the times of users performing endurance exercises significantly improved with the use of albuterol (4). Interestingly these improvements were accomplished without the drug negatively impacting the VO2, respiratory exchange ratio, heart rate or plasma free fatty acid and glycerol concentration of users during the exercise conducted. Rather the plasma lactate and potassium concentrations were altered. This would all bode well for endurance athletes who are looking to improve their athletic output and not negatively impact other areas of their performance capabilities.

With these performance enhancing benefits, albuterol also offers health benefits for the user by way of positively impacting their overall cholesterol levels. It has been demonstrated that albuterol elevates high-density lipoprotein cholesterol, while also lowering low-density lipoprotein cholesterol (5). The mechanism by which this takes place is somewhat unknown at this time with more research on the subject needing to be done to determine the exact nature of this result.

Like clenbuterol, albuterol also decreases the level of taurine, an amino acid, in users when administered (6). This would indicate that users may be well served to supplement with the taurine while using albuterol. It is believed by many that low levels of taurine can result in muscular cramping. However there is little scientific research to indicate that this is true or that supplementation is necessary to avoid this effect.

Along with the side effect of decreasing taurine levels in users, clenbuterol and albuterol also share many other of their characteristics with each other. This should be expected with two selective beta-adrenergic agonists/antagonists, but it is the differences in them that should be noted by users. For the most part, a highly significant difference between the two drugs is the half lives of each. While the half life of clenbuterol is approximately seven to nine hours, the half life of albuterol is about three to four hours. This is important for several reasons. First, by having a shorter half life the effects of albuterol will be felt for a shorter period of time. This allows users to take doses but then have them wear off when one wants to sleep, rest or simply does not want to feel the side effects of the drug. With clenbuterol, these effects, and their duration, can hinder the ability of a user to sleep comfortably or conduct their normal routine throughout the day.

This longer half life is believed by some to also contribute to the effect that clenbuterol has on the heart. In numerous animal studies it has been shown that heart damage has occurred in animals given doses of clenbuterol over extended periods of time. With albuterol, no such damage has ever been demonstrated. This may be due to the length of time that a user is exposed to the drug and therefore the likelihood that damage could occur. That theory however is simply speculation.

The difference in the half lives is also responsible for the differing levels of receptor down-regulation that is experienced with both albuterol and clenbuterol. Over time the beta-2 receptors that are targeted by both clenbuterol and albuterol are down-regulated by their exposure to the drugs and the drugs become less effective. However this down-regulation is much more significant with the use of clenbuterol then it is with albuterol. In fact, most users will not find that they have to take any steps to combat receptor down-regulation with albuterol as long as they remain within the general parameters of regular dosing and cycling of the drug. With clenbuterol however, it is likely that a user will have to administer ketoifen and/or Benadryl approximately every third week of running the compound to help and restore receptor function (7). This same protocol can be used with albuterol if a user feels that the effect of the drug has been diminished over time with its use, or else has been using a large quantity of the compound for an extended period of time. By using ketoifen or Benedryl the user is able to at least slow the desensitization of the receptor to the drugs and therefore these drugs are able to function at a much higher level for longer periods of time.

So now that it has been established that albuterol has significantly less potential damaging side effects then clenbuterol, the differences in their efficiency in terms of lypolysis and performance enhancement can be explored. Since the primary difference between the two compounds is their half lives, it is obvious that if single doses of the separate drugs were given, clenbuterol would have a much longer lasting effect on the user and the effects of the drug would be active for a longer period of time. However this benefit of clenbuterol is circumvented simply by spacing the dosages administered of albuterol to much shorter periods of time. This requires much more frequent dosing, but this inconvenience may be well worth the fact that the effects of the drug cease much more quickly once administration of it is stopped.

In terms of the performance enhancing abilities of the drugs there is little information comparing the two compounds and their effects. However one study was conducted comparing the muscle and protein anabolic effects of both clenbuterol and albuterol in rats (8). For the most part the effects of each compound were comparable in their ability to increase muscle weight and protein content in the body. Clenbuterol was slightly more efficient in producing these results, showing greater increases, but both it and albuterol showed that they were both capable of producing significant results.


Use/Dosing

When prescribed medically, albuterol is usually administered via inhalers. This method allows the drug to reach the lungs as rapidly as possible and alleviate the symptoms associated with breathing difficulty. For the purpose of performance enhancement however, oral administration is preferred. This is due to the slower release of the drug into the system of the user, as well as the larger doses needed to reap the performance enhancing effects of the compound.

It appears from the available research that when used to improve strength, athletic performance, or alter body composition, the maximum dosage administered is sixteen milligrams per day in humans. The usual protocol in the majority of the studies reviewed was to increase the dosages administered and make adjustments as dictated by the negative side effects experienced by the participants. These first doses ranged between two to four milligrams per day to begin. This would seemingly be the preferable dosage for most users to start at as well, both males and females. While little research exists about users administering dosages larger then sixteen milligrams per day, one could take more if their temperature begins to normalize. However one should remember that the effects of taking dosages above sixteen milligrams have not been investigated for the most part.

