Tomelukast

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Tomelukast

Tomelukast is a pharmaceutical compound that belongs to the class of leukotriene receptor antagonists. It is primarily used in the management of asthma and allergic rhinitis. This article provides a comprehensive overview of Tomelukast, including its mechanism of action, clinical uses, pharmacokinetics, side effects, and related compounds.

Mechanism of Action[edit | edit source]

Tomelukast functions by inhibiting the action of leukotrienes, which are inflammatory mediators derived from arachidonic acid. Leukotrienes are known to contribute to the pathophysiology of asthma and allergic rhinitis by promoting bronchoconstriction, mucus secretion, and inflammation. By blocking the cysteinyl leukotriene receptor (CysLT1), Tomelukast reduces these effects, leading to improved respiratory function and symptom relief.

Clinical Uses[edit | edit source]

Tomelukast is indicated for:

  • The prophylaxis and chronic treatment of asthma in adults and pediatric patients.
  • The relief of symptoms of seasonal allergic rhinitis and perennial allergic rhinitis.
  • The prevention of exercise-induced bronchoconstriction.

Pharmacokinetics[edit | edit source]

Tomelukast is administered orally and is rapidly absorbed from the gastrointestinal tract. It reaches peak plasma concentrations within 3 to 4 hours. The drug is extensively metabolized in the liver, primarily by the cytochrome P450 enzyme system, and is excreted in the bile. The half-life of Tomelukast is approximately 2.7 to 5.5 hours.

Side Effects[edit | edit source]

Common side effects of Tomelukast include:

  • Headache
  • Abdominal pain
  • Cough
  • Diarrhea
  • Upper respiratory tract infection

Rare but serious side effects may include:

  • Neuropsychiatric events such as agitation, aggression, depression, and suicidal thoughts.
  • Hypersensitivity reactions including anaphylaxis and angioedema.

Related Compounds[edit | edit source]

Tomelukast is part of a class of medications known as leukotriene receptor antagonists. Other drugs in this class include:

Also see[edit | edit source]

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Contributors: Prab R. Tumpati, MD