Ketotifen (Keto) is an H1-antihistamine. It is an orally administered compound that has been used in research with positive results related to the prevention of asthma attacks as well as inducing sleep and appetite as seen in research. Ketotifen / Keto is made popular by its ability to inhibit the down regulation of beta receptors caused by drugs like Liquid Clen / Clenbuterol. Liquid Clen, albuterol, and Ephedrine used to be cycled on and off during research because they desensitize the various receptors they act on to produce their lipolytic effect. Ketotifen / Keto would therefore allow a longer duration of research with the use of these fat burning drugs. Ketotifen / Keto also (potentially) improves insulin sensitivity within muscle tissue.
Ketotifen is a medically used anti-histamine to treat asthma and allergies. What's relative to this article is that ketotifen / Keto has been shown to inhibit the down regulation of the beta 2 receptors caused by clenbuterol. Consequently, you can continue taking clenbuterol for a longer period of time without having to cycle off to regenerate the receptor sensitivity by adding ketotifen / Keto. Additionally, it means that you don't need as much clenbuterol to get the same benefits. Although no studies have been done to find the most effective dose of ketotifen for this purpose, most users find a daily dose of 2-3 milligrams (mgs) to be ideal, and this dosage can be split or taken in one sitting. Meanwhile, higher doses are likely to cause drowsiness and increased appetite that can be sometimes severe.
Ketotifen is very safe antihistamine used extensively in Europe to treat bronchial asthma, allergies and weight loss. 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 oxymethadone, a steroid like Megace that 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.
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 mucuos membranes) appetite stimulation and weight gain.
No studies have been done to find the most effective dose but the German researchers used 4 mg ED. Dan Duchaine (who discovered ketos use for BB) suggested 10mg ED but in my experience this much is not needed and makes u far too sleepy. I find that 3-4mg ED 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 u hungry for solid foods. You can take it divided in the day or all at once.
Ketotifen's magic is that it upregulates the beta-receptors including the beta 2s that clen uses. As long as you are taking ketotifen, it will continue to clean these receptors, never allowing them to 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 ED can upregulate even severely shut down receptors within a week.
It also means that you don't need as much clen to get the same benefits when on Keto diet. It seems u can take about 30-40% less clen and it be equally effective. FONZ posted that it also increases the number of receptor sites on the surface of the cell, allowing more clen to attach and perhaps this is the reason for the increased efficacy. Ketotifen also seems to lessen the sides of clen including the jitters.
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.
Ketotifen fumarate is a second-generation H1-antihistamine/mast cell stabilizer. Ketotifen is also known for its effect of up-regulating the beta-2 adrenergic receptors, and can for that reason be combined with clenbuterol for treatment of especially severe asthma. Ketotifen inhibits phosphodiesterase, a chemical involved in the homeostatic feedback loop of beta-2 adrenergic activity.