INSTRUCTIONS FOR MEDICAL USE

MONTELEKOR

Trade name of the drug: Montelecor

Active ingredients (INN) : montelukast sodium/levocetirizine hydrochloride

Dosage form: suspension

Compound:

Every 5 ml of suspension contains:

active substances : sodium montelukast USP

equivalent to montelukast 4 mg

levocetirizine hydrochloride 2.5 mg;

excipients : sucrose, glycerol, xanthan gum, sorbitol solution 70% (non-crystalline), sodium methylhydroxybenzoate, sodium propylhydroxybenzoate, sodium benzoate, colloidal anhydrous silicon, acrysol K-150, sucralose, disodium edetate, sweet orange flavor No. 1, orange oil, Sunset Yellow Supra, sodium hydroxide, purified water.

Description: orange suspension with a characteristic taste and odor

Pharmacotherapeutic group: leukotriene receptor antagonist, antihistamine

ATX code: R03DC53

Pharmacological properties

Pharmacodynamics

Combined antiallergic drug montelukast sodium and levocetirizine.

Montelukast — selectively blocks leukotriene receptors. Specifically inhibits CysLT ₁ receptors of cysteinyl leukotrienes (LC ₄ , LTD ₄ and LTE ₄ ) — the most powerful mediators of chronic persistent inflammation that supports bronchial hyperreactivity in bronchial asthma.

Reduces the severity of spasm of smooth muscles of bronchioles and blood vessels, swelling, migration of eosinophils and macrophages; reduces mucus secretion and improves mucociliary transport. Highly active when taken orally. The bronchodilator effect develops within one day and lasts for a long time.

Levocetirizine, the (R)-enantiomer of cetirizine, is a selective antagonist of peripheral histamine H1 _receptors .

Blocks H1 _— histamine receptors. The affinity for H1 _— histamine receptors of levocetirizine is 2 times higher than that of cetirizine. It affects the histamine-dependent stage of allergic reactions, reduces the migration of eosinophils, vascular permeability, and limits the release of inflammatory mediators.

Prevents the development and facilitates the course of allergic reactions, has antiexudative, antipruritic, anti-inflammatory effects, and has practically no anticholinergic and antiserotonin effects. In therapeutic doses it has virtually no sedative effect.

Pharmacokinetics

Montelukast

After oral administration, montelukast is quickly and almost completely absorbed from the gastrointestinal tract. In adults, when taken at a dose of 5-10 mg, Cmax _in blood plasma is achieved after 2-3 hours. Bioavailability when taken orally is 64-73%.

The binding of montelukast to plasma proteins is more than 99%. Vd averages 8-11 liters _.

With a single dose of 10 mg 1 time/day, a moderate (about 14%) accumulation of the active substance in plasma is observed.

Montelukast is actively metabolized in the liver. When used in therapeutic doses, the concentration of montelukast metabolites in plasma at steady state in adults and children is not determined.

It is assumed that the isoenzymes CYP3A4 and CYP2C9 are involved in the metabolism of montelukast, while at therapeutic concentrations montelukast does not inhibit the isoenzymes CYP3A4, 2C9, 1A2, 2A6, 2C19 and 2D6.

T1 _/2 of montelukast in young healthy adults ranges from 2.7 to 5.5 hours. The clearance of montelukast in healthy adults averages 45 ml/min. After oral administration of montelukast, 86% is excreted in feces within 5 days and less than 0.2% is excreted in urine, confirming that montelukast and its metabolites are excreted almost exclusively in bile.

Levocetirizine

After oral administration, levocetirizine is rapidly absorbed from the gastrointestinal tract. Eating does not affect the completeness of absorption, although its speed decreases. Cmax in blood plasma _is reached 0.9 hours after a single oral dose. The equilibrium state is achieved after 2 days. Cmax after a single and repeated (5 mg daily) dose is 270 ng/ml and 308 ng/ml, respectively _.

Plasma protein binding is 90%. There are no data on the distribution of the drug in tissues and penetration through the BBB. Vd _is 0.4 l/kg. Excreted in breast milk.

Less than 14% of the administered dose is metabolized in the liver by aromatic ring oxidation, N- and O-dealkylation, and conjugation with taurine. Dealkylation is predominantly catalyzed by CYP3A4, and CYP isoforms are involved in the oxidation of the aromatic ring. Levocetirizine does not affect the activity of the isoenzymes CYP1A2, 2C9, 2C19, 2D6, 2E1 and 3A4 at concentrations much higher than peak concentrations after oral administration of 5 mg due to negligible metabolism and the lack of metabolic suppression; interaction of levocetirizine with other substances is unlikely.

T1 _/2 is 7.9±1.9 hours. The total clearance is 0.63 ml/min/kg. Levocetirizine and its metabolite are excreted primarily by the kidneys (85.4% of the dose taken), through glomerular filtration and active tubular secretion. Excretion through the intestines is 12.9%.

Indications for use

Prevention and long-term treatment of bronchial asthma, including prevention of symptoms of the disease during the day and night; treatment of bronchial asthma in patients with hypersensitivity to acetylsalicylic acid; prevention of bronchospasm caused by physical activity.

The drug is indicated for the treatment of symptoms of seasonal or chronic allergic rhinitis; for the prevention of seasonal allergic rhinitis and the treatment of asthma accompanied by allergic rhinitis.

The drug also relieves the symptoms of seasonal allergic rhinitis.

Indicated for the prevention of asthma, in which the dominant component is exercise-induced bronchospasm.

Directions for use and doses

Children (2-5 years): 5 ml 1 time per day (in the evening, 1 hour before or 2 hours after meals). Due to the lack of clinical data, the use of this product in children under 2 years of age is not recommended.

