Search results for "Theophylline"
showing 10 items of 60 documents
The novel combination of theophylline and bambuterol as a potential treatment of hypoxemia in humans.
2017
Hypoxemia can be life-threatening, both acutely and chronically. Because hypoxemia causes vascular dysregulation that further restricts oxygen availability to tissue, it can be pharmacologically addressed. We hypothesized that theophylline can be safely combined with the β2-adrenergic vasodilator bambuterol to improve oxygen availability in hypoxemic patients. Ergogenicity and hemodynamic effects of bambuterol and theophylline were measured in rats under hypobaric and normobaric hypoxia (12% O2). Feasibility in humans was assessed using randomized, double-blind testing of the influence of combined slow-release theophylline (300 mg) and bambuterol (20 mg) on adverse events (AEs), plasma K+,…
Investigation into the role of phosphodiesterase IV in bronchorelaxation, including studies with human bronchus.
1993
1. We have investigated the role of cyclic nucleotide phosphodiesterase IV (PDE IV) in the relaxation of human bronchus and guinea-pig trachea in vitro and in guinea-pigs in vivo. 2. Functional studies showed that the selective PDE IV inhibitors, rolipram and denbufylline, relaxed human and guinea-pig preparations in vitro. 3. Two clinically used xanthine non-selective PDE inhibitors, theophylline and pentoxifylline, were also effective in these preparations, but were much less potent than the selective agents used. 4. The rank order of potency for the four PDE inhibitors in both species was similar. 5. Biochemical studies indicated that PDE IV was the major PDE isoform present in the human…
Effects of dantrolene on the responses to methylxanthines in the isolated guinea-pig trachea.
1991
The effect of dantrolene on the responses to methylxanthines (caffeine and theophylline) and a beta-adrenoceptor agonist (salbutamol) was studied in isolated guinea-pig trachea. Caffeine and theophylline (1 microM-10 mM) and salbutamol (1 nM-10 microM) produced concentration-dependent relaxation of spontaneous and stimulated (acetylcholine 1 mM) tone. Responses to high concentrations (10 mM) of caffeine and theophylline added to tracheal strips either unstimulated (spontaneous tone) or indomethacin (2.8 microM)-treated were reversed to contractions in the presence of dantrolene (3 microM-0.3 mM). This effect was not observed for salbutamol or when relaxant responses to the agonists were gen…
Purinoceptor-mediated modulation by endogenous and exogenous agonists of stimulation-evoked [3H]noradrenaline release on rat iris.
1992
To investigate whether endogenous purinoceptor agonists affect the sympathetic neurotransmission in the rat isolated iris, and to classify the purinoceptors modulating exocytotic [3H]-noradrenaline release, we have determined the effect of adenosine receptor antagonists on, and the relative potency of selected agonists in modulating, the field stimulation-evoked (3 Hz, 2 min) [3H]-noradrenaline overflow. In addition, the apparent affinity constants of 8-phenyltheophylline (8-PT) and 1,3-dipropyl-8-cyclopentylxanthine (DPCPX) in antagonizing the prejunctional effects of purinoceptor agonists were estimated. The relatively A1-selective DPCPX 10 and 100 nmol/l increased the evoked [3H]-noradre…
Determination of trimethoprim by the linear absorbances method
1995
The determination of trimethoprim in the presence of dyphylline, proxyphylline, theophylline and caffeine by the linear absorbances method is described. Collinear couples of wavelengths, for the interfering dyphylline-proxyphylline-theophylline-caffeine system (in H2SO4, 0.05 mol/L), are provided in order to allow the determination of the analyte in the presence of these interfering substances.
Thermo-responsive hydrogels from cellulose-based polyelectrolytes and catanionic vesicles for biomedical application.
2016
In this study, negatively charged catanionic vesicles/hydrophobically modified hydroxyethylcellulose polymers thermo-responsive hydrogels have been fabricated. Vesicular aggregates were found to act as multifunctional junctions for networking of modified-cellulose water solutions. The contributions of the electrostatic and hydrophobic interactions were evaluated by changing either vesicles composition or the polymer hydrophobic substitution. Thermal-induced size and lamellarity of hydrogel-enclosed vesicles were detected, with further polygonal shape changes induced by cellulose-based polymer addition. The thermal transition was also found to tune hydrogel mechanical behaviour. The network …
Evidence that adenosine is not involved in the non-adrenergic non-cholinergic relaxation in the rat duodenum.
1990
In rat isolated duodenal segments, adenosine induced, in the presence of atropine and guanethidine, a dose-dependent, long-lasting (about 20 s), tetrodotoxin (TTX)-resistant relaxation both in endoluminal pressure and in isometric tension. Electrical field stimulation (EFS) induced, in the presence of atropine and guanethidine, a TTX-sensitive short-lasting (about 6 s) relaxation followed by a sustained rebound contraction. Theophylline, a P1 receptor antagonist, at the concentration of 100 microM caused a marked inhibition of the adenosine-induced relaxation, while the EFS-induced relaxation was not modified. Our results suggest that adenosine induces relaxation of the rat duodenal smooth …
The reluctant polymorph: investigation into the effect of self-association on the solvent mediated phase transformation and nucleation of theophylline
2015
Little is known concerning the pathway of the crystallization of the thermodynamically stable polymorph of theophylline, form IV. Here we study the reasons why the thermodynamically stable theophylline form IV can be obtained only by slow, solvent mediated phase transformation (SMPT) in specific solvents, and whether the presence of prenucleation aggregates affect the polymorphic outcome. Solution concentration, polymorphic composition and morphology were monitored over time during the transformation from form II to form IV in several solvents. NMR and FTIR spectroscopy were used to detect prenucleation molecular aggregates present in the solutions. It was determined that theophylline self-…
Determination of theophylline and paraxanthine in urine samples by liquid chromatography using the H-point standard additions method
1992
Abstract The simultaneous determination of theophylline and paraxanthine in urine samples by the H-point standard additions method (HPSAM) is described. Samples are extracted with C 18 solid-phase extraction cartridges and chromatographed using a Hypersil C 18 -ODS column and a mobile phase consisting of acetonirile-phosphate buffer in the gradient elution mode. Under these conditions theophylline and paraxanthine are eluted with short retention times. Although their chromatographic peaks are overlapped and their spectra are very similar, the H-point standard additions method provides excellent results in the determination of both xanthines at therapeutic levels.
The relaxant effects of cromakalim (BRL 34915) on human isolated airway smooth muscle
1992
Cromakalim (BRL 34915) is a potassium channel opener with therapeutic potential as a bronchodilator in asthma. Cromakalim (0.1–30 μmol/l) inhibited the spontaneous tone of human isolated bronchi n a concentration-related manner being nearly as effective as isoprenaline or theophylline. The order of relaxant potencies (expressed as -log10 IC50 mol/l; mean ±SEM) was isoprenaline (7.29 ± 0.27; n = 8) > cromakalim (5.89 ± 0.12; n = 7) > theophylline (4.07 ±0.13; n = 10). In human bronchi where tone had been raised by addition of histamine (0.1 mmol/l), acetylcholine (0.1 mmol/l) or leukotriene D4 (LTD4, 0.1 μmol/l), the relaxant effect of cromakalim was substantially reduced. Cromakalim suppres…