Almont Chewable tablets 5mg, 98pcs

Composition

Active ingredient:

montelukast 5.00 mg (as montelukast sodium 5.20 mg);

excipients:

mannitol 201,20 mg,

microcrystalline cellulose of 66.00 mg

of hyprolose of 9.00 mg,

croscarmellose sodium 9,00 mg,

dye Pigment Blend PB – 24880 (lactose monohydrate 4,50 mg, dye iron oxide red 0,50 mg) 5.00 mg,

magnesium stearate 3,00 mg,

aspartame 1,50 mg,

cherry flavor (Silarom Cherry Flavour 1219813182) 0,10 mg.

Pharmacological properties

Pharmacotherapeutic group: Anti-inflammatory anti-bronchoconstrictor agent-leukotriene receptor blocker: R. 03. D. C. 03 Montelukast Pharmacodynamics : Cysteinyl leukotrienes (LTC4, LTD4, LTE4) are strong pro – inflammatory eicosanoids that are released from various cells, including mast cells and eosinophils. These important pro-asthmatic mediators bind to cysteinyl-leukotriene receptors (CysLTs), which are present in the human respiratory tract and are responsible for the bronchospasm response, sputum production, vascular permeability, and increased eosinophil count. Montelukast is an orally active compound that has a high affinity and selectivity for CysLT1 receptors. Montelukast at a dose of less than 5 mg relieves bronchospasm induced by LTD4 inhalation. The bronchodilating effect is observed within 2 hours after oral use. The bronchodilating effect of beta-2-adrenomimetics is enhanced by taking montelukast. Montelukast suppresses both the early and late stages of bronchospasm caused by exposure to antigens. Montelukast reduces the number of eosinophils in the peripheral blood of adults and children, and significantly reduces the number of eosinophils in the respiratory tract. In patients with hypersensitivity to acetylsalicylic acid receiving inhaled and/or oral glucocorticosteroids (corticosteroids), the addition of montelukast to therapy provides better disease control. Pharmacokinetics: Absorption After oral use, montelukast is rapidly 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 blood plasma (Cmax) is reached in 2 hours. The average bioavailability is 73%, this value decreases to 63% when taking montelukast with food. After taking chewable tablets at a dose of 4 mg on an empty stomach in patients aged 2 to 5 years, Cmax is reached in 2 hours. The average Cmax value in this group of patients is 66% higher, and the average Cmax value is lower than the same value in adults when taking 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 at steady state averages 8-11 liters. Preclinical studies revealed minimal penetration of montelukast through the blood-brain barrier. 24 hours after use, the concentration of montelukast is minimal in other tissues. Metabolism Montelukast is actively metabolized in the liver. When used in therapeutic doses, the concentration of montelukast metabolites in the blood plasma at steady state in adults and children is not determined. In vitro studies have shown that cytochrome P 450 isoenzymes (3 A 4,2 A 6, and 2 C 9) are involved in the metabolism of montelukast, while at therapeutic concentrations montelukast does not inhibit cytochrome P 450 isoenzymes: 3 A 4,2 C 9,1 A 2,2 A 6,2 C 19, and 2D6. The metabolites have a slight therapeutic effect of montelukast. Elimination The elimination half-life of montelukast in young healthy adult volunteers is 2.7 to 5.5 hours. The plasma clearance of montelukast in healthy adult volunteers averages 45 ml/min. After oral use of montelukast,86% of the total amount is excreted through the intestine within 5 days and less than 0.2% – through the kidneys, which, along with data on its bioavailability, confirms the excretion of montelukast and its metabolites mainly in bile. Pharmacokinetics in special casesthe pharmacokinetics of montelukast in women and men are the same. In elderly patients or patients with mild to moderate hepatic insufficiency, no adjustment of the dosage regimen of montelukast is required. The pharmacokinetics of montelukast in patients with renal insufficiency have not been evaluated. Since montelukast and its metabolites are not excreted by the kidneys, no dose adjustment is required in this category of patients. There are no data on the pharmacokinetics of montelukast in patients with severe hepatic impairment (more than 9 points on the Child-Pugh scale). When taking high doses of montelukast (20 and 60 times higher than the recommended doses for adults), a decrease in the concentration of theophylline in blood plasma is observed. When taking montelukast in the recommended doses of 10 mg 1 time a day, this effect is not observed.

