Chewing Singulair 4mg MSD treats chronic bronchial asthma (4 blisters x 7 tablets)

Dosage form Box of 4 blisters x 7 tablets
Specifications Montelukast

Ingredient

Composition information	Content
Montelukast	4mg

Uses

indications

Singulair 4 mg is indicated in the following cases:

Elderly and children over 6 months old to prevent and treat chronic bronchial asthma, including preventing both day and night asthma symptoms, treating asthma sensitive to aspirin, and preventing bronchospasm due to exertion. Adults and children 6 months and older). These important intermediates are attached to cysteinyl leukotriene receptors (CYSLT1). Cyslt type 1 receptors (CYSLT1) are found in human airfields, including smooth muscle cells and macrophages of the airway and in other pre -inflammatory cells (including EOSIN leukemia and some bone marrow stem cells).

CYSLT is associated with the pathogenesis of asthma and allergic rhinitis. In asthma, Leukotriene intermediate effects include a number of effects on the airway, such as bronchospasm, mucus secretion, increased capillary permeability and eucalyptus mobilization. In allergic rhinitis, CYSLT is secreted from the nasal mucosa after exposure to allergens in the reactions in fast and slow phases and is related to allergic rhinitis symptoms. CYSLT in the nose will increase the obstruction of the airway and congestion symptoms.

Montelukast oral form is anti -inflammatory substance, improving inflammatory parameters in asthma. Based on biochemical and pharmacological tests, Montelukast proves high affinity and selective selection with CYSLT receptor (this effect is superior to other receptors that are also important in pharmacological, such as Prostanoid, Cholinergic or β-Adrenergic). Montelukast strongly inhibits the physiological effects of LTC4, LTD4, LTE4 at CYSLT1 receptor without the effect of march.

In asthma patients, Montelukast inhibits cysteinyl leucotriene receptors in the airway proving through the ability to inhibit bronchospasm due to Ltd4 inhalation. With doses of less than 5 mg closed the bronchospasm of Ltd4. Montelukast causes bronchiectasis for 2 hours after drinking; These effects are coordinated with bronchodilators by using the agonist β.

Clinical research in asthma

In clinical studies, Singulair takes effect in adults and children to prevent and treat chronic asthma, including preventing bronchospasm due to exercise. Singulair is valid when used separately or when combined with other drugs in maintenance indications for chronic asthma treatment. Singulair can be coordinated with inhaled corticosteroids, which will have a synergistic effect to control asthma or to reduce the dose of inhaled corticosteroids while maintaining clinical stability.

People aged 15 and over

In two double blind studies, lasting 12 weeks, with a control, similarly designed, in patients aged 15 years and older with asthma, using Singulair to take 1 dose per dose of 10mg in the evening, showing significant improvement of asthma control parameters through asthma symptoms, consequences of asthma, respiratory function and "need" of use.

Singulair significantly improves daytime symptoms of the patient's report and wake up at night, compared to Placebo. The specific consequences of asthma, including the appearance of asthma attacks, need the help of corticosteroids, stop the drug due to asthma attacks worse, asthma attacks and the number of days of escape from asthma are improved compared to the placebo.

General assessments of doctors and patients on asthma, as well as assessments of specific quality of life with asthma (in all fields, including normal daily activities and asthma symptoms) are significantly better than in the control group. Singulair significantly improves exhalation volume in the first second in the morning (FEV1), the maximum breathing speed in the morning and afternoon (PEFR) and also reduces the demand for the demand for the owner of the agreement β when compared to the Placebo.

The treatment effect is usually achieved after the first dose and maintained for about 24 hours. The therapeutic effect is also stable when used continuously once a day in tests that lasts up to 1 year. Stop the drug after using Singulair for 12 weeks does not cause reverse reaction to make asthma worse.

Comparison with inhaled Beclomethasone (each time 200 μg, 2 times daily with diffuse tools), sees Singulair has a faster initial response, although through a 12 -week study, Beclomethasone has a larger average treatment effect. However, the group using Singulair has a high percentage of clinical meetings equivalent to the inhaled Beclomethasone.

Children from 6 years old to 14 years old

Children 6 - 14 years old, using a 5 mg chewing tablet in the evening reducing a henotic drama, improving the evaluation of specific quality of life due to asthma, compared to Placebo. Singulair also improves the morning FEV1 in the morning, reducing the total "need" of the day of the day of the owner of the agonist β. The effectiveness achieved after the first dose and stable up to 6 months continuously once a day.

growth in children with asthma

Two control clinical studies show that Montelukast does not affect the ability to develop the body in children before puberty has asthma. In a study on children from 6 years old to 11 years old, the body development is assessed by the development of the length of the legs, the group using Montelukast 5 mg once a day for 3 weeks of the results is similar to the placebo group, and in the group using Budesonide gas (200 μg twice a day) for 3 weeks is lower than a statistical way compared to the placebo group.

