Ectalust - instructions for use, doses, side effects, contraindications

Composition:1 tablet chewing 4 mg contains:
active substance: Montelukast sodium 4.16 mg, calculated as montelukast 4 mg; Excipients: dextrates 80 mg, mannitol 69.44 mg, salted (microcrystalline cellulose 98%, silicon dioxide colloid 2%) 80 mg, strawberry flavoring 3.2 mg, aspartame 0.8 mg, magnesium stearate 2.4 mg.
1 tablet chewing 5 mg contains:
active substance: Montelukast sodium 5.2 mg, calculated as montelukast 5 mg; Excipients: dextrates 100 mg, mannitol 86.8 mg, salted (microcrystalline cellulose 98%, silicon dioxide colloid 2%) 100 mg, strawberry flavoring 4 mg, aspartame 1 mg, magnesium stearate 3 mg.

Description:Round, biconvex tablets, white or almost white.

Pharmacotherapeutic group:Anti-inflammatory anti-bronchoconstrictive means - leukotriene receptor blocker.

ATX: & nbsp

R.03.D.C.03 Montelukast

Pharmacodynamics: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 administration of the 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 expiration (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 weakens bronchospasm, which occurs against the background of physical exertion. In patients with bronchial asthma sensitive to acetylsalicylic acid and taking concomitant inhalation oral glucocorticosteroids, 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.

Pharmacokinetics: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 4 and 5 mg tablets, the time to reach the maximum concentration (TCmax) is 2 hours. After taking 4 mg of chewing tablets by children from 2 to 5 years of age, TCmax is 2 hours. The mean maximum concentration (C max) (66%) is higher, while the mean minimum concentration (Cmin) in children is lower than in adults taking 10 mg.
Distribution
Montelukast binds to plasma proteins more than 99%. The volume distribution of Montelukast averages 8-11 liters.
Preclinical studies revealed minimal penetration of the drug through the blood-brain barrier. Concentration of montelukast 24 hours after application of the drug was minimal in all tissues of the body.
Metabolism
Montelukast is actively metabolized 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 (ZA4 and 2C9) are involved in the metabolism of montelukast, while in therapeutic concentrations montelukast does not inhibit cytochrome P450 isoenzymes CYP: ZA4, 2C9, 1A2, 2A6, 2C19 and 2D6.
Excretion
The clearance of montelukast is 45 ml / min in healthy adults. After oral administration of montelukast, 86% of the accepted dose is excreted with feces for 5 days and less than 0.2% with urine, which confirms that montelukast and its metabolites are excreted almost exclusively with bile. The half-life in young healthy adults ranges from 2.7 to 5.5 hours.
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.
Pharmacokinetics in different patient groups
Floor: The pharmacokinetics of montelukast in men and women is similar.
Age: When administered once daily montelukasta in a dose of 10 mg, the pharmacokinetic profile and bioavailability are similar in the elderly and in young patients.
Ethnicity: There were no differences in clinically significant pharmacokinetic effects in patients of different races.
Renal insufficiency: Because the montelukast and its metabolites are not excreted in the urine, the pharmacokinetics of montelukast in patients with renal insufficiency has not been evaluated. A dose adjustment for this group of patients is not required.
Liver failure: 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 area under the pharmacokinetic concentration-time curve (AUC) 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 half-life is 7.4 hours). Changes in the dose of montelukast for patients with mild to moderate hepatic insufficiency are not required. There is no data on the pharmacokinetics of montelukast with severe hepatic insufficiency (more than 9 on the Child-Pugh scale).

Indications:- Prolonged treatment and prevention of bronchial asthma, including prevention of day and night symptoms of the disease;
- Treatment of "aspirin" asthma;
- Prevention of bronchospasm caused by physical exertion;
- Cupping of day and night symptoms of permanent and seasonal allergic rhinitis.

Contraindications:- Hypersensitivity to any of the components of the drug;
- Phenylketonuria;
- Children under 2 years of age (for a dosage of 4 mg);
- Children under 6 years of age (for a dosage of 5 mg).

Pregnancy and lactation:Ectalust® should be used during pregnancy and during breastfeeding only if the expected benefit to the mother exceeds the potential risk to the fetus or child.

Dosing and Administration:Ectalust® is taken orally, the tablet should be chewed 1 hour before meals or 2 hours after eating, once a day. 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 aged 15 years and over it is recommended to use other dosage forms of montelukast (for example, film-coated tablets, 10 mg).
Children from 2 to 5 years: one chewable tablet in a dose of 4 mg once a day, before bedtime.The dosage for this age group is not required.
For children from 6 to 14 years: one chewable tablet at a dose of 5 mg once a day, before bedtime. The dosage for this age group is not required.
General recommendations
The therapeutic effect of the drug Ektalust® on symptoms reflecting the course of bronchial asthma manifests itself during the first day. The patient should continue taking the drug Ektalust® both 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 and / or moderate hepatic impairment, dose adjustment is not required.
The administration of ECtalust® simultaneously with other asthma treatments of ECTALUS® can be added to the treatment of the patient with bronchodilators and inhaled glucocorticosteroids (see section "Interaction with other drugs").

