Ketotifen fumarate is a kind of strong anti-allergic drugs containing simultaneously of both tricyclic structure as well as piperidine structure. It is characterized by both a strong antagonism effect on histamine H1 receptor and inhibitory effect of the release of the mediator of allergic reaction. It can inhibit the release various kinds of mediators of mast cells, basophils and macrophages, including the release of slow reacting substances and other active substances. It also has antagonism effect on the calcium ion; can inhibit the activity of phosphodiesterase; increase the intracellular cAMP level inside mast cells. Moreover, it can also inhibiting the chemotaxis and inflammation of neutrophil with an effect 10 times as strong as that of chlorpheniramine, and it also has a long duration time which is better compared with sodium cromolyn. Ketotifen fumarate has therapeutic effect on both Ⅰ and Ⅲ type of allergic reaction. Its peak blood concentrations can sustain for 2 to 3 hours with a half-life of 22 hours during which 60% goes through urinary excretion, 40% goes through the fecal excretion. Children usually have a faster excretion rate of it than adults. Long-term treatment will not cause resistance. No rebound phenomenon will occur with interruption of treatment.
Product Name: Ketotifen fumarate
Properties: white or pale yellow crystalline powder
Usage: Antiasthmatic; antiallergic.
Catalogue: Pharmaceutical materials drug
It has been more than 20 years since ketotifen fumarate have been applied to the prevention and treatment of asthma and childhood asthma. It is a kind of drug with dual effect of both prevention and treatment in the prevention and treatment of asthma and childhood asthma. It should be particularly noted that ketotifen had ever taken as the long-term controlling drug of asthma and childhood long-term asthma and was subject to wide application in many countries. Since the early 1980s, ketotifen fumarate had already been applied in Western Europe, Asia, and China for the prevention and treatment of asthma and asthma in children. But since entering into 21st century, the annual applied amount has decreased year by year. Because of its side effect of inhibition of the central nervous system, its oral tablet currently has still not approved by the FDA and thus failing to enter the US market with only ketotifen fumarate eye drops had been approved by the FDA in 1999. Recent studies have also shown the effectiveness of ketotifen asthma still demands further studies. Moreover, ketotifen fumarate has several additional advantages. First, it can cause sleepiness of the schoolchildren and thus being able to affect their academic performance; second, it can also do harm to the mental development of infants and young children. Thirdly, it is also be able to affect the metabolism of sustained-release tea and thus negatively affecting its anti-inflammatory effects of theophylline. For all the above points, it is not recommended by the GINA (affiliated organization of WHO) to apply ketotifen fumarate for the treatment and prevention of asthma and childhood asthma. But from the perspective of clinical economics, ketotifen fumarate is a suitable anti-allergic drug for being applied in developing countries and rural areas for treating asthma and childhood asthma with certain efficacy due to its relative low price.
This product is white (or light-yellow) crystalline powder, and is odorless with bitter taste. It is slightly soluble in water and ethanol, and easily soluble in methanol but very slightly soluble in chloroform and acetone.
Dermatology applies it to the treatment of allergic diseases such as urticaria, pruritus, eczema, atopic dermatitis, and neurodermatitis; it is recently reported that it is also effective in the treatment of scleroderma. For medicine, it has a good efficacy in treating asthma, especially with a significant effect on treating allergic asthma, followed by mixed asthma, and being effective in half of cases for infecting type. It can also be used for the prevention of asthma.
The pharmacological effect of ketotifen fumarate is very complicated. It has achieved a certain efficacy in the prevention and treatment of asthma and childhood asthma. But the detailed mechanism of its pharmacology remains to be unclear. From the current research information, the pharmacological mechanisms of ketotifen fumarate in treating asthma and childhood asthma include the following several aspects:
1. Antagonizing effect on inflammatory mediators: Clinical studies have already demonstrated that ketotifen fumarate can effectively inhibit the histamine-induced bronchospasm with its intensity being comparable to Azelastine, suggesting that ketotifen fumarate has strong histamine antagonistic effect. Modern studies have shown that ketotifen fumarate may also other inflammatory mediators such as antagonize leukotrienes and platelet activating factor. From this perspective, it is considered that ketotifen is a drug which can antagonize a variety of inflammatory mediators. This may be the primary mechanism for its prevention and treatment of asthma as well as childhood asthma.
2. The membrane protective effect of mast cells/basophils: the related pharmacological studies of ketotifen fumarate have confirmed that it can inhibit mast cell /basophil cells to release inflammatory mediators such as histamine, leukotrienes and platelet activating factor, suggesting that it has a strong membrane protective effects on mast cells/basophils membrane. This may be the major mechanism underlying the dual property of ketotifen fumarate for being able to both prevent and treat the asthma and childhood asthma.
3. The inhibition of airway inflammatory cell infiltration: fumarate ketotifen can inhibit the infiltration of the airways of eosinophil and neutrophil. However, the mechanism remains to be unclear.
4. Regulation of T cell activity: ketotifen fumarate can inhibit the biosynthesis of intracellular lgE through regulating the release activity of CD4 + and CD8 + lymphocytes. The mechanisms of inhibition of the biosynthesis of lgE and the above two mechanisms determines the airway anti-inflammatory effects of ketotifen fumarate.
5. Other effects: Some studies have suggested that ketotifen fumarate can reverse the low-regulation of β2-receptor caused by the long-term administration of β2-receptor agonist and also increase the density of airway β2-receptor as well as enhance the effect of β2-receptor. Some studies have also suggested that ketotifen fumarate also having blocking effect on the calcium channels.
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