Montelukast; Uses, Dosage, Side Effects, Drug Interactions

Montelukast
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Montelukast is a leukotriene receptor antagonist (LTRA) used for the maintenance treatment of asthma and to relieve symptoms of seasonal allergies. It is usually administered orally. Montelukast blocks the action of leukotriene D4 on the cysteinyl leukotriene receptor CysLT1 in the lungs and bronchial tubes by binding to it. This reduces the bronchoconstriction otherwise caused by the leukotriene, and results in less inflammation. Because of its method of operation, it is not useful for the treatment of acute asthma attacks. Again because of its very specific locus of operation, it does not interact with other allergy medications such as theophylline. Montelukast is marketed in United States and many other countries by Merck & amp; Co. with the brand name Singulair. It is available as oral tablets, chewable tablets, and oral granules.

Montelukast blocks the action of leukotriene D4 on the cysteinyl leukotriene receptor CysLT1 in the lungs and bronchial tubes by binding to it. This reduces the bronchoconstriction otherwise caused by the leukotriene, and results in less inflammation. Because of its method of operation, it is not useful for the treatment of acute asthma attacks.

Mechanism of action of Montelukast

Montelukast selectively antagonizes leukotriene D4 (LTD4) at the cysteinyl leukotriene receptor, CysLT1, in the human airway. Montelukast inhibits the actions of LTD4 at the CysLT1 receptor, preventing airway edema, smooth muscle contraction, and enhanced secretion of thick, viscous mucus. Montelukast, like zafirlukast, is a leukotriene receptor antagonist used as an alternative to anti-inflammatory medications in the management and chronic treatment of asthma and exercise-induced bronchospasm (EIB). Unlike zafirlukast, montelukast does not inhibit CYP2C9 or CYP3A4 and is, therefore, not expected to affect the hepatic clearance of drugs metabolized by these enzymes.

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Montelukast inhibits bronchoconstriction due to antigen challenge. Montelukast is a selective leukotriene receptor antagonist of the cysteinyl leukotriene CysLT1 receptor. The cysteinyl leukotrienes (LTC4 , LTD4, LTE4) are products of arachidonic acid metabolism that are released from various cells, including mast cells and eosinophils. They bind to cysteinyl leukotriene receptors (CysLT) found in the human airway. Binding of cysteinyl leukotrienes to leukotriene receptors has been correlated with the pathophysiology of asthma, including airway edema, smooth muscle contraction, and altered cellular activity associated with the inflammatory process, factors that contribute to the signs and symptoms of asthma. 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 receptors, without any agonist activity.

Indications of Montelukast

Contra-Indications of Montelukast

  • Increased Eosinophils in the Blood
  • Having Thoughts of Suicide
  • Depression
  • Inflammation of Blood Vessels in the Skin
  • anxiety disorder
Allergies to
  • Montelukast
  • Leukotriene Receptor Antagonist

Dosages of Montelukast

Strengths: 5 mg; 4 mg; 10 mg;

Adult dosage (ages 15 years and older)

  • The typical dosage is one 10-mg tablet taken once daily in the evening.

Child dosage (ages 6–14 years)

  • The typical dosage is one 5-mg chewable tablet taken once daily in the evening.

Child dosage (ages 2–5 years)

  • The typical dosage is one 4-mg chewable tablet once daily in the evening.

Child dosage (ages 0–1 year)

  • It has not been determined that the use of montelukast oral tablet is safe or effective for asthma in children younger than 12 months.

Allergic Rhinitis

  • 10 mg orally once a day

Asthma – Maintenance

  • 10 mg orally once a day

Bronchospasm Prophylaxis

  • 10 mg orally once a day at least 2 hours before exercise
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Pediatric Dose for Asthma

12 to 23 months
  • One sachet of 4 mg oral granules once a day

2 to 5 years

  • 4 mg chewable tablet or one sachet oral granules once a day

6 to 14 years

  • 5 mg chewable tablet orally once a day

15 years or older

  • 10 mg tablet orally once a day

Allergic Rhinitis

Seasonal Allergic Rhinitis
  • Less than 2 years: Not approved.

2 to 5 years

  • 4 mg chewable tablet or one sachet of 4 mg oral granules once a day

6 to 14 years

  • 5 mg chewable tablet orally once a day

15 years or older

  • 10 mg tablet orally once a day

Perennial Allergic Rhinitis

6 to 23 months
  • One sachet of 4 mg oral granules once a day

2 to 5 years

  • 4 mg chewable tablet orally once a day

6 to 14 years

  • 5 mg chewable tablet orally once a day

15 years or older

  • 10 mg tablet orally once a day

Bronchospasm Prophylaxis

  • Less than 6 years: Not approved.

6 to 14 years

  • 5 mg chewable tablet orally once a day

15 years or older

  • 10 mg tablet orally once a day

Side Effects of Montelukast

The most common

Common

Rare

Drug Interactions of Montelukast

Montelukast may interact with following drugs,supplement & may change the efficacy of drugs

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Pregnancy & Lactation Montelukast

FDA Pregnancy category B.

Pregnancy

Montelukast falls into category B. There are no well-done studies that have been done in humans with montelukast. But in animal studies, pregnant animals were given this medication, and the babies did not show any medical issues related to this medication.

Lactation

It is not known if montelukast passes into breast milk. If you are a breast-feeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding.

References

 

montelukast

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