Zafirlukast Tablets

In the pathophysiology of asthma, it is believed that the effects of leukotriene products (LT) binding to their receptors, including smooth muscle contraction, airway edema and changes in inflammatory cell activity (such as eosinophilic lung infiltration), are all related to the symptoms and signs of asthma. As an anti-inflammatory drug, Ancolex can reduce the effects of these inflammatory mediators. As a powerful oral polypeptide leukotriene receptor antagonist of slow-reacting substances such as LTC4, LTD4 and LTE4, it belongs to competitive inhibition and has the characteristics of high selectivity. In vitro studies have shown that Ancolex antagonizes the contractile activity of all three leukotriene polypeptides (leukotriene C4, D4, and E4) in human conducting airway smooth muscle, and the degree is the same. Animal experiments show that the main effects of Ancolex are: 1) effectively preventing the increase in vascular permeability caused by leukotriene polypeptides, which can cause airway edema; 2) inhibiting the infiltration of airway eosinophils produced by leukotriene polypeptides. Clinical studies have also confirmed the specificity of Ancolax, which only acts on leukotriene receptors, but does not affect prostaglandin, thromboxane, cholinergic and histamine receptors. Clinically verified, Ancolax has anti-inflammatory properties. A 5-day dose of Ancolax can reduce cellular and non-cellular inflammatory substances caused by antigen stimulation in the airways. Placebo-controlled studies have found that zafirlukast can inhibit the increase of eosinophils, lymphocytes and tissue cells in bronchoalveolar lavage fluid 48 hours after antigen stimulation, and reduce the peroxides produced by alveolar macrophage stimulation. Ancolax can inhibit antigen-induced airway hyperresponsiveness and bronchospasm caused by platelet activation factors. Furthermore, long-term use of zafirlukast (20 mg once, twice a day) can reduce the sensitivity of airway acetyl methacholine. In clinical observations evaluating long-term treatment with Ancolax, its plasma level was at a low point, and lung function was still improved compared to the baseline level, indicating that airway obstruction caused by inflammatory substances was permanently relieved. The antagonistic effect of Ancol on bronchospasm caused by inhaled leukotriene D4 is shown to be dose-related. Asthmatics are 10 times more sensitive to leukotriene D4 than normal people. A single oral dose of Ancol makes asthmatics 100 times more tolerant to inhaled LTD4 and has a significant protective effect within 12 and 24 hours. Ancol can inhibit bronchospasm caused by various stimuli, such as sulfur dioxide, exercise and cold air. Ancol can also reduce the early and late inflammatory responses caused by various antigens (such as pollen, cat dander, ragweed and mixed antigens). In some patients, Ancol can completely prevent asthma attacks caused by exercise and allergens. For patients with asthma who are not adequately controlled with beta-receptor agonists (as needed), Ancolex can be used as a first-line maintenance treatment. For patients with clinical symptoms, Ancolex can relieve symptoms (reduce diurnal asthma symptoms), improve lung function, reduce the dosage of beta-receptor agonists and the incidence of asthma exacerbations. Clinical studies have found that within 2 hours of taking the drug, the drug plasma concentration has not yet reached its peak, and it can produce a significant first-dose effect on basal bronchial motility. When using Ancolex for treatment, asthma symptoms initially improve within a week, often in the first few days. Ancolex is taken orally twice a day, so it is of special significance for patients with poor compliance or who find it difficult to maintain treatment with inhaled drugs.

Zafirlukast.

This product is a white film-coated tablet.

Suitable for the prevention and long-term treatment of asthma.

