Pharmacokinetics, efficacy and adverse effects of sublingual salbutamol in Patients with asthma
- 1 November 1989
- journal article
- research article
- Published by Springer Nature in European Journal of Clinical Pharmacology
- Vol. 37 (6), 567-571
- https://doi.org/10.1007/bf00562546
Abstract
Summary Administration of drugs by the sublingual route provides rapid systemic absorption and avoids first-pass metabolism. The purpose of the present study was to assess the pharmacokinetics, efficacy and adverse effects of standard salbutamol tablets given by this route to patients with asthma. Seven asthmatic patients were given either sublingual salbutamol tablet 2 mg (SL), swallowed tablet 2 mg (O), metered dose inhaler 200 µg (MDI) or placebo (PL), in a randomized single-blind cross-over design. Airways responses (FEV1, FVC, PEFR), finger tremor (Tr), heart rate (HR), plasma potassium (K) and plasma salbutamol were measured over a 6 h period following drug administration. There were highly significant changes in FEV1 with MDI, O and SL routes compared with PL, although the response to MDI was greater and more rapid than with O or SL. There were similar findings for FVC and PEFR responses. There were no adverse effects with MDI, whereas both 0 and SL produced significant tremor responses. There were no differences between O and SL for any of the pharmacodynamic parameters. In addition, pharmacokinetic profiles for O and SL were also similar apart from an initial delay in absorption with SL. There were however, no significant differences in any of the pharmacokinetic parameters, between O and SL. This suggests that buccal absorption of salbutamol was negligible, and that systemic absorption occurred after swallowing of the dissolved sublingual tablet. These results show that sublingual administration of salbutamol tablet has no clinical benefit over the oral route.Keywords
This publication has 12 references indexed in Scilit:
- Standardization of Spirometry—1987 UpdateAmerican Review of Respiratory Disease, 1987
- Pharmacokinetics and absolute bioavailability of salbutamol in healthy adult volunteersEuropean Journal of Clinical Pharmacology, 1987
- Systemic Cardiovascular and Metabolic Effects Associated with the Inhalation of an Increased Dose of AlbuterolChest, 1987
- Pharmacokinetics of intravenous and oral salbutamol and its sulphate conjugate.British Journal of Clinical Pharmacology, 1986
- Determination of salbutamol in plasma by high-performance liquid chromatography with fluorescence detectionJournal of Chromatography B: Biomedical Sciences and Applications, 1983
- Mouth spraying versus inhalation of fenoterol aerosol in healthy subjects and asthmatic patientsRespiratory Medicine, 1982
- Salbutamol aerosol causes a tachycardia due to the inhaled rather than the swallowed fraction.British Journal of Clinical Pharmacology, 1980
- Buccal absorption characteristics of some selective and non-selective beta-adrenoceptor agonists and antagonists [proceedings]British Journal of Clinical Pharmacology, 1980
- ESTRIP, a BASIC Computer Program for Obtaining Initial Polyexponential Parameter EstimatesJournal of Pharmaceutical Sciences, 1978
- Site of Beta-Adrenergic Receptors in the Respiratory TractChest, 1978