×
Components:
Montelukast
Method of action:
Anti-Bronchoconstrictive, Anti-Inflammatory, Bronchodilator, Drugs For Obstructive Airway Diseases
Available in countries
See all
close
Medically reviewed by Kovalenko Svetlana Olegovna, PharmD. Last updated on 2019.12.16

Name of the medicinal product

Kokast

Qualitative and quantitative composition

Montelukast

Therapeutic indications

The information provided in Therapeutic indications of Kokast is based on data of another medicine with exactly the same composition as the Kokast of the medicine (Montelukast). Be careful and be sure to specify the information on the section Therapeutic indications in the instructions to the drug Kokast directly from the package or from the pharmacist at the pharmacy.
more... close

Kokast is indicated in the treatment of asthma as add-on therapy in those patients with mild to moderate persistent asthma who are inadequately controlled on inhaled corticosteroids and in whom “as-needed” short acting β-agonists provide inadequate clinical control of asthma. In those asthmatic patients in whom Kokast is indicated in asthma, Kokast can also provide symptomatic relief of seasonal allergic rhinitis.

Kokast is also indicated in the prophylaxis of asthma in which the predominant component is exercise-induced bronchoconstriction.

Dosage (Posology) and method of administration

The information provided in Dosage (Posology) and method of administration of Kokast is based on data of another medicine with exactly the same composition as the Kokast of the medicine (Montelukast). Be careful and be sure to specify the information on the section Dosage (Posology) and method of administration in the instructions to the drug Kokast directly from the package or from the pharmacist at the pharmacy.
more... close

Posology

The recommended dose for adults and adolescents 15 years of age and older with asthma, or with asthma and concomitant seasonal allergic rhinitis, is one 10 mg tablet daily to be taken in the evening.

General recommendations

The therapeutic effect of Kokast on parameters of asthma control occurs within one day. Kokast may be taken with or without food. Patients should be advised to continue taking Kokast even if their asthma is under control, as well as during periods of worsening asthma. Kokast should not be used concomitantly with other products containing the same active ingredient, montelukast.

No dosage adjustment is necessary for the elderly, or for patients with renal insufficiency, or mild to moderate hepatic impairment. There are no data on patients with severe hepatic impairment. The dosage is the same for both male and female patients.

Therapy with Kokast in relation to other treatments for asthma

Kokast can be added to a patient's existing treatment regimen.

Inhaled corticosteroids: Treatment with Kokast can be used as add-on therapy in patients when inhaled corticosteroids plus “as needed” short acting β-agonists provide inadequate clinical control. Kokast should not be abruptly substituted for inhaled corticosteroids.

Paediatric population

Do not give Kokast 10 mg film-coated tablets to children less than 15 years of age. The safety and efficacy of Kokast 10 mg film-coated tablets in children less than 15 years has not been established.

5 mg chewable tablets are available for paediatric patients 6 to 14 years of age.

4 mg chewable tablets are available for paediatric patients 2 to 5 years of age.

4 mg granules are available for paediatric patients 6 months to 5 years of age.

Method of administration

Oral use.

Contraindications

The information provided in Contraindications of Kokast is based on data of another medicine with exactly the same composition as the Kokast of the medicine (Montelukast). Be careful and be sure to specify the information on the section Contraindications in the instructions to the drug Kokast directly from the package or from the pharmacist at the pharmacy.
more... close
<

Special warnings and precautions for use

The information provided in Special warnings and precautions for use of Kokast is based on data of another medicine with exactly the same composition as the Kokast of the medicine (Montelukast). Be careful and be sure to specify the information on the section Special warnings and precautions for use in the instructions to the drug Kokast directly from the package or from the pharmacist at the pharmacy.
more... close

Patients should be advised never to use oral montelukast to treat acute asthma attacks and to keep their usual appropriate rescue medication for this purpose readily available. If an acute attack occurs, a short-acting inhaled β-agonist should be used. Patients should seek their doctors' advice as soon as possible if they need more inhalations of short-acting β-agonists than usual.

Montelukast should not be substituted abruptly for inhaled or oral corticosteroids.

There are no data demonstrating that oral corticosteroids can be reduced when montelukast is given concomitantly.

