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Montelukast metabolization

Montelukast is a medication prescribed to treat bronchial asthma and for the relief of annual allergies. It is also used to treat tightness in the chest, wheezing and cough that caused by asthma, as well as to prevent bronchospasm (difficulty breathing) during exercise. It is also prescribed to treat the symptoms of allergic rhinitis (a condition that causes sneezing and itching, nasal congestion and runny nose) both seasonal (occurs only at certain times of the year) and permanent (occurs throughout the year). Montelukast belongs to a class of medications called leukotriene receptor antagonists (LTRA). It works by blocking the action of substances in the body that cause the symptoms of asthma and allergic rhinitis.

ACTION MECHANISM

Montelukast blocks the action of substances such as leukotriene C4, D4 and E4 by acting on the CysLT1 receptor at the level of the lungs and bronchi, binding it. This reduces the bronchoconstriction caused by the leukotrienes and results in less inflammation.

CONTRAINDICATIONS

Hypersensitivity to montelukast.

Montelukast is not indicated in acute asthma attack, nor as monotherapy in moderate persistent asthma; do not abruptly substitute inhaled or oral corticosteroids for montelukast without data demonstrating that oral corticosteroids can be reduced

CAUTIONS

There is a possible association with the onset of Churg-Strauss syndrome (monitoring and reevaluation of treatment in case of eosinophilia, vasculitic rash, worsening of pulmonary symptoms, cardiac complications, and/or neuropathy).

Montelukast is not recommended in children under 6 months of age.

During pregnancy and lactation montelukast should be used only if is clearly necessary.

PHARMACOLOGIC INTERACTIONS

The concentration of montelukast in plasma can be diminished by concomitant treatment with phenytoin, phenobarbital and rifampicin.

If taken together with gemfibrozil, adverse reactions may be increased.

SIDE EFFECTS

Headache, dizziness, heartburn, stomach pain, tiredness, diarrhea, vomiting.

In addition, montelukast may cause more serious side effects on some occasions, such as: difficulty breathing or swallowing, swelling of the face, throat, tongue, lips, eyes, hands, feet, ankles or calves , rash, fever, flu-like symptoms, tingling or numbness in the arms or legs, pain and swelling of the sinuses, upper respiratory infection, elevated serum transaminase levels (ALT, AST), alterations of the judgment, ideas of suicide.

BRAND NAMES

  • Singulair®
  • Pluralais®

Gene or region studied

  • CYP2C8
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