How Do Leukotriene Receptor Antagonists Work?

Reviewed on 10/7/2021

How do leukotriene receptor antagonists work?

Leukotriene receptor antagonists are medications used to treat inflammatory respiratory conditions such as asthma and allergic rhinitis. Leukotriene receptor antagonists relieve the symptoms of asthma and allergic rhinitis by preventing leukotriene-induced inflammation, swelling of airways, excess mucus secretion and airway constriction.

Asthma and rhinitis episodes are triggered by allergens or exercise when the immune system releases inflammatory substances to attack what it perceives as foreign to the body. Cysteinyl leukotrienes are a group of inflammatory molecules released by immune cells such as mast cells, eosinophils, basophils and macrophages in the airway.

Cysteinyl leukotrienes trigger bronchial constriction and inflammation by activating protein molecules known as CysLT1 receptors on the surface of bronchial smooth muscle cells and immune cells in the airway. Cysteinyl leukotrienes promote inflammatory processes which include:

  • Migration and aggregation of other immune cells in the airway which further promote inflammation.
  • Greater permeability of small blood vessels (capillaries), which allows inflammatory proteins and immune cells to leak out.
  • Contraction of the airway smooth muscles.

Leukotriene receptor antagonists prevent inflammation by binding to the CysLT1 receptors and blocking cysteinyl leukotrienes from stimulating them. Leukotriene receptor antagonists block the activity of three types of cysteinyl leukotrienes, LTC4, LTD4 and LTE4.

How are leukotriene receptor antagonists used?

Leukotriene receptor antagonists are oral tablets or granules used in the treatment of the following conditions:

What are side effects of leukotriene receptor antagonists?

Side effects of leukotriene receptor antagonists may include the following:

Information contained herein is not intended to cover all possible side effects, precautions, warnings, drug interactions, allergic reactions, or adverse effects. Check with your doctor or pharmacist to make sure these drugs do not cause any harm when you take them along with other medicines. Never stop taking your medication and never change your dose or frequency without consulting your doctor.


Asthma is a chronic respiratory disease. See Answer

What are names of leukotriene receptor antagonist drugs?

Generic and brand names of leukotriene receptor antagonists include:


Health Solutions From Our Sponsors