Source:http://linkedlifedata.com/resource/pubmed/id/19318692
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
4
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pubmed:dateCreated |
2009-3-25
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pubmed:abstractText |
This nonrandomized, fixed-sequence, 3-period study investigated potential pharmacokinetic interactions between the leukotriene receptor antagonist montelukast, approved for the treatment of asthma, and roflumilast, an oral, once-daily phosphodiesterase 4 inhibitor in clinical development for asthma and chronic obstructive pulmonary disease. Pharmacokinetic interactions are of interest because both drugs may be coadministered and share a common metabolic pathway via cytochrome P450 3A. Single-dose montelukast (10 mg, po) was administered alone in period 1, followed by repeated once-daily roflumilast alone (500 microg, po) for 12 days (period 2). In period 3, 500 microg qd roflumilast was coadministered with 10 mg qd montelukast for 8 days. Different pharmacokinetic parameters were evaluated for montelukast alone, for steady-state roflumilast and its pharmacologically active metabolite roflumilast N-oxide alone, for single-dose montelukast when coadministered with steady-state roflumilast, and for steady-state roflumilast and its N-oxide metabolite when coadministered with steady-state montelukast. The AUC and Cmax of montelukast were modestly increased by 9% and 8%, respectively, when single-dose montelukast was coadministered with steady-state roflumilast. The pharmacokinetics of roflumilast and roflumilast N-oxide in steady state remained unchanged when repeat-dose montelukast was coadministered at steady-state. Concomitant administration of both drugs was well tolerated. These findings suggest that no dose adjustment is warranted for either drug when roflumilast and montelukast are coadministered.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Acetates,
http://linkedlifedata.com/resource/pubmed/chemical/Aminopyridines,
http://linkedlifedata.com/resource/pubmed/chemical/Anti-Asthmatic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Benzamides,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclopropanes,
http://linkedlifedata.com/resource/pubmed/chemical/Leukotriene Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Phosphodiesterase Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Quinolines,
http://linkedlifedata.com/resource/pubmed/chemical/Roflumilast,
http://linkedlifedata.com/resource/pubmed/chemical/montelukast,
http://linkedlifedata.com/resource/pubmed/chemical/roflumilast N-oxide
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pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
0091-2700
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
49
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
389-97
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:19318692-Acetates,
pubmed-meshheading:19318692-Administration, Oral,
pubmed-meshheading:19318692-Adolescent,
pubmed-meshheading:19318692-Adult,
pubmed-meshheading:19318692-Aminopyridines,
pubmed-meshheading:19318692-Anti-Asthmatic Agents,
pubmed-meshheading:19318692-Benzamides,
pubmed-meshheading:19318692-Cyclopropanes,
pubmed-meshheading:19318692-Drug Interactions,
pubmed-meshheading:19318692-Drug Therapy, Combination,
pubmed-meshheading:19318692-Humans,
pubmed-meshheading:19318692-Leukotriene Antagonists,
pubmed-meshheading:19318692-Male,
pubmed-meshheading:19318692-Middle Aged,
pubmed-meshheading:19318692-Phosphodiesterase Inhibitors,
pubmed-meshheading:19318692-Quinolines
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pubmed:year |
2009
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pubmed:articleTitle |
The targeted oral, once-daily phosphodiesterase 4 inhibitor roflumilast and the leukotriene receptor antagonist montelukast do not exhibit significant pharmacokinetic interactions.
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pubmed:affiliation |
Department of Clinical Pharmacology, University Hospital of Tübingen, Otfried-Müller-Str 45, D-72076 Tübingen, Germany. gabriele.boehmer@med.uni-tuebingen.de
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pubmed:publicationType |
Journal Article,
Clinical Trial
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