Muloz

Each chewable tablet contains Montelukast sodium equivalent to Montelukast 5 mg.
A pink brown, round, biconvex tablet engraved with "
Click on icon to see table/diagram/image
" logo on one side and "M" above "5" on the other side.

Pharmacology:Pharmacodynamics: Montelukast sodium is a selective and competitive leukotriene receptor antagonist that affects inflammatory processes involved in asthma and allergic rhinitis. Montelukast is a selective leukotriene receptor antagonist of the cysteinyl leukotriene (CysLT) receptor.
The cysteinyl leukotrienes (LTC₄, LTD₄, LTE₄) are products of arachidonic acid metabolism and are released from various cells, including mast cells and eosinophils. These eicosanoids bind to CysLT receptors. Cysteinyl leukotriene production and receptor occupation have been correlated with the pathophysiology of allergic rhinitis and asthma, including airway edema, smooth muscle constriction, and altered cellular activity associated with the inflammatory process. The CysLT type 1 (CysLT₁) receptor is found in the human airway (including airway smooth muscle cells and airway macrophages) and on other proinflammatory cells (including eosinophils and certain myeloid stem cells). Montelukast binding to the CysLT₁ receptor is high-affinity and selective, preferring the CysLT₁ receptor to other pharmacologically important airway receptors, such as the prostanoid, cholinergic, or beta-adrenergic receptor. Montelukast inhibits physiologic actions of LTD₄ at the CysLT₁ receptor, without any agonist activity.
Pharmacokinetics: Absorption: Montelukast is rapidly absorbed from the GI tract. For the 5 mg chewable tablet, the C_max is achieved in 2 hours after administration in adults in the fasted state. The mean oral bioavailability in adults is 73%.
Distribution: Montelukast is more than 99% bound to plasma proteins. The steady-state volume of distribution of Montelukast is 8-11 L.
Metabolism: Montelukast is extensively metabolized in the liver by cytochrome P450 isoenzymes, mainly by CYP2C8 and to a lesser extent by CYP3A4 and CYP2C9.
Excretion: The mean plasma half-life of Montelukast is 2.7-5.5 hours. The plasma clearance of Montelukast averages 45 mL/min. Following an oral dose of radiolabeled Montelukast, 86% of the radioactivity was recovered feces and <0.2% was recovered in urine. Montelukast is excreted principally in bile as unchanged drug and metabolites.

MULOZ (5 MG CHEWABLE TABLET) is indicated in adult and pediatric patients 6 months of age and older for the prophylaxis and chronic treatment of asthma, including the prevention of day- and nighttime symptoms, the treatment of aspirin-sensitive asthmatic patients, and the prevention of exercise-induced bronchoconstriction.
MULOZ (5 MG CHEWABLE TABLET) is indicated for the relief of daytime and nighttime symptoms of allergic rhinitis (seasonal allergic rhinitis in adults and pediatric patients 2 years of age and older, and perennial allergic rhinitis in adults and pediatric patients 6 months of age and older).

