Almonte - instructions for use, dose, side effects, contraindications

Excipients: mannitol 160.96 mg, microcrystalline cellulose 52.80 mg, giprolose 7.20 mg, croscarmellose sodium 7.20 mg, dye Pigment Blend PB-24880 (lactose monohydrate 3.60 mg, ferric iron oxide red 0.40 mg) 4.00 mg, magnesium stearate 2.40 mg, aspartame 1.20 mg, cherry flavor (Silarom Cherry Flavor 1219813182) 0.08 mg;

1 tablet chewing 5 mg contains:

active substance: montelukast 5.00 mg (in the form of sodium montelukast 5,20 mg);

Excipients: Mannitol 201.20 mg, microcrystalline cellulose 66.00 mg, giprolose 9.00 mg, croscarmellose sodium 9.00 mg, dye Pigment Blend RV-24880 (lactose monohydrate 4.50 mg, iron oxide red dye 0.50 mg) 5.00 mg, magnesium stearate 3.00 mg, aspartame 1.50 mg, cherry flavoringSilarom Cherry Flavor 1219813182) 0.10 mg.

Description:

Tablets 4 mg:

Oval, biconvex tablets are pink in color with interspersed and engraved "M4" on one side.

Tablets 5 mg:

Round, biconvex tablets are pink in color with interspersed and engraved "M5" on one side.

Pharmacotherapeutic group:Anti-inflammatory anti-bronchoconstrictive agent - leukotriene receptor blocker

ATX: & nbsp

R.03.D.C.03 Montelukast

Pharmacodynamics:

Cysteinyl-leukotrienes (LTC₄, LTD₄, LTE₄) are strong pro-inflammatory eicosanoids that are released from different cells, including mast cells and eosinophils. These important proastmatic mediators are associated with cysteinyl-leukotriene receptors (CysLT), present in the respiratory tract of a person and responsible for the reaction of bronchospasm, sputum excretion, permeability of vessels and an increase in the number of eosinophils.

Montelukast is an oral active compound that has a high affinity and selectivity to CysLT₁receptors. Montelukast in a dose of less than 5 mg, heals bronchospasm induced by inhalation LTD₄. Bronchodilator effect is observed within 2 hours after oral administration. Bronchodilator effect of beta₂-adrenomimetics is enhanced when taking montelukast. Montelukast Suppresses both early and late stages of bronchospasm caused by the action of antigens. Montelukast reduces the number of eosinophils in peripheral blood in adults and children, and significantly reduces the number of eosinophils in the airways. In patients with hypersensitivity to acetylsalicylic acid receiving inhaled and / or oral glucocorticosteroids (GCS), the addition to therapy of montelukast provides better control of the disease.

Pharmacokinetics:

Suction

After oral administration montelukast quickly and almost completely absorbed. In adult patients, after taking chewable tablets at a dose of 5 mg on an empty stomach, the maximum concentration in the blood plasma (C_mOh) is achieved after 2 hours. The average bioavailability is 73%, this value is reduced to 63% when taking Montelukast with food. After taking chewable tablets at a dose of 4 mg fasting in patients aged 2 to 5 years, C_mOh is achieved in 2 hours. The average value of C_mOh in this group of patients is 66% higher, and the average value of C_mOh below the similar value in adults with the use of film-coated tablets at a dose of 10 mg.

Distribution

The binding of montelukast to plasma proteins is more than 99%. The volume of distribution in the equilibrium state averages 8-11 liters. Preclinical studies have revealed minimal penetration of montelukast through the blood-brain barrier. After 24 hours after administration, the concentration of montelukast is also minimal in other tissues.

Metabolism

Montelukast is actively metabolized in the liver. When used in therapeutic doses, the concentration of metabolites of Montelukast in blood plasma in an equilibrium state in adults and children is not determined.

In vitro studies have shown that cytochrome P450 isoenzymes (3A4, 2A6 and 2C9) are involved in the metabolism of montelukast, while at therapeutic concentrations montelukast does not inhibit cytochrome P450 isoenzymes: 3A4, 2C9, 1A2, 2A6, 2C19 and 2D6. Metabolites have a slight therapeutic effect of Montelukast.

