Description
release form selectively 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 after ingestion is quite fully and rapidly absorbed. Montelukast is highly active when taken orally. Eating does not affect the bioavailability and maximum concentration in blood plasma. Bioavailability is 64 – 73%. The maximum concentration is reached after 2 to 3 hours. The average volume of distribution of montelukast is an average of 8 – 11 liters.
Montelukast is 99% bound to plasma proteins. Montelukast is metabolized in the liver. It is believed that isoenzymes of cytochrome P450 CYP (2C9 and 3A4) are involved in the metabolism 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. Plasma clearance is 45 ml / min. The half-life of montelukast is from 2.7 to 5.5 hours.
Montelukast reduces the severity of edema, spasm of the smooth muscles of blood vessels 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 fertility did not change with the introduction of the drug 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 test V-79 using mammalian cells, microbiological analysis of mutagenicity, alkaline DNA elution using rat liver cells, in vivo chromosomal aberration accounting in mouse bone marrow cells, a test aimed at detecting chromosomal aberrations using Chinese hamster ovary cells, clastogenic and mutagenic activity of montelukast was not detected.
When administered 200 mg / kg per day to rats for two years and to mice at a dose of 100 mg / kg per day for 92 weeks, no carcinogenic effects were observed. The calculated exposure of the drug in mice was about 25 and 45 times greater, 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 prophylaxis of bronchial asthma, including prevention of symptoms of the disease at night and day time
prevention of bronchospasm caused by physical exertion
therapy of bronchial asthma in patients with hypersensitivity to acetylsalicylic acid srdlkrnnogo symptoms
Contraindications
Hypersensitivity, lactation, pregnancy, age up to 6 years.
Use during pregnancy and lactation
The use of montelukast is contraindicated during pregnancy, since clinical studies have not been conducted on the safety of montelukast during pregnancy in women. Montelukast crosses the hematoplacental barrier in rabbits and rats.
Teratogenic effects were not observed when the drug was administered to rabbits at a dose of 300 mg / kg per day (which is 110 times the area under the concentration curve – time for adults at the maximum allowable daily dose) and to rats at a dose of 400 mg / kg per day (which is 100 times the area under the concentration curve – time for adults at the maximum allowable daily dose).
Breast-feeding should be stopped during montelukast therapy (it is not known whether montelukast is excreted in breast milk of women). Montelukast is excreted in breast milk in rats.
Side effects
Nervous system and sensory organs: hallucinations, unusual vivid dreams, headache, sleep disturbances (including nightmares), somnambulism, drowsiness, agitation, irritability, aggressive behavior, insomnia, fatigue, paresthesia / hypesthesia, court depression, anxiety, disorientation, tremors, suicidal thoughts and suicidal behavior, otitis media.
Digestive system: nausea, dyspepsia, vomiting, abdominal pain, diarrhea, impaired liver function, jaundice and hepatitis (including fulminant), an increase in hepatic transaminases, cholestatic, hepatocellular and mixed forms of hepatitis, pancreatitis.
Musculoskeletal system: myalgia, arthralgia, muscle cramps.
Allergic reactions: angioedema, anaphylaxis, rash, hypersensitivity reactions, urticaria, itching, eosinophilic liver infiltrates, erythema nodosum, erythema multiforme.
Other: a tendency to subcutaneous hemorrhage, increased bleeding, nosebleeds, palpitations, flu-like syndrome, edema, cough, pharyngitis, sinusitis, thrombocytopenia, upper respiratory tract infections, palpitations, pyrexia, Cherge-Strauss syndrome.
Drug interaction
Phenobarbital reduces the area under the concentration-time curve of montelukast by 40%, therefore, adequate clinical monitoring of patients co-taking phenobarbital (as well as other P450 cytochrome inducers — phenobarbital, rifampicin and others) and monteluk is recommended. 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. Montelukast also does not (but there are no clinical studies) on thyroid hormones, decongestants, benzodiazepines, non-steroidal anti-inflammatory drugs.
According to in vitro data, montelukast can inhibit the isoenzyme of the cytochrome P450 2C8 system, but this could not be confirmed in vivo. Therefore, we can assume that montelukast will not affect the pharmacokinetics of drugs that are metabolized with the participation of this enzyme (rosiglitazone, paclitaxel, repaglinide).
Overdose
With an overdose of montelukast, drowsiness, thirst, vomiting, hyperkinesis, mydriasis, psychomotor agitation, abdominal pain, headache develop.
Symptomatic treatment needed.
Terms of delivery from
pharmacies Prescription
dosage form
tablets
Appointment by
Adult by appointment at the doctor’s appointment, Detyam over 6 years
Vertex, Russia
