Metabolite cumulation during chronic propafenone dosing in arrhythmia
| Autor: | Robert E. Kates, Roger A. Winkle, Yin Gail Yee |
|---|---|
| Rok vydání: | 1985 |
| Předmět: |
Adult
Male Time Factors Metabolite Propafenone Pharmacology chemistry.chemical_compound Pharmacokinetics Oral administration medicine Ventricular ectopy Humans Pharmacology (medical) In patient Dosing Aged Propiophenones business.industry Arrhythmias Cardiac Middle Aged chemistry Anesthesia Plasma concentration Female business Anti-Arrhythmia Agents medicine.drug |
| Zdroj: | Clinical pharmacology and therapeutics. 37(6) |
| ISSN: | 0009-9236 |
| Popis: | The cumulation of propafenone and two of its metabolites, 5-hydroxypropafenone (5-OHP) and N-depropylpropafenone (NDPP), was examined in patients with frequent ventricular ectopy. After 2 weeks of propafenone therapy (300 mg twice a day), propafenone was discontinued and blood samples were drawn for 24 hours. The mean (± SD) steady-state concentrations of propafenone, 5-OHP, and NDPP were 1010 ± 411, 174 ± 113, and 179 ± 93 ng/ml. The concentration ratios of 5-OHP/propafenone and NDPP/propafenone were 0.177 ± 0.049 and 0.227 ± 0.203. Plasma concentrations of 5-OHP and NDPP did not decay in a log-linear manner during the sampling period and thus estimates of their disappearance t½s were not possible. At 24 hours after propafenone dosing, concentrations of 5-OHP and NDPP were 63% ± 37% and 50% ± 21% of their mean steady-state levels. Our data indicate that these propafenone metabolites cumulate in the plasma during chronic oral propafenone therapy, and that their clinical role needs to be elucidated. Clinical Pharmacology and Therapeutics (1985) 37, 610–614; doi:10.1038/clpt.1985.97 |
| Databáze: | OpenAIRE |
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