Excretion

The half-life of montelukast in young healthy adult volunteers ranges from 2.7 to 5.5 hours. The plasma clearance of montelukast in healthy adult volunteers averages 45 ml / min. After oral administration of montelukast, 86% of the total is excreted through the intestine for 5 days and less than 0.2% through the kidneys,that along with data on its bioavailability confirms the excretion of montelukast and its metabolites mainly with bile.

Pharmacokinetics in special cases

Pharmacokinetics of Montelukast in women and men is the same.

Patients old age or patients with hepatic insufficiency of mild and moderate severity no correction of the dosage regimen of Montelukast is required.

Pharmacokinetics of Montelukast in patients with renal insufficiency not evaluated. Because the montelukast and its metabolites are not excreted by the kidneys, dose adjustment in this category of patients is not required.

Data on the character of the pharmacokinetics of Montelukast in patients with severe impairment of liver function (more than 9 on the Child-Pugh scale).

When receiving high doses of montelukast (20 and 60 times higher than recommended doses for adults), a decrease in the concentration of theophylline in the blood plasma is observed. When taking montelukast in the recommended doses of 10 mg 1 time per day, this effect is not observed.

Indications:

Prophylaxis and long-term treatment of bronchial asthma in children, including:

prevention of day and night symptoms of the disease (for children from 2 years old and older);
treatment of bronchial asthma in patients with hypersensitivity to acetylsalicylic acid (for children 6 years and older);
prevention of bronchospasm caused by physical exertion (for children from 2 years old and older).

Relief of seasonal and allergic rhinitis symptoms in children from 2 years.

Contraindications:

- Dand sensitivity to the active or any auxiliary substance of the drug;

- Children under 2 years of age (for a dosage of 4 mg) and up to 6 years (for a dosage of 5 mg);

- patients with rare hereditary diseases: galactose intolerance, lactase deficiency or glucose-galactose malabsorption;

- phenylketonuria (contains aspartame).

Pregnancy and lactation:

The use of ALMONT during pregnancy is possible if the intended benefit to the mother exceeds the potential risk to the fetus.

The decision on the abolition of breastfeeding for the period of application of ALMONT is made on the basis of an assessment of the prospective benefit to the mother and the potential risk to the child.

Dosing and Administration:

Inside, the tablet should be chewed.

Admission of the drug by children is carried out under the supervision of adults.

The drug ALMONT should be taken 1 hour before or 2 hours after meals.

With bronchial asthma or bronchial asthma and allergic rhinitis:

For children aged 2 to 6 years - 1 chewable tablet at a dose of 4 mg once a day in the evening.

For children aged 6 to 14 years - 1 chewable tablet in a dose of 5 mg once a day in the evening.

With allergic rhinitis:

For children aged 2 to 6 years - 1 chewable tablet in a dose of 4 mg once a day and for children aged 6 to 14 years - 1 chewable tablet in a dose of 5 mg once a day in an individual mode, depending on the time of the most acute exacerbation of symptoms.

There is no need for dose adjustment within these age groups.

General recommendations

The therapeutic effect of ALMONT, which allows controlling the symptoms of asthma, is reached within 24 hours after taking. The patient is recommended to continue taking the drug both during periods of controlled course of bronchial asthma, and during the exacerbation of bronchial asthma.

Patients with renal insufficiency and patients with hepatic insufficiency light and moderate severity special selection of the dose is not required. No dosage adjustment is required depending on the sex patient.

There is no data on the use of montelukast in patients with severe impairment of liver function.

For treatment of patients of other age groups, another dosage form is available and the dose of the drug is 10 mg tablet coated with a film membrane.

Side effects:

Infectious and parasitic diseases: infections of the upper respiratory tract.

Violations of the blood and lymphatic system: increased tendency to bleeding, thrombocytopenia.

Immune system disorders: hypersensitivity reactions, including anaphylaxis, eosinophilic liver infiltration.