In a 56 -week study in children from 6 to 8 years old, the development chart in children using Montelukast 5 mg once a day is similar to the placebo group (the average LS value for Montelukast and the regarded placebo is: 5.67 and 5.64 cm/year), and in the group using the veclomhasone of the gas (200 μg twice a day), this value is lower than the average value. 4.86cm/year) in children using aerosol, compared to the placebo group [Different difference in the average value of LS (with 95%reliability) is: -0.78 (-1.06; -0.49) cm/year]. Both Montelukast and Beclomethasone give clinical benefits in the treatment of mild asthma patients in a significant way compared to the placebo group.

Children from 6 months to 5 years old

In the 12 -week study, the control of Placebo in children 2-5 years old, giving Singulair once a day 4 mg, improved sustainably asthma control parameters, regardless of treatment in combination with asthma vaccine, compared to Placebo. 60% of patients do not use other asthma control treatment.

Singulair improves daytime symptoms (including cough, wheezing, breathing disorders and limited activity) and night symptoms when compared to Placeboo. Singulair also significantly reduces the "demand" of agonized drugs β, corticosteroid emergency compared to Placebo. Patients using Singulair have more and more asthma that is statistically significant compared to the patient in the Placebo group. The treatment effect immediately after the first dose. In addition, the number of eosin leukemia in the whole blood also decreased significantly.

Singulair's effectiveness in 6 -month -old death to 2 years of age is extracted from the results in children over 2 years of age with asthma and based on similar dynamic pharmacokinetics as well as on the pathology, pathophysiology and the effect of the drug basically equivalent when comparing the two age groups above.

For patients with corticosteroids inhaled inhalation

Separated studies in adults show that Singulair is used in combination with inhaled corticosteroids that have a clinical coordinates and allows a decrease in steroid dose when used in combination. In the study with the control of Placebo, the patient starts to use inhaled corticosteroids at a dose of about 1600 μg per day, during the use of Placebo, it has reduced the rate of steroid use by about 37%. Moreover, Singulair also helps reduce 47% of inhaled corticosteroid dose compared to 30% in the group using Placebo.

In another study, Singulair brings clinical benefits plus the maintenance but untreated objects with inhaled corticosteroids (every day use 400 μg of Beclomethasone). Completely stop and suddenly beclomethasone in patients used to combine Singulair with Beclomethasone causing clinical harm in some cases, proving that the drug should gradually stop with tolerance rather than sudden stopping. For people who are sensitive to aspirin, most of them are when combined with corticosteroids with inhaled and oral forms, Singulair has improved significantly on asthma control parameters.

Pharmacokinetics

absorption

After drinking, Montelukast absorbed quickly and almost completely. With 10 mg film tablets, CMAX concentration reaches 3 hours (TMAX) after taking adults, taking medicine when hungry. Born when taking oral medication is 64%. Birth and CMAX are not affected by a standard meal. With 5 mg chewing tablets, CMAX reached 2 hours after adults drinking. Born when drinking is 37%. Food does not have a great influence in clinical when taking long -term drugs.

With 4 mg chewing tablets, CMAX concentration reaches 2 hours after drinking for children 2-5 years old, taking medicine at hunger.

Distribution

more than 99% Montelukast binds to plasma proteins. The distribution volume (VD) in the stable state of Montelukast is 8 - 11 liters. Research on rats with Montelukast marks that the drug is very little distributed through the bloody brain barrier. Moreover, the concentration of the marker after drinking 24 hours is at least in all other tissues.

Metabolism

Montelukast metabolizes very strongly. In studies with treatment dose, plasma concentrations of Montelukast's metabolites are not found in a stable state in adults and children.

In vitro research, using human liver microsome, showing that Cytochrome P450 3A4 and 2C9 as catalysts for Montelukast's metabolism. Based on other results in vitro on human liver microsome, seeing the concentration of Montelukast's treatment in plasma does not inhibit cytochromes P450 3A4, 2C9, 1A2, 2A6, 2C19 or 2D6.

Elimination

Montelukast's purification in plasma is 45 ml/minute in healthy adults. After taking Montelukast, 86% of the markers are found in the feces of a total of 5 days and less than 0.2% discharged through the urine. This, along with the bioavailability of Montelukast oral, shows that Montelukast and the metabolites of the drug are almost entirely through the bile.