Beyond the initial caution that should be exercised, any increase in the dosage taken by a user should be determined by his or her body temperature if looking for the thermogenic effect of the drug. By monitoring his or her body temperature the user will be able to determine at what dosage the thermogenic effect begins and when it begins to dissipate, with an increase in dosage being warranted assuming of course that the side effects do not prohibit this increase. This is the most effective way to determine at what point a dosage increase is necessary to continue lipolysis.

If however a user is utilizing albuterol for its performance enhancing properties, he or she may be more apt to increase the dosage administered more rapidly then those simply looking to benefit from the thermogenic effect of the drug. This is due to the fact that several studies have indicated that with larger doses does come improved strength and athletic performance (2, 4). This should of course be tempered by the fact that with large doses comes the greater likelihood of significant negative side effects. This, along with the fact that improved performance has been observed at doses as small as two milligrams per day, should help to indicate to users that extremely large doses of albuterol are unneeded.

In terms of length of use, since albuterol down-regulates the beta-2 receptors, the compound will eventually have diminishing results over time. As discussed earlier, this down-regulation should be far slower and less severe then with clenbuterol due to the shorter half life of albuterol, among other reasons. However even without the need to take steps to “up-regulate” the beta-2 receptors, users should at the very least be able to effectively use albuterol at significant dosages for between six to ten weeks with little difficulty. This time frame can vary from user to user of course, but should be applicable to the majority of users.


Side Effects/Risks

Like all beta agonists, albuterol has major stimulant effects on users. This can lead to side effects such as an increase in blood pressure, increased heart rate an/or palpitations, insomnia, tremors, and increased sweating due to the thermogenic effects of the drug, among others (4). Of course the onset and severity of these side effects will vary from one user to another. It is recommended, as is the case with most drugs, that users begin administering relatively small doses of the compound to determine their tolerance level for it. The user then can slowly increase his or her dosages until they find one which provides them with the desired effects, while not producing side effects that the user would find intolerable.

Another aspect of albuterol use is its apparent effect of decreasing the levels of the amino acid taurine in the serum and the heart of users (6), as mentioned previously. This is a similar trait of other beta agonists. Many users will supplement with taurine to counteract this effect. It is believed that when the body is depleted of taurine, muscle cramps are more likely to occur, although there is no real scientific research that supports this assertion.

It should also be noted that there are some studies which have indicated that beta agonists, of which albuterol is one, can impair cardiovascular endurance and/or performance. However they have also been shown to help increase performance. Obviously like all situations where contradictory research exists, users will have to experiment with the drug themselves and see exactly how they react to the compound.

Heart damage, as indicated earlier, is often a worry among users because of animal studies indicating that it occurs in animals given clenbuterol. Due to the similarity of the compounds, there may be some concern among users that these negative effects that have been associated with clenbuterol use and its impact on the heart may also occur with the administration of albuterol. However there is little evidence that this is an issue. For the most part the scientific research has found no link between albuterol use and detrimental changes in the heart. This may be true for a number of reasons. First, the studies that indicated that clenbuterol caused cardiac hypertrophy and necrosis were conducted with animals. This is important because animals have a larger number of beta 2 receptors then humans.

The lack of heart damage attributable to albuterol use may also be due to the shorter half life of the drug relative to clenbuterol. This possible explanation is theoretical in nature, as no research has been conducted on the subject, but could be a contributing factor. However, the main point to be made is that there is no evidence that albuterol could be directly linked to potential heart damage in a user. For the most part, when used in a cautious manner, albuterol is a very safe drug to utilize.



References

1. Yamashita J, Onai T, York DA, Bray GA. Relationship between food intake and metabolic rate in rats treated with beta-adrenoceptor agonists. Int J Obes Relat Metab Disord. 1994 Jun;18(6):429-33

2. Caruso JF, Hamill JL, De Garmo N. Oral albuterol dosing during the latter stages of a resistance exercise program. J Strength Cond Res. 2005 Feb;19(1):102-7.

3. Caruso JF, Signorile JF, Perry AC, Leblanc B, Williams R, Clark M, Bamman MM. The effects of albuterol and isokinetic exercise on the quadriceps muscle group. 1995;27(11):1471-1476

4. van Baak MA, Mayer LH, Kempinski RE, Hartgens F. Effect of salbutamol on muscle strength and endurance performance in nonasthmatic men. Med Sci Sports Exerc. 2000 Jul;32(7):1300-6

5. Maki KC, Skorodin MS, Jessen JH, Laghi F. Effects of oral albuterol on serum lipids and carbohydrate metabolism in healthy men. Metabolism. 1996 Jun;45(6):712-7

6. Bastos ML, Carvalho F, Remiao F, Mendes ME, Ferreira MA, Soares ME, Timbrell JA. Changes in taurine levels in response to repeated administration of the beta 2-agonist salbutamol in lambs. J Vet Pharmacol Ther. 1997 Feb;20(1):33-7.

7. Huszar E, Herjavecz I, Boszormenyi-Nagy G, Slapke J, Schreiber J, Debreczeni LA. Effects of ketotifen and clenbuterol on beta-adrenergic receptor functions of lymphocytes and on plasma TXB-2 levels of asthmatic patients. Z Erkr Atmungsorgane. 1990;175(3):141-6

8.Carter WJ, Lynch ME. Comparison of the effects of salbutamol and clenbuterol on skeletal muscle mass and carcass composition in senescent rats. Metabolism. 1994 Sep;43(9):1119-25.