Almont pills 10mg, 28pcs

Composition

One tablet contains

the Active ingredient-montelukast sodium equivalent to 10 mg montelukast,

excipients: microcrystalline cellulose, lactose monohydrate, hydroxypropylcellulose, sodium croscarmellose, magnesium stearate.

shell composition:  Opadry Yellow (03B52874): hypromellose, macrogol, titanium dioxide (E 171), iron oxide red (E 172), iron oxide yellow (E 172).

Pharmacological action

Pharmacotherapy group

Medications for the treatment of obstructive airway diseases. Other medications for the treatment of obstructive airway diseases for systemic use. Leukotriene receptor antagonists. Montelukast

ATX code R03DC03

Pharmacological properties

Pharmacokinetics

Suction. Montelukast is rapidly absorbed after oral use. In adults, when taking film-coated tablets at a dose of 10 mg on an empty stomach, the average maximum concentration (Cmax) in blood plasma was reached 3 hours (Tmax) after taking the drug. The average oral bioavailability is 64%. Regular food intake did not affect oral bioavailability or Cmax. Safety and efficacy have been confirmed in clinical trials when using 10 mg film-coated tablets, regardless of food intake.

Distribution. Montelukast binds more than 99% to plasma proteins. The volume of distribution of montelukast in the equilibrium state is, on average,8-11 liters. Studies using radioactively labeled montelukast indicate a minimal distribution when penetrating the blood-brain barrier. In addition, concentrations of the radiolabeled substance 24 hours after the dose were minimal in all other tissues.

Metabolism. Montelukast is actively metabolized. At therapeutic doses, plasma concentrations of montelukast metabolites are below the limit of detection at steady state in adults and children. Montelukast is primarily metabolized by the cytochrome P450 2C8 system. CYP 3A4 and 2C9 have a small effect, although the pharmacokinetics of montelukast in healthy volunteers who received montelukast 10 mg 1 time/day did not change when itraconazole, which is a CYP3A4 inhibitor, was prescribed. Clinical studies of human liver microsomes in vitro have shown that therapeutic plasma concentrations of montelukast do not inhibit cytochromes P450 3A4,2C9,1A2,2A6,2C19 or 2D6. The role of metabolites in the therapeutic effect of montelukast is minimal.

Output. The average plasma clearance of montelukast in healthy adults is 45 ml / minute. After oral use of radioactively labeled montelukast,86% of the radioactivity is excreted in the faeces within 5 days and less than 0.2% in the urine, indicating that montelukast and its metabolites are almost completely excreted in the bile.

Features of pharmacokinetics in different groups of patients. There is no need to adjust the dose in elderly patients or in patients with mild to moderate hepatic impairment. Studies involving patients with impaired renal function have not been conducted. Since montelukast and its metabolites are excreted in the bile, it is not expected that a dose adjustment of montelukast will be necessary in patients with impaired renal function. There are no data on the pharmacokinetics of montelukast in patients with severe hepatic impairment (>9 on the Child-Pugh scale).

When using high doses of montelukast (20 and 60 times higher than the recommended dose for adults), a decrease in the concentration of theophylline in blood plasma was observed. This effect was not observed when using the drug at the recommended dose of 10 mg once a day.

Pharmacodynamics

Cysteine leukotrienes (LTC4, LTD4, LTE4) are inflammatory eicosanoids that are released from various cells, including mast cells and eosinophils. The effect of these pro-asthmatic mediators is carried out through cysteine leukotriene receptors (CysLTs) present in the human respiratory tract and is manifested by bronchospasm, mucus secretion, increased vascular permeability and an increase in the number of eosinophils. In allergic rhinitis, leukotrienes are released from the nasal mucosa after exposure to allergen, both in the early and late phases of reactions, and are associated with symptoms of allergic rhinitis. An intranasal test with XSLTs showed increased nasal airway resistance and symptoms of nasal congestion.

Montelukast is an active compound that competitively binds to CysLT1 receptors with high selectivity and chemical affinity. Clinical studies have shown that montelukast suppresses bronchospasm caused by LTD4 inhalation, even when administered at a dose of 5 mg and causes bronchodilation within 2 hours after oral use. Montelukast also has an additive effect on the effect of beta-agonists. Treatment with montelukast suppresses bronchospasm at both early and late stages, reducing the response to antigens. Treatment with montelukast significantly reduces the number of eosinophils in the respiratory tract (confirmed by sputum analysis) and in the peripheral blood, improving control over the clinical course of bronchial asthma.

