Kastair EZ Tab

Kastair EZ Tab

montelukast

Manufacturer:

UNILAB, Inc

Distributor:

UNILAB, Inc
Full Prescribing Info
Contents
Montelukast sodium.
Description
Montelukast (Kastair EZTab) 4 mg Tablet contains 4.2 mg montelukast sodium equivalent to 4 mg of Montelukast.
Montelukast (Kastair EZTab) 5 mg Tablet contains 5.2 mg montelukast sodium equivalent to 5 mg of Montelukast.
Montelukast (Kastair EZTab) 4 mg and 5 mg Tablets are easy to swallow, cherry-flavored tablets that melt in the mouth in less than 30 seconds without chewing. They provide montelukast in a pleasant tasting format that is suitable for both young and older children. They are easy to carry and have the advantage over liquid formats in terms of convenience.
Action
Pharmacology: Pharmacodynamics: Montelukast is a selective leukotriene receptor antagonist that binds to CysLT1 receptor. The cysteinyl leukotrienes (LTC4, LTD4, and LTE4) are formed from the metabolism of arachidonic acid and are produced by a number of cells including eosinophils, basophils, mast cells, macrophages, and monocytes. The effects of these eicosanoids are mediated by binding to cysteinyl leukotriene (CysLT) receptors. The CysLT type-1 (CysLT1) receptor is present in various contractile tissues including airway smooth muscle cells. CysLTs contribute to the pathophysiology of asthma and allergic rhinitis. In asthma, CysLTs are found to increase mucus secretion and vascular permeability, airway edema, bronchoconstriction, and altered cellular activity associated with the inflammatory process. In allergic rhinitis, CysLTs are released within minutes from the nasal mucosa after exposure to allergens. This release leads to inflammation and symptoms such as nasal congestion and rhinorrhea. Montelukast inhibits bronchoconstriction and reduces inflammation of the nasal mucosa induced by exposure to known precipitants.
Pharmacokinetics: Montelukast is readily absorbed after oral administration. Peak plasma concentration (Cmax) of montelukast is achieved within 2 hours (Tmax) after oral administration of a 4 mg chewable tablet to fasted children 2 to 5 years old.
After oral administration of a 5 mg EZTab to fasted adults, peak plasma concentration (Cmax) of montelukast (252.71 ± 63.6 ng/mL) is achieved within 2.75 ± 0.77 hours (Tmax). The elimination half life of montelukast is 4.23 ± 1.238 hours.
In two pharmacokinetic trials in asthmatic pediatric patients aged 2 to 5 years and 6 to 14 years, peak plasma concentrations of montelukast 4 mg (471 ± 65 ng/mL) and 5 mg (495 ± 129 ng/mL) as chewable tablets are attained within 2.07± 0.3 hours and 2.6 ± 1 hours, respectively.
The mean systemic exposure of the 4 mg tablet in children 2 to 5 years old and the 5 mg tablet in children 6 to 14 years old is similar to the mean systemic exposure of the 10 mg tablet in adults.
Montelukast's steady state volume of distribution is 8 to 11 liters. Plasma protein binding is more than 99%.
Montelukast is metabolized in the liver by CYP-450 enzymes 3A4, 2A6, and 2C9. Plasma concentrations of montelukast metabolites are undetectable at steady state in studies in adults and children using therapeutic doses. Metabolism in patients with mild to moderate hepatic impairment is reduced; elimination half life is prolonged. Montelukast is excreted mainly in the feces via the bile as unchanged drug and metabolites.
Animal studies indicate that montelukast crosses the placenta in rats and rabbits and is distributed into milk in rats after oral administration; in humans, it is not known whether the drug crosses the placenta or distributes in milk.
Indications/Uses
For the relief of symptoms of allergic rhinitis: Seasonal allergic rhinitis in children 2 years and older and in adults; Perennial allergic rhinitis in children 6 months old and older and in adults.
For the prophylaxis and chronic treatment of asthma in children 6 months old and older and in adults.
Montelukast is effective alone or when used together with other agents for the management of chronic asthma. Montelukast may be used concomitantly with inhaled corticosteroids to control asthma and to reduce the dose of inhaled corticosteroids required by patients with moderate to severe asthma.
For the prevention of exercise-induced bronchoconstriction in children 2 years and older and in adults.
Dosage/Direction for Use
See table.

