PMID: 3383990Jan 1, 1988Paper

Pharmacokinetics and pharmacodynamics of propafenone during acute and chronic administration

European Journal of Clinical Pharmacology
P GianiR Latini

Abstract

The pharmacokinetics of propafenone and 5-OH-propafenone and their relationship with the antiarrhythmic action and side effects have been studied in 10 patients with stable, frequent, premature ventricular beats (224-928 premature ventricular complexes/h). Observations were made after a single dose of propafenone 300 mg p.o., and after 1 and 3 months (only 5 out of 10 patients) of therapy with 300 mg t.d.s. After 1 month of treatment the plasma elimination half-life of propafenone (6.7 h) was almost twice as long as after a single dose (3.5 h), and the area under the plasma propafenone concentration-time curve (7620 ng.ml-1.h) was significantly larger than after single dose (3522 ng.ml-1.h); this was also true for the metabolite. The ratio of the AUCs of 5-OH-propafenone and propafenone decreased from the single dose (0.63) to 1 month (0.32). These variables remained stable up to 3 months. Eight patients had greater than or equal to 75% reduction of premature ventricular complexes after 3 days of therapy, and in 7 they were completely suppressed; the response was maintained over 1 to 3 months. Side effects were minor and in no case had the drug to be withdrawn or the dose reduced. Thus, the kinetics of propafenone were time-dep...Continue Reading

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Citations

Jan 1, 1992·European Journal of Clinical Pharmacology·R LatiniJ M Castel
Jan 1, 1990·European Journal of Clinical Pharmacology·S VozehF Follath
May 5, 2011·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Graham LappinColin Garner
Dec 5, 1989·The American Journal of Cardiology·P Jaillon, M Drici
May 1, 1991·The American Journal of Cardiology·W E HaefeliF Follath
Dec 2, 1998·British Journal of Clinical Pharmacology·G LiU Klotz
Feb 22, 1990·The New England Journal of Medicine·C Funck-BrentanoD M Roden

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