Ranolazine for the management of coronary artery disease
Despite coronary revascularization and standard antianginal therapy, many patients continue to experience symptoms of stable angina and progression of their disease. Ranolazine is a new class of antianginal agent. Unlike standard antianginal agents, it alters glucose and fatty acid metabolism for a...
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| Veröffentlicht in: | Clinical therapeutics 2006-12, Vol.28 (12), p.1996-2007 |
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| creator | Cheng, Judy W.M. |
| description | Despite coronary revascularization and standard antianginal therapy, many patients continue to experience symptoms of stable angina and progression of their disease. Ranolazine is a new class of antianginal agent. Unlike standard antianginal agents, it alters glucose and fatty acid metabolism for a different approach to the management of coronary artery disease.
This article discusses the clinical pharmacology of ranolazine and its use in the management of chronic stable angina.
Peer-reviewed articles and abstracts were identified from MEDLINE and the Current Contents database (both from 1966 to September 20, 2006) using the search terms
ranolazine, angina, pharmacokinetics, and
pharmacology. Citations from available articles were reviewed for additional references. Abstracts presented at recent professional meetings were also reviewed.
Ranolazine is a cell membrane inhibitor of the late sodium current. Extended-release ranolazine was recently approved in the United States for the treatment of chronic angina. Ranolazine is metabolized in the liver by the cytochrome P-450 (CYP) 3A4 system. Because of its potential to prolong corrected QT (QTc) intervals, ranolazine should not be used in patients with hepatic impairment, those with QTc prolongation, or those taking drugs known to prolong QTc intervals or drugs that are potent CYP 3A4 inhibitors. Other adverse effects of ranolazine include dizziness, headache, constipation, and nausea. Placebo-controlled clinical studies performed to date have found that sustained-release ranolazine 500 to 1500 mg PO BID was associated with significantly increased time to onset of angina (range of increase, 27.0–144.0 s;
P < 0.05 [varied among studies]), exercise duration (range of increase, 23.8–99.0 s;
P < 0.05 [varied among studies] ), and time to 1-mm ST depression (range of increase, 27.6–146.2 s;
P < 0.05 [varied among studies]). In addition, exercise duration was found to be significantly longer with ranolazine compared with atenolol (453 vs 430 s;
P = 0.006).
Ranolazine is a new antianginal agent that is effective in the management of chronic angina. Its unique mechanism of action warrants further study in other cardiovascular conditions such as heart failure and arrhythmias. Ongoing studies will address whether ranolazine can reduce clinical end points such as cardiovascular death and myocardial infarction. |
| doi_str_mv | 10.1016/j.clinthera.2006.12.009 |
| format | Article |
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This article discusses the clinical pharmacology of ranolazine and its use in the management of chronic stable angina.
Peer-reviewed articles and abstracts were identified from MEDLINE and the Current Contents database (both from 1966 to September 20, 2006) using the search terms
ranolazine, angina, pharmacokinetics, and
pharmacology. Citations from available articles were reviewed for additional references. Abstracts presented at recent professional meetings were also reviewed.
Ranolazine is a cell membrane inhibitor of the late sodium current. Extended-release ranolazine was recently approved in the United States for the treatment of chronic angina. Ranolazine is metabolized in the liver by the cytochrome P-450 (CYP) 3A4 system. Because of its potential to prolong corrected QT (QTc) intervals, ranolazine should not be used in patients with hepatic impairment, those with QTc prolongation, or those taking drugs known to prolong QTc intervals or drugs that are potent CYP 3A4 inhibitors. Other adverse effects of ranolazine include dizziness, headache, constipation, and nausea. Placebo-controlled clinical studies performed to date have found that sustained-release ranolazine 500 to 1500 mg PO BID was associated with significantly increased time to onset of angina (range of increase, 27.0–144.0 s;
P < 0.05 [varied among studies]), exercise duration (range of increase, 23.8–99.0 s;
P < 0.05 [varied among studies] ), and time to 1-mm ST depression (range of increase, 27.6–146.2 s;
P < 0.05 [varied among studies]). In addition, exercise duration was found to be significantly longer with ranolazine compared with atenolol (453 vs 430 s;
P = 0.006).
