Ectalust

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Ectalust: instructions for use and reviews

1. Release form and composition
2. Pharmacological properties
3. Indications for use
4. Contraindications
5. Method of application and dosage
6. Side effects
7. Overdose
8. Special instructions
9. Application during pregnancy and lactation
10. Use in childhood
11. In case of impaired renal function
12. For violations of liver function
13. Use in the elderly
14. Drug interactions
15. Analogs
16. Terms and conditions of storage
17. Terms of dispensing from pharmacies
18. Reviews
19. Price in pharmacies

Latin name: Ektalust

ATX code: R03DC03

Active ingredient: montelukast (Montelukast)

Producer: CJSC "Kanonfarma production" (Russia)

Description and photo update: 2019-08-07

Ectalust is a leukotriene receptor blocker, anti-inflammatory anti-bronchoconstrictor agent.

Release form and composition

Ectalust dosage forms:

film-coated tablets: round, convex on both sides, almost white or white; in cross section - from almost white to light yellow;
chewable tablets: round, convex on both sides, almost white or white.

In cardboard packs of 1, 2, 3 or 4 blister contour packages containing 7 tablets; 2–3 blister contour packages containing 10 tablets; 1–2 cell contour packages containing 14 tablets, as well as instructions for the use of Ectalust.

Composition of 1 film-coated tablet:

active substance: montelukast - 10 mg (in the form of montelukast sodium - 10.4 mg);
auxiliary components: mannitol, croscarmellose sodium, microcrystalline cellulose, povidone, calcium hydrogen phosphate, magnesium stearate, hydrogenated castor oil;
film sheath: White opadray, including titanium dioxide, hyprolose (hydroxypropyl cellulose), hypromellose (hydroxypropyl methyl cellulose), talc.

Composition of 1 chewable tablet:

active substance: montelukast - 4 or 5 mg (in the form of montelukast sodium, respectively 4.16 or 5.2 mg);
auxiliary components: salting (98% microcrystalline cellulose, 2% colloidal silicon dioxide), mannitol, aspartame, dextrates, magnesium stearate, strawberry flavor.

Pharmacological properties

Pharmacodynamics

Ectalust is an anti-bronchoconstrictor agent. As an active ingredient, it contains montelukast, a drug that has the ability to suppress bronchospasm caused by inhalation of LTD4 in very low doses. Bronchodilation persists for 2 hours after taking the drug. The action of montelukast supplements the bronchodilation effect caused by beta-agonists.

Ectalust suppresses the early and late phases of bronchospasm, which developed in response to antigen administration. Reduces the number of eosinophils in the peripheral blood and sputum contained in the respiratory tract. Improves the control of bronchial asthma. Significantly increases the morning forced expiratory volume in 1 second (FEV1) and the maximum expiratory volumetric velocity (MOBV). Significantly reduces the need for beta-adrenergic agonists.

The drug weakens well the bronchospasm that develops as a result of physical exertion. In patients with bronchial asthma, sensitive to acetylsalicylic acid and receiving inhaled glucocorticosteroids (GCS), montelukast enhances their effect and significantly improves control over the symptoms of the disease.

There is information about some anti-inflammatory effect of Ectalust.

Pharmacokinetics

The main pharmacokinetic characteristics of montelukast:

