Key result
Propafenone at 150 and 225 mg produced significantly greater beta-blockade in 5 poor metabolizers compared to 9 extensive metabolizers, driven by higher plasma levels of the parent drug.
Why the study?
Does the genetically determined metabolism phenotype affect the degree of beta-blockade produced by propafenone in normal subjects?
Population
14 normal subjects (9 with extensive-metabolizer phenotype, 5 with poor-metabolizer phenotype)
Comparison
Propafenone 150, 225, and 300 mg every eight… vs Placebo
Design
Other
Follow-up
5 days per dose
Authors
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May warrant CYP2D6-guided caution with propafenone dosing; leaves open clinical outcome impact in larger patient cohorts.
Does the genetically determined metabolism phenotype affect the degree of beta-blockade produced by propafenone in normal subjects?
The degree of beta-blockade during propafenone therapy is significantly enhanced in patients with a poor-metabolizer phenotype due to higher plasma levels of the parent drug.
Lee et al. (1990) studied Healthy volunteers (n=14). Propafenone vs. Placebo was evaluated on Reduction in tachycardia produced by boluses of isoproterenol and treadmill exercise. Propafenone at 150 and 225 mg produced significantly greater beta-blockade in 5 poor metabolizers compared to 9 extensive metabolizers, driven by higher plasma levels of the parent drug.
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