For mild persistent asthmatic, MULOZ (5 MG CHEWABLE TABLET) should be taken once daily. For moderate to severe asthma, MULOZ (5 MG CHEWABLE TABLET) should be taken once daily concomitantly with inhaled corticosteroids to provide additional benefit. The dose should be taken in the evening.
For allergic rhinitis, MULOZ (5 MG CHEWABLE TABLET) should be taken once daily. In patients who are not adequately controlled on the standard therapy according to specialized physicians' consideration, concomitant administration of MULOZ (5 MG CHEWABLE TABLET) may result in further improvement of symptoms. The time of administration may be individualized to suit patient needs. Patients with both asthma and allergic rhinitis should take only one dose in the evening.
Adults 15 years of age and older with asthma and/or allergic rhinitis: The dosage of adults 15 years of age and older is 10 mg once daily.
Pediatric patients 6 to 14 years of age with asthma and/or allergic rhinitis: The dosage of pediatric patients 6 to 14 years of age is 5 mg once daily.
For prevention of exercise-induced bronchoconstriction, MULOZ (5 MG CHEWABLE TABLET) should be administered at least 2 hours before exercise. Patients already taking MULOZ (5 MG CHEWABLE TABLET) for another indication, including chronic asthma, should not take an additional dose of the drug to prevent exercise-induced bronchoconstriction. All patients should have a short-acting β₂-agonist available for exacerbations of asthma that may occur after exercise despite Montelukast therapy.
Adults and adolescent 15 years of age and older: The usual dosage of adults and adolescent 15 years of age or older is 10 mg. An additional dose should not be taken within 24 hours of the previous dose.
Children 6-14 years of age: The usual dosage of children 6-14 years of age is 5 mg. An additional dose should not be taken within 24 hours of the previous dose.
General recommendations: The therapeutic effect of MULOZ (5 MG CHEWABLE TABLET) on parameters of asthma control occurs within one day. MULOZ (5 MG CHEWABLE TABLET) can be taken with or without food. Patients should be advised to continue taking MULOZ (5 MG CHEWABLE TABLET) while their asthma is controlled, as well as during periods of worsening asthma.
No dosage adjustment is necessary for pediatric patients, for the elderly, for patients with renal insufficiency, or mild-to-moderate hepatic impairment, or for patients of either gender.
Therapy with MULOZ (5 MG CHEWABLE TABLET) in relation to other treatments of asthma MULOZ (5 MG CHEWABLE TABLET) can be added to a patient's existing treatment regimen.
Reduction in concomitant therapy: Bronchodilator treatments: MULOZ (5 MG CHEWABLE TABLET) can be added to the treatment regimen of patients who are not adequately controlled on bronchodilator alone. When a clinical response is evident (usually after the first dose), the patient's bronchodilator therapy can be reduced as tolerated.
Inhaled corticosteroids: Treatment with MULOZ (5 MG CHEWABLE TABLET) provides additional clinical benefit to patients treated with inhaled corticosteroids. A reduction in the corticosteroid dose can be made as tolerated. The dose should be reduced gradually with medical supervision. In some patients, the dose of inhaled corticosteroids can be tapered off completely. MULOZ (5 MG CHEWABLE TABLET) should not be abruptly substituted for inhaled corticosteroids.

Montelukast has been administered to adults with asthma in dosages up to 200 mg daily for 22 weeks, and in dosages up to 900 mg daily for approximately 1 week without clinically important adverse experiences. There have been reports of acute overdosage with Montelukast doses of up to 1 g in adults and children. The most frequently reported adverse experiences that were reported included abdominal pain, somnolence, thirst, headache, vomiting, and psychomotor hyperactivity.
If acute overdosage of Montelukast occurs, supportive and symptomatic treatment should be initiated and the patient closely observed. If indicated, unabsorbed material should be removed from the GI tract. Whether peritoneal dialysis or hemodialysis removes Montelukast is unknown.

Hypersensitivity to Montelukast or any component of the formulation.

Montelukast is not indicated for use in the relief of bronchospasm in acute asthma attacks, including status asthmaticus. Continue therapy during acute exacerbations of asthma. Advise patients to have appropriate rescue medication available. Patients receiving Montelukast should be provided with and instructed in the use of a short-acting, inhaled β₂-adrenergic bronchodilator as supplement therapy for acute asthma symptoms.
While the dose of concomitant inhaled corticosteroids may be reduced gradually under medical supervision. Montelukast should not be abruptly substituted for oral or inhaled corticosteroids.
Neuropsychiatric events have been reported in adult, adolescent, and pediatric patients taking Montelukast. Be alert for neuropsychiatric events and instruct patients to report the occurrence of these changes. Carefully evaluate the risks and benefits of continuing treatment if such events occur.
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. 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.

Pregnancy: There are no adequate and well-controlled studies to date using Montelukast in pregnant women. Montelukast should be used during pregnancy only when clearly needed. A causal relationship between Montelukast use and the development of these congenital anomalies has not been established.
Lactation: Since it is not known whether Montelukast is distributed in human milk, the drug should be used with caution in nursing women.