Indications

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

• prevention of daytime and nighttime symptoms of the disease (for children 2 years and older);
• treatment of bronchial asthma in patients with hypersensitivity to acetylsalicylic acid (for children 6 years and older);
• prevention of exercise-induced bronchospasm (for children 2 years and older).

Relief of symptoms of seasonal and year-round allergic rhinitis in children from 2 years of age.

Use during 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 to discontinue breastfeeding for the duration of Almont use is made based on an assessment of the intended benefit to the mother and the potential risk to the child.

Contraindications

• Hypersensitivity 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 of age (for a dosage of 5 mg);
• patients with rare hereditary diseases: galactose intolerance, lactase deficiency or glucose-galactose malabsorption;
• phenylketonuria (contains aspartame).

Side effects

Side effects are divided into groups with the following frequency of occurrence: very common (≥ 1/10), common (≥ 1/100, < 1/10), uncommon (≥ 1/1000, < 1/100), rare (≥ 1/10000, < 1/1000), very rare (

Common (≥1/100, < 1/10)

• headache

• abdominal pain

Post-marketing data

Very common (≥ 1/10)

• upper respiratory tract infections*

Common (≥1/100, < 1/10)

• diarrhea**, nausea**, vomiting* *

• Rash* *

• Elevated transaminase (ALT and AST)levels

• pyrexia*

Infrequently (≥ 1/1000,

• hypersensitivity reactions, including anaphylaxis

• abnormal dreams, including nightmares, insomnia, somnambulism, stimulation, agitation, including aggression and hostility, depression, psychomotor hyperactivity, including irritability, anxiety, tremor***

• dizziness, drowsiness, paraesthesia/hypoesthesia, seizures,

• nosebleeds

• , dry mouth, dyspepsia

• • bruises, hives, itching,

• arthralgia, myalgia including muscle cramps,

• asthenia/fatigue, edema

• enuresis in children

Rarely (≥ 1/10000,

• tendency to bleed

• impaired concentration, memory disorders, tic

• palpitation

• angioedema

Very rare (

• eosinophilic liver infiltrates

• hallucinations, disorientation, suicidal intentions and behavior (including suicide attempts)

• Churge-Strauss syndrome

• hepatitis, including cholestatic, hepatocellular and mixed-origin liver lesions

• erythema multiforme, erythema nodosum

• thrombocytopenia

* These adverse events were “very common” in both montelukast-treated patients and placebo-treated patients in clinical trials.

* * These adverse events were “common” in both montelukast-treated patients and placebo-treated patients in clinical trials.

*** It occurred with a frequency of “rarely”.

Interaction

Montelukast can be used with other medications that are commonly used for the prevention and long-term treatment of asthma. In drug interaction studies, the recommended clinical dose of montelukast did not have a clinically significant effect on the pharmacokinetics of the following medications: theophylline, prednisone, prednisone, oral contraceptives (ethinyl estradiol/norethindrone 35/1), terfenadine, digoxin, and warfarin.

The area under the plasma concentration curve (AUC) of montelukast decreased by approximately 40% in patients who used phenobarbital concomitantly. Since montelukast is metabolized by CYP 3A4,2C8 and 2C9, montelukast should be administered with caution, especially in children, simultaneously with inducers of CYP 3A4,2C8 and 2C9, such as phenytoin, phenobarbital and rifampicin.

In vitro studies have shown that montelukast is a strong inhibitor of CYP 2C8. However, data from clinical drug interaction studies that examined the use of montelukast and rosiglitazone (a marker substrate representative of drugs primarily metabolized by CYP 2C8) demonstrated that montelukast does not inhibit CYP 2C8 in vivo. Therefore, montelukast is not expected to significantly affect the metabolism of drugs that are metabolized by this enzyme (for example, paclitaxel, rosiglitazone and repaglinide).

Laboratory studies have shown that montelukast is a substrate for CYP 2C8, and to a lesser extent for 2C9 and 3A4. Data from drug interaction studies involving montelukast and gemfibrozil (an inhibitor of both CYP 2C8 and 2C9) showed that gemfibrozil increased the systemic sensitization of montelukast by 4.4 times. No dose adjustment is required for montelukast when it is co-administered with gemfibrozil or other potential CYP 2C8 inhibitors, but physicians should be aware of the possibility of increased adverse reactions. Clinically important drug interactions with other known CYP 2C8 inhibitors (for example, trimethoprim) are not expected. In addition, concomitant use of montelukast only with itraconazole, which is a strong CYP3A4 inhibitor, did not significantly increase the systemic sensitization of montelukast.

