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Methadone inhibits KCNH2. 10 / 11
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"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 μM), hNav1.5 (11.2 μM tonic block; 5.5 μM phasic block), and hCav1.2 (26.7 μM tonic block; 7.7 μM phasic block)."
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"In contrast, methadone inhibited I hERG , I CaL , and I NaL ."
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"Based on the current literature, methadone, oliceridine, l-α-acetylmethadol (LAAM), and fentanyl were found to inhibit the HERG channel function and were associated with QTc prolongation."
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"Recent methadone isomers were shown to stereoselectively block a cardiac potassium channel (hERG)."
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"Methadone inhibits hERG at concentrations similar to peak plasma levels observed following administration of therapeutic doses ( Katchman et al., 2002; Kuryshev, Bruening-Wright, Brown, & Kirsch, 2010[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"In contrast, methadone, which directly blocks hERG channels, is associated with high TdP risk."
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"Prolonged Cardiac RepolarizationProlonged QT interval (QTc) is a rare, potentially serious adverse effect of methadone and other drugs that can block human ether-a-go-go gene (hERG)-related potassium ion channels and alter cardiac repolarization (Krantz, Martin, Stimmel, Mehta, & Haigney, 2009)."
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"These results showed the possible mechanism for arrythmogenic property of methadone and L-α-acetylmethadol by blocking I HERG channel [ 75 ]."
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"These interactions have been shown for methadone and chlorobutanol, which independently inhibit HERG currents in a concentration-dependent manner, and chlorobutanol potentiates methadone's ability to [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Methadone, an opioid receptor agonist, was found to also inhibit the currents and voltage of the HERG potassium channel in a subset of opioid-dependent patients (Eap et al., 2007)."
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