Kinetics of the oral antiarrhythmie lidocaine congener, tocainide
| Autor: | David Lalka, Melvin B. Meyer, Benjamin R. Duce, Alfred T. Elvin |
|---|---|
| Rok vydání: | 1976 |
| Předmět: |
Adult
Male Time Factors Lidocaine Urinary system Tocainide Administration Oral Biological Availability Absorption (skin) Pharmacology Kidney Drug Administration Schedule chemistry.chemical_compound Pharmacokinetics Ethylamines medicine Humans Anilides Infusions Parenteral Pharmacology (medical) Sodium bicarbonate Chemistry Middle Aged Blood proteins Bioavailability Bicarbonates Kinetics Intestinal Absorption Food Anti-Arrhythmia Agents Half-Life medicine.drug |
| Zdroj: | Clinical Pharmacology & Therapeutics. 19:757-766 |
| ISSN: | 0009-9236 |
| DOI: | 10.1002/cpt1976196757 |
| Popis: | Tocainide, a primary amine analogue of lidocaine, is effective against some experimental and clinical arrhythmias. Its pharmacokinetic behavior was studied in 6 healthy male subjects. Peak blood levels (CB max) and area under the blood concentration-time curve (AUC) were linearly related to dose with slopes of 0.0067 mcg/ml and 6 min mcg/ml per milligram of dose, respectively. Renal clearance of tocainide averaged 59 ml/min when urinary pH was uncontrolled or acidified, while it was reduced to 13 ml/min during intense sodium bicarbonate loading. Blood levels following intravenous infusion were well described by a 2-compartment open model with a volume of the central compartment of 0.92 L/kg. The t 1/2 beta was 11 hr and total body clearance was 166 ml/min. Loo-Riegelman analysis of the absorption rate did not allow unequivocal assignment of an "order" to the absorption process. Bioavailability approached 100%. Administration of drug 5 min after a test meal suppressed CB max 40% but minimally affected AUC. Approximately 50% of the drug was found to be plasma protein bound at clinically effective concentrations. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|