OBJECTIVE To systematically review the evidence for the medium to long term benefits and risks of montelukast as add-on therapy to inhaled corticosteroids (ICS) in comparison with placebo and active controls in mild to moderate asthma. DATA SOURCES Medline, Embase, Cochrane Register of Controlled Trials, reference lists of retrieved articles, clinical trial registries and study results databa...

Montelukast and desloratadine synergistically inhibit the allergen-induced early asthmatic response. Montelukast also suppresses the allergen-induced late asthmatic response, but there are no reports on the effect of desloratadine or the combination on the allergen-induced late asthmatic response. Atopic asthmatics (n = 10) completed a multicentric randomised double-blind crossover study compar...

Developing novel chemo-prevention techniques and advancing treatment are key elements to beating lung cancer, the most common cause of cancer mortality worldwide. Our previous cohort study showed that cysteinyl leukotriene receptor antagonists, mainly montelukast, decreased the lung cancer risk in asthma patients. In the current study, we conducted in vivo and in vitro experiments to demonstrat...

Fexofenadine is the hydrochloride salt of terfenadine’s active metabolite. In 2006, the FDA approved an oral suspension for the management of chronic idiopathic urticaria and seasonal allergic rhinitis in children. This review article summarizes the clinical pharmacology, therapeutic applications, drug-drug interactions, adverse events and food-drug interactions of fexofenadine that have been r...

Montelukast has been recommended as a selective in vitro and in vivo probe of cytochrome P450 (P450) CYP2C8 activity, but its selectivity toward this enzyme remains unclear. We performed detailed characterization of montelukast metabolism in vitro using human liver microsomes (HLMs), expressed P450s, and uridine 59-diphospho-glucuronosyltransferases (UGTs). Kinetic and inhibition experiments pe...

Background—Montelukast, a leukotriene receptor antagonist, improves parameters of asthma control including forced expiratory volume in one second (FEV1) when given orally to patients aged six years or older. This study was undertaken to compare the eVect on FEV1 of intravenous and oral montelukast and placebo during the 24 hour period following administration. Methods—Fifty one asthmatic patien...

BACKGROUND Montelukast, a leucotriene receptor antagonist, binds the cysteinyl leucotriene type 1 receptor. Montelukast is commonly prescribed to asthma patients as add-on therapy to inhaled corticosteroids. Several clinical trials emphasized that montelukast can be considered a safe drug. However, recent evidence reconsidered the benefit/risk ratio of the use of montelukast for both paediatric...

P-glycoprotein (P-gp), encoded by the multidrug resistance 1 gene (MDR1/ABCB1), exhibits very broad substrate specificity and plays important roles in drug disposition. The purpose of the present study was to examine the effect of impaired P-gp activity on the plasma pharmacokinetics of P-gp substrates in collies with or without homozygous mutant alleles producing truncated P-gp. Three therapeu...

Montelukast, a leukotriene receptor antagonist, is the most prescribed nonsteroidal anti-inflammatory drug used as an add-on therapy for asthma. Besides its effect on blocking action, montelukast has been proposed to have secondary properties. This study aimed investigate modulatory of expression major genes involved in airway inflammation (TNF, IL6) and remodeling (MMP9, TGFB1) response lipopo...

UNLABELLED Leukotriene modifiers (receptor antagonist and biosynthesis inhibitor) represent the first mediator specific therapeutic option for asthma. Montelukast, a leukotriene receptor antagonist is the only such agent approved for use in pediatric patients. Montelukast modifies action of leukotrienes, which are the most potent bronchoconstrictors, by blocking Cysteinyl leukotriene receptors....