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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 of Cimaterol
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 of using Cimaterol
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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