Ranolazine is a new antianginal agent that is effective in the management of chronic angina. Its unique mechanism of action warrants further study in other cardiovascular conditions such as heart failure and arrhythmias. Ongoing studies will address whether ranolazine can reduce clinical end points such as cardiovascular death and myocardial infarction.</description><identifier>ISSN: 0149-2918</identifier><identifier>EISSN: 1879-114X</identifier><identifier>DOI: 10.1016/j.clinthera.2006.12.009</identifier><identifier>PMID: 17296457</identifier><language>eng</language><publisher>Belle Mead, NJ: EM Inc USA</publisher><subject>Acetanilides - adverse effects ; Acetanilides - pharmacokinetics ; Acetanilides - therapeutic use ; Angina pectoris ; Angina Pectoris - drug therapy ; Angina Pectoris - etiology ; Biological and medical sciences ; Cardiology. Vascular system ; Cardiovascular disease ; Clinical Trials as Topic ; Coronary heart disease ; Coronary vessels ; Enzyme Inhibitors - adverse effects ; Enzyme Inhibitors - pharmacokinetics ; Enzyme Inhibitors - therapeutic use ; Exercise ; Heart ; Humans ; Ischemia ; Medical sciences ; Metabolism ; Oxidation ; Pharmacokinetics ; Pharmacology. Drug treatments ; Pharmacy ; Piperazines - adverse effects ; Piperazines - pharmacokinetics ; Piperazines - therapeutic use ; Ranolazine ; ranolazine, stable angina, coronary artery disease ; Treatment Outcome ; Vein & artery diseases</subject><ispartof>Clinical therapeutics, 2006-12, Vol.28 (12), p.1996-2007</ispartof><rights>2006 Excerpta Medica, Inc.</rights><rights>2007 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c427t-e80b07f7c09dee3f088ad5ae19b2b7cbcf866b77b83044fcf3bb5492bf6c444b3</citedby><cites>FETCH-LOGICAL-c427t-e80b07f7c09dee3f088ad5ae19b2b7cbcf866b77b83044fcf3bb5492bf6c444b3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0149291806003122$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65306</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=18469432$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/17296457$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Cheng, Judy W.M.</creatorcontrib><title>Ranolazine for the management of coronary artery disease</title><title>Clinical therapeutics</title><addtitle>Clin Ther</addtitle><description>Despite coronary revascularization and standard antianginal therapy, many patients continue to experience symptoms of stable angina and progression of their disease. Ranolazine is a new class of antianginal agent. Unlike standard antianginal agents, it alters glucose and fatty acid metabolism for a different approach to the management of coronary artery disease.
This article discusses the clinical pharmacology of ranolazine and its use in the management of chronic stable angina.
Peer-reviewed articles and abstracts were identified from MEDLINE and the Current Contents database (both from 1966 to September 20, 2006) using the search terms
ranolazine, angina, pharmacokinetics, and
pharmacology. Citations from available articles were reviewed for additional references. Abstracts presented at recent professional meetings were also reviewed.
Ranolazine is a cell membrane inhibitor of the late sodium current. Extended-release ranolazine was recently approved in the United States for the treatment of chronic angina. Ranolazine is metabolized in the liver by the cytochrome P-450 (CYP) 3A4 system. Because of its potential to prolong corrected QT (QTc) intervals, ranolazine should not be used in patients with hepatic impairment, those with QTc prolongation, or those taking drugs known to prolong QTc intervals or drugs that are potent CYP 3A4 inhibitors. Other adverse effects of ranolazine include dizziness, headache, constipation, and nausea. Placebo-controlled clinical studies performed to date have found that sustained-release ranolazine 500 to 1500 mg PO BID was associated with significantly increased time to onset of angina (range of increase, 27.0–144.0 s;
P < 0.05 [varied among studies]), exercise duration (range of increase, 23.8–99.0 s;
P < 0.05 [varied among studies] ), and time to 1-mm ST depression (range of increase, 27.6–146.2 s;
P < 0.05 [varied among studies]). In addition, exercise duration was found to be significantly longer with ranolazine compared with atenolol (453 vs 430 s;
P = 0.006).
