Montelukast pills 10mg, 30pcs

Pharmacological action

Montelukast selectively blocks leukotriene receptors. Specifically inhibits CysLT1-receptors of cysteinyl leukotrienes (C4, D4, E4), which are the strongest mediators of chronic persistent inflammation, which supports bronchial hyperreactivity in bronchial asthma.

Montelukast is fairly fully and rapidly absorbed after oral use. Montelukast is highly active when taken orally. Food intake does not affect the bioavailability and maximum concentration in blood plasma. Bioavailability is 64-73%. The maximum concentration is reached in 2-3 hours. The average volume of distribution of montelukast is 8-11 liters on average.

Montelukast is 99% bound to plasma proteins. Montelukast is metabolized in the liver. Cytochrome P 450 CYP (2C9 and 3A4) isoenzymes are believed to be involved in the metabolic process.

At therapeutic concentrations, montelukast does not inhibit CYP isoenzymes: 2C9,3A4,1A2,2C19,2A6,2D6. It is mainly excreted with bile through the intestines (about 86%), less than 0.2% is excreted by the kidneys. The plasma clearance is 45 ml/min. The elimination half-life of montelukast is 2.7 to 5.5 hours.

Montelukast reduces the severity of edema, spasm of vascular smooth muscle and bronchioles, migration of macrophages and eosinophils. Montelukast improves mucociliary transport and reduces mucus secretion. Within one day, a bronchodilator effect develops and persists for a long period.

Montelukast at a dose of 200 mg / kg per day reduced fertility and fertility indices in female rats. Fertility and fecundity did not change when the drug was administered at a dose of 100 mg/kg per day. Montelukast did not affect the fertility of male rats at a dose of more than 800 mg/kg per day.

According to the V-79 test using mammalian cells, microbiological mutagenicity analysis, the alkaline DNA elution method using rat liver cells, the method of accounting for chromosomal aberrations in vivo in mouse bone marrow cells, the test aimed at detecting chromosomal aberrations using Chinese hamster ovarian cells, no clastogenic or mutagenic activity of montelukast was detected.

When the drug was administered 200 mg/kg per day to rats for two years and mice at a dose of 100 mg/kg per day for 92 weeks, no carcinogenic effects were observed. The estimated exposure of the drug in mice was approximately 25 and 45 times higher, in rats-75 and 120 times the area under the concentration – time curve at the maximum allowable daily dose of the drug for children and adults, respectively.

Indications

• Long-term therapy and prevention of bronchial asthma, including prevention of symptoms of the disease at night and during the day;

• prevention of bronchospasm caused by physical exertion;

• treatment of bronchial asthma in patients with hypersensitivity to acetylsalicylic acid; 

• relief of symptoms of persistent and seasonal allergic rhinitis.

Contraindications

Hypersensitivity, lactation, pregnancy, age up to 6 years.

Side effects

Nervous system and sensory organs:  hallucinations, unusual vivid dreams, headache, sleep disorders (including nightmares), somnambulism, drowsiness, agitation, irritability, aggressive behavior, insomnia, fatigue, paresthesia/hypesthesia, seizures, depression, anxiety, disorientation, tremor, suicidal thoughts and suicidal behavior, otitis media.

Digestive system:  nausea, dyspepsia, vomiting, abdominal pain, diarrhea, impaired liver function, jaundice and hepatitis (including fulminant), increased levels of hepatic transaminases, cholestatic, hepatocellular and mixed forms of hepatitis, pancreatitis.

Musculoskeletal system:  myalgia, arthralgia, muscle cramps.

Allergic reactions:  angioedema, anaphylaxis, rash, hypersensitivity reactions, urticaria, pruritus, eosinophilic liver infiltrates, erythema nodosum, erythema multiforme.

Other services:  tendency to form subcutaneous hemorrhages, increased bleeding, nosebleeds, palpitations, flu-like syndrome, edema, cough, pharyngitis, sinusitis, thrombocytopenia, upper respiratory tract infections, palpitations, pyrexia, Churge-Strauss syndrome.

