Monax - instructions for use, dose, side effects, contraindications

Excipients: Mannitol - 192.38 mg (Pearlitol® 300 DC - 75%, Parteck™ 100 M - 25%), Avicel CE-15 (microcrystalline cellulose - 85%, guar gum - 15%) - 21.38 mg, croscarmellose sodium - 9.6 mg, giprolose (low substituted) - 7.2 mg, cherry flavor - 0.24 mg, ferric oxide red oxide - 0.24 mg, magnesium stearate - 4.8 mg.

Each 5 mg chewing tablet contains:

Active substance: montelukast - 5,00 mg (in the form of sodium montelukast 5,20 mg).

Auxiliary matter: mannitol - 240,475 mg (Pearlitol® 300 DC - 75%, Parteck ™ 100 M - 25%), Avicel CE-15 (microcrystalline cellulose - 85%, gum guar - 15%) - 26,725 mg, croscarmellose sodium - 12,00 mg, giprolase (low-substituted) - 9,0 mg, flavoring cherry - 0,3 mg, dye gland oxide red - 0,3 mg, magnesium stearate - 6,0 mg.

Description:

Tablets 4 mg: Oval, biconvex tablets are pink in color with light pink patches.

Tablets 5 mg: Round, biconvex tablets of pink color with light pink impregnations.

Pharmacotherapeutic group:anti-inflammatory anti-bronchoconstrictive agent - leukotriene receptor blocker

ATX: & nbsp

R.03.D.C.03 Montelukast

Pharmacodynamics:

A leukotriene receptor antagonist. Montelukast inhibits cysteinyl leukotriene receptors of the respiratory epithelium, while exhibiting the ability to inhibit bronchospasm due to the inhalation of cysteinyl leukotriene LTD₄ in patients with bronchial asthma. Doses 5 mg is sufficient to stop the bronchospasm induced by LTD₄. The use of montelukast in doses exceeding 10 mg once a day does not improve the effectiveness of the drug.

Montelukast causes bronchodilation within 2 hours after ingestion and may supplement the bronchodilation induced by beta₂-adrenomimetics.

Pharmacokinetics:

Suction: After oral administration montelukast quickly absorbed. Reception of usual food does not affect FROM_mOh at blood plasma and bioavailability of the drug. FROM_m_Oh in adults after taking an empty stomach 5 mg of chewable tablet was reached after two hours.The average oral bioavailability was 73%. FROM_m_Oh after taking an empty stomach chewing tablet 4 mg children aged 2 to 5 years was reached after two hours

Distribution: Montelukast binds to blood plasma proteins for more than 99%. The volume of distribution in a state of stable equilibrium averages 8-11 liters.

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

It is assumed that the isoenzymes of cytochrome P450 (3A4 and 2C9) are involved in the metabolism of montelukast, while in therapeutic concentrations montelukast does not inhibit cytochrome P450 isoenzymes: 3A4, 2C9,1A2, 2A6, 2C19 and 2D6.

Excretion: The clearance of montelukast is 45 ml / min in healthy adults. The half-life (T_1/2) montelukast in young healthy adults is from 2.7 to 5.5 h. After taking montelukast, an 86% dose is excreted through the intestine for 5 days and less than 0.2% - kidneys, which confirms that montelukast and its metabolites are excreted almost exclusively through the intestine.

When taking montelukast in the morning and evening hours, there is no difference in pharmacokinetics.

Indications:

1. Prophylaxis and long-term treatment of bronchial asthma, including:

- prevention of day and night symptoms of the disease;

- treatment of bronchial asthma in patients with hypersensitivity to acetylsalicylic acid;

- the prevention of bronchospasm, caused by physical exertion.

2. Cupping of day and night symptoms of seasonal allergic rhinitis and all-the-year-round allergic rhinitis.

Contraindications:

- Hypersensitivity to the components of the drug.

- Children under 6 years old for tablets 5 mg and up to 2 years for tablets 4 mg.

Carefully:AT period of pregnancy and breastfeeding.

Pregnancy and lactation:

The drug should be used during pregnancy and during breastfeeding only in cases where the expected benefit for the mother exceeds the potential risk to the fetus or child.

Dosing and Administration:

The drug is taken orally 1 time per day, regardless of food intake. The tablet can be swallowed whole or chewed before swallowing.

For treatment of bronchial asthma the drug should be taken in the evening.

When treatment of allergic rhinitis the drug can be taken at any time of the day.

Children aged from 2 before 5 years: one chewable tablet 4 mg daily.

Children aged 6 to 14 years: one chewable tablet 5 mg daily.

Children over 14 years and adults: two chewable tablets 5 mg once, daily.

The therapeutic effect of the drug on the indicators reflecting the course of bronchial asthma develops during the first day. The patient should continue to take MONAX® both during the control period of symptoms of bronchial asthma and during the period of exacerbation of the disease.

For elderly patients, patients with renal insufficiency, patients with mild or moderate hepatic impairment special selection of the dose is not required.

MONAX® can be added to treatment with bronchodilators and inhaled glucocorticosteroids (GCS).

Side effects:

Frequency of adverse effects: very often (≥ 10%), often (≥ 1%, but <10%), infrequently (≥ 0.1%, but <1%), rarely (≥ 0.01%, but <0.1%), very rarely (<0.01%), including individual reports.

Immune system disorders: very rarely anaphylaxis, angioedema, eosinophilic liver infiltrates.

Violations of the blood and lymphatic system: very rarely - increased bleeding.

