Last Updated on February 19, 2017 by Dr.Derek Fhisher
Most popular brand: Singulair
Active ingredient: Montelukast
Available dosage forms: 4, 5, 10 mg
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Montelukast general information
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The debate concerning the definition of the beneficial reaction to vasodilator therapy remains unsettled. On account of the ominous prognosis connected with pulmonary hypertension from just about any cause, an aggressive way of treatment is warranted when a clinical diagnosis is made. Within this condition, there’s an inflammation of blood vessels (vasculitis), resulting in formation of polyps. The important cause of the sore throat is an infection, whether it’s viral or bacterial. Generally, nasal polyps are due to sinus infections. The individual must understand the essence of the disease along with the goals and expectations of therapy.
Horseradish sauce is among the most effective remedies to alleviate sinus infection. Juice produced from horseradish root may also work wonders to knock out sinus infection. Possessing hot tea and other liquids including soup is the simplest approach to unclog sinuses. You can also drink juice of ripe grapes to diminish the infection. Nasal sprays shouldn’t be used for over 3 days, whereas the suggested usage of oral medicines (pills) is about seven days. They are normally bought over the counter with no prescription.
Some people prefer to keep a wholesome diet in order that they can bulk up and build up some excess muscle mass. The optimal/optimally way still is to prevent the possible reason for your allergy. Since it’s possible you’re not only allergic to an individual form of pollen, you need to expect to get tested for different pollen sources. Fast-acting antihistamines are often given to cure the symptoms following the hay fever episode. In the same way, additionally it is possible to keep away from dust and insects. During the very first day, I truly researched this condition online.
There are various available medication used today to take care of hay fever symptoms. On the opposite hand, long-acting antihistamine doesn’t result to drowsiness. You must be careful in taking this antihistamine as it can induce drowsiness. Doctors don’t advice employing this medication for extended periods because it can result to drug-induced nasal congestion. You need to remember the objective of these medications is always to see to the symptoms. Others are working to slim down.
Description of the active substance Montelukast / Montelukastum.
Formula: C35H36ClNO3S, the chemical name 1 – [[[(R) – M – [(E) – 2 – (7 – chloro – 2 – quinolyl) vinyl] – alpha – [ O – (1 – hydroxy – 1 – метилэтил)фенетил]бензил]тио]метил]циклопропануксусная acid (sodium salt)
Pharmacological group:. intermedianty / prostaglandins, thromboxanes, leukotrienes and their antagonists
Mode of action: bronchodilator
Montelukast selectively blocking leukotriene receptors. Specifically inhibits CysLT1 – cysteinyl leukotriene receptors (C4, D4, E4), are potent mediators of chronic persistent inflammation, which supports the bronchial hyperreactivity in asthma
Montelukast after ingestion adequately and rapidly absorbed.. Montelukast is highly active when taken orally. Food does not affect the bioavailability and maximum plasma concentration. Bioavailability is 64 – 73%. The maximum concentration is reached after 2 – 3 hours. The average volume of distribution of montelukast averages 8 – 11 liters. Montelukast is 99% bound to plasma proteins. Montelukast is metabolised in the liver. It is believed that the cytochrome P450 isozymes CYP (2C9 and 3A4) involved in the metabolism process. At therapeutic concentrations of montelukast do not inhibit the isoenzymes CYP: 2C9, 3A4, 1A2, 2C19, 2A6, 2D6. Mainly excreted in the bile through the intestines (about 86%), kidney output of less than 0.2%. The plasma clearance of 45 ml / min. The half-life of montelukast is from 2.7 to 5.5 hours.
Montelukast reduces the severity of edema, vascular smooth muscle spasm and bronchioles, the migration of macrophages and eosinophils. Montelukast improves mucociliary transport and reduces the secretion of mucus. Within one day bronchodilatory effect develops and persists for a long period.
Montelukast 200 mg / kg per day reduced the fertility and fecundity indices in female rats. Fertility and fecundity was unchanged drug when administered at a dose of 100 mg / kg per day. Montelukast no effect on the fertility of male rats at a dose of 800 mg / kg per day
According Test V -. 79 using mammalian cells, the microbiological analysis of mutagenicity, DNA alkaline elution method using rat liver cells, the method accounting chromosomal aberrations cells in vivo in mouse bone marrow, test which aims to identify chromosome aberrations using Chinese hamster ovary cells and clastogenic montelukast mutagenic activity have been identified.
When administered 200 mg / kg per day of the drug in rats for two years mice and at a dose of 100 mg / kg per day for 92 weeks did not carcinogenic effects were observed. The estimated exposure of the drug in mice is greater than approximately 25 and 45 times, rats – 75 and 120 times the value of the area under the concentration – time at the maximum permissible daily dose of the drug for children and adults, respectively.
The duration of therapy and prophylaxis of asthma, including prevention of disease symptoms in the night and day; prevention of bronchospasm which is caused by physical exertion; asthma therapy in patients with hypersensitivity to acetylsalicylic acid; symptom relief permanent and seasonal allergic rhinitis.