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

Application of the drug Almont during pregnancy is possible if the intended benefit to the mother exceeds the potential risk to the fetus. Decision to discontinue breastfeeding for the duration of the drug’s use Almont is taken 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

Infectious and parasitic diseases: upper respiratory tract infections. Disorders of the blood and lymphatic system: increased tendency to bleeding, thrombocytopenia. Immune system disorders: hypersensitivity reactions, including anaphylaxis, eosinophilic liver infiltration. Mental disorders: abnormal dreams, including nightmares; hallucinations, insomnia, somnambulism, irritability, anxiety, restlessness; agitation, including aggressive behavior or hostility; tremor, depression, disorientation, suicidal thoughts and behavior (suicidality). Nervous system disorders: headache, dizziness, drowsiness, paresthesia/hypesthesia, convulsions. Disorders of the heart: palpitation sensation. Respiratory, thoracic, and mediastinal disorders: nosebleeds. Gastrointestinal disorders: diarrhea, dry mouth, dyspepsia, nausea, vomiting, abdominal pain, pancreatitis. Liver and biliary tract disorders: increased activity of alanine aminotransferase and aspartate aminotransferase, hepatitis (including cholestatic, hepatocellular and mixed liver lesions). Skin and subcutaneous tissue disorders: angioedema, tendency to hematomas, urticaria, pruritus, rash, erythema nodosum, erythema multiforme. Musculoskeletal and connective tissue disorders: arthralgia, myalgia, including muscle cramps. General disorders and disorders at the injection site: asthenia/fatigue, malaise, edema, pyrexia, thirst. In very rare cases, Charge-Strauss syndrome has been reported during treatment with montelukast (see section “Special instructions”).

Interaction

In patients receiving phenobarbital at the same time, the area under the pharmacokinetic curve “concentration-time” of montelukast decreased by about 40%, but no dosage adjustment is required in such patients. Since montelukast is metabolized by the CYP3A4 isoenzyme, caution should be exercised, especially in children, if montelukast is used simultaneously with inducers of the CYP3A4 isoenzyme, such as phenytoin, phenobarbital and rifampicin. Montelukast can be prescribed together with other medications 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, prednisone, oral contraceptives (ethinyl estradiol/norethinodrel 35/1), terfenadine, digoxin and warfarin. In vitro studies have shown that montelukast is a strong inhibitor of the CYP2C8 isoenzyme. However, an in vivo drug interaction study of montelukast and rosiglitazone (a marker substrate, a representative of drugs primarily metabolized by the CYP2C8 isoenzyme) did not confirm the inhibition of the CYP2C8 isoenzyme by montelukast. Thus, in clinical practice, montelukast is not expected to affect the SUR2C8-mediated metabolism of a number of drugs, including paclitaxel, rosiglitazone, and repaglinide. In vitro studies have shown that montelukast is a substrate of the CYP2C8 isoenzyme, and to a lesser extent of the CYP2C9 and 3A4 isoenzymes. Data from a clinical drug interaction study with montelukast and gemfibrozil (an inhibitor of both CYP2C8 and 2C9) demonstrate that gemfibrozil increases the effect of systemic exposure to montelukast by 4.4 times.Co-use of itraconazole, a strong inhibitor of the CYP3A4 isoenzyme, together with gemfibrozil and montelukast did not lead to an additional increase in the effect of systemic exposure to montelukast. The effect of gemfibrozil on the systemic effects of montelukast cannot be considered clinically significant based on safety data when used at doses exceeding the approved dose of 10 mg for adult patients (for example,200 mg/day for adult patients for 22 weeks and up to 900 mg/day for patients taking the drug for about one week, no clinically significant adverse effects were observed). Thus, when co-administered with gemfibrozil, no dose adjustment of montelukast is required. According to the results of in vitro studies, no clinically significant drug interactions are expected with other known inhibitors of the CYP2C8 isoenzyme (for example, trimethoprim). In addition, co-use of montelukast with itraconazole alone did not significantly increase the effect of systemic exposure to montelukast. Combined treatment with bronchodilators ALMONT is a reasonable adjunct to monotherapy with bronchodilators, if the latter do not provide adequate control of bronchial asthma. When the therapeutic effect of treatment with ALMONT is achieved, you can start gradually reducing the dose of bronchodilators. Combined treatment with inhaled corticosteroids Treatment with ALMONT provides an additional therapeutic effect for patients using inhaled corticosteroids. When the condition is stabilized, you can start gradually reducing the dose of corticosteroids under the supervision of a doctor. In some cases, complete withdrawal of inhaled corticosteroids is acceptable, but abrupt replacement of inhaled corticosteroids with ALMONT is not recommended.

