Mechanism of Action and Electrophysiology
Class IB drugs selectively block membrane sodium channels in their inactivated state. They are characterized by very rapid binding and dissociation kinetics (less than 1 second).
As a result, the rate of processes does not exceed the duration of the action potential, which provides important clinical features:
- No effect on normal sinus rhythm (heart rate is not slowed).
- Selective suppression of high-frequency premature impulses.
- Shortening of phase 3 repolarization and the effective refractory period due to potassium efflux.
- No direct effect on calcium currents.
Pharmacological Profile and Indications
The targets of these pharmacological agents are exclusively ventricular structures. They do not reduce myocardial contractility and do not affect pacemakers in the sinoatrial node.
The main indication for use is ventricular rhythm disorders, particularly ventricular extrasystoles. Drugs of this group are indispensable in situations where pathological impulses must be suppressed without the risk of additional depression of the heart muscle.
Key Representatives: Lidocaine, Mexiletine, and Phenytoin
The group includes several clinically significant medications with different pharmacokinetics:
- Lidocaine (xylocaine) — combines antiarrhythmic and local anesthetic properties. It has a high 'first-pass' hepatic metabolism effect, so it is administered exclusively parenterally (intravenous infusion). The main indication is ventricular arrhythmias during myocardial infarction.
- Mexiletine — a structural analog of lidocaine. Due to altered kinetics, it is well absorbed orally (bioavailability up to 100%) and acts for up to 12–16 hours.
- Phenytoin (diphenylhydantoin) — originally an antiepileptic drug, recognized as the drug of choice for arrhythmias caused by overdose or intoxication with cardiac glycosides, while preserving their positive inotropic effect.
Side Effects and Safety Profile
Despite good tolerability, the use of Class IB agents requires monitoring due to the risk of adverse reactions:
- CNS effects: drowsiness, confusion, seizure activity; for phenytoin — ataxia, nystagmus, and diplopia.
- Cardiovascular system: arterial hypotension, depression of atrioventricular conduction, bradycardia, and arrhythmogenic effects.
- Specific manifestations: chronic phenytoin use can cause hyperplastic gingivitis (overgrowth of gum tissue).