The interaction

of Phenobarbital reduces the area under the concentration – time curve of montelukast by 40%, so adequate clinical monitoring is recommended for patients taking phenobarbital (as well as other inducers of the cytochrome P450 system – phenobarbital, rifampicin, and others) and montelukast together. Montelukast is compatible with glucocorticoids (additive effect).

Montelukast in the recommended doses does not affect the pharmacokinetics of prednisone, theophylline, prednisolone, terfenadine, combined oral contraceptives, digoxin, warfarin. Also, montelukast does not affect (but there are no clinical studies) thyroid hormones, decongestants, benzodiazepines, nonsteroidal anti-inflammatory drugs.

According to in vitro data, montelukast can inhibit the cytochrome P4502c8 isoenzyme, but this could not be confirmed in vivo. Therefore, it can be assumed that montelukast will not affect the pharmacokinetics of drugs that are metabolized with the participation of this enzyme (rosiglitazone, paclitaxel, repaglinide).

How to take, course of use and dosage

Montelukast is taken orally.

Patients older than 15 years — 10 mg before bedtime; children 6-14 years-5 mg before bedtime. It is necessary to strictly follow the therapy regimen. It is recommended to continue treatment even if significant improvement is achieved. Montelukast for acute asthmatic attack (including asthmatic status) it does not replace inhaled bronchodilators, so montelukast should not be used for its relief.

If a therapeutic effect appears, the number of inhalations of bronchodilators during the day can be reduced.

There were no clinically significant differences in the effectiveness of montelukast in elderly and young patients. The pharmacokinetic profile and bioavailability of montelukast are similar in elderly and young patients. However, the elimination half-life of montelukast is slightly higher in elderly patients. In older patients, no correction of the montelukast regimen is required.

In patients with clinical signs of liver cirrhosis and mild to moderate hepatic insufficiency, montelukast is metabolized more slowly, the area under the concentration – time curve increases by 41%. The elimination half-life increases slightly. No dose adjustment is required. The pharmacokinetics of montelukast in patients with severe hepatic impairment have not been studied. Montelukast and its metabolites are not excreted in the urine, so the pharmacokinetics of montelukast in patients with renal insufficiency have not been studied. No dose adjustment is required.

Patients with hypersensitivity to acetylsalicylic acid should continue to avoid its use, as well as the use of other nonsteroidal anti-inflammatory drugs during treatment with montelukast. Montelukast effectively improves respiratory ventilation in patients with hypersensitivity to acetylsalicylic acid, but it has not been shown to be effective in relieving the bronchoconstrictor effect of acetylsalicylic acid and other nonsteroidal anti-inflammatory drugs.

When treating montelukast, you can gradually reduce the dose of inhaled forms of glucocorticosteroids, but only under the supervision of a doctor. At the same time, it is not recommended to sharply replace oral and inhaled forms of glucocorticosteroids with montelukast.

In rare cases, patients with bronchial asthma who took montelukast developed systemic eosinophilia, which was sometimes accompanied by systemic vasculitis corresponding to Churge-Strauss syndrome. Systemic use of glucocorticosteroids was often required. It is necessary to pay close attention to the appearance of hemorrhagic rashes, systemic eosinophilia, cardiac complaints, deterioration of respiratory function, complaints related to neuropathy.

If side effects occur during therapy with montelukast, which can reduce the concentration of attention, the speed of psychomotor reactions (drowsiness, dizziness, etc. ), it is necessary to refuse to perform activities where these properties are necessary (including driving vehicles).

Overdose

Overdose with montelukast causes drowsiness, thirst, vomiting, hyperkinesis, mydriasis, psychomotor agitation, abdominal pain, and headache.

Symptomatic treatment is necessary.

Active ingredient

Montelukast

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For children over 6 years of age, For adults as prescribed by a doctor, For children as prescribed by a doctor

Indications

Bronchial asthma, Bronchospasm, Allergic rhinitis