Composition, form of production and packaging
The tablets covered with a film membrane of white or almost white color, round, biconcave; On a cross-section from almost white to light yellow color.
Montelukast sodium 10.4 mg,
which corresponds to the content of montelukast 10 mg
Excipients: calcium hydrophosphate - 50 mg, croscarmellose sodium - 7 mg, mannitol - 78 mg, castor hydrogenated oil - 2 mg, magnesium stearate - 2 mg, povidone - 10 mg, microcrystalline cellulose - 50.6 mg.
Composition of the film coat: Opaprai white - 6 mg, including: hypromellose (hydroxypropylmethylcellulose) - 2.025 mg, giprolose (hydroxypropylcellulose) - 2.025 mg, talc 1.2 mg, titanium dioxide 0.75 mg.
7 pcs. - Cellular outline packaging (aluminum / PVC) (1) - cardboard packs.
7 pcs. - Cellular outline packaging (aluminum / PVC) (2) - cardboard packs.
7 pcs. - Cellular outline packaging (aluminum / PVC) (3) - cardboard packs.
7 pcs. - Cellular outline packaging (aluminum / PVC) (4) - cardboard packs.
10 pieces. - Cellular outline packaging (aluminum / PVC) (2) - cardboard packs.
10 pieces. - Cellular outline packaging (aluminum / PVC) (3) - cardboard packs.
14 pcs. - Cellular outline packaging (aluminum / PVC) (1) - cardboard packs.
14 pcs. - Cellular outline packaging (aluminum / PVC) (2) - cardboard packs.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2015.
Montelukast has the ability to inhibit bronchospasm due to the inhalation of LTD4 in very low doses. Bronchodilation is observed within 2 hours after ingestion. The effect of bronchodilation, caused by beta-adrenomimetics, is supplemented by the action of montelukast. Montelukast inhibits the early and late phases of bronchospasm. caused by the introduction of antigen. Montelukast reduces the number of eosinophils in the peripheral blood, in the respiratory tract (in sputum) of adult patients and children and improves control over the course of bronchial asthma. Montelukast significantly improves the morning volume of forced expiratory flow (FEV) for 1 second, the maximum volumetric expiratory flow rate (MOSV) and significantly reduces the need for beta-adrenomimetics.
Montelukast enhances the effect of inhaled glucocorticosteroids and significantly reduces bronchoconstriction. arising on the background of physical activity. In patients with bronchial asthma sensitive to acetylsalicylic acid and taking concomitant inhalation oral corticosteroids, treatment with montelukast leads to a significant improvement in the control of symptoms of bronchial asthma. In addition, there is evidence of some anti-inflammatory effect of Montelukast.
Absorption and bioavailability
Montelukast quickly and almost completely absorbed after ingestion. Bioavailability for chewable tablets 5 mg for ingestion is 73% and decreases to 63% when eating. After taking chewable tablets 4 and 5 mg, the time to reach C max (TC max ) is 2 hours. After taking 4 mg of fasting tablets in children aged 2 to 5 years, TC maxis 2 hours. The mean C max (66%) is higher, while C min in children is lower than in adults taking 10 mg.
Montelukast binds to plasma proteins more than 99%. V d of Montelukast averages 8-11 liters.
Preclinical studies revealed minimal penetration of the drug through the BBB. Concentration of montelukast 24 hours after application of the drug was minimal in all tissues of the body.
Montelukast is actively masturbating in the liver. When therapeutic doses are used, the concentration of montelukast metabolites in plasma in an equilibrium state in adults and in children is not determined. It is assumed that the isoenzymes of cytochrome P450 CYP (3A4 and 2C9) are involved in the metabolism of montelukast. in therapeutic concentrations, montelukast does not inhibit cytochrome P450 isoenzymes CYP: 3A4, 2C9, 1A2, 2A6, 2C19 and 2D6.
The clearance of montelukast is 45 ml / min in healthy adults. After oral administration of montelukast, 86% of the taken dose is excreted with feces for 5 days and less than 0.2% in urine, which confirms that montelukast and its metabolites are excreted almost exclusively with bile. T 1/2 in young healthy adults ranges from 2.7 to 5.5 h.
The pharmacokinetics of montelukast retains a practically linear character when administered in doses over 50 mg. When taking montelukast in the morning and evening hours, there is no difference in pharmacokinetics.
Pharmacokinistry in different patient groups
Pharmacokinist montelukast in men and women is similar.
When administered 1 time / day montelukasta in a dose of 10 mg, the pharmacokinetic profile and bioavailability are similar in the elderly and in young patients.
There were no differences in clinically significant pharmacokinetic effects in patients of different races.
Since montelukast and its metabolites are not excreted in the urine, the pharmacokinetics of montelukast in patients with renal insufficiency have not been evaluated.A dose adjustment for this group of patients is not required.
