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Montelukast: its role in the treatment of childhood asthma.

Harmanci K - Ther Clin Risk Manag (2007)

Bottom Line: Montelukast is a potent and selective blocker of the CysLT(1) receptor.For treatment of chronic asthma, montelukast is administered once daily to adults as a 10-mg film-coated tablet, to children aged 6-14 years as a 5-mg chewable tablet, and to children aged 2-5 years as a 4-mg chewable tablet form.Given their efficacy, antiinflammatory activity, oral administration, and safety, leukotriene modifiers will play an important role in the treatment of asthmatic children.

View Article: PubMed Central - PubMed

Affiliation: Department of Allergy, Ministry of Health, Ankara Diskapi Children’s Diseases Training and Research Hospital Ankara, Turkey.

ABSTRACT
The cysteinyl leukotrienes, LTC(4), LTD(4), and LTE(4), play an integral role in the pathophysiology of asthma. Acting via the type 1 leukotriene (CysLT(1)) receptor, these proinflammatory mediators have numerous effects in the lungs, including decreased activity of respiratory cilia, increased mucus secretion, increased venopermeability, and promotion of eosinophil migration into airway mucosa. Blocking studies show that Cys-LTs are pivotal mediators in the pathophysiology of asthma. Cys-LTs are key components in the early and late allergic airway response and also contribute to bronchial obstruction after exercise and hyperventilation of cold, dry air in asthmatics. Effects of the cysteinyl leukotrienes are blocked by leukotriene receptor antagonists; these agents inhibit bronchoconstriction in normal subjects provoked with inhaled cysteinyl leukotrienes, as well as in patients with asthma undergoing allergen, exercise, cold air, or aspirin challenge. Montelukast is a potent and selective blocker of the CysLT(1) receptor. For treatment of chronic asthma, montelukast is administered once daily to adults as a 10-mg film-coated tablet, to children aged 6-14 years as a 5-mg chewable tablet, and to children aged 2-5 years as a 4-mg chewable tablet form. Given their efficacy, antiinflammatory activity, oral administration, and safety, leukotriene modifiers will play an important role in the treatment of asthmatic children.

No MeSH data available.


Related in: MedlinePlus

Pathogenesis of airway obstruction in asthma.
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fig1: Pathogenesis of airway obstruction in asthma.

Mentions: Leukotrienes are chemical mediators of asthmatic airway inflammation (Figure 1). They are formed from arachidonic acid, and are secreted by eosinophils, mast cells, neutrophils, lymphocytes, macrophages, and basophils (Turner et al 1996) (Figure 2). After the discovery in the late 1970s that the cysteinyl leukotrienes LTC4 and LTE4 (formerly known collectively as the slow-reacting substance of anaphylaxis [SRS-A]) play a key role in the pathophysiology of asthma a number of specific antagonists of their actions have been developed. The leukotriene receptor antagonists (LTRAs) selectively block the binding of cysteinyl leukotrienes to the CysLT1 receptor, which has been identified as the receptor through which most of their actions are mediated (Drazen et al 1999). These actions include bronchoconstriction, mucus hypersecretion, and increased vascular permeability and eosinophil migration. Consequently, the LTRs inhibit bronchconstriction. Moreover, LTRAs prevent many types of provoked asthmatic responses, including allergen-induced, exercise- and cold-air-hyperventilation-induced, and aspirin-induced asthma (Wright et al 1998). Three drugs of this class are in use at present – zafirlukast, pranlukast, and montelukast. All three are specifically active against the cysteinyl leukotrienes by blocking their receptor, CysLT1. Only montelukast has been extensively studied in children (Jones et al 1995).


Montelukast: its role in the treatment of childhood asthma.

Harmanci K - Ther Clin Risk Manag (2007)

Pathogenesis of airway obstruction in asthma.
© Copyright Policy
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC2376066&req=5

fig1: Pathogenesis of airway obstruction in asthma.
Mentions: Leukotrienes are chemical mediators of asthmatic airway inflammation (Figure 1). They are formed from arachidonic acid, and are secreted by eosinophils, mast cells, neutrophils, lymphocytes, macrophages, and basophils (Turner et al 1996) (Figure 2). After the discovery in the late 1970s that the cysteinyl leukotrienes LTC4 and LTE4 (formerly known collectively as the slow-reacting substance of anaphylaxis [SRS-A]) play a key role in the pathophysiology of asthma a number of specific antagonists of their actions have been developed. The leukotriene receptor antagonists (LTRAs) selectively block the binding of cysteinyl leukotrienes to the CysLT1 receptor, which has been identified as the receptor through which most of their actions are mediated (Drazen et al 1999). These actions include bronchoconstriction, mucus hypersecretion, and increased vascular permeability and eosinophil migration. Consequently, the LTRs inhibit bronchconstriction. Moreover, LTRAs prevent many types of provoked asthmatic responses, including allergen-induced, exercise- and cold-air-hyperventilation-induced, and aspirin-induced asthma (Wright et al 1998). Three drugs of this class are in use at present – zafirlukast, pranlukast, and montelukast. All three are specifically active against the cysteinyl leukotrienes by blocking their receptor, CysLT1. Only montelukast has been extensively studied in children (Jones et al 1995).

Bottom Line: Montelukast is a potent and selective blocker of the CysLT(1) receptor.For treatment of chronic asthma, montelukast is administered once daily to adults as a 10-mg film-coated tablet, to children aged 6-14 years as a 5-mg chewable tablet, and to children aged 2-5 years as a 4-mg chewable tablet form.Given their efficacy, antiinflammatory activity, oral administration, and safety, leukotriene modifiers will play an important role in the treatment of asthmatic children.

View Article: PubMed Central - PubMed

Affiliation: Department of Allergy, Ministry of Health, Ankara Diskapi Children’s Diseases Training and Research Hospital Ankara, Turkey.

ABSTRACT
The cysteinyl leukotrienes, LTC(4), LTD(4), and LTE(4), play an integral role in the pathophysiology of asthma. Acting via the type 1 leukotriene (CysLT(1)) receptor, these proinflammatory mediators have numerous effects in the lungs, including decreased activity of respiratory cilia, increased mucus secretion, increased venopermeability, and promotion of eosinophil migration into airway mucosa. Blocking studies show that Cys-LTs are pivotal mediators in the pathophysiology of asthma. Cys-LTs are key components in the early and late allergic airway response and also contribute to bronchial obstruction after exercise and hyperventilation of cold, dry air in asthmatics. Effects of the cysteinyl leukotrienes are blocked by leukotriene receptor antagonists; these agents inhibit bronchoconstriction in normal subjects provoked with inhaled cysteinyl leukotrienes, as well as in patients with asthma undergoing allergen, exercise, cold air, or aspirin challenge. Montelukast is a potent and selective blocker of the CysLT(1) receptor. For treatment of chronic asthma, montelukast is administered once daily to adults as a 10-mg film-coated tablet, to children aged 6-14 years as a 5-mg chewable tablet, and to children aged 2-5 years as a 4-mg chewable tablet form. Given their efficacy, antiinflammatory activity, oral administration, and safety, leukotriene modifiers will play an important role in the treatment of asthmatic children.

No MeSH data available.


Related in: MedlinePlus