In this study in patients with type 2 diabetes, near maximal glucose-lowering efficacy of sitagliptin after single oral doses was associated with inhibition of plasma DPP-4 activity of 80% or greater, corresponding to a plasma sitagliptin concentration of 100 nm or greater, and an augmentation of active GLP-1 and GIP levels of 2-fold or higher after an OGTT.
This study provides proof of pharmacologic characteristics for sitagliptin in humans. By inhibiting plasma DPP-IV activity, sitagliptin increases the postprandial rise in active glucagon-like peptide 1 concentrations without causing hypoglycemia in normoglycemic healthy male volunteers. Sitagliptin possesses pharmacokinetic and pharmacodynamic characteristics that support a once-daily dosing regimen.
Abstractleukotriene receptor antagonist provide further evidence of the role of leukotrienes Background -A study was undertaken to in the pathogenesis of exercise-induced determine whether montelukast, a new bronchoconstriction. potent cysteinyl leukotriene receptor (Thorax 1997;52:1030-1035 antagonist, attenuates exercise-induced bronchoconstriction. The relationship beKeywords: leukotriene receptor antagonist, exercisetween the urinary excretion of LTE 4 and induced bronchoconstriction, montelukast. exercise-induced bronchoconstriction was also investigated. Methods -Nineteen non-smoking asth-Cysteinyl leukotrienes, synthesised from matic patients with a forced expiratory arachidonic acid through the 5-lipoxygenase volume in one second (FEV 1 ) of [65% of pathway, have an important role in asthma. 1 the predicted value and a reproducible fall Leukotriene C 4 (LTC 4 ) is the dominant metain FEV 1 after exercise of at least 20% were bolite of arachidonic acid released in lung tissue enrolled. Subjects received placebo and but it is very unstable and quickly converted montelukast 100 mg once daily in the even-to leukotriene D 4 (LTD 4 ). In turn, LTD 4 is ing or 50 mg twice daily, each for two days, converted to a less potent metabolite, leukoin a three-period, randomised, double triene E 4 (LTE 4 ), which is excreted in the ilarly against exercise-induced broncho-available, selective, and potent cysteinyl leukoconstriction between plasma concentra-
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