Ketotifen use in Bodybuilding

Ketotifen use in Bodybuilding

Ketotifen Action

Ketotifen is an antihistimine that inhibits down regulation of beta receptors, which are often degraded by fat-burners such as Albuterol and Clenbuterol.

It can be used in combination with these other drugs in order to keep feeling their fat-burning effects for longer periods of time with out the need for periods of on and off cycling. Side effects can include drowsiness, irritability, nosebleeds and dry mouth. Ketoifen increases appetite; therefore another side effect is typically weight gain. Ketotifen also (potentially) improves insulin sensitivity within muscle tissue.

Ketotifen User Notes

Ketotifen was first introduced to the bodybuilding world by Dan Duchaine, who proposed its use for upregulation of Beta – Receptors. Several years after his passing I figured out that Benadryl would work for the same purpose, and Ketotifen was largely abandoned for the more commonly available Benadryl.

It is, however, due to the late Karl Hoffman that we owe the use of Ketotifen for reducing TNF-a and for possible use in PCT. He pioneered this idea (though it didn’t really catch on, per se), and it would seem to be very beneficial as an anti-catabolic, though it’s cost would make it prohibitive for use in up-regulating Beta-Receptors.

Benefit of using Ketotifen

So what will ketotifen do with regards to our research that no other compound will? Well when administered with a beta 2 adrenergic agents such as clenbuterol or albuterol it will allow the compound to remain effective for a longer duration, at a lower effective dose. This eliminates the need for dangerously administering very high doses to research subjects which may come along with higher risks and undesirable side effects. It also allows us to administer the beta 2 agonist continuously without a reduction in effectiveness. This will lead to us observing much faster results in our research than if we were required to stop administration or adapt a 2 week on, 2 week off protocol to our research subjects.

How does Ketotifen work?

Ketotifen has 2 primary effects. First off it is an h1 antihistamine. There are 2 types of antihistamines, h1 and h2. A primary difference is h1 antihistamines cross the blood brain barrier in research subjects and are known to induce drowsiness as a result of this. Ketotifen, being an h1 antihistamine is known to induce this effect. Secondly it is a mast cell stabilizer. Mast cells are cells that are rich in histamine. They are activated via calcium channel transfer; ketotifen blocks this calcium channel transfer. This is of particular note as clenbuterol , via cAMP, activates this calcium channel transfer.

The synergy between clenbuterol and ketotifen in research subjects is complicated to say the least. I mean in all reality they BOTH exhibit antihistamine effects, yet while displaying a synergy at making the other more effective. Just as ketotifen prevents the down regulation of beta 2 receptors, clenbuterol prevents the very same effect in histamine receptors! Luckily for our purposes there is a definitive study which proves that the addition of ketotifen increases the effectiveness of clenbuterol in research subjects. There is also a study which proves its effects on prevention of down regulation of b2 adrenergic receptors. Sometimes science makes it a bit easier. Published, peer reviewed studies proving the effectiveness and synergy of 2 research compounds.