In rare cases, patients on therapy with anti-asthma agents including montelukast may present with systemic eosinophilia, sometimes presenting with clinical features of vasculitis consistent with Churg-Strauss syndrome, a condition which is often treated with systemic corticosteroid therapy. These cases have been sometimes associated with the reduction or withdrawal of oral corticosteroid therapy. Although a causal relationship with leukotriene receptor antagonism has not been established, physicians should be alert to eosinophilia, vasculitic rash, worsening pulmonary symptoms, cardiac complications, and/or neuropathy presenting in their patients. Patients who develop these symptoms should be reassessed and their treatment regimens evaluated.

Treatment with montelukast does not alter the need for patients with aspirin-sensitive asthma to avoid taking aspirin and other non-steroidal anti-inflammatory drugs.

Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.

Effects on ability to drive and use machines

The information provided in Effects on ability to drive and use machines of Kokast is based on data of another medicine with exactly the same composition as the Kokast of the medicine (Montelukast). Be careful and be sure to specify the information on the section Effects on ability to drive and use machines in the instructions to the drug Kokast directly from the package or from the pharmacist at the pharmacy.
more... close

Kokast has no or negligible influence on the ability to drive and use machines. However, individuals have reported drowsiness or dizziness.

Undesirable effects

The information provided in Undesirable effects of Kokast is based on data of another medicine with exactly the same composition as the Kokast of the medicine (Montelukast). Be careful and be sure to specify the information on the section Undesirable effects in the instructions to the drug Kokast directly from the package or from the pharmacist at the pharmacy.
more... close

Montelukast has been evaluated in clinical studies as follows:

- 10 mg film-coated tablets in approximately 4,000 adult and adolescent asthmatic patients 15 years of age and older.

- 10 mg film-coated tablets in approximately 400 adult and adolescent asthmatic patients with seasonal allergic rhinitis 15 years of age and older.

- 5 mg chewable tablets in approximately 1,750 paediatric asthmatic patients 6 to 14 years of age.

The following drug-related adverse reactions in clinical studies were reported commonly (>1/100 to <1/10) in asthmatic patients treated with montelukast and at a greater incidence than in patients treated with placebo:

Body System Class

Adult and Adolescent Patients

15 years and older

(two 12-week studies; n=795)

Paediatric Patients

6 to 14 years old

(one 8-week study; n=201)

(two 56-week studies; n=615)

Nervous system disorders

headache

headache

Gastro-intestinal disorders

abdominal pain

With prolonged treatment in clinical trials with a limited number of patients for up to 2 years for adults, and up to 12 months for paediatric patients 6 to 14 years of age, the safety profile did not change.

Tabulated list of Adverse Reactions

Adverse reactions reported in post-marketing use are listed, by System Organ Class and specific Adverse Reactions, in the table below. Frequency Categories were estimated based on relevant clinical trials.

System Organ Class

Adverse Reactions

Frequency Category*

Infections and infestations

upper respiratory infectionâ€

Very Common

Blood and lymphatic system disorders

increased bleeding tendency

Rare

Immune system disorders

hypersensitivity reactions including anaphylaxis

Uncommon

hepatic eosinophilic infiltration

Very Rare

Psychiatric disorders

dream abnormalities including nightmares, insomnia, somnambulism, anxiety, agitation including aggressive behaviour or hostility, depression, psychomotor hyperactivity (including irritability, restlessness, tremor§)

Uncommon

disturbance in attention, memory impairment

Rare

hallucinations, disorientation, suicidal thinking and behaviour (suicidality)

Very Rare

Nervous system disorders

dizziness, drowsiness, paraesthesia/hypoesthesia, seizure

Uncommon

Cardiac disorders

palpitations

Rare

Respiratory, thoracic and mediastinal disorders

epistaxis

Uncommon

Churg-Strauss Syndrome (CSS)

Very Rare

pulmonary eosinophilia

Very Rare

Gastrointestinal disorders

diarrhoea‡, nausea‡, vomiting‡

Common

dry mouth, dyspepsia

Uncommon

Hepatobiliary disorders

elevated levels of serum transaminases (ALT, AST)

Common

hepatitis (including cholestatic, hepatocellular, and mixed-pattern liver injury).

Very Rare

Skin and subcutaneous tissue disorders

rash‡

Common

bruising, urticaria, pruritus

Uncommon

angiooedema

Rare

erythema nodosum, erythema multiforme

Very Rare

Musculoskeletal and connective tissue disorders

arthralgia, myalgia including muscle cramps

Uncommon

General disorders and administration site conditions

pyrexia‡

Common

asthenia/fatigue, malaise, oedema

Uncommon

* Frequency Category: Defined for each Adverse Reaction by the incidence reported in the clinical trials data base: Very Common (>1/10), Common (>1/100 to <1/10), Uncommon (>1/1,000 to <1/100), Rare (>1/10,000 to <1/1,000), Very Rare (<1/10,000).