Ranolazine is a new antianginal agent that is effective in the management of chronic angina. Its unique mechanism of action warrants further study in other cardiovascular conditions such as heart failure and arrhythmias. Ongoing studies will address whether ranolazine can reduce clinical end points such as cardiovascular death and myocardial infarction.</description><subject>Acetanilides - adverse effects</subject><subject>Acetanilides - pharmacokinetics</subject><subject>Acetanilides - therapeutic use</subject><subject>Angina pectoris</subject><subject>Angina Pectoris - drug therapy</subject><subject>Angina Pectoris - etiology</subject><subject>Biological and medical sciences</subject><subject>Cardiology. Vascular system</subject><subject>Cardiovascular disease</subject><subject>Clinical Trials as Topic</subject><subject>Coronary heart disease</subject><subject>Coronary vessels</subject><subject>Enzyme Inhibitors - adverse effects</subject><subject>Enzyme Inhibitors - pharmacokinetics</subject><subject>Enzyme Inhibitors - therapeutic use</subject><subject>Exercise</subject><subject>Heart</subject><subject>Humans</subject><subject>Ischemia</subject><subject>Medical sciences</subject><subject>Metabolism</subject><subject>Oxidation</subject><subject>Pharmacokinetics</subject><subject>Pharmacology. Drug treatments</subject><subject>Pharmacy</subject><subject>Piperazines - adverse effects</subject><subject>Piperazines - pharmacokinetics</subject><subject>Piperazines - therapeutic use</subject><subject>Ranolazine</subject><subject>ranolazine, stable angina, coronary artery disease</subject><subject>Treatment Outcome</subject><subject>Vein & artery diseases</subject><issn>0149-2918</issn><issn>1879-114X</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2006</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><sourceid>8G5</sourceid><sourceid>BENPR</sourceid><sourceid>GUQSH</sourceid><sourceid>M2O</sourceid><recordid>eNqFkE1rGzEQhkVJaNy0f6FZCDnuZqSVV9LRhHwUAoXSQG5C0o4SGVtypHUh-fVV8NIcyxzm8rzvDA8hZxQ6CnS4XHduE-L0jNl0DGDoKOsA1CeyoFKollL-eEQWQLlqmaLyhHwpZQ0AvVqyz-SECqYGvhQLIn-ZmDbmLURsfMpNrWy2Jpon3GKcmuQbl3KKJr82Jk9Y1xgKmoJfybE3m4Lf5n1KHm6uf1_dtfc_b39cre5bx5mYWpRgQXjhQI2IvQcpzbg0SJVlVjjrvBwGK4SVPXDune-tXXLFrB8c59z2p-T80LvL6WWPZdLrtM-xntQUeqbqQF8pcaBcTqVk9HqXw7Z-XSH9bkyv9T9j-t2YpkxXYzX5fe7f2y2OH7lZUQUuZsAUZzY-m-hC-eAkHxTvWeVWBw6rjT8Bsy4uYHQ4hoxu0mMK_33mL86TjgE</recordid><startdate>20061201</startdate><enddate>20061201</enddate><creator>Cheng, Judy W.M.</creator><general>EM Inc USA</general><general>Excerpta Medica</general><general>Elsevier Limited</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>3V.</scope><scope>7RV</scope><scope>7X7</scope><scope>7XB</scope><scope>88C</scope><scope>88E</scope><scope>8AO</scope><scope>8FI</scope><scope>8FJ</scope><scope>8FK</scope><scope>8G5</scope><scope>ABUWG</scope><scope>AFKRA</scope><scope>AZQEC</scope><scope>BENPR</scope><scope>CCPQU</scope><scope>DWQXO</scope><scope>FYUFA</scope><scope>GHDGH</scope><scope>GNUQQ</scope><scope>GUQSH</scope><scope>K9.</scope><scope>KB0</scope><scope>M0S</scope><scope>M0T</scope><scope>M1P</scope><scope>M2O</scope><scope>M7N</scope><scope>MBDVC</scope><scope>NAPCQ</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><scope>PRINS</scope><scope>Q9U</scope></search><sort><creationdate>20061201</creationdate><title>Ranolazine for the management of coronary artery disease</title><author>Cheng, Judy W.M.