Disorders of the psyche: pathological dreams, including nightmares; hallucinations, insomnia, somnambulism, irritability, anxiety, anxiety; agitation, including aggressive behavior or hostility; tremor, depression, disorientation, suicidal thoughts and behavior (suicidal).

Disturbances from the nervous system: headache, dizziness, drowsiness, paresthesia / hypesthesia, convulsions.

Heart Disease: a feeling of palpitations.

Disturbances from the respiratory system, chest and mediastinal organs: nose bleed.

Disorders from the gastrointestinal tract: diarrhea, dry mouth, dyspepsia, nausea, vomiting, abdominal pain, pancreatitis.

Disorders from the liver and bile ducts: an increase in the activity of alanine aminotransferase and aspartate aminotransferase, hepatitis (including cholestatic, hepatocellular and mixed liver damage).

Disturbances from the skin and subcutaneous tissues: angioedema, an incidence of hematomas, hives, itching, rash, erythema nodosum, erythema multiforme.

Disturbances of musculoskeletal and connective tissue: arthralgia, myalgia, including muscle cramps.

General disorders and disorders at the site of administration: asthenia / fatigue, malaise, swelling, pyrexia, thirst.

In very rare cases, during the treatment with montelukast, the development of the Chard-Strauss syndrome was reported (see "Special instructions").

Overdose:

Symptoms overdose of the drug in patients with chronic bronchial asthma when administered at a dose exceeding 200 mg per day for 22 weeks and at a dose of 900 mg per day for 1 week has not been identified.

There are reports of acute overdose of montelukast (when taking at least 1 g per day) in the postmarketing period and in clinical studies in adults and children. Clinical and laboratory data indicate that the safety profile of the drug is consistent in children, adults and elderly patients. The most common symptoms were thirst, drowsiness, vomiting, psychomotor agitation, headache and abdominal pain.

Treatment: symptomatic therapy.

Data on the possibility of removing montelukast through peritoneal dialysis or hemodialysis are absent.

Interaction:

In patients who simultaneously received phenobarbital, the area under the pharmacokinetic concentration-time curve of montelukast decreased by about 40%, however, correction of the dosing regimen in such patients is not required. Because the montelukast is metabolized by isoenzyme CYP3A4, care should be taken, especially in children, if montelukast simultaneously applied with isoenzyme inducers CYP3A4, such as phenytoin, phenobarbital and rifampicin.

Montelukast can be prescribed together with other drugs traditionally used for the prevention and long-term treatment of bronchial asthma and / or allergic rhinitis.

Montelukast at the recommended therapeutic dose did not have a clinically significant effect on the pharmacokinetics of the following drugs: theophylline, prednisone, prednisolone, oral contraceptives (ethinyl estradiol / norethynodrel 35/1), terfenadine, digoxin and warfarin.

In studies in vitro determined that montelukast is a strong inhibitor of isoenzyme CYP2C8. However, in the study of drug interactions in vivo Montelukast and rosiglitazone (a marker substrate, a representative of preparations primarily metabolized by an isoenzyme CYP2C8) no confirmation of the inhibition of isoenzyme by montelukast CYP2C8. Thus, in clinical practice, the effect of montelukast on CUR2C8-mediated metabolism of a number of medications is not expected, including. paclitaxel, rosiglitazone, repaglinide.

Research in vitro showed that montelukast is a substrate of isoenzyme CYP2C8, and to a lesser extent isoenzymes CYP2C9 and 3A4. Data from the clinical trial of drug interaction for montelukast and gemfibrozil (an inhibitor of both CYP2C8, and 2C9) demonstrate that gemfibrozil increases the effect of systemic exposure of Montelukast 4.4 times. Joint use of itraconazole, a strong inhibitor of isoenzyme CYP3A4, together with gemfibrozil and montelukast did not lead to an additional increase in the effect of systemic effects of montelukast. The effect of gemfibrozil on the systemic effect of montelukast can not be considered clinically significant on the basis of safety data when administered at doses exceeding the approved dose of 10 mg for adult patients (eg 200 mg / day for adult patients for 22 weeks and up to 900 mg / day for patients taking the drug for about one week did not have clinically significant adverse effects). Thus, when combined with gemfibrozilom dose adjustment montelukast is not required. Based on research results in vitro, no clinically significant drug interactions with other known isozyme inhibitors CYP2C8 (for example, with trimethoprim).In addition, the joint administration of montelukast with itraconazole alone did not result in a significant increase in the effect of systemic exposure to montelukast.

