The following article was written by Cycleon
I see a lot of newbies trying to find information on Ketotifen so I thought it would be best to put it all together in one post. I gathered this information from a wide range of trusted sources and added my own experiences too. Ketotifen truly is a wonder drug for bodybuilding.
What Is It?
Ketotifen is very safe antihistamine used extensively in Europe to treat bronchial asthma and allergies. It is also being studied as a treatment for colitis. When used for asthma, weight gain and an increase in appetite are among the most frequent side effects. Ketotifen also protects the cells in the stomach, small intestine and perhaps the rest of the gut from a number of toxins. A number of case studies suggest that it may be helpful treating skin problems such as acne. Ketotifen also reduces edema (swelling and puffiness caused by water retention) around sores.
German researchers have published data showing that ketotifen lowers TNF-Alpha in the test tube. One study used ketotifen in combination with Oxymethalone, a steroid which helps people gain weight, so it is hard to gauge what effect ketotifen had (the study notes a 14% reduction in TNF-Alpha levels and weight gains of 11-12 pounds in less than four weeks). A larger placebo controlled study of this combination is underway. The other study used ketotifen by itself in eight patients with elevated TNF-alpha, (but no wasting). Taking ketotifen for 12 weeks, these patients gained an average of six pounds, had increases in their body cell mass and reductions in their TNF-alpha levels.
Side Effects and Toxicity
Ketotifen is virtually non-toxic (although it is not advised for patients with epilepsy). People who took twenty times the recommended dose (in suicide attempts) suffered no serious consequences (other than embarrassment). Its primary side effects seem to be temporary drowsiness, dry mouth,(and other mucous membranes) appetite stimulation and weight gain.
Dosing and Side-Effects
No studies have been completed to find the most effective dose but the German researchers used 4 mg daily. Dan Duchaine (who discovered Ketotifen’s use for bodybuilding) suggested 10mg daily but in my experience this is too much and is not beneficial as it makes you far too sleepy. I find that 3-4mg daily seems ideal. However, much higher doses have been shown to be quite safe with no adverse affects other than increased drowsiness and appetite – it will make you hungry for solid food. You can split the dose throughout the day or take it all at once, it doesn’t really matter.
Ketotifen and Clenbuterol
Clenbuterol is a beta 2 agonist which has a limited anabolic effect during its first few days of use and afterward is normally used to fight fat. At higher doses, however, it can be catabolic to muscle and it must be cycled on a 2 week on, 2 week of basis or the beta 2 receptors that clenbuterol binds to become saturated and down regulate.
Ketotifen’s magic is that it upregulates the beta-receptors including the beta 2’s that clen uses. As long as you are taking ketotifen, it will continue to clean these receptors, meaning they will not downregulate – even while on a heavy clen cycle. That means you can continue to take clen indefinitely without having to cycle off to regenerate the receptors. 2-3mg daily can upregulate even severely shut down receptors within a week.
It also means that you don’t need as much clenbuterol to get the same benefits. You can take about 30-40% less clenbuterol and it will be equally as effective. It also increases the number of receptor sites on the surface of the cell, allowing more clenbuterol to attach, perhaps this is the reason for the increased efficiency. Ketotifen also seems to lessen the sides of clenbuterol, including the jitters.
For a thorough guide on how to use clenbuterol, make sure to check out:
How to Use Clenbuterol Effectively to Speed up Fat-Loss
Ketotifen and ECA
Perhaps an even better use for ketotifen is taking it with the ECA stack. While the thermogenic effect of ephedrine is not as potent as clen because it doesn’t have a high receptor affinity, and it is not limited to beta-2 receptors. In fact it seems to have a good effect on beta 3 receptors as well, which act as a type of thermogenic messenger and over half of ephedrine effect is from beta-3 stimulation. Clen has almost no effect on beta 3 however. So by keeping the beta 2 receptors up, ketotifen can allow the benefits of continuous beta 2 and beta 3 stimulation from ephedrine.
Ephedrine is believed to have some direct effect on both alpha adrenoceptors and beta adrenoceptors, but AT THERAPEUTIC DOSES, ephedrine exerts its thermogenic effect almost entirely via stimulating noradrenaline release from the sympathetic nerve terminals [endings] . . . at least 40% of the [thermogenic] response is mediated by an atypical receptor, which is presumed to be the beta 3-adrenoceptor.
For a thorough guide on how to use ECA stack, make sure to check out:
How to Use ECA Stack Effectively to Speed up Fat-Loss