Pharmacokinetics and antiarrhythmic efficacy of intravenous ajmaline in ventricular arrhythmia of acute onset.
21 patients with acute myocardial infarction and ventricular arrhythmia of Lown class II-IIIB of acute onset received a short infusion of (50 mg/5 min) ajmaline (Gilurytmal). 6 of the patients had normal kidney and liver function (Group 1), 4 patients had acute renal failure and hemodialysis treatment (Group 2), 4 patients had impaired hepatic function (Group 3), 3 patients had cardiogenic shock (Group 4), and 4 patients had been pretreated with phenobarbital for seizures for at least 5 days (Group 5). A distribution half-life of 6 +/- 1 min and an elimination half-life of 95 +/- 6 min was determined in Group 1. The total plasma clearance was significantly lower in patients with impaired liver or cardiac function and significantly higher in Group 5, whereas impaired renal function did not affect total plasma clearance. After short infusion, ventricular arrhythmia of Lown II-IIIB completely disappeared for at least 16 to 36 min (mean: 19 min), which was associated with an ajmaline plasma level of 0.1-0.45 micrograms/ml. Additionally, steady-state plasma levels of ajmaline were determined after continuous infusion of 10-50 mg/h to 16 patients (Group 6) with ventricular arrhythmia of acute onset (Lown class IVA-V). Ventricular arrhythmia completely disappeared or at least changed to lower Lown classes at ajmaline plasma levels of 0.4-2.0 micrograms/ml. The ajmaline plasma protein binding was 76 +/- 9%. Ajmaline had a special affinity to alpha 1-acid glycoprotein.
Köppel
C
C
Universitätsklinikum Rudolf Virchow, Freie Universität Berlin, FRG.
Wagemann
A
A
Martens
F
F
D000208:Acute Disease; D000368:Aged; D000404:Ajmaline / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000627:therapeutic use; D001145:Arrhythmias, Cardiac / Q000188:drug therapy* / Q000209:etiology; D001798:Blood Proteins / Q000378:metabolism; D005260:Female; D006352:Heart Ventricles; D006440:Hemofiltration; D006801:Humans; D007262:Infusions, Intravenous; D008104:Liver Cirrhosis, Alcoholic / Q000150:complications / Q000378:metabolism; D008297:Male; D008875:Middle Aged; D008954:Models, Biological; D009203:Myocardial Infarction / Q000188:drug therapy; D015425:Myocardial Reperfusion; D011485:Protein Binding; D006435:Renal Dialysis; D014462:Ultrafiltration
D001798:Blood Proteins; D000404:Ajmaline