Disturbances from the nervous system: often - headache, dizziness; very rarely - drowsiness, paresthesia / hypoesthesia, convulsive seizures, tremor.

Disorders of the psyche: often fatigue; very rarely - excitability, aggressive behavior, anxiety, abnormal dreams, hallucinations, depression, insomnia, irritability, suicidal thinking and behavior.

Heart Disease: very rarely - palpitations.

Disorders from the gastrointestinal tract: often - abdominal pain, diarrhea, dyspepsia, nausea; very rarely - vomiting, pancreatitis.

Disturbances from the liver and bile ducts: rarely - cholestatic hepatitis, damage to hepatocytes on the background of drug therapy or concomitant liver pathology (alcohol and other forms of hepatitis), increased activity of hepatic transaminases.

Disturbances from musculoskeletal and connective tissue: very rarely - arthralgia, myalgia, including muscle cramps.

Disturbances from the skin and subcutaneous tissues: often - hives, rash; very rarely - a tendency to form a hematoma, nodular erythema, itching.

General disorders: often - thirst.

In general, the drug is well tolerated. Side effects are usually mild and, as a rule, do not require withdrawal of treatment.

Overdose:

In case of acute overdose of montelukast (intake of at least 1000 mg per day), the most frequent side effects were: thirst, drowsiness, vomiting, psychomotor agitation, headache and abdominal pain.

Treatment: gastric lavage, symptomatic therapy.

Data on the effectiveness of peritoneal dialysis or hemodialysis Montelukast no.

Interaction:

The drug can be prescribed together with other medications traditionally used for the prevention and long-term treatment of bronchial asthma.

Montelukast at the recommended therapeutic dose did not have a clinically significant effect on the pharmacokinetics of the following drugs: theophylline, prednisone, prednisolone, oral contraceptives (ethinyl estradiol / norethindrone 35/1), terfenadine, digoxin and warfarin.

Phenobarbital accelerates the metabolism of Montelukast in the liver. At simultaneous appointment to patients of phenobarbital and montelukast the area under a curve "concentration-time" (AUC) decreased by approximately 40%.However, dose adjustment is not required.

Combined treatment with bronchodilators:

If the bronchodilators are ineffective, mona therapy of bronchial asthma can be supplemented with MONAX®. When the therapeutic effect is achieved (usually after the first dose), the dose of bronchodilators can be gradually reduced against the background of therapy with montelukast.

Combined treatment with inhaled glucocorticosteroids:

The use of montelukast provides an additional therapeutic effect in patients receiving inhaled glucocorticosteroids. At achievement of stabilization of a status of the patient reduction of a dose of GCS is possible. The dose of GCS should be reduced gradually, under the supervision of a doctor. In some cases, the intake of inhaled glucocorticosteroids can be reversed completely. However, a sharp substitution of inhaled glucocorticosteroids for montelukast Not recommended.

Special instructions:

The drug is not recommended for the treatment of acute attacks of bronchial asthma. In the acute course of bronchial asthma, patients should be prescribed medications for conduction and prevention of seizure therapy.

Treatment with Montelukast does not guarantee absolute prevention of exacerbations, therefore it is recommended that patients with bronchial asthma always have emergency medications. In the event of an acute attack of bronchial asthma, an inhaled beta-agonist of rapid action should be used.

The dose of inhaled glucocorticosteroids used simultaneously with oral montelukast should be reduced gradually under the supervision of a physician. Sharp replacement of inhaled or oral GCS with MONAX® is not allowed.

In patients with aspirin asthma, treatment with montelukast does not negate the need to avoid taking aspirin and other non-steroidal anti-inflammatory drugs.

A decrease in the systemic dose of GCS in patients receiving antiasthmatic drugs, including leukotriene receptor antagonists, was rarely accompanied by the appearance of one or more of the following: eosinophilia, vascular rash, aggravation of lung symptoms, cardiac complications and / or neuropathy, sometimes diagnosed as a syndrome Charge-Ostrich - systemic eosinophilic vasculitis.Although the causal relationship of these adverse events with therapy of leukotriene receptor antagonists has not been established, with a reduction in the systemic dose of GCS in patients taking montelukast, you must be careful and provide them with appropriate medical supervision.

Age differences in the efficacy and safety of montelukast were not revealed.

Effect on the ability to drive transp. cf. and fur:

There is no data on the influence of MONAX® on the ability to drive and other mechanisms. However, due to the fact that the use of MONAX® in some patients may be accompanied by undesirable effects in the form of drowsiness and dizziness, care should be taken when controlling vehicles and mechanisms and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions. In case of occurrence of similar by-effects it is necessary to address to the doctor.

Form release / dosage:Chewable tablets, 4 mg and 5 mg.

Packaging:

For 14 tablets in a blister of Al / Al.

For 2 or 6 blisters in a cardboard pack together with instructions for use.

Storage conditions:In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-001979

Date of registration:23.01.2013 / 25.04.2016

Expiration Date:23.01.2018

The owner of the registration certificate:Zentiva Saalyk Yuryunleri Sanayi ve Tidjaret A.Sh.Zentiva Saalyk Yuryunleri Sanayi ve Tidjaret A.Sh. Turkey

Manufacturer: & nbsp

ZENTIVA SAGLIK URUNLERI SANAYI VE TICARET, A.S. Turkey

Representation: & nbspZENTIVA PHARMA, LLCZENTIVA PHARMA, LLC

Information update date: & nbsp04.10.2016

Illustrated instructions

Instructions

Monax® (Monax®)