absorption and bioavailability: from the gastrointestinal tract, montelukast is absorbed quickly and almost completely. Bioavailability after taking 5 mg chewable tablets is 73% (with food intake it decreases to 63%), after taking 10 mg film-coated tablets - 64%. The bioavailability and maximum plasma concentration (Cmax) of the coated tablets are not affected by food. Cmax after taking the drug on an empty stomach at a dose of 4 and 5 mg is achieved after 2 hours, at a dose of 10 mg - 3 hours. In children, compared with adults taking the drug at a dose of 10 mg, the Cmax of montelukast is higher, and the average minimum concentration (Cmin) below;
distribution: the connection with plasma proteins is more than 99%. The volume of distribution is an average of 8-11 liters. In preclinical studies, minimal drug penetration through the blood-brain barrier has been established. 24 hours after taking Ectalust, its concentrations in all body tissues were minimal;
metabolism: montelukast is actively metabolized in the liver. After reaching the equilibrium state of the drug used in therapeutic doses, plasma metabolites in adults and children are not determined. The isoenzymes of cytochrome P ₄₅₀ CYP (3A4 and 2C9) are presumably involved in the metabolism of montelukast. In therapeutic doses, Ectalust does not inhibit such cytochrome P ₄₅₀ CYP isozymes as 1A2, 2D6, 2C19, 2A6, 2C9 and ZA4;
Excretion: in healthy adult volunteers, the clearance of montelukast averages 45 ml / min. Approximately 86% of the dose received orally is excreted in the feces within 5 days, less than 0.2% in the urine. This confirms the predominant route of excretion of montelukast and its metabolites in the bile. The half-life (T _1/2) in healthy adults is 2.7–5.5 hours.

When using doses of more than 50 mg, the pharmacokinetic parameters of montelukast remain almost linear.

Pharmacokinetics of Ectalust in special cases:

ethnicity: no clinically significant differences were found in patients of different races;
gender: in women and men, the pharmacokinetic characteristics of montelukast are similar;
age: when taking a dose of 10 mg once a day, the bioavailability and pharmacokinetic profile of montelukast in elderly patients are similar to those in the younger age group;
renal function: montelukast and its metabolites are not excreted by the kidneys, therefore, the pharmacokinetics of Ectalust have not been studied in patients with renal insufficiency. No dose adjustment is required;
liver function: with mild to moderate liver failure with clinical manifestations of cirrhosis, the metabolism of montelukast slows down, which is accompanied by an increase in the area under the concentration-time curve (AUC) by about 41% after a single dose of 10 mg. There was also a slight increase in the excretion of the drug from the body in these patients (up to 7.4 hours on average) compared with healthy volunteers. However, a change in the dose of Ectalust is not required. There are no data on the pharmacokinetics of montelukast in patients with severe hepatic insufficiency (on the Child-Pugh scale exceeding 9 points).

Indications for use

long-term treatment and prevention of bronchial asthma, including prevention of night and daytime symptoms of the disease;
prevention of exercise-induced bronchospasm;
treatment of aspirin asthma;
relief of day and night symptoms of seasonal / persistent allergic rhinitis.

Contraindications

In all dosage forms, Ectalust is contraindicated to take with known hypersensitivity to any of its components.

Film-coated tablets are not prescribed for children under 15 years of age.

Chewable tablets are contraindicated for phenylketonuria, as well as for children under 2 years old - at a dosage of 4 mg, for children under 6 years old - at a dosage of 5 mg.

During pregnancy and lactation, Ectalust is used only after a careful assessment of the benefits and risks.

Ectalusta, instructions for use: method and dosage

Film-coated tablets

Ectalust film-coated tablets should be taken orally 1 time per day, regardless of the time of meals.

When treating bronchial asthma, it is necessary to take pills in the evening, with allergic rhinitis - at any convenient time of the day.

Adults and adolescents from 15 years old are prescribed 1 tablet per day.

Chewable tablets

In the form of chewable tablets, Ectalust should be taken once a day, chewed, 2 hours before meals or 2 hours after meals.

Recommended doses depending on age:

children 2–5 years old: 1 tablet at a dose of 4 mg;
children and adolescents 6-14 years old: 1 tablet in a dose of 5 mg;
adolescents and adults over 15 years of age: it is recommended to use Ectalust in the form of film-coated tablets.

In the treatment of bronchial asthma, it is necessary to take the drug before bedtime, in case of allergic rhinitis - at any convenient time of the day.

General recommendations

The therapeutic effect of montelukast in relation to bronchial asthma symptoms appears during the first day. Treatment with Ectalust should be continued not only with an exacerbation of the disease, but also during its controlled course.

In bronchial asthma, Ectalust can be prescribed in addition to other types of treatment, including bronchodilators and inhaled glucocorticosteroids.

