Ketotifen (also known as "Keto") is a second generation antihistamine that inhibits histamine action in the body via 2 ways; blocking histamine to the receptors or by inhibiting the process of the histidine enzyme which would normally catalyze the transformation of histidine into histamine. It is in a class of compounds usually used in the area of research regarding allergies, but there are other unique uses to this compound as well that I will also touch on.

Why is Blocking histamine important in some cases?

Blocking histamine can be an important factor during research because histamine can produce physical symptoms such as runny nose, itchy eyes, depression and lack of energy, just to name a few. Keto blocks a calcium channel essential for releasing histamine and by blocking this channel we block histamine as well. Keto is normally used in two forms for research; in an ophthalmic form (think cream, ointment or eye drops) or in an oral form. Keto can be administered various ways due to its multiple available forms such as; orally, by inhaler, nasal spray and by eye drop. All forms it has been found to be effective in lessening allergies across a number of species and the route of administration would be decided more on the target area of research rather than a generalized "what is the best way to administer Keto". When used as an eye drop results show within minutes, with oral use it may take a bit longer (20-40min) but the effectiveness is there and depending on the target area of research either/or may be the better option.


Keto with Clenbuterol and Albuterol:

Keto is commonly known for and used in asthma and allergy research but that is not the only area of research regarding this compound. There are a few interesting properties that Keto has which I will touch on, but one of the most interesting traits of keto it its synergistic effect when used in combination with Clenbuterol (Clen) or Albuterol (Albut). Administering Keto will Enhance and prolong the effects of Clen and Albut, possibly indefinitely!

This is of big interest because until now all Clen and Albut research slows down at the 2-3 week mark. This happens because the body adapts to the compounds effects in an unfavorable way, thus making the compound much less effective. This enhancement combination should be taken into consideration if researching Clen or Albut. This combination is becoming more and more commonly sought after as a way to greatly enhance Clen or Albut research across a much longer period of time than would normally be possible using either of the compounds alone. When Keto is combined with Clen or Albut researchers are now able to run a research study for many weeks or months without a slowdown in effectiveness! Any researcher looking into Clen or Albut should also look into Keto and how it may enhance their research. Not to is potentially greatly limiting the effectiveness of the research.

Keto and IBS:

Another interesting quality of Keto that was discovered was its ability to inhibit phosphodiesterase and be an effective leukotriene antagonist. This matters because Irritable Bowel Syndrome (IBS) is closely related to this and Keto has been found in research to "increase the threshold of discomfort in hypersensitive IBS subjects" and is "capable of reversing post stress visceral hypersensitivity in rats." This is promising for those researching IBS or any related fields.

Keto and Gout:

Keto has also been found to have a protive effect in gout research. Gout is an extremely painful form of arthritis with very painful relapsing inflammatory attacks in the body. Gout is a common inflammatory joint disease found in many species. Researchers looked into the possible therapeutic effect of Keto on monosodium urate (MSU) crystal-induced inflammation and found that "Ketotifen dose-dependently inhibited MSU-initiated leukocyte infiltration into the air pouch." Keto also decreased "proinflammatory mediators, including nitric oxide, interleukin-1β, and interleukin-6, production in MSU-treated rats." Research like this had led many researches to feel that Keto is a potential new compound that should be looked into as a possible new approach to the management of gout.

Keto and the lung:

Acute lung injury (ALI) is a severe (and sadly common) complication after liver transplantation in many species. After transplantation of liver there is usually an amplified inflammatory response in the body and since Keto has a positive effect on inflammation, it was research as a compound for lessening the occurrence of ALI. In recent research; "Adult male Sprague-Dawley rats received orthotopic autologous liver transplantation (OALT) and were executed 4, 8, 16, and 24 h after OALT.- The rats were pretreated with the mast cell stabilizers cromolyn sodium or ketotifen 15 min before OALT and executed 8 h after OALT- Mast cell stabilization significantly inhibited the activation of mast cells, downregulated pro-inflammatory cytokine levels and translocation of NF-κB, and attenuated OALT-induced ALI." This in simple terms shows that Keto had a very positive effect on inflammation after liver transplantation and that is should definitely be a compound to be utilized in ALI research related to liver transplantation.

Keto and Hepatitis:

Keto has also been found to be effective as a possible tool in hepatitis, in a study related to this; "Thirty Wistar rats were randomly allocated into three groups. A group received antihistamine treatment (ketotifen + vitamin C) additionally. They were sacrificed after 4 weeks- CONCLUSION: Antihistamine treatment may improve liver function and correct Th1/Th2 unbalance." This is big news because hepatitis can be a very life threatening condition in likely all species affected by it and any compound showing positive effects in this condition should be further explored in my opinion.


