Clinical pharmacokinetics of bambuterol

Bambuterol, a biscarbamate ester prodrug of the beta 2 adrenergic agonist terbutaline, has been approved for the treatment of asthma in 28 countries. It is available in 10 and 20mg (25 and 50 mumol) tablets as the hydrochloride salt. Bambuterol is stable to presystemic elimination and is concentrate...

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Veröffentlicht in:Clinical pharmacokinetics 1996-10, Vol.31 (4), p.246-256
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description Bambuterol, a biscarbamate ester prodrug of the beta 2 adrenergic agonist terbutaline, has been approved for the treatment of asthma in 28 countries. It is available in 10 and 20mg (25 and 50 mumol) 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. It is also oxidatively metabolised to products which can be hydrolysed to terbutaline. Peak terbutaline plasma concentrations occur 3.9 to 6.8 hours after bambuterol ingestion, and the peak: trough terbutaline concentration ratio is lower than that after ingestion of terbutaline. Older patients have a greater area under the plasma concentration-time curve for terbutaline over a dose interval at steady-state. Whether genetic variations in the expression of butyrylcholinesterase alter therapeutic response remains to be determined. The efficacy of bambuterol has been demonstrated to last for 24 hours after ingestion; once-daily administration in the evening is recommended. Maximum therapeutic benefit requires more than 1 week of treatment. Except for the suppression of plasma butyrylcholinesterase, the adverse effect profile of bambuterol is essentially that of a beta 2 agonist and is best correlated with circulating terbutaline concentration in plasma. Plasma butyrylcholinesterase activity returns to control values approximately 2 weeks after discontinuation of treatment with bambuterol. This new drug provides oral beta 2 agonist therapy in a more convenient form than was available previously, and may have a better therapeutic: toxic ratio than terbutaline.
doi_str_mv 10.2165/00003088-199631040-00002
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Whether genetic variations in the expression of butyrylcholinesterase alter therapeutic response remains to be determined. The efficacy of bambuterol has been demonstrated to last for 24 hours after ingestion; once-daily administration in the evening is recommended. Maximum therapeutic benefit requires more than 1 week of treatment. Except for the suppression of plasma butyrylcholinesterase, the adverse effect profile of bambuterol is essentially that of a beta 2 agonist and is best correlated with circulating terbutaline concentration in plasma. Plasma butyrylcholinesterase activity returns to control values approximately 2 weeks after discontinuation of treatment with bambuterol. 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S</creatorcontrib><title>Clinical pharmacokinetics of bambuterol</title><title>Clinical pharmacokinetics</title><addtitle>Clin Pharmacokinet</addtitle><description>Bambuterol, a biscarbamate ester prodrug of the beta 2 adrenergic agonist terbutaline, has been approved for the treatment of asthma in 28 countries. It is available in 10 and 20mg (25 and 50 mumol) 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. It is also oxidatively metabolised to products which can be hydrolysed to terbutaline. Peak terbutaline plasma concentrations occur 3.9 to 6.8 hours after bambuterol ingestion, and the peak: trough terbutaline concentration ratio is lower than that after ingestion of terbutaline. 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This new drug provides oral beta 2 agonist therapy in a more convenient form than was available previously, and may have a better therapeutic: toxic ratio than terbutaline.</description><subject>Animals</subject><subject>Asthma - drug therapy</subject><subject>Biological and medical sciences</subject><subject>Bronchodilator Agents - metabolism</subject><subject>Bronchodilator Agents - pharmacokinetics</subject><subject>Bronchodilator Agents - therapeutic use</subject><subject>Humans</subject><subject>Medical sciences</subject><subject>Pharmacology. 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Drug treatments</topic><topic>Prodrugs - metabolism</topic><topic>Prodrugs - pharmacokinetics</topic><topic>Prodrugs - therapeutic use</topic><topic>Respiratory system</topic><topic>Terbutaline - analogs &amp; derivatives</topic><topic>Terbutaline - metabolism</topic><topic>Terbutaline - pharmacokinetics</topic><topic>Terbutaline - therapeutic use</topic><topic>Tissue Distribution</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>SITAR, D. S</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><jtitle>Clinical pharmacokinetics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>SITAR, D. S</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Clinical pharmacokinetics of bambuterol</atitle><jtitle>Clinical pharmacokinetics</jtitle><addtitle>Clin Pharmacokinet</addtitle><date>1996-10-01</date><risdate>1996</risdate><volume>31</volume><issue>4</issue><spage>246</spage><epage>256</epage><pages>246-256</pages><issn>0312-5963</issn><eissn>1179-1926</eissn><coden>CPKNDH</coden><abstract>Bambuterol, a biscarbamate ester prodrug of the beta 2 adrenergic agonist terbutaline, has been approved for the treatment of asthma in 28 countries. It is available in 10 and 20mg (25 and 50 mumol) 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. It is also oxidatively metabolised to products which can be hydrolysed to terbutaline. Peak terbutaline plasma concentrations occur 3.9 to 6.8 hours after bambuterol ingestion, and the peak: trough terbutaline concentration ratio is lower than that after ingestion of terbutaline. Older patients have a greater area under the plasma concentration-time curve for terbutaline over a dose interval at steady-state. Whether genetic variations in the expression of butyrylcholinesterase alter therapeutic response remains to be determined. The efficacy of bambuterol has been demonstrated to last for 24 hours after ingestion; once-daily administration in the evening is recommended. Maximum therapeutic benefit requires more than 1 week of treatment. Except for the suppression of plasma butyrylcholinesterase, the adverse effect profile of bambuterol is essentially that of a beta 2 agonist and is best correlated with circulating terbutaline concentration in plasma. Plasma butyrylcholinesterase activity returns to control values approximately 2 weeks after discontinuation of treatment with bambuterol. This new drug provides oral beta 2 agonist therapy in a more convenient form than was available previously, and may have a better therapeutic: toxic ratio than terbutaline.</abstract><cop>Auckland</cop><pub>Adis international</pub><pmid>8896942</pmid><doi>10.2165/00003088-199631040-00002</doi><tpages>11</tpages></addata></record>
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subjects Animals
Asthma - drug therapy
Biological and medical sciences
Bronchodilator Agents - metabolism
Bronchodilator Agents - pharmacokinetics
Bronchodilator Agents - therapeutic use
Humans
Medical sciences
Pharmacology. Drug treatments
Prodrugs - metabolism
Prodrugs - pharmacokinetics
Prodrugs - therapeutic use
Respiratory system
Terbutaline - analogs & derivatives
Terbutaline - metabolism
Terbutaline - pharmacokinetics
Terbutaline - therapeutic use
Tissue Distribution
title Clinical pharmacokinetics of bambuterol
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