Almont chewable pills 4 mg №98

Mechanism of action

Antagonist of leukotriene receptors. Cysteinyl leukotrienes (LTC₄, LTD₄LTE₄) - strong pro-inflammatory eicosanoids that are released from various cells, including mast cells and eosinophils. These important prostatic mediators bind to cysteinyl-leukotriene receptors (CysLT) present in the human respiratory tract and are responsible for the reaction of bronchospasm, sputum production, vascular permeability and an increase in the number of eosinophils.

Montelukast is an orally-active compound that has high affinity and selectivity for CysLT₁-receptors. montelukast in a dose of less than 5 mg suppresses bronchospasm induced by inhalation LTD₄. Bronchodilating effect is observed within 2 hours after oral administration. Bronchodilating effect beta₂-adrenomimetikov increases when taking montelukast. Montelukast suppresses both the early and late stages of bronchospasm caused by exposure to antigens. Montelukast reduces the number of eosinophils in peripheral blood in adults and children, and also significantly reduces the number of eosinophils in the airways. In patients with hypersensitivity to Acetylsalicylic acid, receiving inhalation and / or oral GCS,addition to montelukast therapy provides better disease control.

Pharmacokinetics

Suction

After oral administration, montelukast is rapidly and almost completely absorbed. In adult patients after taking chewable pills at a dose of 5 mg on an empty stomach._max in blood plasma is reached after 2 hours. The average bioavailability value is 73%, this value is reduced to 63% when taking montelukast with food. After taking chewable pills in a dose of 4 mg on an empty stomach in patients aged 2 to 5 years_maxis reached in 2 hours. Average value_max this group of patients is 66% higher and the average C_minlower than in adults when taking film-pills at a dose of 10 mg. In adult patients after taking fasting film-pills at a dose of 10 mg, the mean value of C_max in blood plasma is reached after 3 hours. The average bioavailability value is 64%; when taken orally with food bioavailability and C_max not violated.

Distribution

Binding of montelukast to plasma proteins is more than 99%. V_din equilibrium, the average is 8-11 liters. Preclinical studies have revealed a minimal penetration of Montelukast through the BBB. 24 h after administration, the concentration of montelukast is minimal in other tissues.

Metabolism

Montelukast is actively metabolized in the liver. When used in therapeutic doses C_ssmontelukast metabolites in plasma 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 in therapeutic concentrations montelukast does not inhibit the isoenzymes of cytochrome P450: 3A4, 2C9, 1A2, 2A6, 2C19 and 2D6. Metabolites have a slight therapeutic effect of montelukast.

Removal

T_1/2 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 amount is excreted through the intestine within 5 days and less than 0.2% by the kidneys, which, along with data on its bioavailability, confirms the excretion of montelukast and its metabolites mainly with bile.

Pharmacokinetics in special clinical situations

The pharmacokinetics of montelukast in women and men are the same.

Elderly patients or patients with mild to moderate hepatic insufficiency do not require correction of the montelukast dosing regimen.

The pharmacokinetics of montelukast in patients with renal insufficiency was not evaluated. Since montelukast and its metabolites are not excreted by the kidneys, dose adjustment is not required in this category of patients. There are no data on the nature of the pharmacokinetics of montelukast in patients with severely impaired liver function (more than 9 points on the Child-Pugh scale).

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

Indications

Prevention and long-term treatment of asthma, including:

- prevention of day and night symptoms of the disease in children aged 2 years and older (for chewable pills 4 mg and 5 mg) and in adults and adolescents from 15 years old (for film-coated tablets, 10 mg);

- treatment of bronchial asthma in children aged 6 years and older (for chewable pills 4 mg and 5 mg) and in adults and adolescents from 15 years old (for film-coated tablets, 10 mg) with hypersensitivity to acetylsalicylic acid;

- prevention of bronchospasm caused by physical activity in children aged 2 years and older (for chewable pills 4 mg and 5 mg) and in adults and adolescents from 15 years old (for film-coated tablets, 10 mg).

Relieving the symptoms of seasonal and year-round allergic rhinitis in children aged 2 years and older (for chewable pills 4 mg and 5 mg) and in adults and adolescents from 15 years old (for film-coated tablets, 10 mg).

Dosing regimen

The drug is taken orally.

Chewable pills are taken 1 hour before or 2 hours after meals; pill should be chewed.

Tablets, film-coated, are taken orally, regardless of the meal, without chewing, with a sufficient amount of liquid.

Adults and teenagers from 15 years appoint 10 mg (1 tablet, film-coated) 1 time / day.

Atbronchial asthma or bronchial asthma and allergic rhinitis children aged 2 to 6 years appoint 1 chewable pill 4 mg 1 time / day in the evening;children aged 6 to 14 years - 1 chewable pill 5 mg 1 time per day in the evening.

Atallergic rhinitis children aged 2 to 6 years appoint 1 chewable pill 4 mg 1 time / day,children aged 6 to 14 years- 1 chewable pill 5 mg 1 time / day in an individual mode, depending on the time of the greatest exacerbation of symptoms.

No dose adjustment is required within these age groups.

Children take the drug under the supervision of adults.

