Related Experiment Videos
Pirmenol kinetics and effective oral dose
Clinical Pharmacology and Therapeutics
|December 1, 1982
Summary
Pirmenol effectively reduced premature ventricular beats (PVBs) in a single oral dose study. This antiarrhythmic drug demonstrated significant PVB suppression with minimal toxicity and a favorable pharmacokinetic profile.
Area of Science:
- Pharmacology
- Cardiology
- Clinical Trials
Background:
- Premature ventricular beats (PVBs) are a common cardiac arrhythmia.
- The oral administration and efficacy of pirmenol for PVBs in humans were previously unestablished.
Purpose of the Study:
- To determine the effective dose and pharmacokinetics of oral pirmenol in patients with chronic, stable PVBs.
- To evaluate the safety and efficacy of pirmenol in a placebo-controlled setting.
Main Methods:
- A dose-ranging study followed by a double-blind, crossover, placebo-controlled trial.
- Eight patients with chronic, stable PVBs received oral pirmenol doses ranging from 150 to 250 mg.
- Efficacy was assessed by percentage suppression of PVBs/hr and duration of effect.
Main Results:
- Oral pirmenol doses (150-250 mg) achieved at least 90% PVB suppression in 18 of 19 administrations.
- A single oral dose suppressed 95% of PVBs/hr for 3 hours (P < 0.01 vs. placebo).
- Median half-life was 9.3 hours, with 82.6% bioavailability and minimal QTc interval prolongation.
Conclusions:
- Pirmenol effectively reduces premature ventricular beats with a single oral dose.
- The drug exhibits favorable pharmacokinetics, including a long half-life and good bioavailability.
- Pirmenol demonstrated minimal toxicity in this initial human study.