Montelukast Sodium Tablets

Pharmacology Cysteinyl leukotrienes (LTC4, LTD4, LTE4) are potent inflammatory mediators released by a variety of cells including mast cells and eosinophils. These important pro-asthmatic mediators bind to cysteinyl leukotriene (CysLT) receptors. Cysteinyl leukotriene type I (CysLT1) receptors are distributed throughout the human airways (including airway smooth muscle cells and airway macrophages) and other pro-inflammatory cells (including eosinophils and certain bone marrow stem cells). CysLTs are associated with the pathophysiology of asthma and allergic rhinitis. In asthma, leukotriene-mediated effects include a range of airway responses such as bronchoconstriction, mucus secretion, increased vascular permeability, and eosinophil accumulation. In allergic rhinitis, CysLTs are released from the nasal mucosa in both the immediate and delayed phases following allergen exposure, which are associated with allergic rhinitis symptoms. Intranasal CysLT provocation increases nasal airway resistance and symptoms of nasal obstruction. This product is a potent 1:3 oral preparation that can significantly improve asthma inflammation indicators. Biochemical and pharmacological bioassays show that montelukast has a high affinity and selectivity for CysLT2 receptors (compared with other pharmacologically important airway receptors such as prostanoids, cholinergic and β-adrenergic receptors). Montelukast can effectively inhibit the physiological effects of LTC, LTD and LTE binding to CysLT2 receptors without any receptor agonist activity. Current studies suggest that montelukast does not antagonize CysLT2 receptors. Toxicology 1. Acute toxicity In mice and rats, no death occurred when a single oral dose of montelukast sodium was as high as 5000 mg/kg (15,000 mg/m2 and 29,500 mg/m2 for mice and rats, respectively). This dose is the maximum tested dose (oral LD50>5000 mg/kg), equivalent to 25,000 times the recommended daily dose for adults*. Long-term toxicity tests in monkeys and rats lasted up to 53 weeks, and in infant monkeys and mice up to 14 weeks. The results showed that montelukast sodium was well tolerated and had a wide safety range at the doses used. No effects on toxicological parameters were found when montelukast sodium was administered to any test animal at least 125 times the recommended human dose*. No cases were found in adult and pediatric patients where therapeutic doses of montelukast sodium could not be used. Carcinogenicity In studies of rats with oral doses up to 200 mg/kg/day for 106 weeks and mice with oral doses up to 100 mg/kg/day for 92 weeks, no montelukast sodium was found to be carcinogenic. These doses are equivalent to 1000 times and 500 times the recommended adult dose*. Mutagenicity No genotoxic or mutagenic effects of montelukast sodium were found. In in vitro microbial mutation tests and V-79 mammalian cell mutation tests, montelukast sodium showed negative reactions regardless of metabolic activity. In vitro genotoxicity was not observed in the rat hepatocyte alkaline washout test and the Chinese hamster ovary cell chromosome aberration test, either with or without the microsomal enzyme activity system. Similarly, no induction of chromosomal abnormalities in bone marrow cells was observed when montelukast sodium was administered orally to male or female mice at doses up to 1200 mg/kg (3600 mg/m2) (6000 times the recommended daily dose for adults*). Reproductive toxicity No effects on fertility or reproductive capacity were observed in oral studies of montelukast sodium in male rats at doses up to 800 mg/kg/day and in female rats at doses up to 100 mg/kg/day. These doses are 4000 and 500 times higher than the recommended adult dose, respectively*. In developmental toxicity studies, no treatment-related adverse effects were observed when montelukast sodium was administered to rats at doses up to 400 mg/kg/day and to rabbits at doses up to 100 mg/kg/day. Fetal exposure to montelukast sodium has been reported in rats and rabbits, and montelukast sodium has been detected in the milk of lactating rats.

The main ingredient of this product is montelukast sodium.

This product is a light yellow irregular film-coated tablet.

This product is indicated for the prevention and long-term treatment of asthma in adults aged 15 years and over, including prevention of daytime and nighttime asthma symptoms, treatment of patients with aspirin-sensitive asthma, and prevention of exercise-induced bronchoconstriction. This product is indicated for the relief of symptoms caused by allergic rhinitis (seasonal allergic rhinitis and perennial allergic rhinitis in adults aged 15 years and over).

Once a day, one tablet (10 mg) each time. Asthma patients should take it before bedtime. Patients with allergic rhinitis can take it when needed according to their own conditions. Patients with both asthma and allergic rhinitis should take the medicine once a night. Adult patients aged 15 years and above with asthma and/or allergic rhinitis should take the medicine once a day, 10 mg each time. It is generally recommended to evaluate the treatment effect with asthma control indicators. The efficacy of this product will appear within one day of medication. This product can be taken with or without food. Patients should be advised to take it regardless of whether their asthma is under control or exacerbated. Elderly patients, patients with renal insufficiency, patients with mild to moderate liver damage, and patients of different genders do not need to adjust the dose. Relationship between Montelukast Sodium Tablets and other asthma treatment drugs: This product can be added to the patient's existing treatment plan. Reduce

This product is generally well tolerated, with mild adverse reactions, and usually no termination of treatment is required. The overall incidence of adverse reactions of this product is similar to that of placebo. Clinical studies have been conducted in approximately 2,600 adult asthma patients aged 15 years and over to evaluate the safety of this product. In two similarly designed, placebo-controlled 12-week clinical studies, the adverse events with a drug-related incidence of ≥1% in the treatment group of this product and higher than that in the placebo group were abdominal pain and headache. However, there was no significant difference in the incidence of these adverse events between the two groups. In clinical studies, a total of 544 patients have been treated with this product for at least 6 months, 253 patients have been treated for 1 year, and 21 patients have been treated for 2 years. The occurrence of adverse events has not changed with the extension of the treatment time of this product. (See the inner package insert for details)

Do not use if you are allergic to any ingredient of this product.

Precautions for children: Safety and efficacy studies have been conducted in children aged 6 months to 14 years. For medication in children aged 2 to 14 years, please refer to the [Usage and Dosage] of Montelukast Sodium Chewable Tablets. The safety and efficacy of children under 6 months of age have not been studied. Studies have shown that this product does not affect the growth rate of children. Precautions for pregnancy and lactation: There is no research data on pregnant women. Pregnant women should avoid taking this product unless it is clearly necessary to take the medicine. Global post-marketing experience shows that there are rare reports of congenital limb defects in newborns after using this product during pregnancy. The vast majority of these women also used other asthma treatment drugs during pregnancy. The causal relationship between the use of this product and these events has not been established. It is not clear whether it can be secreted from breast milk. Since many drugs can be secreted from breast milk, breastfeeding women should use this product with caution. Precautions for the elderly: In clinical studies, there was no age difference in the effectiveness and safety of this product.

This product can be used in combination with other drugs routinely used for the prevention and long-term treatment of asthma and the treatment of allergic rhinitis. In drug interaction studies, the recommended dose of this product did not produce clinically significant pharmacokinetic effects on the following drugs: theophylline, prednisone, prednisolone, oral contraceptives (ethinyl estradiol/norethindrone 35/1), terfenadine, digoxin and warfarin. In patients taking phenobarbital concomitantly, the area under the plasma-concentration-time curve (AUC) of montelukast was reduced by approximately 40%. However, it is not recommended to adjust the dosage of this product. In vitro studies have shown that montelukast is an inhibitor of CYP2C8. However, a clinical study data on the drug interaction between montelukast and rosiglitazone (a typical detection substrate that is mainly metabolized by CYP2C8)

Store at room temperature, moisture-proof and light-proof

10mg*5s (Singulair)

36 months