†This adverse experience, reported as Very Common in the patients who received montelukast, was also reported as Very Common in the patients who received placebo in clinical trials.

‡ This adverse experience, reported as Common in the patients who received montelukast, was also reported as Common in the patients who received placebo in clinical trials.

§ Frequency Category: Rare

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via the Yellow Card Scheme at: www.mhra.gov.uk/yellowcard.

Overdose

The information provided in Overdose of Kokast is based on data of another medicine with exactly the same composition as the Kokast of the medicine (Montelukast). Be careful and be sure to specify the information on the section Overdose in the instructions to the drug Kokast directly from the package or from the pharmacist at the pharmacy.
more... close

In chronic asthma studies, montelukast has been administered at doses up to 200 mg/day to adult patients for 22 weeks and in short term studies, up to 900 mg/day to patients for approximately one week without clinically important adverse experiences.

There have been reports of acute overdose in post-marketing experience and clinical studies with montelukast. These include reports in adults and children with a dose as high as 1,000 mg (approximately 61 mg/kg in a 42 month old child). The clinical and laboratory findings observed were consistent with the safety profile in adults and paediatric patients. There were no adverse experiences in the majority of overdose reports.

Symptoms of overdose

The most frequently occurring adverse experiences were consistent with the safety profile of montelukast and included abdominal pain, somnolence, thirst, headache, vomiting, and psychomotor hyperactivity.

Management of overdose

No specific information is available on the treatment of overdose with montelukast. It is not known whether montelukast is dialysable by peritoneal- or haemodialysis.

Pharmacodynamic properties

The information provided in Pharmacodynamic properties of Kokast is based on data of another medicine with exactly the same composition as the Kokast of the medicine (Montelukast). Be careful and be sure to specify the information on the section Pharmacodynamic properties in the instructions to the drug Kokast directly from the package or from the pharmacist at the pharmacy.
more... close

Pharmacotherapeutic group: Leukotriene receptor antagonist

ATC-code: R03D C03

Mechanism of action

The cysteinyl leukotrienes (LTC4, LTD4, LTE4) are potent inflammatory eicosanoids released from various cells including mast cells and eosinophils. These important pro-asthmatic mediators bind to cysteinyl leukotriene (CysLT) receptors. The CysLT type-1 (CysLT1) receptor is found in the human airway (including airway smooth muscle cells and airway macrophages) and on other pro-inflammatory cells (including eosinophils and certain myeloid stem cells). CysLTs have been correlated with the pathophysiology of asthma and allergic rhinitis. In asthma, leukotriene-mediated effects include bronchoconstriction, mucous secretion, vascular permeability, and eosinophil recruitment. In allergic rhinitis, CysLTs are released from the nasal mucosa after allergen exposure during both early- and late-phase reactions and are associated with symptoms of allergic rhinitis. Intranasal challenge with CysLTs has been shown to increase nasal airway resistance and symptoms of nasal obstruction.

Pharmacodynamic effects

Montelukast is an orally active compound which binds with high affinity and selectivity to the CysLT1 receptor. In clinical studies, montelukast inhibits bronchoconstriction due to inhaled LTD4 at doses as low as 5 mg. Bronchodilation was observed within 2 hours of oral administration. The bronchodilation effect caused by a β-agonist was additive to that caused by montelukast. Treatment with montelukast inhibited both early- and late-phase bronchoconstriction due to antigen challenge. Montelukast, compared with placebo, decreased peripheral blood eosinophils in adult and paediatric patients. In a separate study, treatment with montelukast significantly decreased eosinophils in the airways (as measured in sputum) and in peripheral blood while improving clinical asthma control.

Clinical efficacy and safety

In studies in adults, montelukast, 10 mg once daily, compared with placebo, demonstrated significant improvements in morning FEV1 (10.4% vs 2.7% change from baseline), AM peak expiratory flow rate (PEFR) (24.5 L/min vs 3.3 L/min change from baseline), and significant decrease in total β-agonist use (-26.1% vs -4.6% change from baseline). Improvement in patient-reported daytime and nighttime asthma symptoms scores was significantly better than placebo.