Click on icon to see table/diagram/image

Directions for Use: Patients with allergic rhinitis: The time of administration may be individualized to suit patient needs.
Take everyday, at about the same time each day, or, as prescribed by a physician.
Patients with asthma with or without coexisting allergic rhinitis: The dose should be taken in the evening to obtain simultaneous peak plasma concentration and peak airway reactivity in the morning.
Take at regular intervals (i.e., daily) to be therapeutically effective, even if the patient has no asthma symptoms, or, as prescribed by a physician.
Prevention of exercise-induced bronchoconstriction: Take at least 2 hours before exercise.
Do not take an additional dose within 24 hours of a previous dose.
Do not take an additional dose to prevent exercise-induced bronchoconstriction if the patient is taking montelukast daily for chronic asthma or allergic rhinitis. Consult a physician about treatment of exercise-induced bronchoconstriction.
Montelukast 4 mg and 5 mg tablet can be dissolved in the mouth or chewed before swallowing.
May be taken with or without food.
Younger children (6 months to 2 years old): Montelukast 4 mg tablet can be crushed and administered directly in the mouth; dissolved in 5 mL (1 teaspoonful) of cold or room temperature breast milk or baby formula; mixed with a spoonful of one of the following soft foods at cold or room temperature: applesauce, mashed carrots, rice, or ice cream.
The tablet should not be crushed until ready for use.
The entire dose of the crushed tablet must be administered within 15 minutes. The crushed tablet should not be stored for future use if mixed with food or dissolved in breast milk or baby formula.
The crushed tablet should not be dissolved in liquid other than breast milk or baby formula. However, liquids can be taken after administration.
Overdosage
Montelukast given in doses up to 200 mg/day for 22 weeks and up to 900 mg/day for approximately a week to adult patients showed no clinically important adverse reactions. Acute overdosages in adults and children given montelukast with a dose as high as 1000 mg have been reported. There were no adverse effects reported in majority of overdosage reports. The most frequent adverse effects observed were somnolence, headache, thirst, vomiting, abdominal pain, mydriasis, hyperkinesias, and psychomotor hyperactivity.
There is no specific information available on the treatment of overdosage with montelukast. In case of overdose, institute supportive and symptomatic therapy, i.e., remove unabsorbed material from the gastrointestinal tract. There is no adequate evidence to support the use of dialysis in the treatment of montelukast overdose.
Contraindications
Hypersensitivity to any ingredient in the product.
Special Precautions
Montelukast is not indicated for the treatment of acute asthma attacks, including status asthmaticus. Patients should have appropriate short-acting inhaled B-agonist medication available to treat asthma exacerbations. However, therapy with montelukast can be continued during acute asthmatic attacks.
While using montelukast, consult a physician for medical advice if more than the recommended dose of short-acting inhaled bronchodilators is needed.
Patients taking montelukast should not decrease the dose or stop taking any other medicines for asthma unless directed by a physician.
Avoid aspirin or non-steroidal anti-inflammatory drugs (NSAIDs) while taking montelukast in patients with known aspirin sensitivity.
Neuropsychiatric events have been reported in patients taking montelukast. These postmarketing reports include agitation, aggressive behavior or hostility, anxiousness, depression, disorientation, dream abnormalities, hallucinations, insomnia, irritability, restlessness, somnambulism, suicidal thinking and behavior (including suicide), and tremor. Patients should inform their physician if these changes occur.
Eosinophilia, vasculitic rash, worsening pulmonary symptoms, cardiac complications, and/or neuropathy consistent with Churg-Strauss syndrome have been reported rarely in patients with asthma being treated with montelukast.
Use in Pregnancy: The safe use of the product during pregnancy has not been established. Therefore, montelukast should be used in pregnancy only if the potential benefit justifies the potential risk to the fetus.
There have been rare reports of congenital limb defects in children of patients treated with montelukast. Most of the mothers, however, were receiving other asthma medications in the course of their pregnancies. Since there is no consistent pattern of congenital abnormality development, a relationship between the use of montelukast and the development of congenital anomalies cannot be established.
Use in Lactation: It is not known if montelukast is excreted in human milk. Therefore, do not administer to breastfeeding women unless, in the opinion of a physician, the potential benefits of the drug justify the possible risk.