With mild and moderate impairment of hepatic function, renal failure and in old age, there is no need to adjust the dose of the drug.

Side effects

In general, Ectalust is well tolerated. The resulting side effects are usually mild and do not require discontinuation of the drug. The overall incidence of adverse events with montelukast is comparable to that with placebo.

Possible side reactions:

from the respiratory system: nosebleeds, rhinorrhea, sinusitis, pharyngitis, upper respiratory tract infections, cough;
from the side of the heart: palpitations;
from the immune system: hypersensitivity reactions, including anaphylaxis, in very rare cases - eosinophilic liver infiltration;
on the part of the circulatory and lymphatic systems: increased tendency to bleeding;
from the gastrointestinal tract: abdominal pain, nausea, dry mouth, dyspepsia, diarrhea, vomiting, pancreatitis;
from the central and peripheral nervous system: drowsiness, headache, dizziness, hyperkinesia, paresthesia / hypesthesia; very rarely - convulsions;
from the psyche: agitation, including aggressive behavior or hostility, disorientation, anxiety, hallucinations, pathological dreams, insomnia, somnambulism, anxiety, irritability, tremor, depression, suicidal thoughts and behavior (suicidality);
from the musculoskeletal system: arthralgia, myalgia, including muscle spasms;
from the hepatobiliary system: increased activity of hepatic transaminases in the blood (alanine aminotransferase and aspartate aminotransferase); very rarely - hepatitis (including cholestatic, hepatocellular and mixed liver damage);
on the part of the organ of hearing: otitis media (including medium);
on the part of the skin and subcutaneous tissues: rash, itching, urticaria, erythema nodosum, a tendency to hematoma formation, angioedema, erythema multiforme;
others: thirst, fatigue, edema, pyrexia; rarely in patients with bronchial asthma - Churg (Churg) - Strauss syndrome.

Overdose

In overdose studies, when patients with bronchial asthma were taken montelukast in daily doses of more than 200 mg for 22 weeks and in a daily dose of 900 mg for 1 week, no undesirable symptoms were detected. There are known cases of acute overdose in children who took the drug at a dose of at least 150 mg per day. The following reactions were most often noted: thirst, abdominal pain, drowsiness, hyperkinesis, mydriasis.

There are no data on the specific treatment of overdose. Therapy is symptomatic. There is no information on the effectiveness of peritoneal dialysis and hemodialysis for the elimination of montelukast.

special instructions

The efficacy of montelukast taken orally against acute attacks of bronchial asthma has not been established, therefore Ectalust is not recommended for use in relieving attacks. However, you should not stop taking it during an exacerbation.

Drug treatment should not replace oral or inhaled glucocorticosteroids. Ectalust enhances their effect, however, there is no data on the possibility of reducing the dose of oral GCS.

There are rare cases of development of systemic eosinophilia in patients with bronchial asthma, sometimes accompanied by clinical manifestations of Churge-Strauss syndrome and vasculitis. In this case, the purpose of the GCS is shown. There are no available ways to neither confirm nor deny the possible association of leukotriene receptor antagonists with the occurrence of eosinophilic granulomatosis with angiopathy. Physicians should consider the likelihood of developing eosinophilia, vascular rash, neuropathy, heart complications and / or an increase in pulmonary symptoms during therapy with montelukast. In the event of any of the listed side effects, a re-examination and revision of the therapeutic regimen are required.

Patients with an established allergy to acetylsalicylic acid and / or other non-steroidal anti-inflammatory drugs (NSAIDs) should not use these drugs during therapy with Ectalust. This is due to the fact that although montelukast improves respiratory function, it is not able to completely prevent bronchoconstriction caused by NSAIDs.

Chewable tablets contain aspartame (0.8 mg - in 4 mg tablets, 1 mg - in 5 mg tablets), which should be taken into account in patients with phenylketonuria.