In many studies, Montelukast's plasma sale time is 2.7 - 5.5 hours in healthy young people. Montelukast's pharmacokinetics almost linear. When taken to the dose of 50 mg, there is no difference in pharmacokinetics when taking the drug in the morning or evening. When taking 10 mg Montelukast once a day, very little maxtelukast's mother in plasma (approximately 14%).

Before taking Chewing Singulair 4mg MSD treats chronic bronchial asthma (4 blisters x 7 tablets)

How to use

use Singulair once a day. To treat asthma, need to take medicine in the evening. With allergic rhinitis, the time to use the drug depends on the needs of each object.

For patients with both asthma and allergic rhinitis, should use a dose every day, in the evening.

Dosage

Children 2 - 5 years old with asthma and/or allergic rhinitis

Dosage for children 2 - 5 years old is a chewing daily 4 mg.

Singulair treatments related to other asthma drugs

Singulair can be used in combination with other treatments.

Dose of combined drugs

Bronchodilators: Singulair can be added to the treatment regime for people who have not been fully controlled only by bronchodilators. When there is evidence of clinical response, usually after the first dose, it is possible to reduce bronchodilators if tolerated.

Inhaled corticosteroids: using Singulair to bring more treatment benefits for patients who are using inhaled corticosteroids. Corticosteroid dose can be reduced if tolerated. However, the dose of corticosteroids must gradually decrease under the supervision of the doctor. In some patients, the inhaled corticosteroid dose can be completely withdrawn. Do not suddenly replace corticosteroids inhales with Singulair.

Note: The above dose is for reference only. Specific dosage depends on the condition and level of progression of the disease. For a suitable dose, you need to consult a doctor or medical specialist.What do

do when overdose? In chronic asthma studies, Singulair is used daily doses to 200 mg for adults for 22 weeks and short -term research with a dose of up to 900 mg daily, used for about a week, there is no clinical important reaction.

There are also reports on acute poisoning after bringing the drug to the market and in clinical studies with Singulair. These reports include both children and adults with the highest doses of up to 1000 mg. The results of the laboratory and clinical room are in line with the overview of the safety of adults and children. In most overdose reports, no harmful reactions. The most common reactions are similar to Singulair's safety properties including abdominal pain, drowsiness, thirst, headache, vomiting and excitement.Unknown Montelukast can be separated through the peritoneal or dialysis.

What to do when you forget a dose? However, if close to the next dose, skip the forgotten dose and take the next dose at the time as planned. Note that it should not be used double the prescribed dose.

Side Effects

When using Singulair 4 mg, you may experience unwanted effects (ADR).

In general, Singulair tolerates well. The adverse effects are usually mild and often do not need to stop the drug. The overall ratio of Singulair's adultery effects is equivalent to the Placebo group.

Adults aged 15 years and older have asthma

Evaluate Singulair on about 2600 adults with asthma, aged 15 and older in clinical studies. In the same two studies, clinical trials are controlled with Placebo for 12 weeks, adverse effects related to drugs at ≥ 1% of the patient uses Singulair and has a higher rate than the Placebo group is only abdominal pain and headache. The ratio of these phenomena is not different from statistical significance when comparing two treatment groups.

Total in clinical trials with 544 patients treated with Singulair for at least 6 months, 253 people to a year and 21 people to 2 years. In the case of prolonged treatment, the experience of adultery effects is not changed.

Children from 6 years old to 14 years old with asthma

Review Singulair on about 475 children with asthma, from 6 years to 14 years old shows the safety of the drug in children in general similar to adult groups taking drugs and placo.

In 8 -week clinical trials with pot control, adverse effects related to drugs recorded in> 1% of the patient using Singulair and have a higher rate than the Placebo group is just a headache. The rate of headache has no statistical significance when comparing the two treatment groups.

In evaluation studies, it affects the growth, safety attributes on these children are similar to that of Singulair's previous described safety attribute.

Total in clinical trials with 263 children from 6 years old to 14 years old are treated with Singulair at least 3 months, 164 children to 6 months or more. In the case of prolonged treatment, the experience of adultery effects is not changed.

Children from 2 years old to 5 years old have asthma

Singulair is rated over 573 children with asthma, from 2 years to 5 years old. In a 12 -week clinical trial with a control of Placebo, the adverse effects related to the drug are recorded in> 1% of the pediatric patients using Singulair and have a higher rate than the Placebo group is only thirsty. The thirst ratio has no statistical significance when comparing the two treatment groups.

A total of 426 patients with asthma, from 2 years old to 5 years old using Singulair lasting for at least 3 months, 230 children used for more than 6 months, 63 children used for more than 12 months. When the treatment lasts long, the experience of adultery is not changed.