The adverse reactions from the use of Montelukast may occur: Infections and infestations: Upper respiratory infection.
Blood and lymphatic system disorders: Increased bleeding tendency, thrombocytopenia.
Immune system disorders: Hypersensitivity reactions including anaphylaxis, hepatic eosinophilic infiltration.
Psychiatric disorders: Hyperkinesia, agitation including aggressive behavior or hostility, anxiousness, depression, disorientation, disturbance in attention, dream abnormalities, dysphemia (stuttering), hallucinations, insomnia, memory impairment, obsessive-compulsive symptoms, psychomotor hyperactivity (including irritability, restlessness and tremor), somnambulism, suicidal thinking and behavior (suicidally), tic.
Nervous system disorders: Headache, dizziness, drowsiness, paresthesia/hypoesthesia, seizure.
Cardiac disorders: Palpitations.
Respiratory, thoracic and mediastinal disorders: Asthma, epistaxis, eosinophilic granulomatosis with polyangiitis (Churg-Strauss Syndrome), pulmonary eosinophilia.
Gastrointestinal disorders: Abdominal pain, diarrhea, dyspepsia, nausea, vomiting, dry mouth.
Hepatobiliary disorders: Increased ALT and AST, hepatitis (including cholestatic, hepatocellular, mixed pattern liver injury).
Skin and subcutaneous tissue disorders: Eczematous dermatitis, angioedema, bruising, erythema multiforme, erythema nodosum, pruritus, rash, urticaria.
Musculoskeletal and connective tissue disorders: Arthralgia, myalgia including muscle cramps.
Renal and urinary disorders: Enuresis in children.
General disorders and administration site conditions: Thirst, asthenia/fatigue, edema, pyrexia.

Montelukast may be administered with other therapies routinely used in the prophylaxis and chronic treatment of asthma. In drug-interactions studies, the recommended clinical dose of Montelukast did not have clinically important effects on the pharmacokinetics of the following medicinal products: theophylline, prednisone, prednisolone, oral contraceptives (ethinyl estradiol/norethindrone 35/1), terfenadine, digoxin and warfarin.
The area under the plasma concentration-time curve (AUC) for Montelukast was decreased approximately 40% in subjects with co-administration of phenobarbital. However, no dosage adjustment for Montelukast is recommended.
Data from in vitro studies indicate that Montelukast is a potent inhibitor of CYP2C8. However, data from several clinical drug interaction studies evaluating Montelukast and rosiglitazone or repaglinide, substrates for the CYP2C8 isoenzyme, indicate that Montelukast does not inhibit CYP2C8 in vivo. Therefore, clinical drug interactions involving Montelukast and CYP2C8 substrates (e.g., paclitaxel, rosiglitazone, repaglinide) are not anticipated.
In vitro studies have shown that Montelukast is a substrate of CYP2C8, CYP2C9 and CYP3A4. In a clinical drug-drug interaction study involving Montelukast and gemfibrozil (an inhibitor of both CYP2C8 and 2C9) demonstrated that gemfibrozil increased the systemic exposure of Montelukast by 4.4-fold. Coadministration of itraconazole, a strong CYP3A4 inhibitor, with gemfibrozil and Montelukast did not further increase the systemic exposure of Montelukast. The effect of gemfibrozil on systemic exposure of Montelukast is not considered to be clinically meaningful based on clinical safety data with doses greater than the 10 mg approved dose in adults (e.g., 200 mg/day to adult patients for 22 weeks, and up to 900 mg/day to patients for approximately one week) where clinically important adverse experiences were not observed. Therefore, no dosage adjustment of Montelukast is required upon co-administration with gemfibrozil. Based on in vitro data, clinically important drug interactions with other known inhibitors of CYP2C8 (e.g., trimethoprim) are not anticipated. In addition, co-administration of Montelukast with itraconazole alone resulted in no significant increase in the systemic exposure of Montelukast.

Store below 30°C.
Protect from moisture and light.

Antiasthmatic & COPD Preparations / Antihistamines & Antiallergics

R03DC03 - montelukast ; Belongs to the class of leukotriene receptor antagonists. Used in the systemic treatment of obstructive airway diseases.

D