Compound
One film-coated tablet contains (active ingredients):
- montelukast sodium equivalent to montelukast - 10 mg;
- Levocetirizine dihydrochloride - 5 mg.
Excipients: lactose monohydrate, microcrystalline cellulose, dibasic calcium phosphate anhydrous, croscarmellose sodium, hydroxypropylcellulose, magnesium stearate, opadry yellow 13B52204 (hypromellose, titanium dioxide (E 171), macrogol, yellow iron oxide (E 172), polysorbate 80, iron oxide red (E 172)).
Features of application
Pregnant
There are no reliable and properly controlled clinical studies of the use of this drug in pregnant women. Use during pregnancy is contraindicated.
Given that many drugs are excreted into breast milk in women who are breastfeeding, breastfeeding should be discontinued if use of the drug is necessary.
Children
The drug is used for children over the age of 15 years.
Drivers
No studies have been conducted on the effect of a fixed dose combination of montelukast and levocetirizine on the ability to drive or operate machines. Some patients may feel drowsiness, fatigue and weakness during treatment with levocetirizine. Patients should refrain from driving or operating potentially dangerous machinery while being treated with Glencet Advance.
Glenset
Pharmacokinetics are linear, independent of dose and time, and vary slightly between individuals.
Absorption
Rapidly absorbed when taken orally; food intake does not affect the completeness of absorption, but reduces its speed. Bioavailability - 100%. The time to reach the maximum concentration in the blood (TCmax) is 0.9 hours, the maximum concentration in the blood (Cmax) is 207 ng/ml. Volume of distribution - 0.4 l/kg. The extent of absorption depends on the dose and is not affected by food intake, but with food intake the maximum concentration is reduced and its achievement slows down.
Distribution
Levocetirizine is 90% bound to plasma proteins. There are no data on the distribution of levocetirizine in tissues and its penetration through the blood-brain barrier in humans. Levocetirizine passes into breast milk.
Metabolism
In humans, less than 14% of a dose of levocetirizine is metabolized, as the expected differences in the pharmacokinetic profile of levocetirizine due to genetic polymorphisms or concomitant use of enzyme inhibitors are negligible. Metabolic transformations consist of oxidation of the aromatic ring, N- and O-dealkylation and conjugation with taurine. The dealkylation process is mainly carried out by the CYP3A4 isoenzyme, while the oxidation of the aromatic ring occurs through many and/or unidentified CYP isoforms. Levocetirizine, when taken orally at a dose of 5 mg and/or when maximum plasma concentrations are exceeded, does not affect the activity of CYP isoenzymes 1A2, 2C9, 2C19, 2B6, 2E1, 3A4.
Due to limited metabolism and the absence of metabolic inhibitory activity, interaction of levocetirizine at the metabolic level with other substances is unlikely.
Removal
The half-life (T1/2) is 7-10 hours. The total clearance is 0.63 ml/min/kg. It is completely eliminated from the body within 96 hours. It is excreted mainly in the urine (85.4%) of the dose taken.
Patients with kidney failure
The overall clearance of levocetirizine depends on creatinine clearance (CC), therefore patients with moderate to severe renal failure are advised to increase the intervals between doses of the drug in accordance with the CC.
In patients with anuria and end-stage renal disease, the total clearance of levocetirizine is reduced by approximately 80% compared to healthy individuals. The amount of levocetirizine excreted during a standard 4-hour hemodialysis procedure is less than 10%.
Overdose
Montelukast
There are currently no specific recommendations for the treatment of montelukast overdose. Cases of acute overdose with montelukast have been reported during post-marketing surveillance and during clinical trials. These include reports of overdose in adults and children following doses as high as 1000 mg. Data from clinical and laboratory studies were consistent with the safety profile for adults and children. In most reported cases of overdose, no severe adverse reactions were observed. The most common adverse reactions were consistent with the safety profile of montelukast and included abdominal pain, somnolence, thirst, headache, vomiting and psychomotor hyperactivity. It is not known whether montelukast is eliminated by peritoneal dialysis or hemodialysis.
