Kinetics of onset of rate-dependent effects of Class I antiarrhythmic drugs are important in determining their effects on refractoriness in guinea-pig ventricle, and provide a theoretical basis for their subclassification.

Abstract:

:The kinetics of onset of rate-dependent depression of maximum rate of depolarisation (Vmax) of guinea-pig ventricular action potentials were studied for nine Class I anti-arrhythmic drugs using standard microelectrode techniques. The drugs were found to fall into three well-demarcated subgroups with "fast" (lignocaine, tocainide and mexiletine), "intermediate" (quinidine, disopyramide and procainamide) and "slow" (flecainide, encainide and lorcainide) kinetics. The "fast" drugs were found to share the ability to markedly prolong the effective refractory period (ERP) relative to the action potential duration (APD). The "slow" drugs had only minor effects on this parameter. The "intermediate" drugs produced small to moderate increases in ERP relative to APD but in addition significantly prolonged APD, which was shortened by the "fast" drugs. Thus, using the parameters of speed of onset of rate-dependent depression of Vmax and APD it was possible to subdivide the nine Class I drugs into three distinct subclasses.

journal_name

Cardiovasc Res

journal_title

Cardiovascular research

authors

Campbell TJ

doi

10.1093/cvr/17.6.344

subject

Has Abstract

pub_date

1983-06-01 00:00:00

pages

344-52

issue

6

eissn

0008-6363

issn

1755-3245

journal_volume

17

pub_type

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