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Therapeutic Category
- RESPIRATORY TRACT DRUGS
- Pharmaceutical Form : Film coated tablets
- Composition : Montelukast sodium 10.4 mg Eq. Montelukast 10 mg /F.C.Tab
- Active Substance : Montelukast sodium
Description:
Montelukast Sodium is a selective and orally active leukotriene receptor antagonist that inhibits the Cysteinyl leukatrine (CysL.T1) receptor.
Mechanism of action:
The Cysteinyl leukotrines (LTC4, LTD4, and LTE4) are products of arachidonic acid metabolism and released from various cells, including mast cells and eosinophils. CysL.Ts have been correlated with the pathophysiology of asthma and allergic rhinitis. Montelukast binds with high affinity and selectivity to the CysL.T1 receptor in preference to other pharmacologically important airway receptors. Montelukast inhibits physiologic actions of LTD4 at the CysL.T1 receptor without any agonist activity.
Pharmacokineties:
Absorption: Montelukast is rapidly absorbed following oral administration, the mean peak montelukast plasma concentration (Cmax) is achieved in 3 to 4 hours (Tmax), the mean oral bioavailability is 64%.
Distribution: Montelukast is more than 99% bound to plasma proteins. Its steady state volume of distribution average 8 to 11 liters.
Metabolism: Montelukast is extensively metabolized in liver.
Elimination: Montelukast and its metabolites are almost excreted exclusively via the bite.
Indications:
- Montelukast is indicated for the prophylaxis and chronic treatment of asthma in adults and pediatric patients 12 months of age and older.
- It is indicated for the prevention of exercise induced bronchoconstriction in patients 6 years of age and older.
- It is indicated for the relief of symptoms of seasonal allergic rhinitis in patient 2 years of age and older and perennial allergic rhinitis in patients 6 months of age and older.
Contraindications:
Hypersensitivity to any component of this product
Dosage and administrations:
Asthma:
Montelukast should be taken once daily in the evening. The following doses are recommended:
- For adults and adolescents 15 years of age and older: one 10-mg tablet.
- For pediatric patients 6 to 14 years of age: one 5-mg chewable tablet.
- For pediatric patients 2 to 5 years of age: one 4-mg chewable tablet or one packet of 4-mg (oral granules).
- For pediatric patients 12 to 23 months of age: one packet of 4-mg oral granules.
Safety and effectiveness in pediatric patients less than 12 months of age with asthma have not been established.
Exercise-Induced Bronchoconstriction (EIB)
For prevention of EIB, a single dose of Montelukast should be taken at least 2 hours before exercise.
- For adults and adolescents 15 years of age and older: one 10-mg tablet.
- For pediatric patients 6 to 14 years of age: one 5-mg chewable tablet.
An additional dose of Montelukast should not be taken within 24 hours of a previous dose. Patients already taking Montelukast daily for another indication (including chronic asthma) should not take an additional dose to prevent EIB. All patients should have available for rescue a short-acting β-agonist.
Safety and efficacy in patients younger than 6 years of age have not been established.
Daily administration of Montelukast for the chronic treatment of asthma has not been established to prevent acute episodes of EIB.
Allergic Rhinitis: the dose should be taken once daily (in the evening or in the morning)
The following doses for the treatment of symptoms of seasonal allergic rhinitis are recommended:
- For adults and adolescents 15 years of age and older: one 10-mg tablet.
- For pediatric patients 6 to 14 years of age: one 5-mg chewable tablet.
- For pediatric patients 2 to 5 years of age: one 4-mg chewable tablet or one packet of 4-mg (oral granules).
Safety and effectiveness in pediatric patients younger than 2 years of age with seasonal allergic rhinitis have not been established.
The following doses for the treatment of symptoms of perennial allergic rhinitis are recommended:
For adults and adolescents 15 years of age and older: one 10-mg tablet.
For pediatric patients 6 to 14 years of age: one 5-mg chewable tablet.
For pediatric patients 2 to 5 years of age: one 4-mg chewable tablet or one packet of 4-mg (oral granules).
For pediatric patients 6 to 23 months of age: one packet of 4-mg oral granules.
Safety and effectiveness in pediatric patients younger than 6 months of age with perennial allergic rhinitis have not been established.
Asthma and Allergic Rhinitis:
Patients with both asthma and allergic rhinitis should take only one Montelukast dose daily in the evening.
Instructions for Administration of Oral Granules: Montelukast 4-mg oral granules can be administered
- Either 1. Directly in the mouth,
- Dissolved in 1 teaspoonful (5 mL) of cold or room temperature baby formula or breast milk.
- Mixed with a spoonful of cold or room temperature soft foods: only applesauce, carrots, rice, or ice cream should be used.
- The packet should not be opened until ready to use.
- After opening the packet, the full dose (with or without mixing with baby formula, breast milk, or food) must be administered within 15 minutes.
- If mixed with baby formula, breast milk, or food, the granules must not be stored for future use.
- Discard any unused portion.
- Montelukast oral granules are not intended to be dissolved in any liquid other than baby formula or breast milk for administration. However, liquids may be taken subsequent to administration.
- Montelukast oral granules can be administered without regard to the time of meals.
