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Cysteine leukotrienes (LTC4, LTD4, LTE4) are 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), which are 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.
Almont is an orally active compound that has a high affinity and selectivity for CysLT 1 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. The bronchodilatory effect of beta-adrenomimetikov increases when taking montelukast. Almont suppresses both the early and late stages of bronchospasm caused by exposure to antigens. Almont 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 inhaled and / or oral glucocorticosteroids (GCS), adding to the therapy montelukast provides better control of the disease.
After oral administration, 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 plasma concentration (Cmax) is reached after 2 hours. The average value of bioavailability - 73%, this value is reduced to 63% when taking montelukast with food. After taking chewable tablets in a dose of 4 mg on an empty stomach in patients aged 2 to 5 years, Stax is reached after 2 hours. The average value of Sta in this group of patients is 66% higher, and the average value of Cmin is lower than that in adults when taking film-coated tablets at a dose of 10 mg.
Binding of montelukast to plasma proteins is more than 99%. The volume of distribution in the equilibrium state is on average 8-11 liters. Preclinical studies have revealed the minimal penetration of montelukast through
blood-brain barrier. 24 hours after administration, the concentration of montelukast is minimal in other tissues.
Almont is actively metabolized in the liver. When used in therapeutic doses, the concentration of the metabolites of Montelukast in the blood plasma in an equilibrium state in adults and children is not determined.
In vitro studies have shown that cytochrome P450 isoenzymes (ZA4, 2A6 and 2C9) are involved in the metabolism of montelukast, while in therapeutic concentrations montelukast does not inhibit cytochrome P450 isoenzymes: ZA4, 2C9, 1A2, 2A6, 2C19 and 2D6. Metabolites have a slight therapeutic effect of montelukast.
The half-life of montelukast in young healthy adult volunteers is from 2.7 to 5.5 hours. The plasma clearance of montelukast in healthy adult volunteers is an average of 45 ml / min. After oral administration of montelukast, 86% of the total amount is excreted through the intestines for 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 with bile.
Pharmacokinetics in special cases
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 receiving high doses of montelukast (20 and 60 times higher than the recommended dose for adults) there is a decrease in plasma concentration of theophylline.When taking montelukast in the recommended doses of 10 mg 1 time per day, this effect is not observed.
Prevention and long-term treatment of bronchial asthma in children, including:
- prevention of day and night symptoms of the disease (for children from 2 years old and older);
- treatment of bronchial asthma in patients with hypersensitivity to acetylsalicylic acid (for children 6 years and older);
- prevention of bronchospasm caused by physical activity (for children from 2 years and older).
Relieving symptoms of seasonal and year-round allergic rhinitis in children from 2 years.
Montelukast is marketed under different brands and generic names, and comes in different dosage forms:
|Brand name||Manufacturer||Country||Dosage form|
|Singular||Merck Sharp & Dohme B.V||Netherlands||pills|
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Dosage and Administration
Montelukast is taken by mouth. Patients over 15 years old - 10 mg at bedtime; Children 6-14 years of age - 5 mg at bedtime.
It is necessary to strictly observe the treatment regimen.
It is recommended to continue treatment and achieve a significant improvement.
Montelukast does not replace inhalation bronchodilators for acute asthmatic attack (including those with asthmatic status), so montelukast should not be used to relieve it.
When 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. But the half-life of montelukast is slightly higher in elderly patients. Older patients do not need to adjust the Montelukast regimen.
In patients with clinical manifestations of cirrhosis and mild and moderate liver failure, montelukast is metabolized more slowly, the area under the concentration curve - time increases by 41%. The half-life increases slightly. No dose adjustment is required. The pharmacokinetics of montelukast with severe liver dysfunction has not been studied.
Montelukast and its metabolites are not excreted in the urine; therefore, the pharmacokinetics of Montelukast have not been studied in patients with renal insufficiency. Dose adjustment of the drug is not 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 has not been shown to be effective in alleviating the bronchoconstrictor effect of acetylsalicylic acid and other nonsteroidal anti-inflammatory drugs.
With montelukast treatment, the dose of inhaled forms of glucocorticosteroids can be gradually reduced, but only under the supervision of a physician. At the same time, sharply replacing oral and inhalation forms of glucocorticosteroids with montelukast is not recommended.
In rare cases, patients with bronchial asthma who took montelukast developed systemic eosinophilia, which was sometimes accompanied by systemic vasculitis corresponding to Churga-Strauss syndrome. It often required systemic administration of glucocorticosteroids. You must be careful about the appearance of hemorrhagic rashes, systemic eosinophilia, cardiac complaints, deterioration of the function of the respiratory organs, complaints related to neuropathy.