Use in Children: The safety and efficacy of montelukast in infants younger than 6 months old have not been established.
Use in the Elderly: There were no differences observed between the elderly and younger patients in the efficacy and safety profiles of montelukast.
Use In Pregnancy & Lactation
Pregnancy: The safe use of the product during pregnancy has not been established. Therefore, montelukast should be used in pregnancy only if the potential benefit justifies the potential risk to the fetus.
There have been rare reports of congenital limb defects in children of patients treated with montelukast. Most of the mothers, however, were receiving other asthma medications in the course of their pregnancies. Since there is no consistent pattern of congenital abnormality development, a relationship between the use of montelukast and the development of congenital anomalies cannot be established.
Lactation: It is not known if montelukast is excreted in human milk. Therefore, do not administer to breastfeeding women unless, in the opinion of a physician, the potential benefits of the drug justify the possible risk.
Adverse Reactions
The following adverse effects have been reported: Nervous System: Headache, dizziness, hyperkinesia (in young children), somnolence.
Respiratory: Rhinorrhea, cough, influenza, upper respiratory tract infection, nasal congestion, laryngitis, pharyngitis, sinusitis, rhinitis, pneumonia, wheezing, tonsillitis, acute bronchitis, viral infection.
Gastrointestinal: Diarrhea, abdominal pain, infectious gastroenteritis, nausea, vomiting, dyspepsia, rarely pancreatitis.
Dermatological: Rash, eczema, atopic dermatitis/dermatitis, skin infection, urticaria.
Other Adverse Effects: Asthenia/fatigue, fever, trauma, otic pain, otitis/otitis media, conjunctivitis, myopia, epistaxis, dental pain, varicella, tooth infection, thirst, very rarely dry mouth.
Laboratory Abnormalities: Increased serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) concentration, pyuria.
The following additional adverse effects have been reported in post-marketing studies: Psychiatric: Agitation including aggressive behavior or hostility, anxiousness, depression, disorientation, dream abnormalities, hallucinations, insomnia, irritability, restlessness, somnambulism, suicidal thinking and behavior (including suicide), tremor.
Nervous System: Drowsiness, paresthesia/hypoesthesia, seizures.
Gastrointestinal: Diarrhea, nausea, vomiting, dyspepsia, pancreatitis.
Immune System: Hypersensitivity reactions including anaphylaxis, hepatic eosinophilic infiltration.
Hepatobiliary: Cases of cholestatic hepatitis, hepatocellular liver-injury, and mixed pattern liver injury have been reported in patients treated with montelukast. Confounding factors were present in most of these patients, such as the concomitant use of other drugs or alcohol, or in the presence of coexisting conditions (e.g., other forms of hepatitis).
Dermatologic: Angioedema, bruising, erythema nodosum, pruritus, urticaria, rash.
Other Adverse Effects: Myalgia including muscle cramps, arthralgia, epistaxis, palpitations, edema, increased bleeding tendency.
Drug Interactions
The administration of montelukast with other drugs used in the prophylaxis and chronic treatment of asthma showed no apparent increase in adverse reactions.
Usual dosages of montelukast did not reveal clinically important effects on the pharmacokinetics of the following drugs: theophylline, warfarin, digoxin, oral contraceptives (ethinyl estradiol with norethindrone), prednisone, and prednisolone.
Concomitant use of montelukast with commonly prescribed drugs in clinical studies, e.g., thyroid hormones, sedative hypnotics, non-steroidal anti-inflammatory agents, benzodiazepines, and decongestants, showed no evidence of clinical adverse reactions.
Montelukast-treated patients with known aspirin sensitivity should continue to avoid aspirin and other NSAID5. Although montelukast can improve airway function in asthmatics with aspirin sensitivity, the drug has not been shown to shorten the bronchoconstrictor response to aspirin or other NSAID5 in such patients. An anaphylactic reaction has been reported following exposure to an NSAID in at least one aspirin-sensitive individual receiving montelukast.
The area under the plasma concentration-time curve (AUC) of montelukast decreased by approximately 40% with co-administration of phenobarbital. No dosage adjustment for montelukast is recommended. However, appropriate clinical monitoring should be initiated with concomitant administration of montelukast with potent cytochrome P450 enzyme inducers such as phenobarbital and rifampicin.
Storage
Store at temperatures not exceeding 30°C.
ATC Classification
R03DC03 - montelukast ; Belongs to the class of leukotriene receptor antagonists. Used in the systemic treatment of obstructive airway diseases.
Presentation/Packing
Tab (white with red specks, round, with EZ logo on one side and plain on the other side) 4 mg x 28's. 5 mg x 28's.
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