How to use and dose of montelukast
Montelukast ingested. Patients older than 15 years – 10 mg at bedtime; children 6 – 14 years – 5 mg at bedtime
You must strictly adhere to the regimen
It is recommended to continue treatment and achieve significant improvement
Montelukast in acute asthma attacks (including the status asthmaticus… ) does not replace the inhaled bronchodilator, so his relief montelukast should not be used.
When the therapeutic effect, the amount of inhaled bronchodilators during the day can be reduced.
There were no clinically significant differences in the effectiveness of montelukast in elderly and younger patients . The pharmacokinetic profile and bioavailability of montelukast are similar in elderly and younger patients. But the half-life of montelukast is slightly higher in elderly patients. In older patients receiving montelukast correction circuit is not required
In patients with clinical manifestations of liver cirrhosis and mild to moderate hepatic insufficiency montelukast is metabolized more slowly, the value of area under the curve concentration -. Time increases by 41%. The half-life increased slightly. Dosage adjustment is not required. Montelukast pharmacokinetics has not been studied with severe hepatic impairment.
Montelukast and its metabolites are not excreted in the urine, so the pharmacokinetics of montelukast in patients with renal insufficiency has not been studied. Correction of the dose is not required.
Patients with hypersensitivity to acetylsalicylic acid should continue to avoid using it, as well as the use of other NSAIDs in the treatment of montelukast. Montelukast is effective in improving respiratory ventilation in patients with hypersensitivity to aspirin, but has not been shown to have efficacy in the relief of bronchoconstrictor effect of aspirin and other nonsteroidal anti-inflammatory drugs.
In the treatment of montelukast can gradually reduce the dose of inhaled glucocorticosteroids forms, but only under medical supervision. This sharply is not recommended to substitute oral montelukast and inhaled glucocorticosteroids form
In rare cases, patients with asthma who received montelukast, develop systemic eosinophilia, sometimes accompanied by systemic vasculitis, corresponding syndrome Churg -. Strauss. It is often required systemic administration of corticosteroids. It should be sensitive to the appearance of hemorrhagic lesions, systemic eosinophilia, cardiac complaints, deterioration of respiratory function, complaints associated with neuropathy.
In case of side effects with montelukast therapy, which can reduce the concentration of attention, psychomotor speed reactions (dizziness, drowsiness and others), it is necessary to refuse to perform activities that require these properties (including driving motor vehicles).
Hypersensitivity, lactation, pregnancy, age 6 years.
Restrictions on the use
Pregnancy and breastfeeding
The use of montelukast is contraindicated in pregnancy, as it is not conducted clinical studies safety of montelukast during pregnancy in women. Montelukast penetrates the blood-barrier in rabbits and rats. Teratogenic effects were observed upon administration of the preparation to rabbits at a dose of 300 mg / kg per day (which is 110 times greater than the area under the concentration – time for adults in the maximum daily dose), and to rats in a dose of 400 mg / kg per day (in 100 times larger than the area under the concentration – time for adults with maximum daily dose). At the time of montelukast therapy should stop breast-feeding (it is not known whether montelukast in breast milk of women stands out). Montelukast is excreted in breast milk in rats.
Side effects of montelukast
The nervous system and sensory organs: hallucinations, unusual, vivid dreams, headache, sleep disturbance (including nightmares), somnambulism, lethargy, agitation, irritability, aggressive behavior, insomnia, fatigue, paresthesia / hypoesthesia, seizures, depression, anxiety, disorientation, tremors, suicidal ideation and suicidal behavior, otitis media,
Digestive system: nausea, dyspepsia, vomiting, abdominal pain, diarrhea, dysfunction liver, jaundice and hepatitis (including fulminant), increased liver transaminases, cholestatic, hepatocellular, and mixed forms of hepatitis, pancreatitis
The supporting – motor apparatus:. myalgia, arthralgia, muscle cramps
Other:. trend to the formation of subcutaneous hemorrhage, strengthen bleeding, nosebleeds, palpitations, flu syndrome, edema, cough, pharyngitis, sinusitis, anemia, upper respiratory tract infection, palpitations, pyrexia, Churg syndrome – Strauss.
montelukast Interaction with other substances
Phenobarbital reduces by 40% the area under the concentration – time montelukast therefore recommended adequate clinical follow-up of patients receiving phenobarbital together (as well as other inducers of cytochrome P450 – phenobarbital, rifampicin and others) and montelukast. Montelukast is compatible with glucocorticoids (additive effect). Montelukast at recommended doses has no effect on the pharmacokinetics of prednisone, theophylline, prednisone, terfenadine, combined oral contraceptives, digoxin, warfarin. Also, montelukast did not affect (but no clinical studies) on thyroid hormones, decongestants, benzodiazepines, nonsteroidal anti-inflammatory drugs. In in vitro data of montelukast can inhibit the cytochrome P450 isoenzyme system 2S8, but in vivo could not confirm this. Therefore, we can assume that montelukast does not have any impact on the pharmacokinetics of drugs that are metabolized with the participation of the enzyme (rosiglitazone, paclitaxel, repaglinide).
In case of overdose montelukast developed sleepiness, thirst, vomiting, hyperkinesia, mydriasis, agitation, abdominal pain, headache. It should be symptomatic treatment.