Leukotriene receptor antagonist

Author: Prof. Dr. med. Peter Altmeyer

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Last updated on: 19.04.2021

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Definition
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Leukotrienes are pro-inflammatory messenger substances which - similar to histamine - are released from mast cells and other immune cells and play a role in the development of many symptoms of allergic bronchial asthma. Leukotriene receptor antagonists are drugs that bind to and antagonize the Cys-LT1 receptors present in the airways.

Pharmacodynamics (Effect)
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Leukotriene receptor antagonists antagonize the effects of leukotrienes by binding to leukotriene receptors in the bronchial system. Cysteinyl leukotrienes are pathophyiologically important mediators in bronchial asthma. They contribute to bronchoconstriction and chronic airway inflammation with bronchial hypersecretion. Since their action is mainly mediated by CystLT1 receptors, antagonists of these receptors play a role in the treatment of chronic bronchial asthma.

Leukotriene receptor antagonists improve symptoms by reducing bronchoconstriction, excessive secretion and irritability. The effect is weaker than that of inhaled glucocorticoids.

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Indication
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The indication is mild to moderate allergic asthma as an add-on therapy, for example with an inhaled beta-2-sympathomimetic, when inhaled glucocorticoids or on-demand β2-sympathomimetics alone are not sufficient to control asthma. The approved leukotriene antagonist is not appropriate in severe asthma or acute attack.

Dosage and method of use
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The active ingredient (to date there is only one approved drug in this group of drugs, montelukast ) is taken orally and is preferably used in children (from the age of 6 months) and adolescents.

Preparations
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Currently, there is only one approved active substance from the group of leukotriene receptor antagonists, montelukast. See below Montelukast.

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Montelukast;

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Last updated on: 19.04.2021