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  • Supply Ketotifen fumarate raw Materials Powder Ketotifen fumarate

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    Product Overview:

    Ketotifen fumarate, also known as mepipertiheptaenone, thioperidone, sardesone, thiotrepanone and ketotiphenol, is a powerful antiallergic drug with both tricyclic and piperidine structures, which is characterized by a strong antagonistic effect of histamine H1 receptor and inhibition of the release of allergic reaction mediators. It can inhibit the release of various mediators in mast cells, basophils and macrophages, including the release of slow reactive substances and other active substances, have an antagonistic effect on calcium ions, inhibit phosphodiesterase, and increase the content of cAMP in mast cells. Inhibition of neutrophil chemotaxis and inflammatory response, its effect is 10 times stronger than pramine, and has a long-term effect, stronger than sodium chrominate. Ketotifen fumarate has therapeutic effect on both type I and type III allergic reactions. The peak blood concentration is 2 to 3 hours, the half-life is 22 hours, 60% excreted by urine, 40% excreted by feces, children excreted faster than adults, long-term treatment does not produce resistance, interruption of treatment without rebound phenomenon.

    Supply Ketotifen fumarate raw Materials Powder Ketotifen fumarate Attributes

    Ketotifen fumarate raw Materials Powder

    CAS:34580-14-8

    MF:C23H23NO5S

    Ketotifen fumarate

    MW:425.5

    EINECS:252-100-0

    Specification​: 99% min Ketotifen fumarate Powder

    Sample:Ketotifen fumarate Powder

    Packaging:1kg/bag, 25kg/drum

    Brand: Henrikang

    Appearance:white

    Storage: Cool Dry Place

    Shelf Life: 2 Years

    Test Method: HPLC

    Supply Ketotifen fumarate raw Materials Powder Ketotifen fumarate Details

    Ketotifen fumarate Powder Usage and Synthesis.

    Ketotifen fumarate has been used in clinical prevention and treatment of asthma and childhood asthma for more than 20 years. It is a drug that integrates prevention and treatment of asthma and childhood asthma. Ketotifen in particular has been widely used in many countries as a long-term control drug for childhood asthma and childhood asthma. Since the early 1980s, ketotifen fumarate has been used in Western Europe, Asia and China for the prevention and treatment of asthma and childhood asthma, but since the 21st century, the annual use has been decreasing year by year. Due to the drug has a certain central nervous inhibition side effect, the current oral tablet has not been approved by the FDA, so it has not entered the US market, only ketotifen fumarate eye drop (ZADITOR) was approved by the FDA in 1999.

    Recent studies have shown that the effectiveness of ketotifen on asthma still needs further research. In addition, ketotifen fumarate can affect the academic performance of school-age children with drowsiness, affect the intellectual development of infants, and affect the metabolism of slow-release theophylline and affect the anti-inflammatory effect of theophylline. Therefore, GINA under WHO does not recommend the use of ketotifen fumarate in the prevention and treatment of childhood asthma and childhood asthma. However, from the perspective of clinical economics, ketotifen fumarate is an inexpensive anti-allergy drug suitable for use in developing countries and vast rural areas, and has some effect on asthma and childhood asthma.

    Ketotifen fumarate Powder

    Uses of Ketotifen fumarate.

    Uses Antihistamine, antiasthmatic, used to prevent and treat bronchitis asthma.

    Ketotifen fumarate

    Pharmacological action of Ketotifen fumarate.

    The pharmacological effect of ketotifen fumarate is complex, and it has achieved certain effect in the prevention and treatment of asthma and childhood asthma, but the detailed mechanism of its pharmacology is still unclear. From the current research status, the pharmacological mechanism of ketotifen fumarate in the prevention and treatment of asthma and childhood asthma mainly includes the following aspects:

    1. Antagonistic inflammatory mediators: Clinical studies have confirmed that ketotifen fumarate can effectively inhibit histamine-induced bronchospasm, and its effect is similar to that of Azelastine, suggesting that ketotifen fumarate has a strong histamine-antagonistic effect. Recent studies have shown that ketotifen fumarate can also antagonize inflammatory mediators such as leucotrienes and platelet activators, so it can be considered that ketotifen is a drug that can antagonize a variety of inflammatory mediators, which may be one of the main mechanisms of its prevention and treatment of asthma and childhood asthma.

    2. Mast cell/basophilus cell membrane protective effect: Pharmacological studies on ketotifen fuarate have confirmed that it can inhibit mast cell/basophilus cell membrane release of histamine, leucotrienes and platelet activators, suggesting that it has a strong mast cell/basophilus cell membrane protective effect. This may be the main mechanism by which ketotifen fumarate can prevent and treat the dual nature of asthma and childhood asthma.

    3. Inhibiting inflammatory cell infiltration in the airway: Ketotifen fumarate can inhibit airway infiltration of eosinophils and neutrophils, the mechanism of which is still unclear.

    4. Regulation of T cell activity: Ketotifen fumarate inhibits IgE synthesis in vivo by regulating the release activity of CD4+ and CD8+ lymphocytes. The mechanism of ketotifen fumarate inhibiting IgE synthesis and the above two mechanisms determine the airway anti-inflammatory effect of ketotifen fumarate.

    5. Other effects: Some studies have shown that ketotifen fumarate can reverse the β2-receptor hyporegulation caused by long-term use of β2-receptor agonists and increase the β2-receptor density in the airway, and can enhance the effect of β2-receptor agonists. Some studies have also shown that ketotifen fumarate has calcium channel blocking effects.

    Product Method of Bulk Ketotifen fumarate Powder.

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