Improved bronchodilation with levalbuterol compared with racemic albuterol in patients with asthma☆☆☆★★★

Nelson, Harold S.; Bensch, George; Pleskow, Warren W.; DiSantostefano, Rachael L.; DeGraw, Sidney; Reasner, David S.; Rollins, Thomas E.; Rubin, Paul

doi:10.1016/s0091-6749(98)70332-x

Cited by 180 publications

(110 citation statements)

References 29 publications

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“…9 Nelson ve arkadaşlarının yaptığı çalışmada da genç hastaların 2,5 mg salbutamol kullanımı sonrasında kalp hızının arttığı bildirilmiştir. 10 Yüksek doz beta-2 mimetik tedavisi alan hastaların kan salbutamol düzeyi de yüksek bulunmuş ve bu hastalarda SVT riskinin arttığı saptanmıştır. 11,12 Hastamı-za uygulanmış olan salbutamol dozu 0,15 mg/kg/doz idi.…”

Section: Discussionunclassified

A case report with supraventricular tachycardia secondary to albuterol treatment

Giray¹,

Çöl²,

Yalvaç³

et al. 2015

Turk J Ped Em Int Care Med

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Section: Discussionunclassified

A case report with supraventricular tachycardia secondary to albuterol treatment

Giray¹,

Çöl²,

Yalvaç³

et al. 2015

Turk J Ped Em Int Care Med

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“…For regular administration in chronic stable asthma, the evidence from randomised double-blind studies is mixed, with one study supporting [61] and one not supporting [62] a therapeutic advantage for levalbuterol. There do not appear to have been any double-blind studies comparing levalbuterol and racemic albuterol in the management of asthma exacerbations in adults, and several recent double-blind studies in acute asthma in children have failed to find a therapeutic advantage for levalbuterol [63][64][65].…”

Section: -Agonists In the Management Of Exacerbationsmentioning

confidence: 99%

“…There do not appear to have been any double-blind studies comparing levalbuterol and racemic albuterol in the management of asthma exacerbations in adults, and several recent double-blind studies in acute asthma in children have failed to find a therapeutic advantage for levalbuterol [63][64][65]. The observed development of bronchodilator tolerance with regular administration of SABA [66] is obviously of concern in the context of increasing b 2 -agonist usage during asthma exacerbations, but the initial suggestion that such tachyphylaxis may be due to (S)-albuterol [61] appears not to be supported by evidence [67,68].…”

Section: -Agonists In the Management Of Exacerbationsmentioning

confidence: 99%

Pharmacological strategies for self-management of asthma exacerbations: Table 1—

Reddel

Barnes²

2006

Eur Respir J

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Written action plans are effective within asthma self-management, but there are few guidelines about the specific medication adjustments which can be recommended for selftreatment of exacerbations.This review examines pharmacological strategies for self-management of asthma exacerbations in adults, including those for inhaled corticosteroid/long-acting b 2 -agonist (ICS/LABA) users.Oral corticosteroids are well-established in clinical practice and clinical trials for the treatment of severe exacerbations, including during combination therapy. Evidence supports 7-10 days treatment, with no need to taper except to reduce side-effects. Doubling the dose of ICS is not effective. Several studies have shown benefit from high-dose ICS (2,400-4,000 mg beclomethasone equivalent) for 1-2 weeks. This may be achieved by adding a high-dose ICS inhaler to maintenance ICS or ICS/LABA therapy. There is inconclusive evidence about acutely increasing the dose of maintenance budesonide/formoterol for exacerbations, and no studies of this approach with fluticasone/salmeterol. For patients taking maintenance budesonide/formoterol, use of the same medication as-needed reduces exacerbations. Short-acting b 2 -agonists are still effective in producing bronchodilation during combination therapy; however, a higher dose may be required.There is a need for further studies to clarify remaining issues about self-management of asthma exacerbations, particularly with regard to side-effects of treatment and patient acceptability.

