Search results for "salbutamol"
showing 10 items of 27 documents
Modelling intestinal absorption of salbutamol sulphate in rats
2005
The objective was to develop a semiphysiological population pharmacokinetic model that describes the complex salbutamol sulphate absorption in rat small intestine. In situ techniques were used to characterize the salbutamol sulphate absorption at different concentrations (range: 0.15-18 mM). Salbutamol sulphate at concentration of 0.29 mM was administered in presence of verapamil (10 and 20 mM), grapefruit juice and sodium azide (NaN3) (0.3, 3 and 6 mM). Different pharmacokinetic models were fitted to the dataset using NONMEM. Parametric and non-parametric bootstrap analyses were employed as internal model evaluation techniques. The validated model suggested instantaneous equilibrium betwee…
The influence of active secretion processes on intestinal absorption of salbutamol in the rat.
2001
Abstract Salbutamol was perfused in the small intestine of rat using a standard rat gut ‘in situ’ preparation: (1) in inhibitor-free solution at seven different concentrations (0.15, 0.29, 1.20, 5.0, 9.0, 13.0 and 18.0 mM); (2) at a 0.29 mM concentration – thought to be close to the allometric dose in man – in the presence of a non-specific enzyme inhibitor, sodium azide (0.3, 3.0 and 6.0 mM); and (3) at 0.29 mM in the presence of a selective secretion inhibitor, verapamil (10.0 and 20.0 mM). In free solution, the mixed-order rate constants, k ′ a , of salbutamol increase as the solute concentration increases until an apparent asymptotic value is reached. This could be due to the saturation…
Use of asthma medication during pregnancy and risk of specific congenital anomalies: A European case-malformed control study.
2015
Background: Pregnant women with asthma need to take medication during pregnancy.Objective: We sought to identify whether there is an increased risk of specific congenital anomalies after exposure to antiasthma medication in the first trimester of pregnancy.Methods: We performed a population-based case-malformed control study testing signals identified in a literature review. Odds ratios (ORs) of exposure to the main groups of asthma medication were calculated for each of the 10 signal anomalies compared with registrations with nonchromosomal, nonsignal anomalies as control registrations. In addition, exploratory analyses were done for each nonsignal anomaly. The data set included 76,249 reg…
How Effective and Safe Is Bronchial Thermoplasty in “Real Life” Asthmatics Compared to Those Enrolled in Randomized Clinical Trials?
2016
There is limited information on the efficacy and safety of bronchial thermoplasty (BT) inreal life. We evaluated the outcomes of the randomized clinical trials for BT in severe asthmatics, in whom the exclusion criteria were not strictly controlled. A case series of seven asthmatics (M/F: 4/3; age:54.6±2.9years) is reported. Subjects had a statistically significant improvement in AQLQ (from a mean of3.96±1.1to4.5±1.2and5.5±0.6after 6 and 12 months of treatment;p=0.0007) and in the ACQ score (from2.77±0.8to1.83±1.2and1.5±0.8after 6 and 12 months;p<0.001). In the year after BT, severe exacerbations, salbutamol use, and OCS use were significantly lower compared with the 1-yr pretreatment pe…
The human near-term myometrialβ3-adrenoceptor but not theβ2-adrenoceptor is resistant to desensitisation after sustained agonist stimulation
2004
1. In order to compare the beta(2)- and beta(3)-adrenoceptor (beta-AR) desensitisation process in human near-term myometrium, we examined the influence of a pretreatment of myometrial strips with either a beta(2)- or a beta(3)-AR agonist (salbutamol or SR 59119A, respectively, both at 10 microm, for 5 and 15 h) on the relaxation and the cyclic adenosine monophosphate (cAMP) production induced by these agonists. 2. To assess some of the mechanisms potentially implicated in the beta-AR desensitisation process, we studied the influence of such treatment on the number of beta(2)- and beta(3)-AR binding sites, the beta(2)- and beta(3)-AR transcripts expression and the phosphodiesterase 4 (PDE4) …
Efficacy, tolerability, and effects on quality of life of inhaled salmeterol and oral theophylline in patients with mild-to-moderate chronic obstruct…
1998
Abstract The aims of management in mild-to-moderate stable chronic obstructive pulmonary disease (COPD) are to improve symptoms and quality of life (QOL), reduce decline in lung function, prevent and treat complications, increase survival while maintaining QOL, and minimize the adverse effects of treatment. Bronchodilator therapy is the keystone of improving COPD symptoms and functional capacity. The primary objective of this open-label study was to compare the efficacy and tolerability of salmeterol 50 μg BID administered by metered-dose inhaler versus oral, titrated, sustained-release theophylline BID, both given for 3 months to patients with a clinical history of chronic bronchitis. The …
Conditioning following powder micronization: influence on particle growth of salbutamol sulfate.
2003
Micronization is a high-energy process that induces changes in the crystallinity of materials. As a result, the crystalline structures on the particles' surface are being destroyed and amorphous areas are formed. After micronization of salbutamol sulfate to be used in dry powder inhalers, only small amounts of amorphous material are produced. Nevertheless, even these small amounts can have important effects on the physical stability of the powder. The amorphous state is thermodynamically unstable and tends to convert to the stable, crystalline state. The recrystallization process of disordered regions on the particles' surface leads to particle growth of milled particles. In this case, brid…
A pilot study demonstrating how inhaled furosemide enhances the bronchodilator effect of salbutamol
1993
Abstract To investigate whether inhaled furosemide can improve the bronchodilator effect of salbutamol, a single-blind crossover study in 10 subjects with stable asthma was designed. Each subject inhaled two puffs of salbutamol (200 μg) 1 hour after premedication with an aerosol preparation of either furosemide or placebo. Forced expiratory volume in 1 second (FEV 1 ) was measured before premedication, again before inhalation of salbutamol, and again 30, 60, and 90 minutes after, and 2, 3, 4, and 5 hours after inhalation of salbutamol. The FEV 1 at each time interval was greater on furosemide days but the difference was significant at 1, 4, and 5 hours after salbutamol inhalation. The areas…
Severe Brochostenosis by Oral Propafenone Immediately After Commencing Treatment
2011
Propafenone is a membrane-stabilizing agent belonging to a subgroup of the Vaughan Williams class I antidysrhythmic agents, structurally resembling propranolol and characterized by weaker beta-blocking activity. Despite respiratory complications having been reported as examples of side effects, very few reports have been published in the literature.We describe the case of an elderly woman with a history of hypertension and allergy to Parietaria, grass, olive, mites, and with periodic asthmatic manifestations, for whom the administration of oral propafenone for recurrent supraventricular dysrhythmia was associated with the sudden onset of severe bronchostenosis.A 78-year-old woman was freque…
Fluticasone/formoterol combination therapy versus budesonide/formoterol for the treatment of asthma: a randomized, controlled, non-inferiority trial …
2012
The inhaled corticosteroid fluticasone propionate (fluticasone) and the long-acting β₂ agonist formoterol fumarate (formoterol) have been combined in a single aerosol inhaler fluticasone/formoterol (flutiform(®)). This study compared the efficacy and safety of fluticasone/formoterol with the combination product budesonide/formoterol (Symbicort(®) Turbohaler(®)).A randomized, double-blind, double-dummy, multicenter, Phase 3 study comprising a 7- (± 3) day screening, 2-4-week run-in, and 12-week treatment periods. Patients aged ≥ 12 years with moderate to severe persistent asthma for ≥ 6 months before screening and forced expiratory volume in one second (FEV₁) 50-80% predicted and ≥ 15% rever…