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Cimaterol


 
Pharmaceutical Name: Cimaterol
Drug Classification: beta-2 agonist/antagonist
Active Life: depends on how drug is administered




Similar to albuterol and clenbuterol, cimaterol is a thermogenic aid that bodybuilders and strength athletes utilize to help reduce body fat levels, amongst other things. Also like albuterol and clenbuterol, cimaterol is able to stimulate lypolisis as it acts as a beta-adrenergic agonist. However unlike the two other substances, cimaterol is a beta-1, 2, and 3 receptor stimulator. Clenbuterol and albuterol are only said to have the ability to stimulate the beta 2 and 3 receptors.

A second benefit to the administration of cimaterol for athletes is an increase in strength as well as a possible increase in muscle size/lean body mass that the compound may provide. It has been repeatedly demonstrated in animal studies that cimaterol contributes to an increase in muscle mass, weight and protein content of muscles (1, 2). The exact mechanism by which this takes place has still not been definitively identified but it can be concluded that it is far different then the response produced by anabolic steroids. However, it has been theorized that the increased nitrogen retention that cimaterol has been demonstrated to stimulate (3) may be one contributing factor.

An encouraging characteristic of the drug is also its ability to stimulate blood flow and mobilizing lactic acid out of muscles (1). This would obviously be of great benefit to athletes, including endurance athletes, who require both cardiovascular and muscular endurance. This would also be encouraging for those worried about the reported cardiovascular problems that can result from clenbuterol administration (4). There are no studies that indicate that cardiovascular distress is associated with use of cimaterol.


Use/Dosing

There are both oral and injectable versions of cimaterol available. For the most part, the injectable version is administered subcutaneously. In most research it has been indicated that doses equating to approximately 0.15 milligram per kilogram, for both men and women, should be an effective dosage for most users looking for the beneficial aspects of the drug if injecting subcutaneously. However, as always, an inexperienced user will likely want to err on the side of dosing their initial attempts on the low end of the spectrum rather then starting out too large and running into unbearable or potentially dangerous side effects.

Prior to the start of administering cimaterol the user should monitor his or her body temperature to obtain a �normal� reading. Throughout the use of cimaterol the user should continue to monitor their body temperature to determine the effectiveness of the dose used, as well as when to increase it. Many believe that simply going by �feel� and/or the presence of noticeable side effects is enough to determine whether or not the compound is accomplishing what the user desires. This is simply not true. The only accurate way to do this is to constantly monitor one�s body temperature.

Due to the fact that cimaterol is a beta-2 agonist/antagonist the downregulation of the cardiac, pulmonary and central nervous system beta-adrenergic receptors is an issue that users must combat when using this compound (5). A proven method to help alleviate this effect and ensure that the cimaterol remains effective throughout its use is via the administration of ketoifen (6). Ketoifen is a prescription anti-histamines that acts to reduce beta-2 receptor activity. By reducing this activity, the receptor function is restored to nearly its original capability and the potency of the cimaterol remains in effect. Doses of two to ten milligrams of ketoifen have been used by users of cimaterol, but most would be well served to start at lower doses. It is unlikely that many will need doses higher then 5 milligrams per day. Taking ketoifen for seven days every two to three weeks should be enough to maintain well functioning beta-2 receptors and ensure that the cimaterol maintains its effectiveness.

An alternative to ketoifen may be diphenhydramine, commonly referred to as Benedryl. Benadryl is a cationic ampiphylic drug, with this fact being significant because cationic ampiphylic drugs have the ability to inhibit phospholipase A2 and therefore upgrade beta-2 receptors (7). The inhibition of the enzyme phospholipase A2 is key due to it being responsible for methylated phospholipids. It is thought that by reducing and/or ending this action this allows the phospholipid membrane to remain relatively intact and the beta-adrenoreceptors will be able to remain functioning at their full capacity, or near to it, for much longer. For most, an effective dose would be 50-100mgs per day for seven days every three weeks while running clenbuterol. Users would be well served to take this dosage just prior to going to sleep as it will likely cause drowsiness.