Side effects

Infections and infestations: very often — infections of the upper respiratory tract.

Disorders of the blood and lymphatic system: rarely — increased tendency to bleeding.

Immune system disorders: uncommon – hypersensitivity reactions, including anaphylaxis; very rarely — eosinophilic infiltration of the liver.

Mental disorders: uncommon — pathological dreams, including nightmares, insomnia, somnambulism, restlessness, agitation, including aggressive behavior or hostility, depression, psychomotor hyperactivity (including irritability, restlessness and tremor ^* ); rarely — memory impairment, impaired attention; very rarely — hallucinations, disorientation, suicidal thoughts and behavior (suicidality).

Nervous system disorders: uncommon – dizziness, drowsiness, paresthesia/hypesthesia, convulsions.

Cardiac disorders: rarely – palpitations.

Disorders of the respiratory system, chest and mediastinal organs: infrequently — nosebleeds; very rarely — Churg-Strauss syndrome, pulmonary eosinophilia.

Gastrointestinal disorders: often – diarrhea, nausea, vomiting; uncommon – dry mouth, dyspepsia.

Disorders of the hepatobiliary system: often — increased levels of transaminases (ALT, AST) in the blood serum; very rarely — hepatitis (including cholestatic, hepatocellular, and mixed liver damage).

Disorders of the skin and subcutaneous tissue: often – rash; uncommon – bruising, urticaria, itching; rarely – angioedema; very rarely — erythema nodosum, erythema multiforme.

Musculoskeletal and connective tissue disorders: uncommon – arthralgia, myalgia, including muscle spasms.

Violations of the general condition and those associated with the method of administration of the drug: often — pyrexia; uncommon – asthenia/fatigue, malaise, edema.

Contraindications

hypersensitivity to levocetirizine, cetirizine, montelukast or other components of the drug;
the drug is also contraindicated in patients with severe renal failure with creatinine clearance less than 10 ml/min and in patients undergoing hemodialysis.

Drug interactions

Montelukast

With a single dose of 10 mg of montelukast during phenobarbital therapy, the AUC of montelukast is reduced by 40%. There are no recommendations for dose adjustments of montelukast. The advisability of adequate clinical monitoring of patients who, during therapy with montelukast, receive drugs that have the ability to induce the cytochrome P450 system, such as phenobarbital, phenytoin, rifampicin, is noted.

Levocetirizine

A decrease in the clearance of cetirizine (16%) was observed with repeated administrations of theophylline (400 mg 1 time/day); however, the pharmacokinetics of theophylline did not change with simultaneous administration of cetirizine.

In susceptible patients, concomitant use of levocetirizine and ethanol or other CNS depressants may result in potentiation of the CNS depressant effect.

special instructions

Montelukast

It is not recommended to use montelukast to relieve brochospasm during acute attacks of bronchial asthma, including status asthmaticus.

In rare cases, systemic eosinophilia has developed in patients with asthma receiving montelukast, sometimes accompanied by a clinical picture of systemic vasculitis consistent with Churg-Strauss syndrome, a condition often requiring systemic corticosteroids. It is noted that the development of this formidable condition is often, although not in all cases, preceded by a reduction in doses of oral forms of glucocorticosteroids. Specialists should be attentive to the appearance in patients taking monelukast of symptoms such as systemic eosinophilia, hemorrhagic rashes (corresponding to the vasculitic purpuric type of bleeding), deterioration in respiratory function, cardiac complaints, and complaints associated with neuropathy. At the same time, it should be noted that a reliable cause-and-effect relationship between taking montelukast and the development of these pathological conditions has not been established.

Levocetirizine

Elderly patients with moderate or severe renal impairment may require dosage adjustment.

Patients with impaired renal function require adjustment of the dosage regimen depending on creatinine clearance.

Patients with isolated liver dysfunction do not require any dose changes. For patients with concomitant impairment of liver and kidney function, dose adjustment is recommended.

Patients should avoid drinking alcohol while using levocetirizine.

Pregnancy and lactation

Since sufficient, controlled clinical studies of the safety of the use of montelukast or levocetirizine during pregnancy in humans have not been conducted, the drug can be prescribed only in cases of extreme necessity.

Since levocetirizine is excreted in breast milk, taking the drug during breastfeeding is not recommended.

Impact on the ability to drive vehicles and operate machinery

Comparative clinical studies showed no evidence of impairment in wakefulness, reaction time, or driving ability after taking recommended doses of levocetirizine. However, some patients may experience drowsiness, fatigue, or asthenia during use. It should be used with caution in patients driving vehicles and engaging in activities that require rapid psychomotor reactions.

Overdose

Symptoms : increased side effects.

Treatment : gastric lavage; carry out symptomatic and supportive therapy.

Release form

Orange suspension in a 30 ml dark glass bottle. 1 bottle complete with 10 ml measuring cup in a cardboard box with instructions for medical use.

Storage conditions:

Store at a temperature not exceeding 30°C in a dry place. Protect from light.

Keep out of the reach of children.

Best before date

3 years.

Do not use after expiration date.

Conditions for dispensing from pharmacies

On prescription.

Manufacturer

«CORAL LABORATORIES LTD.»

Plot No.57/1 (16), Bhenslore,

Dunetha, Nani Daman-396 210, India

Email: exports@corallab.com

Website: www.corallab.com

Name and address of the organization accepting claims (suggestions) regarding the quality of the medicinal product in the territory of the Republic of Uzbekistan

SHAYANA FARM LLC

700057, Republic of Uzbekistan, Tashkent, st. Usta Shirin, building 117.

Tel.: 99 (871) 2281692(93/94)

Fax: 99 (871) 2281695

MONTELEKOR

Price on Request

MONTELEKOR

Price on Request