The therapeutic effect of the drug Almont, which allows to control the symptoms of asthma, is achieved within a day after taking it. The patient is recommended to continue taking the drug, both during periods of controlled flow of asthma, and in the period of exacerbation of bronchial asthma.

Patients with renal failure and patients with mild to moderate hepatic insufficiency no special dose selection is required. There is no data on the use of montelukast in patients withsevere abnormal liver function.

Elderly patients dose adjustment is not required.

No dose adjustment required depending on the gender of the patient.

Side effect

Infection:upper respiratory tract infection.

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

Immune system: hypersensitivity reactions, incl. anaphylaxis, eosinophilic infiltration of the liver.

From 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 (suicidality).

Nervous system:headache, dizziness, drowsiness, paresthesia / hypesthesia, convulsions.

Cardiovascular:feeling of heartbeat.

On the part of the respiratory system:nose bleed.

From the digestive tract:diarrhea, dry mouth, dyspepsia, nausea, vomiting, abdominal pain, pancreatitis.

Liver and biliary tract:increased activity of ALT and AST, hepatitis (including cholestatic, hepatocellular and mixed liver damage).

Skin and Subcutaneous Tissues:angioedema, tendency to hematomas, urticaria, pruritus, rash, erythema nodosum, erythema multiforme.

From the musculoskeletal system:arthralgia, myalgia, including muscle cramps.

Other: asthenia / fatigue, malaise, edema, pyrexia, thirst; in very rare cases during treatment with montelukast, the development of Churg-Strauss syndrome has been reported.

Contraindications

- hypersensitivity to the active substance or any auxiliary component of the drug;

- children's age up to 2 years (for chewable pills 4 mg);

- children's age up to 6 years (for chewable pills 5 mg);

- children's age up to 15 years (for pills of 10 mg);

- rare hereditary diseases such as galactose intolerance, lactase deficiency or glucose-galactose malabsorption;

- Phenylketonuria (for chewable tablets), because pills contain aspartame.

Use during pregnancy and lactation

The use of the drug Almont during pregnancy is possible if the intended benefit to the mother outweighs the potential risk to the fetus.

The decision to cancel breastfeeding for the period of use of the drug Almont is made on the basis of an assessment of the intended benefits to the mother and the potential risk to the child.

Application for violations of the liver

Patients with mild-to-moderate hepatic insufficiencyno special dose selection is required. There is no data on the use of montelukast in patients withsevere abnormal liver function.

Application for violations of kidney function

Patients with renal failureno special dose selection is required.

Use in children

The drug is contraindicated in children under 2 years of age (for a dosage of 4 mg), children under 6 years of age (for a dosage of 5 mg), children and adolescents under 15 years of age (for pills of 10 mg).

Use in elderly patients

Elderly patients dose adjustment is not required.

special instructions

Almont is not recommended for treatment of acute attacks of asthma. Patients with bronchial asthma are advised to always carry emergency medications with them. In the event of an acute attack, inhalation beta should be used.₂- short acting adrenomimetics. Patients should consult their doctor as soon as possible if they need more inhalations of beta.₂-adrenomimetic short-acting than usual.

Do not abruptly replace the drug Almont therapy inhaled or oral GCS. There are no data proving the possibility of reducing the dose of oral corticosteroids against the background of simultaneous montelukast.

In rare cases, patients who receive anti-asthma drugs, including montelukast, can develop systemic eosinophilia, which is sometimes accompanied by clinical signs of vasculitis, the so-called Churg-Strauss syndrome, a condition that is eliminated by taking systemic corticosteroids. These cases are usually associated with dose reduction or cancellation of therapy with oral corticosteroids. It is impossible to exclude or establish the likelihood that leukotriene receptor antagonists may be associated with the development of Churg-Strauss syndrome. Therefore, physicians should be warned about the possibility of eosinophilia, vascular rash, increased severity of pulmonary symptoms, cardiac complications and / or neuropathy in patients.Patients who have developed the aforementioned symptoms need to undergo a re-examination, and their treatment regimen should be reviewed. Almont treatment does not lead to the prevention of the development of bronchospasm in patients with hypersensitivity to acetylsalicylic acid when using acetylsalicylic acid and other NSAIDs .

The drug Almont in the form of chewable pills 4 mg and 5 mg contains aspartame - a source of phenylalanine. This drug may be harmful to patients with phenylketonuria.

Almont contains lactose monohydrate, so you should not take the drug in patients with rare hereditary diseases, such as galactose intolerance, lactase deficiency or glucose-galactose malabsorption.

Influence on ability to drive motor transport and control mechanisms

As a rule, Montelukast does not affect the ability to drive vehicles or work with other mechanisms, but very rarely drowsiness and dizziness were noted in some patients. With the appearance of these signs, patients are not recommended to drive vehicles and engage in other activities that require concentration of attention and quickness of psychomotor reactions.

Overdose

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

There are reports of acute overdose of montelukast (when taking at least 1 g / day) in the post-marketing period and in clinical studies in adults and children. Clinical and laboratory data testify to the compliance of the safety profile of the drug in children, adults and elderly patients. The most frequent symptoms were thirst, drowsiness, vomiting, agitation, headache and abdominal pain.

Treatment:conducting symptomatic therapy. Data on the possibility of removal of montelukast by peritoneal dialysis or hemodialysis are not available.

Drug interaction