IndraLab

Statements

Hydroxychloroquine inhibits Kr. 11 / 11
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"In patch clamped HEK293 cells expressing human cardiac ion channels, HCQ inhibited I Kr and I K1 at a therapeutic concentrations (IC 50 s: 10 ± 0.6 and 34 ± 5.0 μM)."
34661080
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"As modelled in this study, despite the absence of QT prolongation in baseline conditions because of a normal I Kr 85 and regardless of the origin of low repolarization reserve, these patients are at high risk of TdP when I Kr blockers such as HCQ are used."
34009333
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"XREF_BIBR In particular, the magnitude of the proarrhythmic potential of these drugs, specifically related to their QT prolongation effects, is questioned : On the one hand, the fact chloroquine and hydroxychloroquine block the I Kr potassium-channel at the myocyte level, therefore causing QT prolongation, is well documented."
32380291
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"As HCQ primarily blocks I Kr channels, the same drug concentrations would be expected to lead to significantly less pronounced APD prolongation in humans than in GP hearts."
34430945
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"By blocking -in order of increasing potency -the delayed (I Kr ) and inwardly-rectifying (I K1 ) K + currents [80] , and the latter preferentially at depolarised E m , CQ and HCQ significantly prolong the QT interval and slow ventricular conduction, thereby predisposing to early-after-depolarisation and, by extension, torsades de pointe."
| DOI
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"XREF_BIBR As modelled in the present study, cardiomyocytes harbouring mutations leading to haplo-insufficiency in KCNQ1 may present very minimal action potential prolongation because of a normal I Kr, XREF_BIBR but I Kr blockers such as HCQ, can lead to marked action potential prolongation in limited repolarization reserve."
34009333
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"to antagonize fibrillation following action potential shortening and inhomogeneity during ischemia.In SA node cells, Purkinje fibers and ventricular myocytes, hydroxychloroquine was shown to decrease the amplitude of the rapid delayed rectifier I Kr by 35 % [61] ."
| DOI
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"Hydroxychloroquine reduces a repolarizing current (I Kr), while AZM increases a depolarizing current (late I Na)."
34009333
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"Chloroquine and hydroxychloroquine inhibited I Kr (IC 50 : 1microM and 3-7microM, respectively) and I K1 currents (IC 50 : 5 and 44microM, respectively)."
33620150
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"37 As modelled in the present study, cardiomyocytes harbouring mutations leading to haploinsufficiency in KCNQ1 may present very minimal action potential prolongation because of a normal I Kr , 85 but I Kr blockers such as HCQ, can lead to marked action potential prolongation in limited repolarization reserve."
34009333
reach
"As modelled in this study, despite the absence of QT prolongation in baseline conditions because of a normal I Kr XREF_BIBR and regardless of the origin of low repolarization reserve, these patients are at high risk of TdP when I Kr blockers such as HCQ are used."
34009333