Studies in adults demonstrated the ability of montelukast to add to the clinical effect of inhaled corticosteroid (% change from baseline for inhaled beclomethasone plus montelukast vs beclomethasone, respectively for FEV1: 5.43% vs 1.04%; β-agonist use: -8.70% vs 2.64%). Compared with inhaled beclomethasone (200 μg twice daily with a spacer device), montelukast demonstrated a more rapid initial response, although over the 12-week study, beclomethasone provided a greater average treatment effect (% change from baseline for montelukast vs beclomethasone, respectively for FEV1: 7.49% vs 13.3%; β-agonist use: -28.28% vs -43.89%). However, compared with beclomethasone, a high percentage of patients treated with montelukast achieved similar clinical responses (e.g., 50% of patients treated with beclomethasone achieved an improvement in FEV1 of approximately 11% or more over baseline while approximately 42% of patients treated with montelukast achieved the same response).

A clinical study was conducted to evaluate montelukast for the symptomatic treatment of seasonal allergic rhinitis in adult and adolescent asthmatic patients 15 years of age and older with concomitant seasonal allergic rhinitis. In this study, montelukast 10 mg tablets administered once daily demonstrated a statistically significant improvement in the Daily Rhinitis Symptoms score, compared with placebo. The Daily Rhinitis Symptoms score is the average of the Daytime Nasal Symptoms score (mean of nasal congestion, rhinorrhea, sneezing, nasal itching) and the Nighttime Symptoms score (mean of nasal congestion upon awakening, difficulty going to sleep, and nighttime awakenings scores). Global evaluations of allergic rhinitis by patients and physicians were significantly improved, compared with placebo. The evaluation of asthma efficacy was not a primary objective in this study.

In an 8-week study in paediatric patients 6 to 14 years of age, montelukast 5 mg once daily, compared with placebo, significantly improved respiratory function (FEV1 8.71% vs 4.16% change from baseline; AM PEFR 27.9 L/min vs 17.8 L/min change from baseline) and decreased “as-needed”  β-agonist use (-11.7% vs +8.2% change from baseline).

Significant reduction of exercise-induced bronchoconstriction (EIB) was demonstrated in a 12-week study in adults (maximal fall in FEV1 22.33% for montelukast vs 32.40% for placebo; time to recovery to within 5% of baseline FEV1 44.22 min vs 60.64 min). This effect was consistent throughout the 12-week study period. Reduction in EIB was also demonstrated in a short term study in paediatric patients (maximal fall in FEV1 18.27% vs 26.11%; time to recovery to within 5% of baseline FEV1 17.76 min vs 27.98 min). The effect in both studies was demonstrated at the end of the once-daily dosing interval.

In aspirin-sensitive asthmatic patients receiving concomitant inhaled and/or oral corticosteroids, treatment with montelukast, compared with placebo, resulted in significant improvement in asthma control (FEV1 8.55% vs -1.74% change from baseline and decrease in total β-agonist use -27.78% vs 2.09% change from baseline).

Pharmacokinetic properties

The information provided in Pharmacokinetic properties of Kokast is based on data of another medicine with exactly the same composition as the Kokast of the medicine (Montelukast). Be careful and be sure to specify the information on the section Pharmacokinetic properties in the instructions to the drug Kokast directly from the package or from the pharmacist at the pharmacy.
more... close

Absorption

Montelukast is rapidly absorbed following oral administration. For the 10 mg film-coated tablet, the mean peak plasma concentration (Cmax) is achieved 3 hours (Tmax) after administration in adults in the fasted state. The mean oral bioavailability is 64%. The oral bioavailability and Cmax are not influenced by a standard meal. Safety and efficacy were demonstrated in clinical trials where the 10 mg film-coated tablet was administered without regard to the timing of food ingestion.

For the 5 mg chewable tablet, the Cmax is achieved in 2 hours after administration in adults in the fasted state. The mean oral bioavailability is 73% and is decreased to 63% by a standard meal.

Distribution

Montelukast is more than 99% bound to plasma proteins. The steady-state volume of distribution of montelukast averages 8-11 litres. Studies in rats with radiolabelled montelukast indicate minimal distribution across the blood-brain barrier. In addition, concentrations of radiolabelled material at 24 hours post-dose were minimal in all other tissues.

Biotransformation

Montelukast is extensively metabolised. In studies with therapeutic doses, plasma concentrations of metabolites of montelukast are undetectable at steady state in adults and children.

