Clinical pharmacology of montelukast

Knorr, Barbara; Holland, Stephen M.; Schwartz, Jules I.; Rogers, John; Reiss, Theodore F.

doi:10.1046/j.1472-9725.2001.t01-1-00011.x

Cited by 17 publications

(38 citation statements)

References 20 publications

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“…The concentrations of montelukast used in the current study (1-2 mM) closely approximate peak serum levels of ,1 mM attained during chemotherapy with this agent [14]. The concentration of formoterol in the airways is, however, more difficult to ascertain.…”

Section: Chemicals and Reagentsmentioning

confidence: 92%

Interactive inhibitory effects of formoterol and montelukast on activated human neutrophils

Gravett¹,

Theron²,

Steel³

et al. 2010

European Respiratory Journal

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The research question addressed in the current study was: do formoterol (1 and 10 nM) and montelukast (2 mM) possess interactive inhibitory effects on activated human neutrophils, particularly in relation to alterations in cyclic AMP and cytosolic Ca 2+ fluxes?Isolated human blood neutrophils were activated with the chemoattractant N-formyl-Lmethionyl-L-leucyl-L-phenylalanine (fMLP) (1 mM) in combination with cytochalasin B (CB; 3 mM). Fura-2-acetoxymethyl ester-based spectrofluorimetry, lucigenin-enhanced chemiluminescence, colorimetric and flow cytometric procedures were used to measure cytosolic Ca 2+ fluxes, production of superoxide, elastase release and beta-2 integrin (CR3) expression, respectively, while cyclic AMP and leukotriene (LT)B 4 were assayed using competitive binding ELISA procedures. Activation of the cells with fMLP/CB resulted in abrupt and sustained increases in cytosolic Ca 2+, as well as release of elastase and production of superoxide and LTB 4 , and expression of CR3, all of which were attenuated by formoterol and montelukast individually, and especially by the combination of these agents. These anti-inflammatory effects of each agent, as well as the combination, were associated with significant increases in cyclic AMP.The findings of the current study may explain the efficacy of montelukast and formoterol when used in combination with inhaled corticosteroids in the treatment of severe asthma, possibly by controlling neutrophil-driven inflammation of the airways.

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Section: Chemicals and Reagentsmentioning

confidence: 92%

Interactive inhibitory effects of formoterol and montelukast on activated human neutrophils

Gravett¹,

Theron²,

Steel³

et al. 2010

European Respiratory Journal

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“…Montelukast USA, dissolved in dimethyl sulphoxide (DMSO) to a stock concentration of 10 mM, and used at a fixed, final concentration of 100 nM, which is a therapeutically relevant concentration of this agent [5,6]. Unless indicated, all other chemicals and reagents were purchased from Sigma-Aldrich.…”

Section: Methodsmentioning

confidence: 99%

Leukotrienes C4 and D4 sensitize human neutrophils for hyperreactivity to chemoattractants

et al. 2009

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“…The mechanism of action is through high affinity and selectively binding to the Cys-LT 1 receptor without agonist activity 62. Gender and advanced age do not significantly influence montelukast pharmacokinetics 59,62. Montelukast is extensively bound to plasma proteins with a volume of distribution average of 8–11 liters, minimal distribution across the blood–brain barrier, and minimal tissue concentrations 24 hours after administration 59,62.…”

Section: Pharmacology Mode Of Action and Pharmacokinetics Of Montelmentioning

confidence: 98%

“…Once daily dosing at bedtime was chosen based on higher plasma levels at night when the circadian variation for asthma-related airway obstruction tends to be worse59 and when there may be a higher concentration of alveolar-tissue CD4 + lymphocytes 63. Pajaron-Fernandez and colleagues found no statistical difference in exercise challenge results when comparing morning vs evening montelukast dosing in 24 children aged 6–14 years, but showed better outcomes in some children with evening dosing 63.…”

Section: Pharmacology Mode Of Action and Pharmacokinetics Of Montelmentioning

confidence: 99%

“…Singulair is available in multiple oral formulations including a 10 mg film-coated tablet, 4 mg and 5 mg chewable tablets, and 4 mg oral granules 3. Singulair is administered 10 mg once daily to adults, 5 mg once daily to children aged 6–14 years, and 4 mg once daily to children aged 2–5 years for asthma treatment 59,62. In April 2007, the US Food and Drug Administration (FDA) approved montelukast as a single-dose preventative for EIB in patients aged 15 years or older 17.…”

Section: Pharmacology Mode Of Action and Pharmacokinetics Of Montelmentioning

confidence: 99%

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Exercise-induced asthma: critical analysis of the protective role of montelukast

Carver¹

2009

JAA

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Exercise-induced asthma/exercise-induced bronchospasm (EIA/EIB) is a prevalent and clinically important disease affecting young children through older adulthood. These terms are often used interchangeably and the differences are not clearly defined in the literature. The pathogenesis of EIA/EIB may be different in those with persistent asthma compared to those with exercise-induced symptoms only. The natural history of EIA is unclear and may be different for elite athletes. Leukotriene biology has helped the understanding of EIB. The type and intensity of exercise are important factors for EIB. Exercise participation is necessary for proper development and control of EIA is recommended. Symptoms of EIB should be confirmed by proper testing. Biologic markers may also be helpful in diagnosis. Not all exercise symptoms are from EIB. Many medication and nonpharmacologic treatments are available. Asthma education is an important component of managing EIA. Many medications have been tested and the comparisons are complicated. Montelukast is a US Food and Drug Administration-approved asthma and EIB controller and has a number of potential advantages to other asthma medications including short onset of action, ease of use, and lack of tolerance. Not all patients improve with montelukast and rescue medication should be available.

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Clinical pharmacology of montelukast

Cited by 17 publications

References 20 publications

Interactive inhibitory effects of formoterol and montelukast on activated human neutrophils

Interactive inhibitory effects of formoterol and montelukast on activated human neutrophils

Leukotrienes C4 and D4 sensitize human neutrophils for hyperreactivity to chemoattractants

Exercise-induced asthma: critical analysis of the protective role of montelukast

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