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Disposition and antiarrhythmic effect of lorcainide
International Journal of Clinical Pharmacology and Biopharmacy
|April 1, 1979
Summary
Lorcainide effectively treats ventricular premature beats (VPB) by maintaining therapeutic plasma levels. Oral lorcainide demonstrates complete bioavailability and appears effective for long-term arrhythmia prevention.
Area of Science:
- Pharmacology
- Clinical Therapeutics
- Cardiology
Background:
- Ventricular premature beats (VPB) are a common cardiac arrhythmia.
- Assessing the disposition and antiarrhythmic effects of novel drugs is crucial for effective treatment.
Purpose of the Study:
- To investigate the pharmacokinetic disposition of lorcainide.
- To evaluate the antiarrhythmic efficacy of lorcainide in patients with VPB.
Main Methods:
- Single intravenous doses (100 mg or 2 mg/kg) and multiple intravenous/oral doses were administered to 11 patients.
- Pharmacokinetic parameters were calculated using a two-compartment open model.
- Plasma concentrations and antiarrhythmic effects were monitored.
Main Results:
- Lorcainide exhibited a terminal half-life (t 1/2 (beta)) of 7.8 +/- 2.5 hr.
- Complete bioavailability was observed for multiple oral doses.
- Antiarrhythmic effects on VPB were sustained when plasma concentrations exceeded 120-150 ng/ml, with a therapeutic range of 150-400 ng/ml.
Conclusions:
- Lorcainide demonstrates favorable pharmacokinetic properties and significant antiarrhythmic effects.
- Oral administration of lorcainide, particularly 100 mg three times daily, is effective for managing ventricular arrhythmias.