In patients with hepatic insufficiency of mild and moderate severity and clinical manifestations of cirrhosis, a decrease in montelukast metabolism was noted, accompanied by an increase in the AUC area by approximately 41% after a single dose of 10 mg. The excretion of montelukast in these patients is slightly increased in comparison with healthy people (mean T 1/2 - 7.4 h). Changes in the dose of montelukast for patients with mild to moderate hepatic insufficiency are not required.Data on the pharmacokinetics of montelukast with severe hepatic insufficiency (more than 9 on the Child-Pyo scale) are not available.
- long-term treatment and prevention of bronchial asthma, including the prevention of day and night symptoms of the disease;
- treatment of "aspirin" asthma;
- prevention of bronchospasm caused by physical exertion;
- relief of day and night symptoms of permanent and seasonal allergic rhinitis.
Inside, 1 time / day, regardless of food intake. For treatment of bronchial asthma, the drug should be taken in the evening. In the treatment of allergic rhinitis drug can be taken at any time of the day at the request of the patient.
Adults and children from 15 years: 1 tablet (10 mg) / day.
The therapeutic effect of the drug Ectalust В® on symptoms reflecting the course of bronchial asthma manifests itself during the first day. The patient should continue taking ECtalust В® as during the controlled course of bronchial asthma, and during the period of exacerbation of the disease. For elderly patients, patients with renal insufficiency, patients with mild or moderate liver function disorders, dose adjustment is not required. The dose of the drug is the same for both female and male patients.
The administration of ECtalust В® concomitantly with other types of asthma treatment
Ectalust В® can be added to the treatment of the patient with bronchodilators and inhaled glucocorticosteroids (see section "Interaction with other drugs").
In general, ECTALUSВ® is well tolerated. Side effects are usually mild and, as a rule, do not require withdrawal of treatment. The overall incidence of adverse events reported with the use of montelukast. comparable to that of placebo :.
Disorders from the blood and lymphatic system: increased tendency to bleeding.
Immune system disorders: reactions of hygiene, incl. anaphylaxis, eosinophilic liver infiltration (very rarely 0.01%).
Disorders of the psyche: agitation, incl. aggressive behavior or hostility, anxiety, depression, disorientation, pathological dreams, hallucinations, insomnia, irritability, anxiety, somnambulism, suicidal thoughts and behavior (suicidal). tremor.
Nervous system disorders: headache, dizziness, drowsiness, paresthesia / hypoesthesia, hyperkinesia, seizures (very rarely <0.01%).
Violations from the heart: rapid heartbeat.
Disturbances from the respiratory system, chest and mediastinal organs: nasal bleeding, upper respiratory tract infections, pharyngitis, cough, sinusitis, rhinorrhea.
Hearing disorders and labyrinthine disorders: otitis media (including the middle one).
Disorders from the digestive tract: diarrhea, dyspepsia, nausea, vomiting, pancreatitis, abdominal pain, dry mouth.
Disturbances from the liver and bile ducts: an increase in the activity of hepatic transaminases in the blood ALT, ACT, hepatitis (including cholestatic, hepatocellular and mixed liver damage) (very rarely <0.01%).
Disturbances from the skin and subcutaneous tissues: angioedema, a tendency to form a hematoma, erythema nodosum, erythema multiforme, itching, rashes, urticaria.
Disorders from the skeleton-muscle and connective tissue: arthralgia, myalgia, including muscle spasms.
General disorders and disorders at the site of administration: asthenia (weakness) / fatigue, swelling, pyrexia, thirst. In rare cases, patients with bronchial asthma develop the syndrome of Chardz-Strauss.
- hypersensitivity to any of the components of the drug;
- Children under 15 years.
PREGNANCY AND LACTATION
Ectalust В® should be used during pregnancy and during breastfeeding only if the expected benefit for the mother exceeds the potential risk to the fetus or the baby.
APPLICATION FOR FUNCTIONS OF THE LIVER
For patients with renal insufficiency, dose adjustment is not required.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
For patients with mild and / or moderate hepatic dysfunction, dose adjustment is not required.
APPLICATION FOR CHILDREN
It is forbidden to use the drug for children under 15 years.
APPLICATION IN ELDERLY PATIENTS
For elderly patients, dose adjustment is not required.
The effectiveness of the preparation Ectalust В® for oral administration with respect to the treatment of acute attacks of bronchial asthma is not established, therefore the preparation of ECTALUSВ® in tablets is not recommended for the treatment of acute attacks of bronchial asthma. The preparation Ectalust В® should not replace inhaled or oral GCS.