Treatment is symptomatic.
Levocetirizine
Cases of overdose with levocetirizine have been reported. Symptoms of overdose may include drowsiness in adults and, in children, initial agitation and restlessness followed by drowsiness. There is no known specific antidote to levocetirizine. In case of overdose, symptomatic or supportive therapy is recommended. Levocetirizine is not excreted by dialysis.
Glencet Advance tablets No. 14
Montelukast
Acute episode of bronchial asthma Montelukast is not intended to eliminate bronchospasm during acute attacks of bronchial asthma, including status asthmaticus. In such cases, patients should use available emergency treatment. Montelukast therapy can be continued during exacerbation of bronchial asthma. Patients whose asthma exacerbations occur after exercise should carry short-acting β-agonist inhalers.
Concomitant use with corticosteroids: If the dose of inhaled corticosteroids can be gradually reduced under medical supervision, montelukast should not be suddenly replaced by inhaled or oral corticosteroids.
Aspirin Hypersensitivity: Patients with known aspirin hypersensitivity should avoid using aspirin or nonsteroidal anti-inflammatory drugs while receiving montelukast. Although montelukast is effective in improving airway function in patients with asthma with documented aspirin hypersensitivity, it does not reduce the bronchoconstrictor response to aspirin and other nonsteroidal anti-inflammatory drugs in patients with asthma who are sensitive to aspirin.
Neuropsychiatric disorders: Cases of neuropsychiatric phenomena have been reported while taking montelukast in adults, adolescents and children. During post-marketing surveillance, the following adverse events were reported while taking montelukast: agitation, aggressive behavior or hostility, anxiety, depression, disorientation, sleep disturbance, hallucinations, insomnia, irritability, restlessness, tremor, somnambulism, suicidal ideation and suicidal behavior (including suicide).
Clinical details of some post-marketing reports of adverse events with montelukast are consistent with an effect induced by this drug. Doctors who prescribe this drug, as well as patients, should be aware of the possibility of neuropsychiatric disorders. Patients should be warned that if symptoms occur, they should notify their doctor. If such events occur in a patient, the physician should carefully weigh the risks and benefits of continuing montelukast therapy.
Eosinophilic conditions: Patients with asthma while taking montelukast may develop systemic eosinophilia, which sometimes manifests as clinical signs of vasculitis, indicating Churg-Strauss syndrome, a condition for which systemic corticosteroid therapy is often indicated. As a rule, these phenomena are associated with a reduction in the dose of oral corticosteroids. The physician should carefully monitor the patient's condition in order to promptly identify symptoms of eosinophilia, vasculitic skin rashes, as well as increased pulmonary symptoms, cardiac complications and/or neuropathy.
Levocetirizine
Use with caution in patients with chronic renal failure (dosage regimen adjustment is required) and in elderly patients (glomerular filtration rate may decrease).
When prescribing the drug in patients with certain factors that provoke urinary retention (for example, spinal cord injuries, prostatic hyperplasia), it is necessary to take into account that levocetirizine increases the risk of urinary retention.
Antihistamines suppress the response to a skin allergy test, so before the test, the drug must be stopped 3 days before the test (withdrawal period).
Itching may occur after discontinuation of levocetirizine, even if these symptoms were not present before treatment. Symptoms may go away on their own. In some cases, symptoms may be severe and re-treatment with the drug may be required after discontinuation.
During clinical studies, cases of drowsiness, increased fatigue and general weakness occurred in some patients while taking levocetirizine. Patients should be warned that during treatment they should avoid activities that require increased mental activity and precise coordination of movements, in particular working with machinery or driving vehicles.
During therapy with levocetirizine, it is necessary to avoid drinking alcohol and taking central nervous system (CNS) antidepressants, as this may result in an additional decrease in activity and increased depression of CNS activity.
Glencet Advance contains lactose and should not be used in patients with rare hereditary diseases such as galactose intolerance, Sami lactase deficiency or glucose-galactose malabsorption syndrome.
Use in elderly patients.
