Topic
Bitolterol
About: Bitolterol is a research topic. Over the lifetime, 33 publications have been published within this topic receiving 504 citations. The topic is also known as: Bitolterol Mesylate & Bitolterolum.
Papers
TL;DR: The pharmacological properties, clinical efficacy and adverse effects of these 2 categories of ~2agonists are compared and discussed, to better define their therapeutic usefulness in treating asthma.
Abstract: Evaluation of the role of adrenergic agents as bronchodilators started at the beginning of the century. In 1900, Solis-Cohen discovered a bronchodilator substance derived from the adrenal glands, later identified as epinephrine (adrenaline) [SolisCohen 1900]. A Chinese compound, ephedrine, was then introduced in 1924 for asthma treatment. In 1948, Ahlquist described (Xand ~-adreno receptors, and a ~-selective agent, isoprenaline (isoproterenol), was synthetised (Ahlquist 1948). Following the description of subclasses of ~ receptors, ~I and ~2 (Lands et al. 1967), a new category of agents with ~2-adrenoreceptor specificity was developed, including salbutamol (albuterol), terbutaline, fenoterol, rimiterol and pirbuterol. They provided more prolonged bronchodilator effects, lasting over 4 to 6 hours, with no or minimal cardiac stimulation. They were followed by other agents such as procaterol and bitolterol, which are similar to salbutamol in the magnitude and duration of the bronchodilatation provided (Petty et al. 1988). More recently, ~2-agonists with a prolonged duration of action were synthesised, such as bambuterol, salmeterol and formoterol (Johnson 1991a; LOfdahl 1990). Nonselective ~-adrenoceptor agents are no longer recommended in the treatment of asthma, but even the selective short-acting ~2-agonists have been recently reported to induce untoward effects during regular use, leading to close scrutiny of ~2-selective agents with long (> 12 hour) durations of action (Kuitert 1992; LOfdahl & Svedmyr 1991; Nelson et al. 1991; Page & Costello 1992; Skorodin 1993; Spitzer et al. 1992). In this review, the pharmacological properties, clinical efficacy and adverse effects of these 2 categories of ~2agonists are compared and discussed, to better define their therapeutic usefulness in treating asthma. The properties of ~2-agonists are summarised in table 1.
54 citations
TL;DR: If theophylline perturbed sleep when compared with beta 2-agonists and to determine which agent achieved best control of daytime and nocturnal pulmonary symptoms and lung dysfunction are evaluated.
Abstract: Many asthmatics complain of increased symptoms, awakenings, and need for additional medications during the sleeping hours. Sustained-release theophylline (THEO) may be superior to conventional inhaled bronchodilators in preventing nocturnal asthma symptoms and the early morning decrement in lung function common to this population. However, recent studies have demonstrated that THEO may delay sleep onset and perturb sleep stage distribution. No previous study has evaluated electroencephalographic, cardiac, and gas exchange indices during sleep in asthmatics treated with THEO compared with a long-acting inhaled beta2-agonist. The study goals were to determine if theophylline perturbed sleep when compared with beta2-agonists and to determine which agent achieved best control of daytime and nocturnal pulmonary symptoms and lung dysfunction. We evaluated 26 subjects with mild to moderate asthma and a history of frequent nocturnal symptoms who previously demonstrated decrements in AM lung function. THEO was com...
52 citations
TL;DR: The heavy rat appears to be a sensitive model for studying the interaction of these classes of drugs and the severity of the myocardial lesions produced by isoproterenol or bitolterol in heavy rats was significantly enhanced by aminophylline.
52 citations
TL;DR: There is no evidence from cardiac monitoring that therapeutic doses of bitolterol mesylate or theophylline alone or in combination have cardiotoxic effects.
Abstract: A higher incidence of fatal asthma after increased use of combined inhaled beta 2 -agonists and theophylline has been attributed to additive cardiac toxicity of these agents. This study had three major objectives: first, to evaluate the efficacy and safety of a new long-acting beta 2 -agonist, bitolterol mesylate, given as metered-dose aerosol in a regular "round-the-clock" asthma medication regimen; second, to compare the efficacy and safety of bitolterol with those of sustained-release theophylline alone and of the combination of bitolterol and theophylline; third, to use 24 hr Holter monitoring to evaluate cardiac toxicity of the three medication regimens. This was a 6 wk double-blind study of regular, daily medication in 36 young non-steroid-dependent and 37 older steroid-dependent stable asthmatic patients. All patients had two 24 hr Holter ECG monitorings during the 2 wk baseline period when all patients received theophylline only and four further 24 hr Holter monitorings during the double-blind period. All Holter recordings from the study groups showed no significant abnormalities in any treatment group. Pulmonary function studies were performed on 4 study days in the 6 wk double-blind period. The largest increase in bronchodilator effect was obtained with combined medication and the smallest with theophylline alone. Mean duration of action was markedly longer in the combined treatment group (>7 hr) than with bitolterol mesylate aerosol or theophylline alone (>5 and >4 hr. respectively) in the non-steroid-dependent patients. Degree of bronchodilation and during of action was less in the steroid-dependent patients in all treatment groups. There is no evidence from cardiac monitoring that therapeutic doses of bitolterol mesylate or theophylline alone or in combination have cardiotoxic-effects.
45 citations
TL;DR: The heart rate increases induced by the controlled-release formulations were gradual in onset, and the total increase in heart rate over a 6-hr period was less than that associated with the plain drug powder.
28 citations
Related Topics (5)
Performance Metrics
| Year | Papers |
|---|---|
| 2007 | 1 |
| 1996 | 1 |
| 1994 | 2 |
| 1993 | 1 |
| 1992 | 1 |
| 1990 | 1 |