There is no data suggesting the possibility of reducing the dose of oral GCS with the concomitant use of the drug Ektalust В® . In rare cases, patients receiving bronchial asthma medications, including ECTALUSВ®, may experience systemic eosinophilia, sometimes accompanied by clinical manifestations of vasculitis and Charge-Strauss syndrome. This condition is usually treated with systemic SCS. Such cases are usually, but not always, related to dose reduction or cancellation of oral GCS. We can neither exclude nor confirm the likelihood that the reception of leukotriene receptor antagonists can be associated with the emergence of the Charge-Strauss syndrome. Doctors should be aware of the possibility of patients developing eosinophilia, vasculitic rash, an increase in pulmonary symptoms, complications from the heart and / or neuropathy. Patients who have the above symptoms should undergo a second examination, and their treatment regimen should be reviewed.
The drug is not used to stop attacks of bronchial asthma as an emergency medicine, but its reception should not be discontinued during the period of exacerbation.
Patients with a confirmed allergy to acetylsalicylic acid and other NSAIDs should not take these drugs during the treatment with the drug EctalustВ®, because it, while improving respiratory function in patients with allergic bronchial asthma, nevertheless can not completely prevent bronchoconstriction caused by NSAIDs.
Patients with phenylketonuria should be informed that in 1 chewable tablet 4 mg contains an average of 0.8 mg of aspartame, and in 1 chewable tablet 5 mg - an average of 1 mg of aspartame.
Impact on the ability to drive vehicles and engage in other potentially hazardous activities
Data showing that the administration of ECtalust В® affects the ability to drive vehicles or moving mechanisms has not been identified. However, when the drug is used, there are side effects such as dizziness and drowsiness. In view of this, care should be taken when driving vehicles and work requiring quickness of psychomotor reactions.
Symptoms: There were no data on overdose symptoms when taking a drug in patients with bronchial asthma at a dose exceeding 200 mg / day for 22 weeks and at a dose of 900 mg / day for 1 week.
There are reports of acute overdose of montelukast in children (taking at least 150 mg per day). The most frequent adverse events were thirst, drowsiness, mydriasis, hyperkinesia and abdominal pain.
Treatment: symptomatic. Information about the specific treatment of an overdose with the drug Ektalust В® is absent.
There is no data on the possibility of removing montelukast by peritoneal dialysis or hemodialysis.
Ectalust В® can be prescribed together with other drugs traditionally used for the prevention and long-term treatment of bronchial asthma. The recommended clinical dose of montelukast had no clinically significant effect on the pharmacokinetics of the following drugs: theophylline, isrednisone, prednisolop, oral contraceptives (ethinylestradiol / norethindrone 35/1), terfenadine, digoxin and warfarin.
AUC is reduced in persons who simultaneously receive phenobarbital (approximately 40%). However, correction of the dosage regimen of ECtalust В® is not required for such patients.
Since montelukast is metabolized by the CYP3A4 isoenzyme, caution should be used, especially in children, while administering montelukast with CYP3A4 isoenzyme-inducing drugs such as phenytoin. phenobarbital and rifampicin.
In vitro studies have shown that montelukast is a potential inhibitor of the CYP2C8 isoenzyme. however, clinical trials of drug-drug interactions, including montelukast and rosiglitazone (a preliminary substrate of a representative of medicinal products primarily metabolized by the CYP2C8 isoenzyme) showed that the dosages of montelukast do not inhibit the CYP2C8 isoenzyme in vivo. Consequently, montelukast does not have a significant effect on the metabolism of drugs metabolized by this enzyme (for example, paclitaxel, rosiglitazone and repaglinide).
When taking high doses of montelukast (at a 20- and 60-fold excess of the recommended dose for adults), a decrease in the concentration of theophylline in the plasma is observed. This effect is not observed when taking the drug at recommended doses - 10 mg / day.
Р‘СЂРѕРЅС…РѕРґРЅР»Р°С‚Р°С‚РѕСЂС‹: Ectalust В® can be added to the treatment of patients whose asthma is not controlled by the use of single bronchodilators. When the therapeutic effect is reached (usually after the first dose), the dose of bronchodilators can be gradually reduced against the background of therapy with the drug EktalustВ®.
Inhalational GCS: treatment with the drug Ektalust В® provides an additional therapeutic effect to patients receiving inhaled glucocorticosteroids. At achievement of stabilization of a status of the patient reduction of a dose of GCS is possible. The dose of GCS should be reduced gradually, under the supervision of a doctor. In some patients, the intake of inhaled glucocorticosteroids can be completely abolished. It is not recommended to sharply replace therapy with inhaled glucocorticosteroids by the prescription of the drug EctalustВ®.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored in a dry, protected from light and out of reach of children at a temperature of no higher than 25 В° C. Shelf life - 2 years.
Do not use after the expiration date.