Montelukast
No differences in the safety and efficacy profile were observed between the use of this drug in older and younger patients, and there is no evidence in clinical practice that would indicate a difference in response to this drug in these two populations, however, the presence of higher Sensitivity to this drug cannot be excluded.
Levocetirizine
The number of patients aged 65 years or older in clinical trials with levocetirizine for each approved indication was insufficient to determine whether their response to therapy would differ from that of younger patients. In clinical practice, there is no evidence of differences in responses to this drug in older and younger patients.
In general, dose selection in elderly patients should be done with caution; As a rule, therapy should be initiated at the lower end of the recommended dose range, given that these patients have a higher incidence of decreased liver, renal or cardiac function, as well as concomitant diseases and concomitant use of other drugs.
Side effects
Montelukast
The following are the most common adverse reactions reported during post-marketing surveillance.
Infections and parasitic diseases: very common (≥ 1/10) - upper respiratory tract infection.
From the gastrointestinal tract: often (from ≥ 1/100 to < 1/10) - diarrhea, nausea, vomiting.
Hepatobiliary system: often (from ≥ 1/100 to < 1/10) - increased serum levels of transaminases (ALT, AST).
From the skin and subcutaneous tissue: often (from ≥ 1/100 to < 1/10) - skin rashes.
Levocetirizine
The following adverse reactions have been reported and observed during clinical studies:
- often (from > 1/100 to < 1/10) - headache, drowsiness, dry mouth, increased fatigue;
- uncommon (from ≥ 1/1000 to < 1/100) - general weakness, abdominal pain.
Glenzeth
Side effects of the drug are divided into system-organ classes in accordance with the classification of the Medical Dictionary of Regulatory Activities (MedDRA) indicating their frequency of occurrence: often (> 1/100 and 1/1000 and
Immune system disorders: very rare: hypersensitivity reactions, including anaphylactic reactions.
Metabolic and eating disorders: frequency unknown: increased appetite.
Nervous system disorders: often: headache; uncommon: drowsiness; rarely: dizziness; very rarely: aggression, agitation, hallucinations, depression, convulsions; frequency unknown: insomnia, dural sinus thrombosis, paresthesia, syncope, anxiety, tremor, dysgeusia, suicidal ideation.
Hearing disorders: frequency unknown: vertigo.
Visual disorders: frequency unknown: blurred vision, inflammatory manifestations.
Disorders of the cardiovascular system: very rarely: palpitations, tachycardia; frequency unknown: jugular vein thrombosis, angina pectoris.
Respiratory, thoracic and mediastinal disorders: Very rare: shortness of breath; frequency unknown: increased symptoms of rhinitis.
Gastrointestinal disorders: often: dryness of the oral mucosa; uncommon: abdominal pain; very rarely: nausea, diarrhea; frequency unknown: vomiting.
Renal and urinary system disorders: frequency unknown: dysuria, urinary retention.
Disorders of the liver and biliary tract: very rarely: hepatitis.
Skin and subcutaneous tissue disorders: very rare: angioedema, itching, rash, including drug rash, urticaria; frequency unknown: hypotrichosis, fissures, photosensitivity.
Musculoskeletal and connective tissue disorders: very rare: myalgia.
General disorders: often: fatigue; uncommon: asthenia; frequency unknown: peripheral edema.
Violations of laboratory and instrumental data: very rarely: abnormal liver function tests, weight gain.
Other: frequency unknown: cross-reactivity.
Symptoms of overdose may include drowsiness in adults and agitation and restlessness followed by drowsiness in children. There are no specific antidotes for levocetirizine. In case of overdose, symptomatic or supportive treatment is recommended. If little time has passed after taking the drug, gastric lavage should be performed. Levocetirizine is practically not excreted during hemodialysis.
Note!
Description of the drug Glencet Advance table. p/o No. 28 on this page is a simplified author’s version of the apteka911 website, created on the basis of the instructions for use.
Before purchasing or using the drug, you should consult your doctor and read the manufacturer's original instructions (attached to each package of the drug). Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use.
