The Research Behind Terbutaline

Persson, Henry

doi:10.1111/j.1600-0773.1995.tb01935.x

Cited by 5 publications

(4 citation statements)

References 11 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…65 lt was specifically developed to relax the trachea without affecting the cardiac muscle, and was first introduced in 1970. 66 Bronchodilation occurs rapidly after inhalation and effects may persist for 4-6 h (Table 2). Terbutaline is useful for as-needed medication.…”

Section: Terbutalinementioning

confidence: 99%

Past, present and future—β2-adrenoceptor agonists in asthma management

Sears

Lötvall

2005

Respiratory Medicine

129

View full text Add to dashboard Cite

The beta-adrenoceptor agonists (beta-agonists) have been used to relieve bronchoconstriction for at least 5000 years. beta-agonists are based on adrenaline and early forms, such as isoprenaline, Lacked bronchial selectivity and had unpleasant side effects. Modern beta-agonists are more selective for the beta2-adrenoceptors (beta2-receptors) located in bronchial smooth muscle and have less cardiotoxicity. Traditional beta2-adrenoceptor agonists (beta2-agonists), such as salbutamol, terbutaline and fenoterol, were characterised by a rapid onset but relatively short duration of action. While valuable as reliever medication, their short duration gave inadequate night-time relief and limited protection from exercise-induced bronchoconstriction. beta2-agonists with longer durations of action, formoterol and salmeterol, were subsequently discovered or developed. When combined with inhaled corticosteroids they improved lung function, and reduced symptoms and exacerbations more than an increased dose of corticosteroids. However, tolerance to the bronchprotective effects of long-acting beta2-agonists and cross-tolerance to the bronchodilator effects of short-acting beta2-agonists is apparent despite use of inhaled corticosteroids. The role of beta2-receptor polymorphisms in the development of tolerance has yet to be fully determined. Formoterol is unique in having both a long-lasting bronchodilator effect (> 12 h) and a fast onset of action (1-3min from inhalation), making it effective both as maintenance and reliever medication. The recent change in classification from short- and long-acting beta2-agonists to rapid-acting and/or long-acting agents reflects the ongoing evolution of beta2-agonist therapy.

show abstract

Section: Terbutalinementioning

confidence: 99%

Past, present and future—β2-adrenoceptor agonists in asthma management

Sears

Lötvall

2005

Respiratory Medicine

129

View full text Add to dashboard Cite

show abstract

“…For patients whose asthma is poorly controlled by ICS alone, β 2 ‐agonists with a long duration of action offer further potential benefits over short‐acting β 2 ‐agonists. Studies have shown that in these patients, when used in addition to low‐dose ICS, long‐acting β 2 ‐agonists are more effective than increasing the dose of ICS in patients whose asthma is poorly controlled by ICS alone 36,4–43 and are therefore a preferable clinical option. The exact mechanisms underlying the complementary benefits of adding a β 2 ‐agonist with a long duration of action to an ICS are not known 44 …”

Section: Benefits Of Long‐acting β2‐agonistsmentioning

confidence: 99%

“…The identification of selective β 2 ‐agonists (salbutamol, terbutaline and fenoterol) provided the next major improvement in therapy. Systemic side‐effects emanating from β 1 ‐receptor activity were effectively eliminated at normally used doses and, compared with previous β‐agonists, a far safer means of bronchodilatation for relief of symptoms was provided 6–8 . Development of inhalation systems that provide precise, efficient and targeted delivery to the lungs 9 has resulted in further reductions in unwanted systemic effects.…”

Section: Development Of β‐Agonistsmentioning

confidence: 99%

From Adrenaline to Formoterol: Advances in Β‐agonist Therapy in the Treatment of Asthma

2002

Int J Clinical Practice

View full text Add to dashboard Cite

SUMMARYLong‐acting β2‐agonists (formoterol and salmeterol) represent the latest advance in a series of improvements in β2‐agonist asthma therapy since the introduction of isoprenaline. Traditional inhaled short‐acting β2‐agonists (salbutamol and terbutaline) provide rapid as‐needed symptom relief and short‐term prophylactic protection against bronchoconstriction induced by exercise or other stimuli. Where symptoms are not adequately controlled by corticosteroids alone, inhaled selective long‐acting β2‐agonists are used additionally for maintenance. Salmeterol and formoterol are well tolerated, provide effective long‐term symptom control and reduce the incidence of exacerbations; any development of tolerance or masking of underlying inflammation with continual use does not appear to be clinically relevant. Formoterol is both rapid acting (as fast as salbutamol) and long acting (similar to salmeterol). Increasing clinical evidence suggests that inhaled formoterol is a convenient and well‐tolerated treatment that is effective both for regular maintenance and as‐needed relief of symptoms.

show abstract

“…[11] Nevertheless, the high enantiomeric excess obtained in the reduction of acetophenones substituted with electron-donating groups prompted us to extend the investigation to other electron-rich acetophenones. Their corresponding alcohols are present in numerous biologically active compounds like the topselling pharmaceuticals (R)-denopamine (3), [12] salmeterol (4) [13] and terbutaline (5) [14] ( Figure 2). The direct reduction of the ketones leading to compounds like 3-5 can, however, be difficult due to their additional functionality and possible chelating abilities.…”

Section: Introductionmentioning

confidence: 99%