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Anti Allergic Drugs Ketotifen Fumarate For Antiasthmatic , Cas 34580-14-8
Product Name: Ketotifen fumarate
Synonyms: 10h-benzo(4,5)cyclohepta(1,2-b)thiophen-10-one,4,9-dihydro-4-(1-methyl-4-pipe;hc20-511fumarate;zaditen;4-(1-methyl-4-piperidylidene)-4h-benzo[4,5]cyclohepta[1,2-b]thiophen-10(9h)-one hydrogen fumarate;4,9-DIHYDRO-4-(1-METHYL-4-PIPERIDINYLIDENE-10H-BENZO[4,5]CYCLOHEPTA[1,2-B]THIOPHEN-10-ONE) FUMARATE;KETOTIFEN FUMARATE;KETOTIFEN FUMARATE SALT;4,9-dihydro-4-(1-methylpiperidin-4-ylidene)-10H-benzo[4,5]cyclohepta[1,2-b]thiophene-10-one fumarate
Product Categories: Antagonists;Histaminergics;Neurotransmitters;Histamine receptor;Aromatics;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Sulfur & Selenium Compounds;Pharmaceutical raw material;SERC;Other APIs;Antiallergic agents
Melting point 192℃
Storage temp. Store at RT
Chemical Properties Off-White Solid
Usage : vasodilator .
Usage Antiasthmatic ; antiallergic.
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.
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 (ZADITOR) 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 .
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