Prevent an allergic reaction from happening at school.

Montelukast Sodium

Pronunciation

Pronunciation: MON-te-LOO-kast SOE-dee-um
Class: Leukotriene receptor antagonist

Trade Names

Singulair
- Tablets, oral 10 mg
- Tablets, chewable, oral 4 mg
- Tablets, chewable, oral 5 mg
- Granules, oral 4 mg/packet

Pharmacology

Binds to cysteinyl leukotriene type 1 (CysLT 1 ) receptor in the upper and lower airways to prevent leukotriene-mediated effects associated with asthma and allergic rhinitis.

Slideshow: What is Asthma? Causes, Symptoms, and Treatment

Pharmacokinetics

Absorption

Rapidly absorbed. T max is 3 to 4 h and bioavailability is 64% for the 10 mg oral tablet in the fasted state. T max is 2 to 2.5 h and bioavailability is 73% (63% if taken with food) for the 5 mg chewable tablet. T max is 2 h for the 4 mg chewable tablet taken without food. The 4 mg granule formulation is bioequivalent to the 4 mg chewable tablet when administered in the fasted state. Administration of granules with a high-fat meal does not affect AUC, but prolongs T max to 6.4 h and decreases C max by 35%.

Distribution

Protein binding is more than 99%. Vd is 8 to 11 L.

Metabolism

Extensively metabolized; plasma concentrations of metabolites are undetectable at steady state. CYP-450 3A4 and 2C9 are involved in metabolism.

Elimination

Plasma Cl averages 45 mL/min and mean plasma half-life is 2.7 to 5.5 h; 86% is recovered in feces and less than 0.2% in urine.

Special Populations

Renal Function Impairment

Pharmacokinetics were not evaluated in patients with renal impairment.

Hepatic Function Impairment

AUC increased 41% and half-life was prolonged to 7.4 h in patients with mild to moderate hepatic impairment and cirrhosis. Patients with severe hepatic impairment or hepatitis have not been evaluated.

Elderly

Plasma half-life is slightly longer.

Children

In children 6 to 23 mo of age, the systemic exposure to montelukast is higher than in adults.

Gender

Pharmacokinetics are similar in male and female patients.

Race

Differences have not been studied.

Indications and Usage

Prophylaxis and long-term treatment of asthma in patients 12 mo and older; relief of symptoms of seasonal allergic rhinitis in patients 2 y and older; relief of symptoms of perennial allergic rhinitis in patients 6 mo and older; prevention of exercise-induced bronchoconstriction (EIB) in patients 6 y and older.

Unlabeled Uses

Atopic dermatitis, chronic urticaria.

Contraindications

Hypersensitivity to any component of the product.

Dosage and Administration

Asthma
Adults and adolescents 15 y and older

PO 10 mg daily in the evening.

Children 6 to 14 y of age

PO 5 mg daily in the evening (chewable tablet).

Children 2 to 5 y of age

PO 4 mg daily in the evening (chewable tablet or granules).

Children 12 to 23 mo of age

PO 4 mg daily in the evening (granules).

Exercise-induced bronchoconstriction
Adults and adolescents 15 y and older

PO 10 mg at least 2 h prior to exercise. An additional dose should not be taken within 24 h of the previous dose.

Children 6 to 14 y of age

PO 5 mg at least 2 h prior to exercise (chewable tablet). An additional dose should not be taken within 24 h of the previous dose.

Perennial Allergic Rhinitis
Adults and adolescents 15 y and older

PO 10 mg daily.

Children 6 to 14 y of age

PO 5 mg once daily (chewable tablet).

Children 2 to 5 y of age

PO 4 mg daily (chewable tablet or granules).

Children 6 to 23 mo of age

PO 4 mg daily (granules).

Seasonal Allergic Rhinitis
Adults and adolescents 15 y and older

PO 10 mg daily.

Children 6 to 14 y of age

PO 5 mg daily (chewable tablet).

Children 2 to 5 y of age

PO 4 mg daily (chewable tablet or granules).

General Advice

  • Provide patients with appropriate rescue medication.
  • Patients taking a daily dose for a particular indication, including chronic asthma, should not take an additional dose to prevent EIB.
  • Patients with both asthma and allergic rhinitis should take only 1 tablet daily in the evening.
  • May be taken with or without food.
  • Oral granules
  • Do not open a packet containing granules until ready for use; the full dose must be administered within 15 min of opening the packet.
  • Granules can be administered directly in the mouth, dissolved in 5 mL of cold or room temperature baby formula or breast milk, or mixed with a spoonful of cold or room temperature soft foods (applesauce, carrots, rice, or ice cream only). If mixing with baby formula, breast milk, or food, do not prepare it ahead of time or store for future use. Discard any unused portion.
  • Do not dissolve granules in any liquid other than baby formula or breast milk for administration; however, liquids can be taken subsequent to administration.

Storage/Stability

Store between 59° and 86°F. Protect from moisture and light. Store in original package. When bulk bottle product container is subdivided, repackage into well-closed, light-resistant containers.

Drug Interactions

Gemfibrozil

Montelukast plasma concentrations may be elevated, increasing the pharmacologic effects and risk of adverse reactions. Monitor the clinical response and adjust the montelukast dose as needed.

CYP-450 inducers (eg, phenobarbital, rifampin)

May decrease montelukast levels. Monitor the clinical response and adjust the montelukast dose as needed.