Cytochrome P450 2C8 is the major enzyme in the metabolism of montelukast. Additionally CYP 3A4 and 2C9 may have a minor contribution, although itraconazole, an inhibitor of CYP 3A4, was shown not to change pharmacokinetic variables of montelukast in healthy subjects that received 10 mg montelukast daily. Based on in vitro results in human liver microsomes, therapeutic plasma concentrations of montelukast do not inhibit cytochromes P450 3A4, 2C9, 1A2, 2A6, 2C19, or 2D6. The contribution of metabolites to the therapeutic effect of montelukast is minimal.

Elimination

The plasma clearance of montelukast averages 45 ml/min in healthy adults. Following an oral dose of radiolabeled montelukast, 86% of the radioactivity was recovered in 5-day faecal collections and <0.2% was recovered in urine. Coupled with estimates of montelukast oral bioavailability, this indicates that montelukast and its metabolites are excreted almost exclusively via the bile.

Characteristics in Patients

No dosage adjustment is necessary for the elderly or mild to moderate hepatic insufficiency. Studies in patients with renal impairment have not been undertaken. Because montelukast and its metabolites are eliminated by the biliary route, no dose adjustment is anticipated to be necessary in patients with renal impairment. There are no data on the pharmacokinetics of montelukast in patients with severe hepatic insufficiency (Child-Pugh score >9).

With high doses of montelukast (20- and 60-fold the recommended adult dose), decrease in plasma theophylline concentration was observed. This effect was not seen at the recommended dose of 10 mg once daily.

Preclinical safety data

The information provided in Preclinical safety data of Kokast is based on data of another medicine with exactly the same composition as the Kokast of the medicine (Montelukast). Be careful and be sure to specify the information on the section Preclinical safety data in the instructions to the drug Kokast directly from the package or from the pharmacist at the pharmacy.
more... close

In animal toxicity studies, minor serum biochemical alterations in ALT, glucose, phosphorus and triglycerides were observed which were transient in nature. The signs of toxicity in animals were increased excretion of saliva, gastrointestinal symptoms, loose stools and ion imbalance. These occurred at dosages which provided >17-fold the systemic exposure seen at the clinical dosage. In monkeys, the adverse effects appeared at doses from 150 mg/kg/day (>232-fold the systemic exposure seen at the clinical dose). In animal studies, montelukast did not affect fertility or reproductive performance at systemic exposure exceeding the clinical systemic exposure by greater than 24-fold. A slight decrease in pup body weight was noted in the female fertility study in rats at 200 mg/kg/day (>69-fold the clinical systemic exposure). In studies in rabbits, a higher incidence of incomplete ossification, compared with concurrent control animals, was seen at systemic exposure >24-fold the clinical systemic exposure seen at the clinical dose. No abnormalities were seen in rats. Montelukast has been shown to cross the placental barrier and is excreted in breast milk of animals.

No deaths occurred following a single oral administration of montelukast sodium at doses up to 5,000 mg/kg in mice and rats (15,000 mg/m2 and 30,000 mg/m2 in mice and rats, respectively), the maximum dose tested. This dose is equivalent to 25,000 times the recommended daily adult human dose (based on an adult patient weight of 50 kg).

Montelukast was determined not to be phototoxic in mice for UVA, UVB or visible light spectra at doses up to 500 mg/kg/day (approximately >200-fold based on systemic exposure).

Montelukast was neither mutagenic in in vitro and in vivo tests nor tumorigenic in rodent species.

Incompatibilities

The information provided in Incompatibilities of Kokast is based on data of another medicine with exactly the same composition as the Kokast of the medicine (Montelukast). Be careful and be sure to specify the information on the section Incompatibilities in the instructions to the drug Kokast directly from the package or from the pharmacist at the pharmacy.
more... close

Not applicable.

Special precautions for disposal and other handling

The information provided in Special precautions for disposal and other handling of Kokast is based on data of another medicine with exactly the same composition as the Kokast of the medicine (Montelukast). Be careful and be sure to specify the information on the section Special precautions for disposal and other handling in the instructions to the drug Kokast directly from the package or from the pharmacist at the pharmacy.
more... close

Any unused medicinal product or waste material should be disposed of in accordance with local requirements.

Site feedback

How easy to use our site?

Commentary is required, without it we won't know how to become better
The maximum length of review is 1000 symbols

Thanks!

You help us to become better