Influence on the ability to drive vehicles and complex mechanisms

There is no data on the negative impact of montelukast on the ability to drive a car, work with complex mechanisms and perform functions that have potentially dangerous consequences. However, in some patients, the use of Ectalust causes drowsiness and dizziness, so it is recommended to be careful when doing activities that require a high speed of reactions and / or increased concentration.

Application during pregnancy and lactation

For pregnant and breastfeeding women, Ectalust is prescribed only if the doctor believes that the benefits of taking the drug are higher than the potential risks.

Pediatric use

Chewable tablets in a dosage of 4 mg are contraindicated in children under 2 years of age, in a dosage of 5 mg - up to 6 years.

Film-coated tablets should not be used by children and adolescents under 15 years of age.

With impaired renal function

The kidneys are not involved in the elimination of montelukast from the body, therefore, if the renal function is impaired, the dosage regimen does not need to be adjusted.

For violations of liver function

For patients with mild to moderate hepatic impairment, dose reduction of Ectalust is not required.

The pharmacokinetics of the drug in patients with severe hepatic insufficiency (on the Child-Pugh scale exceeding 9 points) has not been studied.

Use in the elderly

The bioavailability and pharmacokinetic profile of montelukast in the elderly are similar to those in young patients, so there is no need to adjust the treatment regimen with Ectalust.

Drug interactions

Ectalust can be used in combination with other drugs that are traditionally used for long-term treatment and prevention of bronchial asthma.

Montelukast complements the therapeutic effect of inhaled GCS. After stabilization of the condition, their dose can be reduced, however, gradually, under the close supervision of a physician. In some patients, Ectalust allows you to completely cancel GCS. Abrupt replacement of inhaled GCS with montelukast is not recommended.

Montelukast complements the therapeutic effect of inhaled bronchodilators. After stabilization of the condition, their dose can be gradually reduced.

Ectalust in the recommended clinical doses does not have a significant effect on the pharmacokinetics of the following drugs: prednisone, prednisone, theophylline, warfarin, digoxin, terfenadine, oral contraceptives (with a ratio of ethinylestradiol to norethindrone - 35 ÷ 1).

Increased caution should be observed, especially when treating children, in the case of concomitant use of drugs that induce the isoenzyme CYP3A4, such as rifampicin, phenobarbital, phenytoin. Phenobarbital reduces the AUC of montelukast by about 40%, but does not require dosage adjustment.

Montelukast, used in doses 20 and 60 times higher than recommended for adults, reduces the plasma concentration of theophylline taken simultaneously. However, when taking Ectalust in therapeutic doses (10 mg), this effect is absent.

In vitro studies have shown that montelukast is a potential CYP2C8 inhibitor. However, when studying the interaction with rosiglitazone (a preliminary substrate of a representative of drugs primarily metabolized by the CYP2C8 isoenzyme), it was found that montelukast does not suppress the CYP2C8 isoenzyme in vivo. Therefore, it cannot have a significant effect on the biotransformation of drugs that are metabolized with the participation of this enzyme (for example, rosiglitazone, repaglinide and paclitaxel).

Analogs

Ectalust's analogues are Glemont, Monax, Monkasta, Montelar, Montelukast, Singlon, Simplaer, Singular, etc.

Terms and conditions of storage

Keep out of the reach of children, protected from moisture and light, at a temperature not exceeding 25 ° C.

Shelf life is 2 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Ectalust

On specialized sites and forums, there are few reviews about Ectalust, but most of them are positive: the drug effectively eliminates bronchodilation and prevents the development of bronchospasm, does not cause adverse reactions, costs an order of magnitude cheaper than the popular analogue containing the same active ingredient.

Ectalust chewable tablets are mentioned separately. They have a pleasant taste, so children take them with pleasure.

Price for Ectalusta in pharmacies

Approximate prices for Ectalust (14 tablets per pack):

chewable tablets, 4 mg - 441-475 rubles;
chewable tablets, 5 mg - 473–560 rubles;
film-coated tablets, 10 mg - 575 rubles.

Maria Kulkes Medical journalist About the author

Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!