Warning and precautions:
Acute Asthma:
Montelukast is not indicated for use in the reversal of bronchospasm in acute asthma attacks, including status asthmaticus. Therapy with Montelukast can be continued during acute exacerbations of asthma. Patients who have exacerbations of asthma after exercise should have available for rescue a short-acting inhaled β-agonist.
Concomitant Corticosteroid Use:
While the dose of inhaled corticosteroid may be reduced gradually under medical supervision, Montelukast should not be abruptly substituted for inhaled or oral corticosteroids.
Aspirin Sensitivity:
Patients with known aspirin sensitivity should continue avoidance of aspirin or non-steroidal anti-inflammatory agents while taking Montelukast. Although Montelukast is effective in improving airway function in asthmatics with documented aspirin sensitivity, it has not been shown to truncate bronchoconstrictor response to aspirin and other non-steroidal anti-inflammatory drugs in aspirin sensitive asthmatic patients.
Neuropsychiatric Events:
Neuropsychiatric events have been reported in adult, adolescent, and pediatric patients taking Montelukast. Patients and prescribers should be alert for neuropsychiatric events. Patients should be instructed to notify their prescriber if neuropsychiatric changes occur. Prescribers should carefully evaluate the risks and benefits of continuing treatment with Montelukast if these events occur.
Eosinophilic Conditions:
Patients with asthma on therapy with 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 events have been sometimes associated with the reduction of oral corticosteroid therapy. Physicians should be alert to eosinophilia, vasculitic rash, worsening pulmonary symptoms, cardiac complications, and/or neuropathy presenting in their patients.
Phenylketonuria
Phenylketonuric patients should be informed that the 4-mg and 5-mg chewable tablets contain phenylalanine.
Pregnancy
Pregnancy Category B: There are no adequate and well-controlled studies in pregnant women, should be used during pregnancy only if clearly needed
Nursing Mothers
Because many drug are excreted in human milk, it is not known if montelukast is excreted in human milks, caution should be exercised when Montelukast is given to a nursing mother
Pediatric use:
The safety and effectiveness in pediatric patients below the age of 12 months with asthma, 6 months with perennial allergic rhinitis, and 6 years with exercise-induced bronchoconstriction have not been established
Geriatric use:
No dosage adjustment in the elderly is required
Hepatic Insufficiency
No dosage adjustment is required in patients with mild-to-moderate hepatic insufficiency
Renal Insufficiency
No dosage adjustment is recommended in patients with renal insufficiency
Adverse reaction:
The most common adverse reactions in clinical trials were: upper respiratory infection, fever, headache, pharyngitis, cough, abdominal pain, diarrhea, otitis media, influenza, rhinorrhea, sinusitis, otitis.
Adults and Adolescents 15 Years of Age and Older with Asthma: abdominal Pain, Asthenia /fatigue, Fever, Trauma, Dyspepsia, dental Pain, infectious Gastroenteritis, Headache, Dizziness, Influenza, Cough, nasal Congestion, Rash, increased ALT & AST, Pyuria
Pediatric Patients 6 to 14 Years of Age with Asthma: pharyngitis, influenza, fever, sinusitis, nausea, diarrhea, dyspepsia, otitis, viral infection, and laryngitis
Pediatric Patients 2 to 5 Years of Age with Asthma: fever, cough, abdominal pain, diarrhea, headache, rhinorrhea, sinusitis, otitis, influenza, rash, ear pain, gastroenteritis, eczema, urticaria, varicella, pneumonia, dermatitis, and conjunctivitis.
Pediatric Patients 6 to 23 Months of Age with Asthma: upper respiratory infection, wheezing; otitis media; pharyngitis, tonsillitis, cough; and rhinitis.
Adults and Adolescents 15 Years of Age and Older with Seasonal Allergic Rhinitis: upper respiratory infection.
Pediatric Patients 2 to 14 Years of Age with Seasonal Allergic Rhinitis: headache, otitis media, pharyngitis, and upper respiratory infection
Adults and Adolescents 15 Years of Age and Older with Perennial Allergic Rhinitis: Sinusitis, upper respiratory infection, sinus headache, cough, epistaxis, and increased ALT
DRUG INTERACTIONS:
No dose adjustment is needed when Montelukast is co-administered with theophylline, prednisone, prednisolone, oral contraceptives, terfenadine, digoxin, warfarin, gemfibrozil, itraconazole, thyroid hormones, sedative, hypnotics, non-steroidal anti-inflammatory agents, benzodiazepines, decongestants, and Cytochrome P450 (CYP) enzyme inducers.
OVERDOSAGE:
In the event of overdose, it is reasonable to employ the usual supportive measures; e.g., remove unabsorbed material from the gastrointestinal tract, employ clinical monitoring, and institute supportive therapy, if required.
The most frequently occurring adverse experiences include abdominal pain, somnolence, thirst, headache, vomiting and psychomotor hyperactivity.
It is not known whether montelukast is removed by peritoneal dialysis or hemodialysis
Storage conditions: Store below 30°C protected from moisture and light.
How supplied:
Singomed (4-5) box of 20 chewable tablets.
Singomed 10 box of 20 film coated tablets.