Food does not affect the bioavailability and maximum concentration (C max ) in the blood plasma. Oral bioavailability is 64%. After receiving tablets, film-coated tablets, 10 mg, the time to reach maximum concentration (TC max ) -. 3 h The average volume of distribution of montelukast averages 8-11 liters. Testosterone propionate cycle is extensively metabolised in the liver. When using therapeutic doses of the drug concentration of metabolites of montelukast in plasma at steady state in adults and children is not determined. Because montelukast and its metabolites are excreted through the intestine for patients there is no need with renal insufficiency dose adjustments.
• Prevention and long-term treatment of asthma, including prevention of daytime and nighttime symptoms of the disease;
• the treatment of asthma in patients with hypersensitivity to acetylsalicylic acid;
• prevention of bronchospasm caused by exercise;
• relief of symptoms of seasonal and perennial allergic rhinitis.
• Hypersensitivity to any component of the drug;
• rare hereditary disorders such as galactose intolerance, lactase deficiency or glucose-galactose malabsorption;
• Children up to age 15 years (for a given dosage form).
Application of pregnancy and during breastfeeding
Application of medication Montelar ® during pregnancy and lactation is possible only if the expected benefit to the mother outweighs the potential risk to the fetus or child.
Dosing and Administration
The is taken orally 1 time / day regardless of the meal, before going to sleep. For the treatment of bronchial asthma, relief of allergic rhinitis symptoms in children from 15 years and adults . 1 tablet of 10 mg once a day, at bedtime therapeutic effect of montelukast on indicators showing for asthma, developed for the first day. The patient should continue taking montelukast in a period to achieve control of asthma symptoms, and in the period of exacerbation of the disease. To prevent children from 15 years and adults suffering from bronchospasm caused by exercise: 1 tablet 10 mg once a day, at bedtime for 2-4 weeks, in the absence of a satisfactory effect it is necessary to appoint additional or alternative therapy. For older patients, patients with renal failure, patients with mild or moderate hepatic impairment, as well as based on gender specific dose adjustment is required. not Montelukast It is recommended as monotherapy in patients with bronchial asthma of average gravity constant flow.
According to the World Health Organization (WHO), undesirable effects are classified according to their rate of development as follows: very common (≥1 / 10), common (of ≥1 / 100 to <1/10), uncommon (from ≥1 / 1,000 to <1/100), rarely (from ≥1 / 10,000 to <1 / 1,000), very rare (<1 / 10,000); the frequency is unknown – according to available data to set the frequency of occurrence was not possible.
As a result, clinical trials of drugs containing montelukast in patients with intermittent or persistent asthma data for the following side effects have been obtained:
Patients aged 15 years and older (two 12-week-old studies; n = 795): On the part of the central nervous system: often: . headache gastro-intestinal tract (GIT): common: abdominal pain.
Post-marketing surveillance Infectious and parasitic diseases: very common: Upper respiratory tract infection. Immune system: rare: hypersensitivity reactions, including anaphylaxis, rarely angioedema, very rare: eosinophilic infiltration of the liver. Skin and subcutaneous tissue: common: rash ; rarely: tendency to the formation of hematoma, urticaria, pruritus; very rare: erythema nodosum, erythema multiforme.On the part of the central nervous system: infrequently: headache, dizziness, somnolence, paresthesia / hypoesthesia, seizures. Psychiatric disorders: uncommon: sleep disorders ( including nightmares), insomnia, somnambulism, irritability, restlessness, agitation including aggressive behavior or hostility), depression, rare: tremor, very rare: hallucinations, confusion, suicidal ideation and testosterone propionate cycle suicidal behavior.Since the cardiovascular system: rarely: palpitations. From the blood and lymphatic system: rare: increased bleeding tendency. On the part of the gastrointestinal tract (GIT): often: . abdominal pain, diarrhea, nausea, vomiting, pancreatitis rare: dyspepsia, dry oral mucosa . on the part of the liver and biliary tract: common: increased activity of “liver” transaminases (alanine aminotransferase (ALT), aspartate aminotransferase, (ACT)); very rare: cholestatic hepatitis, damage to hepatocytes, often against a background of concomitant drug therapy or an existing liver disease ( various forms of hepatitis). On the part of the musculoskeletal and connective tissue disorders: uncommon: arthralgia, myalgia including muscle cramps. The respiratory system: infrequent: epistaxis very rare: Churg-Strauss syndrome. From the senses: otitis media (including including fatigue, malaise, edema, flu-like symptoms, pyrexia.
Data on overdose symptoms while taking montelukast patients with asthma in a dose exceeding 200 mg per day for 22 weeks and 900 mg per day for one week, were found.
There are reports of acute overdose Montelukast in children (reception least 1000 mg of the drug per day). Clinical and laboratory data at the same time demonstrate compliance montelukast safety profile in children’s safety profile in adults and elderly patients.
The most common symptoms are thirst, drowsiness, vomiting, mydriasis, hyperkinesia, agitation, headache, and abdominal pain. Treatment: carrying symptomatic therapy. the possibility of elimination of montelukast Data by peritoneal dialysis or hemodialysis is not.
Interaction with other drugs
Montelukast may be administered together with other drugs, traditionally used for prevention and long-term treatment of asthma, such as bronchodilators and inhaled corticosteroids.
