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Pharmacokinetics of bambuterol during oral administration to asthmatic children
Vise andre og tillknytning
1999 Inngår i: Br J Clin Pharmacol, Vol. 48, s. 299-308Artikkel i tidsskrift (Fagfellevurdert) Published
sted, utgiver, år, opplag, sider
1999. Vol. 48, s. 299-308
Identifikatorer
URN: urn:nbn:se:uu:diva-89460OAI: oai:DiVA.org:uu-89460DiVA, id: diva2:160909
Tilgjengelig fra: 2001-10-03 Laget: 2001-10-03bibliografisk kontrollert
Inngår i avhandling
1. Clinical-Pharmacokinetic Aspects of Prolonged Effect Duration as Illustrated by β2-Agonists
Åpne denne publikasjonen i ny fane eller vindu >>Clinical-Pharmacokinetic Aspects of Prolonged Effect Duration as Illustrated by β2-Agonists
2001 (engelsk)Doktoravhandling, med artikler (Annet vitenskapelig)
Abstract [en]

Regularity is a key element of maintenance drug treatment; compliance is crucial for treatment success. Once- or twice-daily intake of a drug is always easier to comply with than regimens requiring more frequent dosing. Bronchodilating treatment was used as an example to illustrate how sustained duration of effect can be achieved by two different approaches: oral administration of the terbutaline prodrug bambuterol and inhalation of formoterol. Bioanalytical methods were employed to monitor the kinetic fate of bambuterol and formoterol in plasma, urine, or faeces. Generated terbutaline in plasma was used as a marker of effect for bambuterol. Established clinical laboratory tests were used to assess local and systemic effects of inhaled formoterol compared with salbutamol.

Recommended doses of bambuterol, 10-20 mg once daily in adults, normally produced plasma concentrations of the active moiety terbutaline within therapeutically relevant limits. Dose proportionality for terbutaline makes dosing with bambuterol predictable. Compared with adults, children should be given higher doses than indicated by their lower body weight. Pharmacokinetic analysis indicated that absorption of bambuterol was slow and multi-phasic and that slow biotransformation to terbutaline occurred both presystemically and systemically.

Systemically circulating formoterol was rapidly eliminated, the inactive (S;S)-formoterol more rapidly than the active (R;R)-formoterol. An inactive phenol glucuronide was the main metabolite, and a previously unknown sulphate metabolite was discovered. Duration of systemically mediated cardiovascular or metabolic side-effects of inhaled formoterol seemed not to differ from those of an inhaled systemically equieffective dose of salbutamol. There was a trend suggesting that the magnitude of systemic side-effects may be less pronounced after inhalation of formoterol compared with a locally equieffective dose of inhaled salbutamol.

Both approaches to sustaining stimulation of β2-adrenoceptors have their pros and cons. Bambuterol can be dosed orally once daily, but full effect is reached slowly. The effect of formoterol is reached within a few minutes, but administration must occur via the lungs, often twice daily. Both treatments, however, give 24-h symptom relief during regular treatment.

sted, utgiver, år, opplag, sider
Uppsala: Acta Universitatis Upsaliensis, 2001. s. 41
Serie
Comprehensive Summaries of Uppsala Dissertations from the Faculty of Pharmacy, ISSN 0282-7484 ; 256
Emneord
Pharmaceutical biosciences, Farmaceutisk biovetenskap
HSV kategori
Forskningsprogram
galenisk farmaci
Identifikatorer
urn:nbn:se:uu:diva-1399 (URN)91-554-5099-7 (ISBN)
Disputas
2001-09-21, Uppsala Biomedical Center, lecture hall B41, Uppsala, 10:15
Opponent
Tilgjengelig fra: 2001-10-03 Laget: 2001-10-03 Sist oppdatert: 2018-01-13bibliografisk kontrollert

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