Adverse Reactions

CNS

Headache (18%); asthenia/fatigue, dizziness (2%); abnormal dreams, agitation (including aggressive behavior or hostility), anxiousness, depression, disorientation, drowsiness, hallucinations, hypoesthesia, insomnia, irritability, paraesthesia, restlessness, seizures, somnambulism, suicidal thinking and behavior (including suicide), tremor (postmarketing).

Dermatologic

Atopic dermatitis, dermatitis, eczema, rash, skin infection, urticaria (at least 2%); erythema multiforme, erythema nodosum, pruritus, urticaria, vasculitic rash (postmarketing).

EENT

Conjunctivitis, ear pain, laryngitis, myopia, otitis, otitis media, pharyngitis, rhinitis, rhinorrhea, sinusitis, tonsillitis (at least 2%); nasal congestion (2%); epistaxis, sinus headache (at least 1%).

GI

Abdominal pain (3%); diarrhea, dyspepsia, gastroenteritis, nausea, tooth infection (at least 2%); dental pain, infectious gastroenteritis (2%); pancreatitis, vomiting (postmarketing).

Hematologic-Lymphatic

Bruising, eosinophilia, increased bleeding tendency, thrombocytopenia (postmarketing).

Hepatic

ALT/AST increased (2%); cholestatic hepatitis, hepatocellular liver injury, mixed-pattern liver injury (postmarketing).

Hypersensitivity

Anaphylaxis, angioedema, hepatic eosinophilic infiltration (postmarketing).

Musculoskeletal

Arthralgia, myalgia (including muscle cramps) (postmarketing).

Respiratory

Influenza (4%); cough (3%); acute bronchitis, pneumonia, upper respiratory tract infection, wheezing (at least 2%).

Miscellaneous

Fever, varicella, viral infection (at least 2%); pyuria, trauma (1%); edema, palpitations (postmarketing).

Precautions

Monitor

Monitor patients for mood or behavioral changes, including suicidal thinking and behavior.


Pregnancy

Category B .

Lactation

Undetermined.

Children

Safety and efficacy not established for treatment of EIB in patients younger than 6 y. Safety and efficacy not established for treatment of seasonal allergic rhinitis in patients younger than 2 y. Safety and efficacy not established for treatment of asthma in patients younger than 12 mo. Safety and efficacy not established for treatment of perennial allergic rhinitis in patients younger than 6 mo.

Elderly

Greater sensitivity cannot be ruled out.

Acute asthma attacks

Not indicated for use in the reversal of bronchospasm in acute asthma attacks, including status asthmaticus. Patients should have appropriate rescue medication available.

Aspirin sensitivity

Continue to avoid aspirin or NSAIDs in patients with aspirin sensitivity; montelukast has not been shown to truncate bronchoconstrictor response to aspirin and other NSAIDs in aspirin-sensitive asthmatic patients.

Concurrent corticosteroids

Do not abruptly substitute montelukast for inhaled or oral corticosteroids.

Eosinophilia

Systemic eosinophilia may occur, sometimes presenting with clinical features of vasculitis consistent with Churg-Strauss syndrome.

Neuropsychiatric events

Carefully evaluate the risk/benefit of continuing treatment if these events occur.

Phenylketonuria

Montelukast contains phenylalanine 0.674 and 0.842 mg per 4 and 5 mg chewable tablet, respectively.

Overdosage

Symptoms

Abdominal pain, headache, psychomotor hyperactivity, somnolence, thirst, vomiting.

Patient Information

  • Advise patients to read the patient information leaflet before using this medicine for the first time and to reread and check for new information with each refill.
  • Caution patients with asthma not to decrease the dose or stop taking any other asthma medications unless advised by their health care provider.
  • Advise patients that montelukast can be taken without regard to meals but to take it with food if stomach upset occurs.
  • Advise patients with asthma or asthma and allergic rhinitis to take the prescribed dose once daily in the evening.
  • Advise patients with allergic rhinitis to take the prescribed dose once daily at a time that is convenient, but at about the same time each day.
  • Advise patients or caregivers using granules that the packet containing granules should not be opened until ready for use and that the full dose must be administered within 15 min. Granules can be administered directly in the mouth, dissolved in 5 mL of cold or room temperature formula or breast milk, or mixed with a spoonful of cold or room temperature soft foods (applesauce, carrots, rice, or ice cream only). Caution patients or caregivers mixing granules with baby formula, breast milk, or food not to prepare it ahead of time or store it for future use. Instruct patients to discard any unused portion.
  • Caution patients with asthma that this medication is not to be used to treat acute asthma attacks. Instruct patients to always have a short-acting beta-agonist available for acute treatment of asthma symptoms.
  • Instruct patients to take montelukast every day as prescribed, even when symptoms have been controlled.
  • Caution patients not to increase their montelukast dose or frequency of use, but to notify their health care provider if symptoms return or worsen. Caution patients with asthma to notify their health care provider if the need for rescue medication increases or if rescue medication does not seem to work as well.
  • Advise patients with EIB to use the usual regimen of beta-agonists as prophylaxis unless otherwise instructed by their health care provider.
  • Advise patients with known aspirin sensitivity to continue avoidance of aspirin and NSAIDs while taking montelukast.
  • Inform phenylketonuric patients that the chewable tablets contain phenylalanine.
  • Advise patients to notify their health care provider if neuropsychiatric events occur.

Copyright © 2009 Wolters Kluwer Health.

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