Clinical Pharmacokinetics of Bambuterol

@article{Sitar1996ClinicalPO,
  title={Clinical Pharmacokinetics of Bambuterol},
  author={Daniel S. Sitar},
  journal={Clinical Pharmacokinetics},
  year={1996},
  volume={31},
  pages={246-256}
}
  • D. Sitar
  • Published 1 October 1996
  • Biology, Medicine
  • Clinical Pharmacokinetics
SummaryBambuterol, a biscarbamate ester prodrug of the β2 adrenergic agonist terbutaline, has been approved for the treatment of asthma in 28 countries. It is available in 10 and 20mg (25 and 50 μmol) tablets as the hydrochloride salt.Bambuterol is stable to presystemic elimination and is concentrated by lung tissue after absorption from the gastrointestinal tract. The prodrug is hydrolysed to terbutaline primarily by butyrylcholinesterase, and lung tissue is capable of this metabolic pathway… 
Interaction of Human Butyrylcholinesterase Variants with Bambuterol and Terbutaline
TLDR
The affinity of all studied BChE variants for terbutaline was low, which suggests that ter butaline originating from bambuterol hydrolysis should not affect the hydrolytic of bambutanol by B ChE.
Prospective of human butyrylcholinesterase as a detoxifying antidote and potential regulator of controlled‐release drugs
TLDR
Clinical trials aimed at providing pharmacokinetic data and evaluation of safety issues of acute and chronic administration of purified HuBChE are expected to advance the concept of using the enzyme as a multipurpose drug.
THE STUDY OF THE KINETIC BEHAVIOR OF HORSE SERUM BUTYRYLCHOLINESTERASE WITH FLUOXETINE
TLDR
Low Ki value suggests that fluoxetine is a potent inhibitor of Butyrylcholinesterase even at therapeutic doses but the molecular mechanisms explaining the benefit of BChE inhibition in diseases remain to be elucidated.
Stereoselective Inhibition of Human Butyrylcholinesterase by the Enantiomers of Bambuterol and Their Intermediates
TLDR
The data indicate that MONO contribute significantly to the inhibition of BChE occurring in humans upon administration of normal doses of bambuterol, and the hydrolysis of MONO resulted in the rate-limiting step in the conversion of bamuterol in its pharmacologically active metabolite terbutaline.
Preparative HPLC separation of bambuterol enantiomers and stereoselective inhibition of human cholinesterases
TLDR
Both enantiomers inhibited all studied BChE variants; however, the rate of inhibition was about five times faster than with the (S)-enantiomer, and the inhibition rates for heterozygotes were between the respective constants for the corresponding homozygotes.
Effects of bambuterol and terbutaline on isolated rat’s tracheal smooth muscle
TLDR
This preparation was used to test the effects of bambuterol on isolated rat’s tracheal smooth muscle compared with terbutaline and indicated that adding bambutol induced a significant further contraction to 10−6 M methacholine-induced contraction when the preparation was increased to 10+4 M.
Sustained release of metformin via red blood cell accumulated sulfenamide prodrug.
TLDR
Because metformin was slowly liberated into plasma, the sulfenamide prodrug showed a sustained-release pharmacokinetic profile and longer plasma half-life for met formin after oral administration, which has great potential to improve meetformin therapy as the daily doses could be reduced.
In vivo metabolism study of (R)-bambuterol in humans using ultra high performance liquid chromatography with tandem mass spectrometry.
TLDR
It is shown that (R)-bambuterol was metabolized via hydrolysis, demethylation, oxygenation, glucuronidation, and sulfation pathways in vivo and this combined method was accurate and sensitive to identify the possible metabolites and to better understand the metabolism of (R-bambutol in vivo.
Bambuterol versus Montelukast in Patients with Chronic Asthma
TLDR
Both bambuterol and mont­elukast sodium showed significant improvement in asthma symptoms, pulmonary function test values and pulse oximetry after 4-week therapy, however, bambutol showed more significant improved in PFT values compared to montelukasts.
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  • Biology, Chemistry
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TLDR
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TLDR
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SummaryA method is presented for quantitative determination of terbutaline after administration of its prodrug Bambuterol. Terbutaline is extracted from plasma by liquid-solid extraction on small
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