Keto and Asthma:

As already mentioned earlier, Keto has also been used in asthma research and it has been found to be very effective in this area due to the fact bronchial allergic inflammation is a big factor in the cause of an asthma attack. In a study using the animal model of the brown Norway rat it was found that "Various drugs, administered twice, 5 min and 5 h after the anaphylactic reaction, have been evaluated for their effects on the 24-h inflammation obtained in actively sensitized rats and Ketotifen fumarate, salbutamol (2 mg/kg) and disodium cromoglycate (50 mg/kg) all given intraperitoneally, reduced the number of eosinophils." This effect has been noted in various animal models and studies, not just rats.

All in all Keto is an amazing research compound! From greatly enhancing & prolonging Clen or Albut's effects during research, to exploring many other medical conditions that are still being investigated, Keto is not a compound to pass up in your research! Keto, one for the books!


Check it out >> Keto 30ml 1mg/ml


Ref:
1) Stress-induced visceral hypersensitivity in maternally separated rats can be reversed by peripherally restricted histamine-1-receptor antagonists.Stanisor OI1, van Diest SA, Yu Z, Welting O, Bekkali N, Shi J, de Jonge WJ http://www.ncbi.nlm.nih.gov/pubmed/23776699
2) Mast Cell Stabilizer Ketotifen Inhibits Gouty Inflammation in Rats.Hsu DZ1, Chu PY, Chen SJ, Liu MY. http://www.ncbi.nlm.nih.gov/pubmed/23884077
3) Opposite effect of mast cell stabilizers ketotifen and tranilast on the vasoconstrictor response to electrical field stimulation in rat mesenteric artery.Sastre E1, Caracuel L, Xavier FE, Balfag?n G, Blanco-Rivero J. http://www.ncbi.nlm.nih.gov/pubmed/23977380
4) Mast cell stabilization alleviates acute lung injury after orthotopic autologous liver transplantation in rats by downregulating inflammation.Zhang A1, Chi X, Luo G, Hei Z, Xia H, Luo C, Wang Y, Mao X, Xia Z. http://www.ncbi.nlm.nih.gov/pubmed/24116032
5) [Effects of antihistamine treatment on immune fuction in rats with experimental hepatitis].Li H1, Zhao LF, Hao YQ, Han DW. http://www.ncbi.nlm.nih.gov/pubmed/24331635
6) Model of bronchial allergic inflammation in the brown Norway rat. Pharmacological modulation. Tarayre JP1, Aliaga M, Barbara M, Tisseyre N, Vieu S, Tisne-Versailles J. http://www.ncbi.nlm.nih.gov/pubmed/1512077
7) Ketotifen inhibits exacerbation of allergic airway hyperreactivity by racemic salbutamol in the guinea pig.Hoshiko K1, Kristersson A, Morley J. http://www.ncbi.nlm.nih.gov/pubmed/8473680
8) Comparison of the modulatory effect of ketotifen, sodium cromoglycate, procaterol and salbutamol in human skin, lung and tonsil mast cells. Okayama Y1, Church MK. http://www.ncbi.nlm.nih.gov/pubmed/1375203
9) Effect of Apafant on bronchial hyperresponsiveness and down-regulation of beta-adrenoceptors induced by endotoxin in guinea pigs. Sugimoto Y1, Mihara T, Hayakawa T, Nakayama Y, Kishida H, Kamei C. http://www.ncbi.nlm.nih.gov/pubmed/9272241
10) Two pharmacological phases in antigen-induced immediate airway response in rats.Miyagawa N1, Iwasaki H, Kato T, Tanaka M, Shibata T, Wakitani K. http://www.ncbi.nlm.nih.gov/pubmed/19043210
11) Pharmacological analysis of antigen-induced late airway response in rats. Miyagawa N1, Iwasaki H, Kato T, Tanaka M, Shibata T, Wakitani K. http://www.ncbi.nlm.nih.gov/pubmed/19252284
12) Ketotifen Fumarate and Salbutamol Sulphate Combined Transdermal Patch Formulations: In vitro release and Ex vivo Permeation Studies. Yousuf M, Ahmad M, Usman M, Ali I. http://www.ncbi.nlm.nih.gov/pubmed/24403658