Combined treatment with bronchodilators

The drug ALMONT is a justified addition to monotherapy with bronchodilators if the latter do not provide adequate control of bronchial asthma. When the therapeutic effect is achieved from ALMONT treatment, a gradual decrease in the dose of bronchodilators can be started.

Combined treatment with inhaled glucocorticosteroids

Treatment with ALMONT provides an additional therapeutic effect to patients who use inhaled GCS. Once the stabilization of the condition is achieved, it is possible to begin a gradual reduction in the dose of GCS under the supervision of a physician. In some cases, complete cancellation of inhaled glucocorticosteroids is permissible, but a sharp replacement of inhaled glucocorticosteroids by ALMONT is not recommended.

Special instructions:

The drug ALMONT is not recommended for the treatment of acute attacks of bronchial asthma. Patients with bronchial asthma should always have emergency medications.When an acute attack occurs, inhalation beta should be used₂-adrenomimetiki short-acting. Patients should consult their doctor as soon as possible if they need more inhalation of beta₂-adrenomimetics short-acting than usual.

Do not abruptly replace the drug ALMONT therapy with inhalation or oral GCS. There are no data proving the possibility of reducing the dose of oral GCS against the background of simultaneous administration of montelukast.

In rare cases, patients who receive anti-asthma drugs, including montelukast, systemic eosinophilia may develop, which is sometimes accompanied by clinical signs of vasculitis, the so-called Chard-Strauss syndrome, a condition that is eliminated by the use of systemic SCS. These cases, as a rule, are associated with a decrease in dose or cancellation of oral corticosteroids. It is impossible to exclude or establish the possibility that leukotriene receptor antagonists may be associated with the development of the Chard-Strauss syndrome. Therefore, doctors should be warned about the possibility of eosinophilia, vascular rash, increased pulmonary symptoms, heart complications and / or neuropathy in patients.Patients who developed the above symptoms, it is necessary to undergo a second examination, and the scheme of their treatment should be reviewed.

Treatment with ALMONT does not lead to the prevention of bronchospasm in patients with hypersensitivity to acetylsalicylic acid with acetylsalicylic acid and other non-steroidal anti-inflammatory drugs.

The ALMONT preparation contains aspartame, a source of phenylalanine. This drug may cause harm to patients with phenylketonuria.

The drug contains lactose monohydrate and should not be taken to patients with rare hereditary diseases: galactose intolerance, lactase deficiency or glucose-galactose malabsorption.

Effect on the ability to drive transp. cf. and fur:

Usually, montelukast does not affect the ability to drive vehicles or work with other mechanisms, but very rarely some patients reported drowsiness and dizziness, when these signs appear, patients are not recommended to drive vehicles and engage in other activities requiring concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Tablets are chewable, 4 mg, 5 mg.

Packaging:

Tablets 4 mg: For 10 or 14 tablets in Al / Al blister. For 3 blisters (10 tablets), 2 or 7 blisters (14 tablets each) in a cardboard box, along with instructions for medical use.

Tablets 5 mg: For 10 or 7 tablets in Al / Al blister. For 3 blisters (10 tablets), for 4 or 14 blisters (7 tablets) in a cardboard box, along with instructions for medical use.

Storage conditions:At temperatures not higher than 30 ° C, in the original packaging.

Keep out of the reach of children!

Shelf life:

3 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002407

Date of registration:21.03.2014 / 05.04.2017

Expiration Date:21.03.2019

The owner of the registration certificate:Actavis PTS ehf GroupActavis PTS ehf Group Iceland

Manufacturer: & nbsp

ACTAVIS, Ltd. Iceland

Representation: & nbspAktavis, Open Company Aktavis, Open Company

Information update date: & nbsp12.07.2017

Illustrated instructions

Instructions

Almonte (Almont)