Trial reportBritish journal of clinical pharmacology2000
Enantiomeric disposition of inhaled, intravenous and oral racemic-salbutamol in man--no evidence of enantioselective lung metabolism.
Trial report in British journal of clinical pharmacology, 2000. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
16 citing papers in PubMed.
- Beclomethasone dipropionate: absolute bioavailability, pharmacokinetics and metabolism following intravenous, oral, intranasal and inhaled administration in man.British journal of clinical pharmacology · 2001Trial
- Subject-Specific Whole-Lung CFPD Coupled with PBPK/PD to Predict Inhaled Bronchodilator Response in Asthmatic and Healthy Subjects.Journal of aerosol science · 2026Article
- BetaDrug testing and analysis · 2025Article
- Development of an HPLC-MS/MS Method for Chiral Separation and Quantitation of (Molecules (Basel, Switzerland) · 2023Article
- Management of IgE-mediated food allergy in the 21st century.Clinical and experimental allergy : journal of the British Society for Allergy and Clinical Immunology · 2023Review
- Salbutamol in the Management of Asthma: A Review.International journal of molecular sciences · 2022Review
- Muscle hypertrophic effect of inhaled betaThe Journal of physiology · 2022Article
- Inferring pulmonary exposure based on clinical PK data: accuracy and precision of model-based deconvolution methods.Journal of pharmacokinetics and pharmacodynamics · 2022Article
- An Abductive Inference Approach to Assess the Performance-Enhancing Effects of Drugs Included on the World Anti-Doping Agency Prohibited List.Sports medicine (Auckland, N.Z.) · 2021Review
- Bronchopulmonary pharmacokinetics of (R)-salbutamol and (S)-salbutamol enantiomers in pulmonary epithelial lining fluid and lung tissue of horses.British journal of clinical pharmacology · 2017Article
- Beta2-Agonist Doping Control and Optical Isomer Challenges.Sports medicine (Auckland, N.Z.) · 2016Article
- Comparative pharmacokinetics and bile transformation of R-enantiomer and racemic bambuterol after single-dose intravenous, oral administration in rats and beagle dogs.European journal of drug metabolism and pharmacokinetics · 2015Article
- An aerosol formulation of R-salbutamol sulfate for pulmonary inhalation.Acta pharmaceutica Sinica. B · 2014Article
- Albuterol enantiomer levels, lung function and QTc interval in patients with acute severe asthma and COPD in the emergency department.International journal of emergency medicine · 2011Article
- The pharmacokinetics of levosalbutamol: what are the clinical implications?Clinical pharmacokinetics · 2001Review
- Comparative study of the bronchodilator efficacy and adverse effects of salbutamol and hyoscine butylbromide in horses with severe asthma.Journal of veterinary internal medicineArticle
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
6 authors.
Funding
Abstract
Aims To establish whether enantioselective metabolism of racemic (rac )-salbutamol occurs in the lungs by determining its enantiomeric disposition following inhalation, in the absence and presence of oral charcoal, compared with that following the oral and intravenous routes. Methods Fifteen healthy subjects (eight male) were randomized into an open design, crossover study. Plasma and urine salbutamol enantiomer concentrations were measured for 24 h following oral (2 mg) with or without oral charcoal (to block oral absorption), inhaled (MDI; 1200 microg) with or without oral charcoal and intravenous (500 microg) rac-salbutamol. Systemic exposure (plasma AUC(0,infinity) and urinary excretion (Au24h ) of both enantiomers were calculated, and relative exposure to (R)-salbutamol both in plasma (AUC(R)-/AUC(S)- ) and urine (Au(R)-/Au(S)- ) was derived for each route. Relative exposure after the inhaled with charcoal and oral routes were compared with the intravenous route. Results AUC(R)-/AUC(S)- [geometric mean (95% CI)] was similar following the intravenous [0.32 (0.28, 0.36)] and inhaled with charcoal rates [0.29 (0.24, 0.36); P=0.046], but was far lower following oral dosing [0.05 (0.03, 0.07); P<0.001]. Similar results were found when relative exposure was analysed using Au24h. Conclusions These results show no evidence of significant enantioselective presystemic metabolism in the lungs, whilst confirming it in the gut and systemic circulation, indicating that the (R)- and (S)-enantiomers are present in similar quantities in the airways following inhaled rac-salbutamol.
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