Experience after bringing the drug to the market

There are the following adverse effects when bringing the drug to the market:

Infections and parasites: Upper respiratory tract infections. Attention, unusual dreams, hallucinations, insomnia, memory impairment, mental - excessive hyperactive movement (including easily agitated, restless restlessness, muscle vibration), sleepwalking, thoughts and suicide behavior. Respiratory, chest and mediastinum: Nasal bleeding, eosinophilic lung disease Note, itching, rash, urticaria.

When experiencing side effects of the drug, it is necessary to stop using and notify the doctor or go to the nearest medical facility for timely treatment.

Warnings

Before using the drug you need to read the instructions carefully and refer to the information below.

contraindicated

Singulair 4 mg is contraindicated in cases of hypersensitivity to any component of the drug.

Caution when used

has not been valid when taking Singulair in the treatment of acute asthma attacks. Therefore, Singulair should not be used for oral forms to treat acute asthma attacks. Patients need to be instructed to use the appropriate treatment.

may have to reduce the inhaled corticosteroids gradually with the supervision of a doctor, but not to suddenly replace oral corticosteroid or inhalation with Singulair.

There has been a report on mental - mental effects in patients using Singulair (see side effects). Because there are other factors that can contribute to these effects, it is still unknown whether these effects are related to Singulair. Doctors should discuss these adverse effects with patients and/or patients care. Should instruct patients and/or patients to notify the doctor if these effects occur.

In some rare cases, patients use other anti -asthma drugs, including Leukotriene receptor antagonists who have experienced one or some of the following phenomena: Eosin hyperpses, vasculitis rash, bad respiratory symptoms, heart complications and/or neurological diseases sometimes churg syndrome - strauss, is an EOSIN hypotension with EOSIN hypotension. These cases are sometimes related to corticosteroid reduction or stopping. Although the cause and effect has not been identified with the Leukotriene receptor antagonist, caution and clinical monitoring need to be closely monitored when using Singulair.

The ability to drive and operate machinery

There is no basis to prove Singulair has an influence on the ability to drive and operate the machine.

Pregnancy

has not studied Singulair in pregnant women. Only use Singulair when pregnant when really necessary. In the process of circulating products on the market, there was a rare report on cases of birth defects in children of mothers using Singulair during pregnancy. Most mothers also use other asthma medications during pregnancy. All causes of these events with the unchanged use of Singulair.

The period of breastfeeding. Because many of these drugs can be excreted through breast milk, the mother needs to be cautious when using Singulair during breastfeeding.

Drug interaction

can use Singulair with other commonly used drugs in preventive and chronic treatment of asthma and allergic rhinitis treatment. In studies on drug interactions, the recommended dose of Montelukast's treatment does not significantly affect the pharmacokinetics of the following drugs: Theophylline, Prednisone, Prednisolone, Ethinyl Estradiol/Norethindrone 35/1), Terfenadine, Digoxin and Warfarin.

The area under the curve (AUC) of Montelukast decreased by about 40% in people with phenobarbital. No need to adjust the dosage Singulair.

In vitro studies show that Montelukast is a CYP 2C8 inhibitor. However, data from drug interactive studies with each other clinically by Montelukast and Rosiglitazone (the substrate that represents drugs is metabolized mainly by CYP2C8) shows that Montelukast does not inhibit CYP2C8 In Vivo. Therefore, Montelukast does not change the metabolism of drugs that are metabolized mainly through this enzyme (such as Paclitaxel, Rosiglitazone, Repaglinide).

In vitro studies show that Montelukast is a substrate of CYP 2C8, 2C9 and 3A4. Data from a clinical interactive study study with the participation of Montelukast and Gemfibrozil (an inhibitor both CYP 2C8 and 2C9) showed that Gemfibrozil increased Montelukast's systemic contact level to 4.4 times. Simultaneous use of Itraconazole, a strong CYP 3A4 inhibitor with Gemfibrozil and Montelukast does not increase Montelukast's systemic contact.

The effect of Gemfibrozil on Montelukast's systemic contact level is not considered clinical significance based on clinical safety data with a greater dosage of more than 10 mg approved for adults (200 mg/day in adult patients for 22 weeks and up to 900 mg/day for nearly a week), do not observe unwanted effects of clinical significance. Therefore, there is no need to adjust the dose of Montelukast in patients to use simultaneously with Gemfibrozil.

Based on in vitro data, clinical important drug interactions with known CYP 2C8 inhibitors (as trimethoprim) are not predicted. In addition, simultaneous use of Montelukast with Itraconazole alone does not significantly increase Montelukast's body contact.

Storage

Singulair 4 mg chewing is below 30 ° C (86 ° F), avoiding moisture and avoiding light.

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