IndraLab

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Methadone inhibits KCNH2. 21 / 22
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"Methadone, buprenorphine and many structurally diverse drugs can block the hERG XREF_BIBR, XREF_BIBR resulting in a prolonged QTc interval XREF_BIBR."
20407978
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"While methadone is known to prolong the QT interval by blocking the cardiac human ether-a-go-go-related (hERG) potassium channel, the effect of methadone on QTc is associated with chronic dosing in adults rather than an isolated dose and it is the daily methadone dose that correlates positively with the QTc interval."
24666686
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"Both S- and R-form of methadone inhibit the cardiac potassium channel hERG (S-methadone is more potent blocker) [XREF_BIBR], which may increase heart risk."
26960809
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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)."
30310721
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No evidence text available
14527710
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"The opioid agonist methadone has previously been demonstrated to inhibit hERG currents, and there are reports of serious cardiac arrhythmias and deaths from TdP and ventricular fibrillation in patients taking methadone."
20467834
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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."
37015297
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"Inhibition of hERG by methadone is problematic, as methadone treatment may lead to cardiotoxicity (long QT syndrome) [XREF_BIBR, XREF_BIBR]."
22918821
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"QTc prolongation by hERG channel blockers such as methadone provides the substrate for torsade de pointes arrhythmia, but an additional trigger is typically required to initiate arrhythmia."
24666686
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"Methadone inhibits the cardiac potassium channel hERG and can cause a prolonged QT interval."
17329992
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"Methadone blocks the cardiac ionic channels hERG, the human ether-a-Go-Go tetrameric channel encoded by KCNH2 and responsible for the IKr current, in a concentration dependent manner (Katchman et al.,[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
24875677
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"In contrast, methadone inhibited I hERG , I CaL , and I NaL ."
33157550
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"Both methadone and heroin inhibit hERG currents in a concentration dependent manner."
20467834
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"In contrast, methadone, which directly blocks hERG channels, is associated with high TdP risk."
33157550
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"Furthermore, methadone blocks hERG in a concentration dependent manner (Katchman et al., 2002)."
24875677
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"Methadone is the most prescribed heroin maintenance treatment and is known to inhibit the cardiac potassium channel hERG, which recapitulates IKr."
24875677
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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)."
20930594
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"Methadone inhibition of hERG has been suggested to be caused possibly by direct binding to the hERG channel, perhaps at the voltage sensor [XREF_BIBR]."
22918821
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"Additionally, unsuspected polymorphisms in the gene for the hERG channel occur in 2% of the healthy population and may be associated with increased sensitivity to hERG channel blockade by methadone or similar compounds."
22026519
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"Methadone causes the blockade of hERG current and causes clinically significant QTc prolongation."
21253542
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"It was without surprise that methadone racemate was demonstrated to block I hERG1 in transfected HEK293 cells with an IC 50 of ~ 10 muM."
21833176