Title : Increased cardiac risk in concomitant methadone and diazepam treatment: pharmacodynamic interactions in cardiac ion channels.

Pub. Date : 2010 Oct

PMID : 20930594






2 Functional Relationships(s)
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1 Using patch clamp recording in human stem cell-derived cardiomyocytes and stably transfected mammalian cells, we found that methadone produced concentration-dependent AP prolongation and ion channel block at low micromolar concentrations: hERG (IC50 = 1.7 muM), hNav1.5 (11.2 muM tonic block; 5.5 muM phasic block), and hCav1.2 (26.7 muM tonic block; 7.7 muM phasic block). Methadone ETS transcription factor ERG Homo sapiens
2 Thus, although diazepam alone does not prolong the QT interval, the relief of methadone-induced Na channel block may leave hERG K channel block uncompensated, thereby increasing cardiac risk. Methadone ETS transcription factor ERG Homo sapiens