Singulair 10mg MSD treats chronic bronchial asthma (4 blisters x 7 tablets)

These important mediators are attached to cysteinyl leukotriene receptors (CYSLT).

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).

GYSLT is associated with the pathogenesis of asthma and allergic rhinitis. In asthma, the intermediate effects of Leukotriene include a number of effects on the airway, such as bronchospasm, mucus secretion, increase in capillaries and mobilizing eucalyptus eosin. 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.

Montelukasi oral form is anti -inflammatory substance, improving inflammatory parameters in asthma. Based on biochemical and pharmacological tests, Mantelukast proves high affinity and selective selection with CYSLT receptor (this form is superior to other receptors that are also important in pharmacological, such as Prostanoid, Cholinergic or 8-ADRENERGIC).

Montelukast strongly inhibits the physiological effects of LTC4, LTD4 LTE4 at CYSLT receptor; Without no effect. In asthma patients, Montelukast inhibits the cysteinyl leucotriene receptors in the airway to prove through the ability to inhibit bronchospasm due to Ltd inhalation. With doses of less than 5 mg, the bronchospasm of Ltd, Montelukast causes bronchiectasis for 2 hours after taken; These effects are in union with bronchodilator by using the owner b.

Pharmacokinetics

absorption

4 mg oral nuggets are biological equivalent with 4 mg chewing tablets when used for adults when hungry. The use of Montelukast in the form of grain nuggets with apple sauce or during a standard meal does not significantly affect the pharmacokinetics of the drug determined by the area under the AUC curve (1.225.7 compared to 1,223.1 ng - hour/ml with apple sauce and 1,191.8 compared to 1,148.5 ng - hour/ml with or without standard meals).

Effect and safety have been shown through clinical studies, when using 4 mg chewing tablets, 5 mg chewing tablets, 10 mg film tablets, orally, regardless of meal time. The safety of Singulair is also proven in clinical research for drinking 4 mg grain nuggets without including meal time.

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 shows that it is very little distributed through the 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 2C6 as catalysts for Montelukast's metabolism. Based on other Invitro results on human liver microsomes, seeing Montelukast's treatment concentrations 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 total door for 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 dynamic pharmacokinetics almost linear when taken to 90 mg. There is no difference in pharmacokinetics when taking medicine in the morning or evening. When taking 10 mg Montelukast once a day, very little maxtelukast's mother in plasma (approximately 14%).

General recommendation:

Singular®'s treatment effect is based on asthma test parameters in one day.

It is necessary to tell patients to continue using Singular® even though the asthma attacks are controlled, as well as in periods of severe asthma.

No need to adjust the dose for children in each age group, for the elderly, people with kidney failure, mild and medium liver failure, or for each gender.

Singular treatment related to other asthma medications: Singular® can be used for patients with other treatment regimes.

Dosage of combined drugs: Bronchodilators: Singular® can be added to the treatment regime for patients who have not been fully controlled only by bronchodilators.

When there is evidence of clinical response, usually after the first dose, bronchodilator can be reduced if tolerated.

Inhaled corticosteroids: Together with Singular®, it has 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 completely withdraw. Do not sudden replacement cortico-steroids inhaled with Singular®.

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 to do when overdose?

There is no specific information about treatment when using Singular overdose.

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

What to do when you forget 1 dose? However, if the time to relax with the next dose is too short, skip the dose and continue the calendar of the drug. Do not use double dose to compensate for missed dose.

Systemic: Abdominal pain and headache (patient> 15 years old), headache (patients 6 to 14 years old), thirst (patients 2 to 5 years old), diarrhea, agitation, asthma, dermatitis and rash (patients 6 months to 2 years old).