How to take, course of use and dosage

Inside, the tablet should be chewed. The drug is taken by children under adult supervision. ALMONT should be taken 1 hour before or 2 hours after a meal. For bronchial asthma or bronchial asthma and allergic rhinitis:For children aged 2 to 6 years – 1 chewable tablet in a dose of 4 mg once a day in the evening. For children aged 6 to 14 years – 1 chewable tablet at a dose of 5 mg once a day in the evening. For allergic rhinitis:For children aged 2 to 6 years – 1 chewable tablet at a dose of 4 mg once a day and for children aged 6 to 14 years-1 chewable tablet at a dose of 5 mg once a day individually, depending on the time of the greatest exacerbation of symptoms. No dose adjustment is required within these age groups. General recommendationsthe therapeutic effect of ALMONT, which allows you 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 course of bronchial asthma, and during the period of exacerbation of bronchial asthma. Patients with renal insufficiency and patients with mild to moderate hepatic insufficiency do not require special dose adjustment. No dose adjustment is required depending on the patient’s gender. There are no data on the use of montelukast in patients with severe hepatic impairment. For the treatment of patients of other age groups, a different dosage form and dose of the drug is available – film-coated tablets,10 mg.

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.

There are no data on the possibility of elimination of montelukast by peritoneal dialysis or hemodialysis.

Special instructions

ALMONT is not recommended for the treatment of acute asthma attacks. Patients with asthma are advised to always carry emergency medications. When an acute attack occurs, short-acting inhaled beta-2-adrenomimetics should be used. Patients should consult their doctor as soon as possible if they need more short-acting beta-2-adrenomimetics inhaled than usual. Do not abruptly replace ALMONT with inhaled or oral corticosteroid therapy. There are no data proving the possibility of reducing the dose of oral corticosteroids against the background of simultaneous use of montelukast. In rare cases, patients who receive anti-asthmatic medications, including montelukast, may develop systemic eosinophilia, which is sometimes accompanied by clinical signs of vasculitis, the so-called Charge-Strauss syndrome, a condition that is eliminated by taking systemic corticosteroids. These cases are usually associated with dose reduction or discontinuation of oral corticosteroid therapy. The possibility that leukotriene receptor antagonists may be associated with the development of Charge-Strauss syndrome cannot be excluded or established. Therefore, doctors 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 above-mentioned symptoms should be re-examined, and their treatment regimen should be reviewed. Treatment with ALMONT does not lead to the prevention of bronchospasm in patients with hypersensitivity to acetylsalicylic acid when using acetylsalicylic acid and other nonsteroidal anti-inflammatory drugs. ALMONT contains aspartame, a source of phenylalanine. This medication may be harmful to the health of patients with phenylketonuria. The drug contains lactose monohydrate and should not be used in patients with rare hereditary diseases: galactose intolerance, lactase deficiency or glucose-galactose malabsorption. Influence on the ability to drive vehicles and 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. When these signs appear, patients are not recommended to drive vehicles and engage in other activities that require concentration and speed of psychomotor reactions.

Form of production

Chewable tablets are round, biconvex, pink in color with inclusions and with the inscription “M 5” on one side.

Shelf

life is 3 years.

Active ingredient

Montelukast

Conditions of release from pharmacies

By prescription

Dosage form

tablets for resorption

Purpose

Children as prescribed by a doctor, Children over 6 years of age, Adults as prescribed by a doctor

Indications

Bronchospasm, Bronchial asthma, Runny nose