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c427t-e80b07f7c09dee3f088ad5ae19b2b7cbcf866b77b83044fcf3bb5492bf6c444b3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2006</creationdate><topic>Acetanilides - adverse effects</topic><topic>Acetanilides - pharmacokinetics</topic><topic>Acetanilides - therapeutic use</topic><topic>Angina pectoris</topic><topic>Angina Pectoris - drug therapy</topic><topic>Angina Pectoris - etiology</topic><topic>Biological and medical sciences</topic><topic>Cardiology. Vascular system</topic><topic>Cardiovascular disease</topic><topic>Clinical Trials as Topic</topic><topic>Coronary heart disease</topic><topic>Coronary vessels</topic><topic>Enzyme Inhibitors - adverse effects</topic><topic>Enzyme Inhibitors - pharmacokinetics</topic><topic>Enzyme Inhibitors - therapeutic use</topic><topic>Exercise</topic><topic>Heart</topic><topic>Humans</topic><topic>Ischemia</topic><topic>Medical sciences</topic><topic>Metabolism</topic><topic>Oxidation</topic><topic>Pharmacokinetics</topic><topic>Pharmacology. Drug treatments</topic><topic>Pharmacy</topic><topic>Piperazines - adverse effects</topic><topic>Piperazines - pharmacokinetics</topic><topic>Piperazines - therapeutic use</topic><topic>Ranolazine</topic><topic>ranolazine, stable angina, coronary artery disease</topic><topic>Treatment Outcome</topic><topic>Vein & artery diseases</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Cheng, Judy W.M.</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><collection>ProQuest Central (Corporate)</collection><collection>Nursing & Allied Health Database</collection><collection>Health & Medical Collection</collection><collection>ProQuest Central (purchase pre-March 2016)</collection><collection>Healthcare Administration Database (Alumni)</collection><collection>Medical Database (Alumni Edition)</collection><collection>ProQuest Pharma Collection</collection><collection>Hospital Premium Collection</collection><collection>Hospital Premium Collection (Alumni Edition)</collection><collection>ProQuest Central (Alumni) (purchase pre-March 2016)</collection><collection>Research Library (Alumni Edition)</collection><collection>ProQuest Central (Alumni Edition)</collection><collection>ProQuest Central UK/Ireland</collection><collection>ProQuest Central Essentials</collection><collection>ProQuest Central</collection><collection>ProQuest One Community College</collection><collection>ProQuest Central Korea</collection><collection>Health Research Premium Collection</collection><collection>Health Research Premium Collection (Alumni)</collection><collection>ProQuest Central Student</collection><collection>Research Library Prep</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><collection>Nursing & Allied Health Database (Alumni Edition)</collection><collection>Health & Medical Collection (Alumni Edition)</collection><collection>Healthcare Administration Database</collection><collection>Medical Database</collection><collection>Research Library</collection><collection>Algology Mycology and Protozoology Abstracts (Microbiology C)</collection><collection>Research Library (Corporate)</collection><collection>Nursing & Allied Health Premium</collection><collection>ProQuest One Academic Eastern Edition (DO NOT USE)</collection><collection>ProQuest One Academic</collection><collection>ProQuest One Academic UKI Edition</collection><collection>ProQuest Central China</collection><collection>ProQuest Central Basic</collection><jtitle>Clinical therapeutics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Cheng, Judy W.M.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Ranolazine for the management of coronary artery disease</atitle><jtitle>Clinical therapeutics</jtitle><addtitle>Clin Ther</addtitle><date>2006-12-01</date><risdate>2006</risdate><volume>28</volume><issue>12</issue><spage>1996</spage><epage>2007</epage><pages>1996-2007</pages><issn>0149-2918</issn><eissn>1879-114X</eissn><abstract>Despite coronary revascularization and standard antianginal therapy, many patients continue to experience symptoms of stable angina and progression of their disease. Ranolazine is a new class of antianginal agent. Unlike standard antianginal agents, it alters glucose and fatty acid metabolism for a different approach to the management of coronary artery disease.