Side effects:In general, the drug Ectalust® is well tolerated. Side effects are usually mild and, as a rule, do not require withdrawal of treatment. The overall incidence of side effects reported with the use of montelukast is comparable to that of placebo:
Violations from the blood and lymphatic system: increased tendency to bleeding.
Immune system disorders: hypersensitivity reactions, including anaphylaxis, eosinophilic liver infiltration (very rarely - <0.01%).
Disorders of the psyche: agitation including aggressive behavior or hostility, anxiety, depression, disorientation, abnormal dreams, hallucinations, insomnia, irritability, restlessness, somnambulism, suicidal ideation and behavior (suicidality), tremor.
Impaired nervous system: headache, dizziness, drowsiness, paresthesia / hypoesthesia, hyperkinesia, seizures (very rarely - <0.01%).
Heart Disease: cardiopalmus.
Disturbances from the respiratory system, chest and mediastinal organs: nosebleeds, upper respiratory tract infections, pharyngitis, cough, sinusitis, rhinorrhea.
Hearing impairment and labyrinthine disturbances: otitis media (including the middle one).
Disorders from the gastrointestinal tract: diarrhea, dyspepsia, nausea, vomiting, pancreatitis, abdominal pain, dry mouth.
Disorders from the liver and bile ducts: increased activity of "hepatic" transaminases in the blood (alanine aminotransferase (ALT), aspartate aminotransferase (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 hematomas, erythema nodosum, erythema multiforme, itching, rashes, urticaria.
Disturbances from the musculoskeletal 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.

Overdose:Symptoms: Data on the symptoms of overdose when taking the drug by patients with bronchial asthma at a dose exceeding 200 mg per day for 22 weeks and at a dose of 900 mg per day for 1 week was not revealed.
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.
Treated: Treatment is symptomatic. Information on the specific treatment of an overdose with the drug Ektalust® is absent.
There is no data on the possibility of removing montelukast by peritoneal dialysis or hemodialysis.

Interaction:Ectalust® 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, prednisone, prednisolone, oral contraceptives (ethinyl estradiol / norethindrone 35/1), terfenadine, digoxin and warfarin.
AUC is reduced in persons who simultaneously receive phenobarbital (by about 40%). However, correction of the dosage regimen of ECtalust® is not required by such patients.
Because the 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 ri-fumpticin.
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 medical preparations primarily metabolized by the CYP2C8 isoenzyme) showed that the doses 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 repagli-nid).
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 per day.
Bronchodilators: Ectalus® can be added to the treatment of patients whose asthma is not controlled by the use of single bronchodilators. When the therapeutic effect is achieved (usually after the first dose), the dose of bronchodilators can be gradually reduced against the background of therapy with the drug Ektalust®.
Inhaled glucocorticosteroids: Treatment with the drug Ektalust® provides an additional therapeutic effect to patients receiving treatment with inhaled glucocorticosteroids. When the stabilization of the patient is achieved, a reduction in the dose of glucocorticosteroids is possible. The dose of glucocorticosteroids should be reduced gradually, under the supervision of a doctor. In some patients, the intake of inhaled glucocorticosteroids can be completely abolished. Not recommended harsh
replacing therapy with inhaled glucocorticosteroids with the prescription of the drug Ektalust®.

Special instructions:The effectiveness of the preparation Ectalust® for ingestion with regard to the treatment of acute attacks of bronchial asthma is not established, therefore the preparation of ECTALUS® in tablets is not recommended for the treatment of acute attacks of bronchial asthma.
The drug Ektalust® should not replace inhaled or oral glucocorticosteroids.
There are no data indicating the possibility of reducing the dose of oral glucocorticosteroids with the concomitant use of the drug Ektalust®.
In rare cases, patients taking medications for the treatment of bronchial asthma, including the drug Ektalust®,there may be systemic eosinophilia, sometimes accompanied by clinical manifestations of vasculitis and the syndrome of Charles-Strauss. This condition is usually treated with systemic glucocorticosteroids. Such cases are usually, but not always, associated with a decrease in dose or with withdrawal of oral glucocorticosteroids. 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 non-steroidal anti-inflammatory drugs (NSAIDs) should not take these drugs during the treatment with the drug Ektalust®,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 aspartame, and in 1 chewable tablet 5 mg - an average of 1 mg aspartame.

Effect on the ability to drive transp. cf. and fur:Data indicating that the administration of ECtalust® 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.

Form release / dosage:Tablets chewing 4 mg, 5 mg.

Packaging:By 7, 10 or 14 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.
According to 1, 2, 3, 4 contour cell packs of 7 tablets or 2, 3 contour packs of 10 tablets, or 1, 2 contour packs of 14 tablets together with instructions for use are placed ina pack of cardboard.

Storage conditions:In a dry, protected from light place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:2 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002248

Date of registration:25.09.2013

Expiration Date:25.09.2018

The owner of the registration certificate:CANONFARMA PRODUCTION, CJSC CANONFARMA PRODUCTION, CJSC Russia

Manufacturer: & nbsp

CANONFARMA PRODUCTION, CJSC Russia

Information update date: & nbsp2016-08-21

Illustrated instructions

Instructions

Ektalust® (Ektalust®)