Clinical Pharmacokinetics of Bambuterol

  title={Clinical Pharmacokinetics of Bambuterol},
  author={Daniel S. Sitar},
  journal={Clinical Pharmacokinetics},
  • 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
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
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.
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
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
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
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.
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.
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
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.


The effect of bambuterol (carbamylated terbutaline) on plasma cholinesterase activity and suxamethonium‐induced neuromuscular blockade in genotypically normal patients
The effect of bambuterol on suxamethonium‐induced neuromuscular blockade was studied in 10 patients undergoing elective laparotomy and five patients with very low plasma cholinesterase activity developed a long‐lasting phase II block.
Bambuterol, a carbamate ester prodrug of terbutaline, as inhibitor of cholinesterases in human blood.
  • A. Tunek, L. Svensson
  • Biology, Chemistry
    Drug metabolism and disposition: the biological fate of chemicals
  • 1988
Results indicate that bambuterol is a remarkably selective and potent inhibitor of cholinesterase.
Pharmacokinetics and pharmacodynamics of bambuterol, a long‐acting bronchodilator pro‐drug of terbutaline, in young and elderly patients with asthma
Bambuterol appears to offer the possibility of once‐daily therapy in both younger and older patients with asthma, and there was a greater area under the concentration versus time curve for terbutaline during a dose interval in older patients compared with younger patients.
The influence of 10 mg and 20 mg of bambuterol on the duration of succinylcholine‐induced neuromuscular blockade
A prolonged duration of action of succinylcholine can be expected in patients being treated with bambuterol in patients undergoing surgery under general anaesthesia.
The metabolism of terbutaline in man.
The metabolism of terbutaline has been investigated in man after oral, intravenous and subcutaneous administration of the tritium-labelled drug and hydrolysis of urine with β-glucuronidase and/or sulphatase indicates that the major metabolite is a sulphate conjugate of ter butaline.
The effect of bambuterol on plasma cholinesterase activity and suxamethonium‐induced neuromuscular blockade in subjects heterozygous for abnormal plasma cholinesterase
It is concluded that in patients heterozygous for abnormal plasma cholinesterase, bambuterol 20 mg taken 2 h before anaesthesia causes a 2–3 times prolongation of the neuromuscular blockade following suxamethonium 1 mg ± kg‐1 and in some patients a phase II block.
Bambuterol: clinical effects of different doses of a long-acting bronchodilator prodrug.
Bambuterol administrations of 0.185, 0.270 and 0.400 mg/kg gave effective and long-lasting bronchodilation, for at least 24 h, with the two higher doses probably close to the maximal effect of the drug.
Comparison between a new once-daily, bronchodilating drug, bambuterol, and terbutaline sustained-release, twice daily.
Whether bambuterol, given once daily, can control symptoms in asthmatic patients and to compare the bronchodilating effect and the side effects with those of terbutaline sustained-release (SR) tablets given twice daily are evaluated.
Quantitative determination of terbutaline in human plasma after administration of bambuterol using coupled columns and electrochemical detection
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