If side effects occur during montelukast therapy, which can reduce concentration of attention, speed of psychomotor reactions (drowsiness and other drowsiness), it is necessary to refuse to perform activities where these properties are necessary (including driving a motor vehicle).
Nervous system and sensory organs: hallucinations, unusual vivid dreams, headache, sleep disturbances (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, abnormal 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.
Others: a tendency to the formation of subcutaneous hemorrhages, increased bleeding, nosebleeds, palpitations, flu-like syndrome, edema, cough, pharyngitis, sinusitis, thrombocytopenia, upper respiratory tract infections, feeling of palpitations, pyrexia, Churga-Stross syndrome.
Hypersensitivity, lactation, pregnancy, age up to 6 years.
Phenobarbital reduces by 40% the area under the concentration curve - montelukast time, therefore, adequate clinical observation is recommended for patients co-administering phenobarbital (as well as other cytochrome P450 inducers - phenobarbital, rifampicin and others) and montelukast. Montelukast is compatible with glucocorticoids (additive effect). The recommended doses of Montelukast do 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 isoenzyme of the cytochrome P450 2S8 system, but it was not possible to confirm this 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).
Pregnancy and Lactation
The use of montelukast is contraindicated during pregnancy, as no clinical studies have been conducted on the safety of using montelukast during pregnancy in women. Montelukast penetrates the hemato-placental 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 more than the area under the concentration curve - time for adults with the maximum allowable daily dose) and rats at 400 mg / kg per day (which is 100 times the area under the concentration curve - time for adults at the maximum allowable daily dose). At the time of treatment with montelukast, breastfeeding should be stopped (it is not known whether montelukast is excreted in breast milk of women). Montelukast is excreted in breast milk in rats.
When overdose montelukastom develop drowsiness, thirst, vomiting, hyperkinesis, mydriasis, psychomotor agitation, abdominal pain, headache. Symptomatic treatment is required.
- Brand name: Almont
- Active ingredient: Montelukast
- Manufacturer: Actavis Ltd
- Country of Origin: Iceland
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- Quantification of montelukast, a selective cysteinyl leukotriene receptor (CysLT1) antagonist in human plasma by liquid chromatography–mass spectrometry: validation and its application to a human pharmacokinetic study
- New and Improved Synthesis of Montelukast, an Antiasthmatic Drug.
- Treatment with the leukotriene inhibitor montelukast for 10 days attenuates portal hypertension in rat liver cirrhosis
- Determination of montelukast sodium by capillary electrophoresis
- Montelukast therapy and psychological distress in chronic obstructive pulmonary disease (COPD): A preliminary report
- Pregnancy outcome following gestational exposure to montelukast: A prospective cotrolled study
- Population pharmacokinetic profile of montelukast in children aged 3 to 6 months with bronchiolitis
- Telithromycin, but not montelukast, increases the plasma concentrations and effects of the cytochrome P450 3A4 and 2C8 substrate repaglinide
- PIII-54An open-label, randomized, 2-period, crossover study, to assess the effects of montelukast on the pharmacokinetics of rosiglitazone, a CYP2C8 substrate, in healthy adults
- A rapid and sensitive method for the quantitation of montelukast in sheep plasma using liquid chromatography/tandem mass spectrometry
- A simple bioanalytical assay for determination of montelukast in human plasma: Application to a pharmacokinetic study
- Complexation study of cinalukast and montelukast with cyclodextrines
- Effect of light and heat on the stability of montelukast in solution and in its solid state
- Identification, synthesis, isolation and spectral characterization of potential impurities of montelukast sodium
- Dose-related protection of exercise bronchoconstriction by montelukast, a cysteinyl leukotriene–receptor antagonist, at the end of a once-daily dosing interval*
- Montelukast causes prolonged, potent leukotriene D4-receptor antagonism in the airways of patients with asthma*
- Expedient liquid chromatographic method with fluorescence detection for montelukast sodium in micro-samples of plasma
- Determination of montelukast sodium in human plasma by column-switching high-performance liquid chromatography with fluorescence detection
- Simultaneous determination of montelukast and loratadine by HPLC and derivative spectrophotometric methods
- A semi-automated 96-well protein precipitation method for the determination of montelukast in human plasma using high performance liquid chromatography/fluorescence detection
- Determination of montelukast (MK-0476) and its S-enantiomer in human plasma by stereoselective high-performance liquid chromatography with column-switching
- Failure of montelukast to prevent anaphylaxis to diclofenac
- Successful treatment of delayed pressure urticaria with montelukast