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“…The possibility that these effects are due to the distomers of b 2 -agonists has been addressed in a recent clinical study by NELSON et al [17]. In a placebo-controlled parallel group study, these investigators compared equivalent doses of R-and R,S-salbutamol given regularly by nebulizer over a four week period, and found evidence of a detrimental effect on the forced expiratory volume in one second (FEV1) with the racemate, which they attributed to the presence of the distomer.…”

mentioning

confidence: 99%

“…The validity of their findings and their clinical relevance has been debated [18]. More germane to the current question is the suggestion that the reason for any toxic effects attributable to b 2 -agonists is the longer half-life of the distomers, allowing them to exert negative effects in the absence of the mitigating actions of the bronchodilating eutomers [8,17]. Unfortunately, this argument is weakened by the fact that salbutamol is unique among the b 2 -agonists in undergoing more rapid enantioselective first pass metabolism of the eutomer.…”

mentioning

confidence: 99%

ß<SUB>2</SUB>-Agonist enantiomers: is there a glitch with the chiral switch?

Fawcett¹,

Taylor²

1999

Eur Respir J

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Current guidelines for the treatment of chronic asthma emphasize the use of anti-inflammatory medication and indicate that short-acting b 2 -agonists should only be taken on an as-needed basis [1]. This approach has been adopted because of the inflammatory nature of asthma and because, somewhat controversially, regular use of shortacting b 2 -agonists at best confers no distinct benefit on overall asthma control [2], and at worst may cause a deterioration [3].A number of possible mechanisms have been proposed to explain the adverse effects of chronic short-acting b 2 -agonist therapy [4], but the debate continues. One possible explanation currently under consideration is related to the fact that b 2 -agonists are chiral and are administered as racemic mixtures of a pharmacologically active eutomer (e.g. R-salbutamol) and an inactive distomer (e.g. S-salbutamol). The possibility that the distomers are selectively responsible for the toxic effects occurring during chronic treatment with racemates (e.g. R,S-salbutamol or R,S-fenoterol) has been extensively discussed [5,6], although no firm conclusions have been reached. In animal studies, the administration of racemates and distomers has been shown to enhance bronchial hyperresponsiveness [7,8], but this has not yet been demonstrated in human subjects during chronic dosing.The paper by SCHMEKEL et al. [9] in this issue of the Journal contributes to the debate by providing further data related to the pharmacokinetics of salbutamol enantiomers. The results confirm earlier findings [10±12] that an oral dose of R,S-salbutamol is subject to extensive stereoselective first pass metabolism which leads to a high S:R ratio in the plasma, and to exposure to the more slowly cleared distomer in the absence of the eutomer. In addition, it is shown that salbutamol administered by inhalation is also subject to stereoselective metabolism, and that multiple dosing by inhalation at clinically relevant time intervals leads to an increase in the S:R ratio as steady state is approached. Since there is some evidence that S-salbutamol acts as a functional antagonist to the active enantiomer [12], the potential for exposure to high levels of S-salbutamol provides an attractive alternative to tolerance to explain the reduction in bronchodilator efficacy during chronic dosing with racemic drug.The fact that salbutamol delivered by inhalation undergoes similar enantioselective first pass metabolism to that given orally is not surprising since inhalation of dry powder inevitably involves considerable oral ingestion. It also seems likely that lung metabolism of inhaled salbutamol may be stereoselective, as suggested by in vitro studies [13] and by the results reported by SCHMEKEL et al. [9]. Endotracheal aerosol administration resulted in higher plasma concentration of S-salbutamol but, in the absence of a comparative intravenous study in the same group of patients, it is difficult to quantify pre-systemic metabolism by the lung. In fact, the slow rate of absorption after endotracheal aerosol ...

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Improved bronchodilation with levalbuterol compared with racemic albuterol in patients with asthma☆☆☆★★★

Cited by 180 publications

References 29 publications

A case report with supraventricular tachycardia secondary to albuterol treatment

A case report with supraventricular tachycardia secondary to albuterol treatment

Pharmacological strategies for self-management of asthma exacerbations: Table 1—

ß<SUB>2</SUB>-Agonist enantiomers: is there a glitch with the chiral switch?

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