Plasma and saliva propafenone concentrations at steady state. 1987

W D Mason, and R C Lanman, and E B Kirsten

Twenty-four healthy male subjects were administered 300 mg of propafenone every 8 h for 6 d in each of two phases that were separated by 2 d. Plasma samples were collected during the approach to steady state for each phase, and plasma and saliva samples were collected frequently at steady state. Both plasma and saliva propafenone were assayed by a specific HPLC method. Two estimates of elimination half-life (t1/2), mean steady-state concentration (CPss), time to maximal concentration (tmax), and maximal concentration (CPmax) were estimated for each subject. Also mean steady-state saliva concentrations (CSss), time to maximal saliva concentration (tSmax), and maximal saliva concentrations (CSmax) were estimated. A large intersubject variance in both t1/2 and CPss were observed in the 24 subjects, with the t1/2 values ranging from 2.1 to 27.2 h and the CPss values from 0.3 to 3.03 microgram/mL. Each subject was quite consistent for the two phases, suggesting a relatively low intrasubject variance for propafenone kinetics. A histogram shows most subjects to have t1/2 values between 2 and 10 h, with diminishing numbers of subjects at greater t1/2 values rather than a bimodal distribution. Saliva concentrations ranged from 12 to 72% of the corresponding plasma concentrations, being 24.7 +/- 11.1% of the simultaneously collected plasma sample overall (mean +/- SD). a significant (p less than 0.001) positive correlation exists between CPss and CSss.

UI MeSH Term Description Entries
D008297 Male Males
D008991 Monitoring, Physiologic The continuous measurement of physiological processes, blood pressure, heart rate, renal output, reflexes, respiration, etc., in a patient or experimental animal; includes pharmacologic monitoring, the measurement of administered drugs or their metabolites in the blood, tissues, or urine. Patient Monitoring,Monitoring, Physiological,Physiologic Monitoring,Monitoring, Patient,Physiological Monitoring
D011405 Propafenone An antiarrhythmia agent that is particularly effective in ventricular arrhythmias. It also has weak beta-blocking activity. Apo-Propafenone,Arythmol,Baxarytmon,Cuxafenon,Fenoprain,Jutanorm,Nistaken,Norfenon,Pintoform,Prolecofen,Propafenon AL,Propafenon Hexal,Propafenon Minden,Propafenone Hydrochloride,Propafenone Hydrochloride, (R)-Isomer,Propafenone Hydrochloride, (S)-Isomer,Propafenone, (+-)-Isomer,Propafenone, (R)-Isomer,Propafenone, (S)-Isomer,Propamerck,Rythmol,Rytmo-Puren,Rytmogenat,Rytmonorm,SA-79,Hydrochloride, Propafenone,SA 79,SA79
D006207 Half-Life The time it takes for a substance (drug, radioactive nuclide, or other) to lose half of its pharmacologic, physiologic, or radiologic activity. Halflife,Half Life,Half-Lifes,Halflifes
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000328 Adult A person having attained full growth or maturity. Adults are of 19 through 44 years of age. For a person between 19 and 24 years of age, YOUNG ADULT is available. Adults
D012463 Saliva The clear, viscous fluid secreted by the SALIVARY GLANDS and mucous glands of the mouth. It contains MUCINS, water, organic salts, and ptylin. Salivas

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