How to take, course of use and dosage

For patients with asthma or with asthma and concomitant seasonal allergic rhinitis aged 15 years and older, the dose is 10 mg per day (1 tablet), in the evening.

General recommendations. The therapeutic effect of Almont 10 on the indicators of bronchial asthma control develops within 1 day. Patients should be advised to continue taking Almont 10 even if asthma control is achieved, as well as during periods of worsening asthma. The drug should not be taken simultaneously with other drugs containing-montelukast.

No dose adjustment is necessary for patients with renal or hepatic impairment of mild to moderate severity. There are no data on patients with severe hepatic impairment. The dosage is the same for males and females.

Almont 10 as an alternative treatment method instead of low-dose inhaled corticosteroids for persistent mild asthma. Almont 10 is not recommended as monotherapy for patients with moderate persistent asthma.

Treatment with Almont 10 depends on other asthma treatments. Almont 10 can be used as an adjunct therapy in patients in whom the use of inhaled corticosteroids and short-acting beta-agonists, if necessary, does not provide sufficient clinical control of asthma. Inhaled corticosteroids should not be abruptly replaced with Almont 10.

Overdose

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

There have been reports of acute overdose of montelukast (when taking at least 1 g per day) in the post-marketing 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: performing symptomatic therapy.

Special instructions

Patients should be aware that montelukast for oral use is never used to treat acute asthma attacks, and that they should always have the appropriate emergency medication with them. In an acute attack, short-acting inhaled beta-agonists should be used. Patients should consult a doctor as soon as possible if they need more of a short-acting beta-agonist than usual.

Montelukast should not abruptly replace inhaled or oral corticosteroids.

There are no data confirming that the dose of oral corticosteroids can be reduced with simultaneous use of montelukast.

In rare cases, patients treated with anti-asthmatic medications, including Almont 10, may experience systemic eosinophilia, sometimes with clinical manifestations of vasculitis characteristic of Churge–Strauss syndrome (a condition that is often treated with systemic corticosteroids). Sometimes these cases are associated with the withdrawal or reduction of the dose of oral corticosteroids. A link between treatment with leukotriene receptor antagonists and the occurrence of Churge-Strauss syndrome cannot be excluded or confirmed. However, if symptoms such as eosinophilia, vascular rash, worsening of pulmonary symptoms, cardiac complications, and/or neuropathy occur, additional evaluation and review of treatment strategies are necessary.

Treatment with montelukast does not allow patients with aspirin-sensitive asthma to take aspirin or other non-steroidal anti-inflammatory drugs.

Neuropsychiatric disorders. Mental disorders were reported in adults, adolescents, and children taking Almont 10. Mental disorders included such side effects as: agitation, aggressive behavior, hostility, anxiety, depression, disorientation, impaired concentration, abnormal dreams, hallucinations, insomnia, irritability, memory disorders, anxiety, somnambulism, suicidal thoughts and attempts (including suicide), and tremor. Data from post-marketing reports are comparable to clinical data obtained during drug therapy. Patients and healthcare professionals should be aware of the possibility of such events occurring. Patients are advised to notify their healthcare provider if these side effects occur. The benefit / risk ratio should be evaluated for continuing therapy with Almont 10 if these side effects occur.

Pregnancy and lactation

Pregnancy: The limited information available in the pregnancy database does not indicate a causal relationship between the use of Almont 10 and the occurrence of malformations (such as limb defects), which have rarely been reported in the global post-marketing experience.

Lactation period: it is not known whether montelukast passes into breast milk.

Features of the drug’s effect on the ability to drive a vehicle or potentially dangerous mechanisms

Montelukast is not expected to affect the patient’s ability to drive vehicles or mechanisms. However, in rare cases, drowsiness or dizziness have been reported, and caution should be exercised when driving vehicles or potentially dangerous machinery.

Storage conditions

At a temperature not exceeding 30°C, in the original packaging. Keep out of reach of children!

Shelf

life is 3 years.

Active ingredient

Montelukast

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

Children prescribed by a doctor, Children over 15 years of age, Adults prescribed by a doctor

Indications

Bronchospasm, Runny Nose, Bronchial asthma