The recommended therapeutic dose of montelukast did not have a clinically meaningful effect on the pharmacokinetics of the following drugs: theophylline, prednisone, prednisolone, oral contraceptives (ethinyl estradiol / noretinsteron 35/1), terfenadine, digoxin and warfarin. The index value is the area under the curve “concentration-time» (AUC) decreasing in subjects while receiving phenobarbital (approximately 40%), however, the dosing regime montelukast correction such patients is not required.
In studies in vitro demonstrated that montelukast is a potent inhibitor of isozyme CYP 2S8 cytochrome P450, but the data from clinical studies of the interaction “drug-drug”, involving montelukast and rosiglitazone (a preliminary substrate representative of medicinal products primarily metabolized by CYP isoenzymes 2S8) have shown that the dose of montelukast does not inhibit CYP isoenzymes 2S8 in vivo.
Therefore, montelukast is not significant effect on the metabolism of medicinal products metabolized by this enzyme (eg, paclitaxel, rosiglitazone, and repaglinide).
studies in vitro have shown that montelukast is a substrate of CYP 2C8, 2C9 and 3A4.
these clinical studies of drug interactions in relation to montelukast and gemfibrozil (an inhibitor of both CYP 2C8, and 2C9) demonstrated that the effect of gemfibrozil increases the systemic exposure of montelukast 4.4 times. Joint reception of itraconazole, a potent inhibitor of CYP 3A4, with gemfibrozil and montelukast did not lead to a further increase in the effect of the systemic exposure of montelukast.Effect of gemfibrozil on systemic exposure of montelukast can not be considered clinically significant on grounds of safety when used at doses higher than the approved dose testosterone propionate cycle of 10 mg for adults (for example, 200 mg / day for adult patients for 22 weeks, and up to 900 mg / day patients taking the drug for approximately one week, no clinically meaningful adverse effects). Thus, when co-administered with gemfibrozil montelukast dose adjustment is required. According to the results of studies in vitro is not expected clinically significant drug interactions with other known inhibitors of CYP 2C8 (such as trimethoprim). In addition, co-administration of montelukast with itraconazole alone did not lead to a significant increase in the effect of the systemic exposure of montelukast.
Combined treatment with bronchodilators.
The drug is a reasonable addition to bronchodilators alone, if they do not provide adequate control of asthma. Upon reaching the therapeutic effect (usually after the first dose) of the drug treatment can start a gradual reduction in the dose of bronchodilators.
The combined treatment with inhaled corticosteroids.
Treatment with provides additional therapeutic benefit to patients applying inhaled glucocorticosteroids. In stabilization, you can start a gradual reduction of the dose of glucocorticosteroid under the supervision of a physician. In some cases a complete abolition of inhaled glucocorticosteroids, but abrupt replacement of inhaled glucocorticosteroids on drug is not recommended.
Since montelukast is metabolized by isoenzyme CYP 3A4, caution should be exercised, particularly in children older than 15 years if montelukast simultaneously assigned with drugs testosterone propionate cycle that induce CYP isoenzymes 3A4, such as phenytoin, phenobarbital and rifampicin.
It is recommended to continue taking montelukast and after achieving significant improvements.
Montelukast is not recommended for the treatment of acute asthma attacks.
In acute bronchial asthma patients should use drugs emergency cupping (inhaled beta2-agonists short-acting).
Reduction of the systemic dose glucocorticoids ( GCS) in patients receiving anti-asthma agents including leukotriene receptor antagonists, followed in rare cases development of Churg-Strauss syndrome (systemic eosinophilic vasculitis), which manifests itself in the form of eosinophilia, vascular rash, increased severity of pulmonary symptoms, and, in the absence of proper treatment, cardiac complications and / or neuropathy. Although a causal relationship between these adverse events from treatment leukotriene-receptor antagonist has not been established, while reducing the systemic dose corticosteroids in patients taking montelukast, you must be careful and conduct appropriate clinical supervision.
The dose of corticosteroids used together with montelukast, should be reduced gradually under supervision of a physician. We do not recommend sharp replacement therapy with inhaled or oral corticosteroids appointment montelukast. Patients with confirmed allergy to aspirin and other nonsteroidal anti-inflammatory drugs (NSAIDs) that the period of treatment montelukast avoid contact with these drugs as montelukast, improving pulmonary function in patients with allergic asthma, however, does not prevent the bronchoconstriction due to the action of NSAIDs .
By reducing the dose of systemic corticosteroids in patients taking montelukast, you must be careful to carry out the relevant clinical observation.
Age differences of efficacy and safety profile of montelukast was not revealed.
Special precautions for the destruction of unused medicinal product
No need for special precautions during the destruction of unused medication Montelar ® .
Effects on ability to drive and doing other activities that require concentration and speed of psychomotor reactions .
There is no evidence that receiving montelukast affect the ability to drive a car or moving machinery, is not revealed. However, reports of somnolence and dizziness, so the appearance of these symptoms is not recommended in patients as the management of vehicles and occupation of other activities that require concentration and speed of psychomotor reactions. Running low dose t3 clen cycle trying to lose bodyfat isn’t a real hot idea imo.