This article discusses the clinical pharmacology of ranolazine and its use in the management of chronic stable angina.
Peer-reviewed articles and abstracts were identified from MEDLINE and the Current Contents database (both from 1966 to September 20, 2006) using the search terms
ranolazine, angina, pharmacokinetics, and
pharmacology. Citations from available articles were reviewed for additional references. Abstracts presented at recent professional meetings were also reviewed.
Ranolazine is a cell membrane inhibitor of the late sodium current. Extended-release ranolazine was recently approved in the United States for the treatment of chronic angina. Ranolazine is metabolized in the liver by the cytochrome P-450 (CYP) 3A4 system. Because of its potential to prolong corrected QT (QTc) intervals, ranolazine should not be used in patients with hepatic impairment, those with QTc prolongation, or those taking drugs known to prolong QTc intervals or drugs that are potent CYP 3A4 inhibitors. Other adverse effects of ranolazine include dizziness, headache, constipation, and nausea. Placebo-controlled clinical studies performed to date have found that sustained-release ranolazine 500 to 1500 mg PO BID was associated with significantly increased time to onset of angina (range of increase, 27.0–144.0 s;
P < 0.05 [varied among studies]), exercise duration (range of increase, 23.8–99.0 s;
P < 0.05 [varied among studies] ), and time to 1-mm ST depression (range of increase, 27.6–146.2 s;
P < 0.05 [varied among studies]). In addition, exercise duration was found to be significantly longer with ranolazine compared with atenolol (453 vs 430 s;
P = 0.006).
Ranolazine is a new antianginal agent that is effective in the management of chronic angina. Its unique mechanism of action warrants further study in other cardiovascular conditions such as heart failure and arrhythmias. Ongoing studies will address whether ranolazine can reduce clinical end points such as cardiovascular death and myocardial infarction.</abstract><cop>Belle Mead, NJ</cop><pub>EM Inc USA</pub><pmid>17296457</pmid><doi>10.1016/j.clinthera.2006.12.009</doi><tpages>12</tpages></addata></record> |
| fulltext | fulltext |
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| ispartof | Clinical therapeutics, 2006-12, Vol.28 (12), p.1996-2007 |
| issn | 0149-2918 1879-114X |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Acetanilides - adverse effects Acetanilides - pharmacokinetics Acetanilides - therapeutic use Angina pectoris Angina Pectoris - drug therapy Angina Pectoris - etiology Biological and medical sciences Cardiology. Vascular system Cardiovascular disease Clinical Trials as Topic Coronary heart disease Coronary vessels Enzyme Inhibitors - adverse effects Enzyme Inhibitors - pharmacokinetics Enzyme Inhibitors - therapeutic use Exercise Heart Humans Ischemia Medical sciences Metabolism Oxidation Pharmacokinetics Pharmacology. Drug treatments Pharmacy Piperazines - adverse effects Piperazines - pharmacokinetics Piperazines - therapeutic use Ranolazine ranolazine, stable angina, coronary artery disease Treatment Outcome Vein & artery diseases |
| title | Ranolazine for the management of coronary artery disease |
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