Having said this, there is much more anecdotal feedback in regards to the effectiveness of ketoifen in relation to cimaterol then there is Benedryl simply because ketoifen has been used much longer by strength athletes and bodybuilders for this purpose. As well, there is seemingly more direct research that indicates that ketoifen is effective while only a few studies suggest the same of Benedryl. That is not to say that Benedryl is ineffective, just that there is less �real world� feedback as to its use with cimaterol.


Risks/Side Effects

The side effects associated with cimaterol are similar to those of clenbuterol and albuterol. Common side effects that are reported by users include tremors, increased heart rate, increased sweating, restlessness, headaches, and loss of appetite. The only way to prevent or reduce such symptoms from occurring is to either reduce the dosing being administered or ceasing to use the drug completely. The problem however is that the vast majority of the scientific research that has been conducted using cimaterol has been performed using animals. The problem with this is the fact that animals have quite different beta-2 receptor reactions then humans in some cases as well as having a larger quantity of these receptors in the relevant tissues. This obviously could lead to differing reactions in humans then those found in various animals. However due to the lack of research available conducted with human subjects, we are left to decipher the applicability of the animal research that has been conducted.

One side effect that has been widely reported by users anecdotally is an increase in blood pressure, making it necessary for it to be monitored constantly when using cimaterol. Due to the mechanism by which the compound works, some users will undoubtedly suffer from hypertension when using it. A reduction in dosage or complete cessation from the drug may be necessary to correct this side effect.

It should also be noted that there are some studies which have indicated that beta agonists, of which cimaterol 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.

A similar trait of other beta agonists (8, 9, 10), cimaterol may also decrease the levels of the amino acid taurine in the serum and the heart of users. 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.

References

1. Byrem TM, Beermann DH, Robinson TF. The beta-agonist cimaterol directly enhances chronic protein accretion in skeletal muscle. J Anim Sci. 1998 Apr;76(4):988-98.

2. Stallion A, Foley-Nelson T, Chance WT, James JH, Fischer JE. Anticatabolic effect of the beta 2-agonist cimaterol in vivo in tumor-bearing animals. J Surg Res. 1995 Sep;59(3):387-92.

3. Cleale RM, Ingling JM, Search DJ, Had**** JR, Pausch MH. Effects of alpha2-adrenoceptor antagonists on metabolic processes of swine: II. Nitrogen balance responses. J Anim Sci. 1998 Jul;76(7):1849-58.

4. Kearns CF, McKeever KH. Clenbuterol diminishes aerobic performance in horses. Med Sci Sports Exerc. 2002 Dec;34(12):1976-85.

5. Schiavone A, Tarantola M, Perona G, Pagliasso S, Badino P, Odore R, Cuniberti B, Lussiana C. Effect of dietary clenbuterol and cimaterol on muscle composition, beta-adrenergic and androgen receptor concentrations in broiler chickens. J Anim Physiol Anim Nutr (Berl). 2004 Apr;88(3-4):94-100.

6. 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.

7. Hirata F, Tallman JF, Henneberry RC, Mallorga P, Strittmatter WJ, Axelrod J. Phospholipid methylation: a possible mechanism of signal transduction across biomembranes. Prog Clin Biol Res. 1981;63:383-8.

8. 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.

9. Doheny MH, Waterfield CJ, Timbrell JA. The effects of the beta 2-agonist drug clenbuterol on taurine levels in heart and other tissues in the rat. Amino Acids. 1998;15(1-2):13-25.

10. Waterfield CJ, Carvalho F, Timbrell JA. Effect of treatment with beta-agonists on tissue and urinary taurine levels in rats. Mechanism and implications for protection. Adv Exp Med Biol. 1996;403:233-45.






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