This drug is used to prevent asthma attacks, so it should be used continuously. The starting dose for adults and children over 12 years old (including 12 years old) should be 20 mg bid, and the general maintenance dose is 20 mg bid. The dose is gradually increased to a maximum of 40 mg once a day. Twice a day may be more effective, and the dosage should not exceed the maximum recommended dose. Because food can reduce the bioavailability of zafirlukast, this drug should be avoided when taken with food. Elderly people over 65 years old have a reduced clearance rate for zafirlukast, so the peak concentration (Cmax) and area under the curve (AUC) are about twice that of young people. However, there is no data to prove the accumulation of zafirlukast in the elderly. In clinical use, the elderly will not increase the side effects of the drug or stop taking the drug due to side effects when taking 20 mg bid. The starting dose for the elderly should be 20 mg bid, and then the dosage should be adjusted according to the clinical response. Children There is no report on the efficacy and safety of this drug for children under 12 years old. No dose adjustment is required for patients with renal insufficiency. In patients with stable alcoholic cirrhosis, the clearance of zafirlukast is reduced, and the peak concentration (Cmax) and area under the curve (AUC) are approximately twice that of normal people. The starting dose should be 20 mg bid, and then adjusted according to clinical response. The use of this drug in patients with liver damage caused by other reasons has not been observed, nor has long-term observation been conducted on patients with cirrhosis.

; Ancol; is well tolerated. It may cause headache or gastrointestinal reactions when used. These symptoms are usually mild. The following have been reported after using ; Ancol; * Rash, including blisters * Allergic reactions, including urticaria and angioedema (very rare) * Mild limb edema (very rare) * Bleeding disorder after contusion * Agranulocytosis The above events usually return to normal after discontinuation of the drug. In clinical trials, it has been observed that transaminase levels may increase with the use of ; Ancol;, but it is uncommon. It can return to normal after continued treatment or discontinuation of the drug. In a very small number of patients, transaminase levels remain abnormal due to drug-mediated hepatitis, which often returns to normal after discontinuation of ; Ancol;. In post-marketing experience, there have been very few cases of signs of hepatitis, some of which are accompanied by hyperbilirubinemia, and some are not. These reports are related to the use of ; Ancol;. Such events usually return to normal after discontinuation of ; Ancol;. Most reports are from female patients. There are rare reports of liver failure. There are rare reports of hyperbilirubinemia associated with taking Ancolax, but it does not increase liver function test results. Placebo-controlled observations have found that the incidence of infection in elderly patients using Ancolax increases, but the symptoms are mild, mainly affecting the respiratory tract, and there is no need to discontinue treatment. There are rare reports of nonspecific joint pain and nonspecific myalgia associated with Ancolax.

Patients who are allergic to this drug and its components are contraindicated.

Precautions for children: There are no reports on the efficacy and safety of Ankelai for children under 12 years old. Precautions for pregnancy and lactation: The safety of Ankelai for pregnant women has not been established. It is not suitable for lactating women. Precautions for the elderly: Please refer to the section on medication for the elderly in the Usage and Dosage section.

Accolade can be used in combination with other conventional treatments for asthma and allergies. No adverse interactions were observed when it was used in combination with inhaled corticosteroids, inhaled and oral bronchodilators, antibiotics and antihistamines. No adverse interactions were observed when Accolade was taken with oral contraceptives. When used in combination with aspirin, the plasma concentration of zafirlukast can be increased by about 45%, but it does not cause corresponding clinical effects. The plasma concentration of zafirlukast is reduced by about 40% when used in combination with erythromycin. In clinical trials, the combined use of theophylline can cause a decrease in the plasma level of zafirlukast by about 30%, but it has no effect on the plasma level of theophylline. However, in post-marketing monitoring, a very small number of patients had elevated theophylline levels after taking Accolade. The combination with terfenadine can cause a 54% decrease in the area under the curve of zafirlukast, but has no effect on the plasma level of terfenadine. The combination with warfarin can lead to a prolongation of the maximum prothrombin time by about 35%. Therefore, when Accolade is used in combination with warfarin, it is recommended to closely monitor the prothrombin time. The interaction between the two may be due to the inhibition of cytochrome P450-2C9 isomerase system by zafirlukast.

Store below 30°C.

20 mg

24 months